Bio Pharma Compiled

BIOPHARMACEUTICS-I
OBJECTIVES OF CHAPTER 1, 2, 3 & 4
DEPARTMENT OF PHARMACY
QUAID-A-I-AZAM UNIVERSITY ISLAMABAD
CHAPTER 1
INTRODUCTION TO BIOPHARMACEUTICS AND
PHARMACOKINETICS
SHORT QUESTIONS:
1. What is drug?
Drugs are substances intended for use in the diagnostic, cure, mitigation, treatment or
prevention of diseases.
(Applied bio pharmaceutics and pharmacokinetics by Leon Shargel sixth edition chapter 1,
Introduction to biopharmaceutics and pharmacokinetics, page1)
2. How can you define drug product performance?
Drug product performance is defined as the release of the drug substance from the drug product
either of local drug action or for drug absorption into the plasma for systemic therapeutic activity.
(applied bio pharmaceutics and pharmacokinetics by Leon shargel sixth edition chapter 1,
3. Define biopharmaceutics.
Biopharmaceutics is the science that examines this interrelationship of the physicochemical

properties of the drug, the dosage form in which the drug is given, and the route of
administration on the rate and extent of systemic drug absorption.
4. Define bioavailability?
Bioavailability is a measure of systemic availability of a drug.
(applied bio pharmaceutics and pharmacokinetics by Leon Shargel sixth edition chapter 1,
5. What are the major factors discussed in biopharmaceutics?
Biopharmaceutics involves following factors that influence
 The design of drug product.

 The stability of the drug within the drug product.
 The manufacture of drug product.
 The release of the drug from the drug product.
 The rate of dissolution/release of the drug at the absorption site.
 The systemic absorption of the drug
 Delivery of drug to the site of action
6. Define therapeutic objective?
Drug is intended for rapid relief of symptoms, slow extended action given once per day (week or
long) or chronic use is drug for local action or systemic action.
7. What is pharmacokinetics?
Pharmacokinetics is the science of the kinetics of drug absorption, distribution, and elimination
(ie, excretion and metabolism).
8. Define drug disposition?
The description of drug distribution and elimination is often termed drug disposition.
9. What are the important biopharmaceutical considerations in drug product design?
Following are the important biopharmaceutical considerations in drug product design:
1-therapeutic objective
2-drug API
3-Route of administration
4-Drug dosage and dosage regimens
5-type of drug product
6-excipients
7-method of manufacture
10. Define pharmacodynamics
Pharmacodynamics refers to the relationship between the drug concentration at the site of
action (receptor) and pharmacologic response, including biochemical and physiologic effects
that influence the interaction of drug with the receptor. The interaction of a drug molecule with a
receptor causes the initiation of a sequence of molecular events resulting in a pharmacologic or
toxic response.
11. What is the drug response?

Drug response refers to a direct measure of the pharmacologic effect of the drug.
12. What is the difference between invasive and non-invasive methods?
Invasive methods include sampling blood, spinal fluid, synovial fluid, tissue biopsy, or any
biologic material that requires parenteral or surgical intervention in the patient.
In contrast, noninvasive methods include sampling of urine, saliva, feces, expired air, or any
biologic material that can be obtained without parenteral or surgical intervention.
13. What is clinical toxicology?
Clinical toxicology is the study of adverse effects of drugs and toxic substances (poisons) in the
body.
14. What is the significance of pharmacokinetic models?
Pharmacokinetic models are used to:
1. Predict plasma, tissue, and urine drug levels with any dosage regimen
2. Calculate the optimum dosage regimen for each patient individually
3. Estimate the possible accumulation of drugs and/or metabolites
4. Correlate drug concentrations with pharmacologic or toxicologic activity
5. Evaluate differences in the rate or extent of availability between formulations (bioequivalence)

6. Describe how changes in physiology or disease affect the absorption, distribution, or
elimination of the drug
7. Explain drug interactions
15. What is a compartment?
A compartment is not a real physiologic or anatomic region but is considered as a tissue or

group of tissues that have similar blood flow and drug affinity.
16. Define bioequivalence:
Bioequivalence studies are drug product performance tests that compare the bioavailability of
the same active pharmaceutical ingredient from one drug product (test) to a second drug
product (reference)
Drug product performance,In-vivo: bioavailability and bioequivalence , page 403)
17. Define generic equivalence.
The process of dispensing a different brand or an unbranded drug product in place of the
prescribed drug product. The substitution drug product contains the same active ingredients or
therapeutic moiety as the same salt or ester in the same dosage form but is made by a different
manufacturer.
Drug product performance, In-vivo: bioavailability and bioequivalence , page 441)
18. What are therapeutic equivalent drugs?
Drug products are considered to be therapeutic equivalents only if they are pharmaceutical
equivalents and if they can be expected to have the same clinical effect and safety profile when
administered to patients under the conditions specified in the labeling.
19. What does MEC and MTC represents ?
MEC and MTC represent the minimum effective concentration and minimum toxic concentration
of the drug. MEC reflects the minimum concentration of drug needed at the receptors to
produce the desired pharmacologic effect. Similarly,MTC represents the drug concentration
needed to just barely produce a toxic effect. (page # 7,8)
20. Define drug delivery systems.
Delivery systems: The formulations that release and deliver drugs to the site of action to
produce the therapeutic effect and are specially designed to meet patients needs.
21. Differentiate between mammillary and catenary model…….(ch:1, page:13)
Answer: Mammillary model consists of one or more compartments around a central

compartment like satellites whereas catenary model consists of compartments joined to one
another like the compartments of a train.
22. Why chromatographic and mass spectrophotometric methods are most frequently
employed for drug concentration measurement?
Chromatographic and mass spectrophotometric methods are most frequently employed for drug
concentration measurement, because chromatography separates the drug from other related
materials that may cause assay interference and mass spectrophotometry allows detection of
molecules and molecule fragments based on their mass to charge ratio. (Page 6)
23. How does the pharmacokinetics change from linear to non-linear?
At very high doses, the drug concentration in the body may saturate enzymes involved in the
absorption, biotransformation, or active renal secretion mechanisms, thereby changing the
pharmacokinetics from linear to nonlinear pharmacokinetics. (Page 6)
24. Define pharmaceutical equivalents.
Drug products in identical dosage form that contain the same active ingredients, i.e. the same
salt or ester, are of the same dosage form, use the same route of administration and are
identical in strength or concentration. (Page 441)
25. What is clinical pharmacokinetics?
Clinical pharmacokinetics is the application of pharmacokinetic methods to the drug therapy.

It involves a multidisciplinary approach to individually optimized dosing strategies based on
the patient’s disease state and patient specific considerations. (Page 4)
26. What is meant by toxicokinetics?
Toxicokinetics is the application of pharmacokinetic principles to the design, conduct and

interpretation of the drug safety evaluation studies and in validating dose related exposure in
animals. (Page 5)
27. What is a model?

A model is a hypothesis using mathematical terms to describe quantitative relationships
concisely.
28. List the types of models used for pharmacokinetic studies. (Page 11)
1. Empirical models
2. Physiological models
3. Compartment models
4. Mammillary models
5. Caternary models
FILL IN THE BLANKS:
1. Drugs are substances intended for use in the diagnostic, cure, mitigation, treatment or
prevention of diseases.
2. Studies of biopharmaceutics use both in vitro and in vivo methods. (Page No: 03)
3. biopharmaceutics is interrelationship of the physicochemical properties of the drug, the
dosage form in which the drug is given, and the route of administration on the rate and
extent of systemic drug absorption.
4. Toxicology and efficacy studies provide information on the safety and effectiveness of
the drug during development and in special patient population. (Page No: 05)
5. Biopharmaceutics examines the interrelationship of the physical/ chemical properties of

the drug, the dosage form (drug product) in which the drug is given, and the route of
administration on the rate and extent of systemic drug absorption.
6. If the drug concentration at the site of action exceeds the minimum effective
concentration (MEC), a pharmacologic response results.
7. Bioavailability is a measure of systemic availability of a drug.
8. bioavailability may differ from one drug product to another containing the same drug,
even from same ROA.
9. The manufacture of a new drug product must submit a New Drug Application (NDA) to
FDA.
10. The description of drug distribution and elimination is often termed drug disposition.
11. elimination of the drug involves excretion and metabolism
12. Pharmacokinetics is the science of the kinetics of drug absorption, distribution, and
elimination.
13. In-vitro methods are procedures employing test apparatus and equipment without lab
animals and humans.
14. In-vivo methods are complex studies involving human subjects and lab animals.
Introduction to biopharmaceutics and pharmcokinetics, page3)
15. Drug is intended for rapid relief of symptoms, slow extended action given once per day
(week or long) or chronic use is drug for local action or systemic action is called
therapeutic objective
16. LADME stands for Liberation, Absorption, Distribution, Metabolism and Excretion.
17. Clinical pharmacokinetics is also applied to therapeutic drug monitoring (TDM) for
very potent drugs.
18. Pharmacodynamics refers to the relationship between the drug concentration at the
site of action (receptor) and pharmacologic response.
19. Pharmacokinetic-pharmacodynamics models are constructed to relate plasma drug level

to drug concentration in the site of action.
Introduction to biopharmaceutics and pharmacokinetics, page5 )
20. Toxicokinetics is the application of pharmacokinetic principles to the design, conduct,

and interpretation of drug safety evaluation studies.
21. Clinical toxicology is the study of adverse effects of drugs and toxic substances
(poisons) in the body.
22. The time of peak plasma level is the time of maximum drug concentration in the plasma.
23. The AUC is related to the amount of drug absorbed systemically.
24. The therapeutic window is concentration between MEC and MTC

25. The onset time corresponds to the time required for drug to reach MEC.
26. Chromatography and mass spectrometry methods are most frequently employed for
drug concentration measurement.
27. The rate and extent of drug excreted in urine reflects the rate and extent of systemic
drug absorption.
28. Drug concentration can be correlated to pharmacological/toxicological activity by

pharmacokinetic model.
29. A pharmacokinetic model is used to Calculate the optimum dosage regimen for each
patient individually
30. Drug products are considered to be therapeutic equivalents if they can be expected to
have the same clinical effect and safety profile.
31. Plasma is the liquid supernatant obtained after centrifugation of non-clotted whole blood
that contains an anticoagulant. (Page No: 07)
32. Bioequivalence studies compare the bioavailability of the same active pharmaceutical
ingredient from one drug product (test) to a second drug product (reference)
33. The process of dispensing a different brand or an unbranded drug product in place of the
prescribed drug product. The substituted drug product contains the same active
ingredients or therapeutic moiety as the same salt or ester in the same dosage form but
is made by a different manufacturer is called generic equivalence
34. Bioavailability means the rate and extent to which the active ingredient or active moiety
is absorbed from a drug product and becomes available at the site of action.
35. Bioequivalence is generally determined if the 90% confidence intervals for Cmax and
AUC fall within 80% to 125% of the reference listed drug based on log transformation of
the data.
36. Biotransformation Is the process by which the drug is chemically converted in the body
to a metabolite(, Applied Biopharmaceutics and Pharmacokinetics by LEON SHARGEL
6th Edition Page 107)
37. The duration of drug action is the difference between the onset time and the time for the
drug to decline back to MEC . (pg 8 )
38. The release of the drug substance from the drug product either for local drug action or
for drug absorption into the plasma for systemic therapeutic activity is called drug
product performance. pg. no. 1
39. Biopharmaceutics provide the scientific basis for drug product design and drug
product development. pg. no. 2
40. Drug response refers to a direct measure of the pharmacologic effect of the drug. pg:5
41. Measurement of drug in urine is an indirect method to ascertain the bioavailability of a
drug. Pg.no.8
42. Noninvasive methods include sampling of urine, saliva, feces, expired air, or any
biologic material that can be obtained without parenteral or surgical intervention. (Page
6)
43. The saliva/plasma drug concentration ratio is less than 1 for many drugs. (Page 9)
44. The use of salivary drug concentrations as a therapeutic indicator should be used with
caution and preferably as a secondary indicator. (Page 9)
45. In a two-compartment model, drug can move between the central or plasma
compartment to and from the tissue compartment. (Page 12)
46. Ratio between toxic and therapeutic dose is termed as therapeutic index. (pg:8)
47. Pharmacokinetic models allow more accurate interpretation of the relationship
between plasma drug levels and pharmacological response. (Page No: 09)
48. The saliva/plasma drug concentration ratio is influenced by the pKa of drug and the pH
of the saliva. (Page No: 09)
49. Forensic science is the application of science to personal injury, murder, and other
legal proceedings. ( pg no.9)
50. Plasma is obtained from the supernatant of centrifuged whole blood to which
anticoagulant has been added. (Pg#6)
51. Serum does not contain any cellular elements, fibrinogen or other clotting factors from
the blood. (Page:7)
52. Whole blood is generally obtained by venous puncture. (Page :7)
53. Forensic Science is the application of science to personal injury, murder and other legal
proceedings. (Page :9)
54. Drug used in chemotherapy interferes with nucleic acid biosynthesis.(Page :13)
55. The plasma drug concentration time – curve is generated by obtaining the drug
concentration taken at various time intervals after a drug product is administered.
(Page:7)
56. Serum does not contain any cellular elements, fibrinogen or other clotting factors
from the blood.
MULTIPLE CHOICE QUESTIONS:
1. A pharmacological response results when the drug concentration at the site of action
reaches or exceeds the ____________________.
a) Minimum effective concentration (MEC)

b) Area under plasma level time curve (AUC)
c) Maximum plasma concentration( Cmax)
d) Peak plasma concentration time (tmax) (Page No: 02)
2. Substances intended for use in the diagnostic, cure, mitigation, treatment or prevention
of diseases are called
a-dosage form C-drugs

b-medical agents d-dose
3. __________ is the release of the drug substance from the drug product either of local
drug action or for drug absorption into the plasma for systemic therapeutic activity.
A-drug product performance C-pharmacokinetics

b-pharmacodynamics d-bioavailability
4. The interrelationship of the physicochemical properties of the drug, the dosage form in
which the drug is given, and the route of administration on the rate and extent of
systemic drug absorption.
a-bioavailability c-drug product performance
b-biopharmaceutics d-pharmaceutics
5. Biopharmaceutics involves the factors that influence:
a) Design of the drug product

b) Stability of drug product
c) Rate of dissolution of drug product
d) All of above
(Page No: 02)
6. If the drug concentration at the site of action exceeds the ______ a pharmacologic
response results.
a-MTC c-TDM
b- minimum effective concentration d-bioavailability
7. ______ a measure of systemic availability of a drug.
a-bioavailabilty c-drug concentration

b-bioequilvalence d-all
8. bioavailability may differ from ____________________
a- one drug product to another containing b-one drug product to another

the different drugs containing the same drug
9. drug distribution and elimination are often termed _____
a-metabolism c-kinetics
b-pharmacodynamics d- drug disposition.
10. elimination of the drug involves _____________
a-excretion and metabolism c-metabolism

b-absortion and distribution d-LADME
11. methods involving human subjects or laboratory animals are _____
a-in-vitro c-can be both

b- In-vivo d-laboratory method
12. toxic response is produced at drug concentrations above
a- MTC c-optimal dose

b-MEC d-none
13. _____ is ranked as #1 diesease
a-diabetes c-ebola
b-heart disease d-neoplasms
14. Pharmacodynamics refers to the relationship between the drug concentration at the site
of action and __________ response.
A. Pharmacokinetical C. Pharmacological
B. Pharmacodynamical D. None
15. _______ is the study of ADR of drugs and toxic substances (poisons) in the body.
a-pharmacokinetics c-clinical toxicology

b-pharmacodynamics d-pharmacology
16. Therapeutic efficacy and toxicity of the drug is determined by:
a) Nature of drug molecule

b) Route of delivery
c) Formulation of dosage form
d) All of above
(Page No: 02)
17. Drugs with a wide therapeutic window are generally considered ___________ than
drugs with a narrow therapeutic window.
a) Toxic
b) Potent
c) Safer
d) Both B and C
(Page No: 08)
18. As drug reaches systemic circulation,plasma drug conc will rise up to ____ if the drug
was given by extravascular route.
A-maximum c-minimum
b--first max then minimum d-zero level
19. A rough marker of average rate of drug absorption is the time of
A-maximum drug concentration in the c-toxic drug levels in plasma

plasma d-none
B-minimum effective concentration
(Applied bio pharmaceutics and pharmacokinetics by Leon shargel sixth edition chapter 1,
20. Therapeutic window is also called as
a-MEC c-AUC
b-MTC d-thearapeutic index
21. The_______ corresponds to the time require for the drug to reach the MEC:
a) Residence time
b) Onset time
c) Tmax
d) None
22. The _____________ is the concentration between MEC and the MTC.
a. Index window
b. Therapeutic window
c. Duration window
d. Both a and b
(PAGE#8)
23. Whole blood is obtained by venous puncture and contains an anticoagulant such as
a. Heparin
b. EDTA
c. Only a
d. Both a and b
(PAGE#7)
24. Measurement of drug in urine is an _______ method to ascertain the bioavailability of a
drug.
i) Direct
ii) Indirect
iii) No relation
iv) Both
25. The saliva/plasma drug concentration ratio is _____ for many drugs
a) >1
b) < 1
c) Vary
d) None
26. Drug interactions can be explained by which models?
a-bioequivalence model c- pharmacokinetic model
b-both d-none
27. A compartment is not a real physiologic or anatomic region but is considered as a tissue
or group of tissues that have
a-different blood flow and drug affinity c- similar blood flow,different drug affinity
b- similar blood flow and drug affinity d- different blood flow,samedrug affinity
28. Bioequivalence studies compare the bioavailability of the same active pharmaceutical
ingredient from test product to a
a- second drug product (reference) b-new drug

c-many drugs d-may be all
29. Drug products are considered to be therapeutic equivalents only if they are
a-generic equivalents c-chemical equivalents

b-pharmaceutical equivalents d-substitutes
30. Bioequivalence studies are
a- drug product performance tests c-model

b-drug delivery tests d-none
(, page 403)
CHAPTER 2
GASTRO-INTESTINAL ABSORPTION AND PHYSICO-CHEMICAL

CONSIDERATIONS
SHORT ANSWERS:
1. What is MMC? (Page no 340)
During the fasted or inter-digested state, alternating cycles of activity known as Migrating Motor
Complex. It acts as propulsive movement that empties upper GIT to caecum. In fed state, the
MMC is replaced by irregular contraction, which has effect of mixing intestine contents.
2. What is Transcytosis? (Page no 335)
Ans: It is a process in which by which various macromolecules are transported across the
anterior of a cell. In transcytosis, the vesicle fuses with plasma membrane to release the
encapsulated material to another side of cell. Vesicles are employed to intake the
macromolecules on one side of cell and draw them across the cell and eject them on other side.
3. On which factors systemic absorption of drug depends?
The systemic absorption of a drug is dependent on
(1) The physicochemical properties of the drug
(2) The nature of the drug product
(3) The anatomy and physiology of the drug absorption site.
(Applied bio pharmaceutics and pharmacokinetics by Leon Shargel, sixth edition chapter 13,
physiologic factors related to drug absorption, pg.321)
4. On what factors permeability of drug depends?

The permeability of a drug at the absorption site into the systemic circulation is intimately related
to the molecular structure of the drug and to the physical and biochemical properties of the cell
membranes.
5. What are the different passages of drug across cell membrane?

 passive diffusion
 carrier mediated transport
 active transport
 facilitated diffusion
 influx transporters
 efflux transporters
physiologic factors related to drug absorption, pg326-331)
6. Define passive diffusion?

Passive diffusion is the process by which molecules spontaneously diffuse from a region of
higher concentration to a region of lower concentration.
7. What is driving force for passive diffusion?

The driving force for passive diffusion is higher drug concentrations on the mucosal side
compared to the blood.
8. Why drugs diffuse slowly in brain?

Drugs usually diffuse very rapidly through capillary plasma membranes in the vascular
compartments, in contrast to diffusion through plasma membranes of capillaries in the brain. In
the brain, the capillaries are densely lined with glial cells, so a drug diffuses slowly into the brain
as if a thick lipid membrane existed
9. What is rate-limiting step? (Page#363)

The slowest step in a series of kinetic processes is called rate-limiting step.
10. What is active transport?

Active transport is characterized by the transport of drug against a concentration gradient that
is, from regions of low drug concentrations to regions of high concentrations. It is a carrier-
mediated transmembrane process that plays an important role in the gastrointestinal absorption
and in renal and biliary secretion of many drugs and metabolites.
11. What is facilitated diffusion?

Facilitated diffusion is also a carrier-mediated transport system, differing from active transport in
that the drug moves along a concentration gradient (ie, moves from a region of high drug
concentration to a region of low drug concentration).
12. What is vesicular transport? Write its types.

Vesicular transport is the process of engulfing particles or dissolved materials by the cell.
Pinocytosis and phagocytosis are forms of vesicular transport that differ by the type of
material ingested.
 Pinocytosis refers to the engulfment of small solutes or fluid.

 Phagocytosis refers to the engulfment of larger particles or macromolecules,
generally by macrophages.
10-Define endocytosis and exocytosis?
Endocytosis processes of moving specific macromolecules into a cell.
Exocytosis is processes of moving specific macromolecules out of a cell.
13. What are the major physiological processes occurring in GI system?
The major physiological processes that occur in GI system are secretion, digestion and
absorption.
14. What is the advantage of ODS ( orally disintegrating tablets)?
A major advantage for ODTs is that the drug may be taken without water.
15. Which factors regulate gastrin release?

Gastrin release is regulated by stomach distention (swelling) and the presence of peptides and
amino acids.
16. What is antral milling?

Antral milling is mixing which is intense and pressurized in the antral part of the stomach, a
process of breaking down large food particles.
17. Why duodenum is the major site for passive drug absorption?
Due to its anatomy, which creates a high surface area and high blood flow. The duodenum is
the site where many ester prodrugs are hydrolyzed during absorption.
18. Which factors delay gastric emptying time?

The factors that tend to delay gastric emptying include consumption of meals high in fat, cold
beverages, and anticholinergic drugs.
19. What is the effect of acid on penicillin?

Penicillin are unstable in acid and decompose if stomach emptying is delayed.
20. How motility and absorption of drugs are related to each other?
The drug must have a sufficient time (residence time) at the absorption site for optimum
absorption. In the case of high motility in the intestinal tract, as in diarrhea, the drug has a very
brief residence time and less opportunity for adequate absorption.
21. How can you protect a drug that is physically or chemically unstable from
degradation?
Drugs that are physically or chemically unstable may require special excipients, coatings or
manufacturing processes to protect from degradation.
Bio-pharmaceutic considerations in drug product design and In-Vitro drug product performance,
pg.366)
22. What is stability-pH profile?

The stability-pH profile is a plot of the reaction rate constant for drug degradation versus pH.
pg.366)
23. Define solubility-pH profile?
Solubility-PH profile is a plot of the solubility of the drug at various physiologic PH values.
pg.366)
24. What is the effect of particle size on absorption?

The effective surface area of a drug is increased enormously by a reduction in the particle size.
Because dissolution takes place at the surface of the solute (drug), the greater the surface area,
the more rapid is the rate of drug dissolution.
pg.367)
25. What is lipid by-layer or unit membrane theory? (Page#325)
Originally proposed by Davison and Danielle, considers the plasma membrane to be composed
of two layers of phospholipid between two surface layers of proteins, with hydrophilic head
groups of the phospholipids facing the protein layers and the hydrophobic tail groups of
phospholipids aligned in the interior.
26. What is ion pair formation?
Strong electrolyte drugs are highly ionized or charged molecules, such as quaternary nitrogen
compounds with extreme pKa values. Strong electrolyte drugs maintain their charge at all
physiologic pH values and penetrate membranes poorly. When the ionized drug is linked up
with an oppositely charged ion, an ion pair is formed in which the overall charge of the pair is
neutral. This neutral drug complex diffuses more easily across the membrane. PG NO. 336
27. What are the considerations for an oral dosage form formulation?
The oral dosage form must be designed to account for extreme pH ranges, the presence or
absence of food, degradative enzymes, varying drug permeability in the different regions of the
intestine, and motility of the gastrointestinal tract. (Page 336)
28. What do you know about Convective Transport? (Page:336)
Very small molecules (such as urea, water, and sugars) are able to cross cell membranes
rapidly, as if the membrane contained channels or pores. Although such pores have never been
directly observed by microscopy, the model of drug permeation through aqueous pores is used
to explain renal excretion of drugs and the uptake of drugs into the liver.
29. What are the effects of food on the bioavailability of drug? Page no 343
Ans: Some effect of food on bioavailability of drugs includes
 Delay in gastric timing

 Stimulation of bile flow
 Change in pH of GIT
 An increase in Splanchnic blood flow
 Change in luminal metabolism of drug substance
 Physical & Chemical interaction of meal with drug product
30. What are the major considerations in designing the drug? Page 321
Ans: Major consideration in designing of drug product includes the therapeutic objective, the
application site & systemic drug absorption from the application site. If the drug is intended for
systemic activity drug should completely absorbed from application site.
31. Define diffusion coefficient. What are its dimensions? (Pg#327, 328)
Diffusion coefficient is defined as the amount of the drug that diffuses across a cell membrane
of a unit area per unit time, when concentration gradient is unity.
It’s dimensions are area per unit time or cm2/sec.
32. What is Carrier-Mediated Intestinal Transport?
Various carrier-mediated systems (transporters) are present at the intestinal brush border and
basolateral membrane for the absorption of specific ions and nutrients essential for the body.
Many drugs are absorbed by carriers because of the structural similarity to natural substrates
(Page 330).
FILL IN THE BLANKS
1. According to Fick’s law drug molecules diffuse from a region of high drug concentration
to low drug concentration. (Page No: 327)
2. Enterocytes are intestinal absorptive cell that express transport protein. (Page No:
332)
3. Many drugs or chemicals have dual roles as substrate and or inhibitor between
CYP3A4 & P-glycoprotein. (Page No: 334)
4. Transcytosis is a proposed process for the absorption of orally administered for large
proteins. (Page No: 335)
5. Many drugs are not administered orally because of drug instability in the
gastrointestinal tract or drug degradation by the digestive enzymes in the intestine.
6. The Nasal region is richly supplied with blood vessels. (Page No: 354)
7. Many drugs administered by extravascular routes are intented for Local effect.
8. Transcellular absorption is the process of drug movement across a cell.

9. The CHF patient with persistent edema has reduced splanchnic blood flow and
develops edema in bowel. (Page No: 352)
10. Optimum size for deep airway penetration of drug particles is 3 to 5 micro meter.
(Page No: 354)
11. Cell membranes are generally thin , approximately 70 to 100Å in thickness.
12. The lipid bilayer theory explains the observation that Lipid soluble drugs tend to
penetrate cell membranes easily than Polar molecules
13. According to fluid mosaic model , the cell membrane consists of Globular proteins
embedded in Lipid bilayer matrix
14. In Passive diffusion no External energy is expanded.
15. If the two sides have the same drug concentration, forward-moving drug molecules are
balanced by molecules moving back, resulting in no net transfer of drug.
16. The driving force for passive diffusion is higher drug concentrations on the mucosal side
compared to the blood
17. Passive diffusion is the major absorption process for most drug.
18. Theoretically, a lipophilic drug may pass through the cell or go around it.
19. Active transport is a carrier-mediated transmembrane process.

20. The term blood brain barrier is used to describe the poor diffusion of water-soluble
molecules across capillary plasma membranes into the brain.
21. In meningitis plasma membranes of brain may be disrupted or become more

permeable to drug diffusion.
22. Nonionized species of the drug are More lipid soluble.
23. In terms of drug absorption, facilitated diffusion seems to play a very minor role
24. Vesicular transport is the process of engulfing particles or dissolved materials by the
cell.
25. Pinocytosis refers to the engulfment of small solutes or fluid.

26. Phagocytosis refers to the engulfment of larger particles or macromolecules.
27. Endocytosis is processes of moving specific macromolecules into of a cell

28. Enzymes in saliva and pancreatic secretions are also involved in the digestion of
carbohydrates and proteins
29. The most important site for drug absorption is the small intestine.
30. saliva is main secretion of oral cavity .and it has PH of about 7

31. Small intestine transit time (SITT) ranges from 3 to 4 hours for most healthy subjects.
32. The stomach is innervated by the vagus nerve.

33. The esophagus connects the pharynx and the cardiac orifice of the stomach
34. hydrochloric acid is secreted by parietal cells
35. Basic drugs are solubilized rapidly in the presence of stomach acid.
36. The pH of duodenum is 6-6.5.
37. Proteolytic enzymes in the duodenum degrades many protein drugs.
38. The small projections which are present in small intestine known as Villi
39. Penicillin, are unstable in acid and decompose if stomach emptying is delayed.
40. Liquids Are generally emptied faster than digested solids from the stomach
41. The presence of food may delay stomach emptying of enteric-coated tablets or non
disintegrating dosage form.
42. The Solubility-PH profile is a plot of the solubility the drug at various physiologic PH
values.
43. A basic drug is more soluble in Acidic medium, forming a soluble salt.
44. The effective surface area of a drug is increased enormously by a reduction in the
particle size.
pg.367)
45. Particle size and particle size distribution studies are important for drugs that have low
water solubility
pg.367)
46. The addition of Surface-active agents may increase wetting as well as solubility of
poorly soluble drugs
pg.367)
47. An In vitro-in vivo correlation establishes a relationship between a biological property

of the drug and physicochemical property of the drug product.
pg.380)
48. Antacids containing Aluminum, Calcium or Magnesium may form complex with drugs
such as tetracycline, ciprofloxacin etc. (Pg. 353)
49. The Trans membrane movement of drug is influenced by the composition & structure
of plasma membrane. (Page no: 325)
50. Cell membrane is composed of phospholipids in form of a bilayer interdispersed with
carbohydrates and proteins groups. (Page No 325)
51. Propranolol forms an ion pair with oleic acid to increase diffusion. (Page:336)
52. About 1500ml of saliva is secreted per day. (Page:337)
53. Enterocytes are intestinal absorptive cell that express transport protein. (Page no 332)
54. Mucin is a glycoprotein that lubricates food. (Page :337)
55. Saliva contains Ptyalin which digests Starches. (Page:337)
56. Stomach acid secretion is stimulated by gastrin and histamine. (Page:338)
57. The Transdermal type drug delivery system includes continuous release of drug over
the time. (Page no 355)
58. The colon lacks villi and has limited drug absorption due to lack of large surface area.
(Page no 339)
59. Celiac disease is an inflammatory disease affecting mostly the proximal small intestine.
(Page 352)
60. The Osmotic pump system is a drug product that contains a small hole from which
dissolved drug is released across a semi-permeable membrane by osmotic pressure.
(Page No: 349)
61. During the fasted or interdigestive state, alternating cycles of activity known as
migrating motor complex (MMC) act as a propulsive movement that empties the
upper GI tract to the cecum. ( pg no.340)
62. Large particles, including tablets and capsules, are delayed from emptying for 3 to 6
hours by the presence of food in the stomach ( pg no.342)
63. For intrathecal injection drug is injected into cerebrospinal fluids (page # 323)
64. The fasting pH of stomach is about 2 to 6. (Page# 338)
65. The fluid mosaic model proposed by Singer and Nicolson explains the Trans cellular
diffusion of polar molecules.
66. MDR1 is one of many proteins known as multidrug-resistance associated protein.
(page#331)
67. The enteral system consists of the alimentary canal from the mouth to the anus.(Page
337)
MULTIPLE CHOICE QUESTIONS
1. The disposition of a compound in a biological system involves:
a. Absorption
b. Distribution
c. Elimination
d. Both b and c
(Page No: 03)
2. The systemic absorption of a drug is dependent upon:
a. Physicochemical properties of the drugs

b. Nature of the drug products
c. Anatomy and physiologic functions at the site of drug absorption
d. All of above
(Page No: 321)
3. Burns will ______ the permeability of drug across the skin compared with normal
intact skin.
a. Decrease
b. Increase
c. No effect
(Page No: 322)
4. Fluid mosaic model explains the _________ diffusion of polar molecules:
a. Active
b. Passive
c. Trans cellular
d. None
(Page No: 326)
5. Burns will ______ the permeability of drug across the skin compared with normal
intact skin.
d. Decrease
e. Increase
f. No effect
(Page No: 322)
6. Fluid mosaic model explains the _________ diffusion of polar molecules:
e. Active
f. Passive
g. Trans cellular
h. None
7. Flux Is _________:
a. Rate of absorption
b. Rate of transfer
c. Rate of excretion
d. Rate of metabolism
(Page No: 327)
8. Weak acid will be rapidly absorbed from:
a. Small intestine
b. Large intestine
c. Stomach
d. Esophagus
(Page No: 329)
9. Small intestine transit time for healthy subjects ranges from:
a. 3 to 4 hours
b. 2 to 4 hours
c. 3 to 5 hours
d. 1 to 4 hours
(Page No: 337)
10. Some polar molecules may not be able to traverse the cell membrane but, instead ,
go through gaps , a process known as ____________
A. Carrier mediated diffusion
B. Para cellular drug diffusion
C. Passive diffusion
D. Active transport
11. Molecules in solution possess ___________ energy and constantly collide with one
another in space.
A. Electric energy B. Chemical energy C. Kinetic energy D. Heat energy
12. The rate of transfer of drug molecule is called

A. Passive diffusion
B. Active diffusion
C. Flux
D. Rate of Transfer
13. _____________ is the major absorption process for most drugs.

A. Active diffusion
B. Passive diffusion
C. Osmosis
14. Which statement is true about passive diffusion?

a. No external energy is expended
b. External energy is expended
c. Movement takes place against the concentration gradient
d. None of the above
15. If the drug has a low molecular weight and is_________, the lipid cell membrane is
not a barrier to drug diffusion and absorption
A. Lipophilic
B. Hydrophilic
C. Lyophilic
D. Lyophobic
16. In the brain, the ________ are densely lined with glial cells
A. Veins
B. Arteries
C. Nerves
D. Capillaries
17. In which disease condition plasma membranes of brain may be disrupted or become
more permeable to drug diffusion
A. Meningitis
B. Alzheimer
C. Parkinson
D. Schizophrenia
18. Most rapid drug absorption takes place from which part of the gastrointestinal tract?
A. Jejunum area of the small intestine
B. Large intestine
C. Duodenal area of the small intestine
D. All of the above
19. Ionized species of the drug are

A. Less water soluble B. More water soluble C. More lipid soluble D. Less lipid soluble
20. Carrier mediated transport is
A. Active transport
B. Passive transport
C. Facilitated transport
D. Both A & C
21. Active transport is characterized by ability to transport the drug

a. Against the concentration gradient
b. Along the concentration gradient
c. Both a and b
d. None of these
22. _______ transport is the process of engulfing particles or dissolved materials by the
cell.
A. Active
B. Passive
C. Vesicular
D. Influx
23. ___________refers to the engulfment of larger particles or macromolecules,

generally by macrophages
A. Pinocytosis
B. Phagocytosis
C. Exocytosis
D. Both A & B
24. The ____ route of administration is the most common and popular route of drug
dosing
A. Transdermal
B. Intravascular
C. Extravascular
D. Oral
25. The major physiologic processes that occur in the GI system are
A. secretion
B. digestion
C. absorption
D. All of above
26. Food constituents are mostly absorbed in the proximal area of the
A. Small intestine.
B. Large intestine
C. Stomach
27. ______ protect the linings of the lumen of the GI tract

A. Bile
B. Mucus
C. Pepsin
D. Electrolytes
28. Saliva is the main secretion of the oral cavity, and it has a pH of about
A. 7
B. 6
C. 8
D. 5
29. Saliva contains ptyalin (salivary amylase), which digests

A. Fats
B. Starches
C. Protein
D. All
30. How much saliva is secreted per day?

A. 1000 ml
B. 1500ml
C. 500ml
D. 700ml
31. The esophagus connects the ______ and the cardiac orifice of the stomach
A. Larynx
B. Pharynx
C. Intestine
32. The pH of the fluids in the esophagus is

A. 5
B. 6
C. 5-6
D. 6-7
33. ___________ sphincter prevents acid reflux from the stomach

A. Oesophageal
B. Gastric
C. Cardiac
D. Pyloric
34. Basic drugs are solubilized ___ in the presence of stomach acid
A. Slowly
B. Rapidly
C. At normal rate
35. The absorption of some antibiotics, such as penicillin and tetracycline, is _____ with
food
A. Increased
B. Decreased
C. Not effected
36. The solubility-PH profile is a plot of the solubility of the drug at various __________
values
A. Physiologic PH
B. Physiologic concentration
C. Both a and b
D. None of the above
37. Smaller particle enhances water penetration into the particles, and increases the
_____ rate
A. Disintegration
B. Dissolution
C. Absorption
Bio-pharmaceutic considerations in drug product design and In-Vitro drug product
performance.pg.367)
38. The effective surface area of a drug is increased enormously by a ___________ in

the particle size
A. Increase
B. Reduction
C. Enhancement
D. None of the above
performance.pg.367)
39. The addition of Surface active agents may increase wetting as well as _____
A. Disintegrants
B. Solubility of the drugs
C. Diluents
D. Binders
performance.pg.367)
40. If the drug is given _______, then conc. in GIT is greater than conc. In Plasma.
(Page 327)
A. IV
B. IM
C. Oral
D. S/C
41. Cell membranes are _______partitions that acts as selective barriers to the passage
of molecules. (Page: 325)
A. Permeable
B. Semi permeable
C. Non permeable
D. Partially permeable
42. In paracellular drug absorption, drug molecules smaller than ______ diffuse into the
tight junctions, or spaces between intestinal epithelial cells. (pg 329)
1. 500 MW C. 700 MW
B.600 MW D. 800MW
43. ……….. transporters move drug molecules into the blood and increase plasma drug
concentrations. (Pg#332)
A. Influx B. Efflux
C.Both D. None
44. Insulin injection is given: (Page No: 323)

A. Orally
B. Subcutaneously
C. Intravenously
D. Intramuscularly
45. Drug distribution and clearance are altered by: (Page No: 322)
A. Pathology
B. Genetic polymorphism
C. Drug – drug interactions
D. All of above
46. Rate of absorption is influenced by: (Page No: 327)

A. Lipid solubility
B. Surface area of membrane
C. Partition coefficient
D. All of above
47. In pinocytosis tiny incuppings called --------------- in the surface of cells close and then
pinch off to form pinosomes: (Chap 13, pg 336)
A. foldings
B. caveolae
C. cup folds
D. none
48. --------------- is a non-absorbable ion exchange resin for the treatment of
hyperlipidemia: (Chap 13, pg 353)
A. warfarin
B. cholestyramine
C. cimetidine
D. None
49. _____ types of pores were inferred to be present in membranes based on capillary
membrane transport studies. (Page:326)
a) 2 b) 3 c) 5 d) 10
50. ________ absorption is the process of drug movement across a cell. (Page: 325)
a) Passive
b) Transcellular
c) Active
d) Cell- mediated
51. Cell membranes are approximately _________ A® in thickness. (Page: 325)
a) 10 – 100
b) 4 – 10
c) 70 – 100
d) 5 – 10
52. The lipid bilayer or unit membrane theory is originally proposed by _____ .
(Page:325)
a) Davson and Danielle
b) Thomas Edison
c) Graham Bell
d) Einstein
53. Cell membranes are _______partitions that acts as selective barriers to the passage
of molecules. (Page: 325)
a) Permeable
b) Semi permeable
c) Non permeable
d) Partially permeable
54. The _________ model is proposed by Singer and Nicolson. (Page :326)
a) Fluid Mosaic Model
b) Physiological Model
c) Mammillary Model
d) Compartment Model
55. Plasma concentrations are often in ___________ range. (Page: 327)
a) ug/ml or ng/ml
b) ng/ml or mg/ml
c) mg/ml or ug/ml
d) kg/ml or ng/ml
56. Phagocytosis refers to the engulfment of _________ particles. (Page:335)
a) Larger
b) Smaller
c) Same
d) Different
57. The fasting pH of the stomach is about. (Page 338)
a. 2-6
b. 1-2
c. 2-3
d. 3-6
58. In the presence of food, the stomach pH is about______, due to hydrochloric acid
secreted by parietal cells. (Page 338)
a. 1.5 to 2
b. 2 to 3
c. 1 to 1.5
d. 2
CHAPTER 3
BIOAVAILABILITY AND BIOEQUIVALENCE
SHORT ANSWERS:
1. WHAT IS A MULTISOURCE DRUG PRODUCT?
A multisource drug product is a drug product that contains the same active drug substance in
the same dosage form and is marketed by more than one pharmaceutical manufacturer.
(PAGE-404)
(applied bio pharmaceutics and pharmacokinetics by Leon shargel sixth edition Chapter 15
Bioavailability and Bioequivalence , page 404)
2. DEFINE BIOAVAILABILITY?
Bioavailability means the rate and extent to which the active ingredient or active moiety is
absorbed from a drug product and becomes available at the site of action.
3. WHAT IS FDA GENERAL CRITERIA FOR THE PRODUCTS WHICH ARE

THERAPEUTICALLY EQUIVALENT?
(1) They are approved as safe and effective;
(2) They are pharmaceutical equivalents in that they
 Contain identical amounts of the same active drug ingredient in the same dosage
form and route of administration, and
 Meet compendia or other applicable standards of strength, quality, purity, and
identity;
(3) They are bioequivalent in that
 They do not present a known or potential bioequivalence problem, and they meet an
acceptable in-vitro standard, or
 If they do present such a known or potential problem, they are shown to meet an
appropriate bioequivalence standard;
(4) They are adequately labeled
(5) They are manufactured in compliance with Current Good Manufacturing Practice
regulations.
4. EXPLAIN PURPOSE OF BIOAVAILABILITY STUDIES?
The purpose of study is to determine the bioavailability and to characterize the

pharmacokinetics of the new formulation, new dosage form, or new salt or ester relative to a
reference formulation.
5. WHAT ARE ESSENTIAL PHARMACOKINETIC PARAMETERS FOR SINGLE AND

MULTI-DOSE ADMINISTRATION?
Essential pharmacokinetic parameters including:
 the rate and extent of systemic absorption,

 elimination half-life, and
 rates of excretion and metabolism, should be established after single- and multiple-
dose administration.
6. WHAT ARE BIOAVAILABILITY STUDIES?
Bioavailability studies are used to define the effect of changes in the physicochemical properties
of the drug substance, the formulation of drug and the manufacture process effect of the drug
product
7. WHAT ARE BIOEQUIVALENCE STUDIES?
Bioequivalence studies are used to compare the bioavailability of the same drug (same salt or
ester) from various drug products.
8. WHAT IS RELATIVE BIOAVAILABILITY AND ITS FORMULA?
Relative (apparent) availability is the availability of the drug from a drug product as compared to
a recognized standard.
When different doses are administered, a correction for the size of the dose is made, as in the
following equation:
Relative bioavailability= [AUC]A/DOSEA
[AUC]B/DOSEB
where drug product B is the recognized reference standard
9. WHAT IS ABSOLUTE BIOAVAILABILITY AND ITS FORMULA?
The absolute availability of drug is the systemic availability of a drug after extravascular
administration (eg, oral, rectal, transdermal, subcutaneous) compared to IV dosing.
10. Absolute Bioavailability after oral drug administration using plasma data can be
determined as follows:
Absolute bioavailability= F= [AUC]PO/[Dose]PO
[AUC] IV/[Dose]IV
11. ON WHICH PARAMETERS, DOES IN-VIVO BIOAVAILABILITY DEPENDS?
Following are the parameters on which in-vivo bioavailability depends:
 Concentration of the active drug ingredient in the blood,

 Cumulative urinary excretion rates
 Pharmacological effects
(Applied bio pharmaceutics and pharmacokinetics by Leon Shargel sixth edition Chapter 15
Bioavailability and Bioequivalence, page 407)
12. WHAT ARE THE OBJECTIVES OF BIOAVAILABILTY STUDIES?
Four main objective of this study:
 the ability to analyze the drug (and metabolites) in biological fluids,

 the pharmacodynamics of the drug substance,
 the route of drug administration, and
 the nature of the drug product
(Applied bio pharmaceutics and pharmacokinetics by Leon shargel sixth edition Chapter 15
13. WHAT ARE THE METHODS FOR ASSESSING BIOAVAILABILITY?
There are two types of methods for assessing bioavailability:
1. DIRECT METHOD
 Plasma drug concentration
2. INDIRECT METHOD
 Urinary drug excretion
 Clinical observations
 Acute pharmacodynamic effect
 In-vitro studies
14. WHICH FACTORS ARE STUDIED UNDER PLASMA DRUG CONCENTRATION?

 Time for peak plasma (blood) concentration (t max)
 Peak plasma drug concentration (C max)
 Area under the plasma drug concentration time curve (AUC)
15. WHAT DOES CMAX INDICATE?
C max, represents the maximum plasma drug concentration obtained after oral administration of
drug and it also indicates warning of possibly toxic levels of drug.
16. WHAT IS AUC, CMAX, TMAX ?

 AUC: area under the concentration-time curve  measure of the extent of bioavailability
• Cmax: the observed maximum concentration of drug  measure of both the rate of
absorption and the extent of bioavailability
• tmax: the time after administration of drug at which Cmax is observed  measure of the
rate of absorption
17. WHICH FACTORS ARE STUDIED UNDER URINARY DRUG EXCRETION?

 Cumulative amount of drug excreted in the urine (D u)
 Rate of drug excretion in the urine (dD u/dt)
 Time for maximum urinary excretion (t)
18. WHAT IS MEANT BY CUMULATIVE AMOUNT OF DRUG EXCRETED IN THE

URINE?
The cumulative amount of drug excreted in the urine, is related directly to the total amount of
drug absorbed. Experimentally, urine samples are collected periodically after administration of a
drug product. Each urine specimen is analyzed for free drug using a specific assay. A graph is
constructed that relates the cumulative drug excreted to the collection-time interval.
19. WHICH FACTORS ARE STUDIED UNDER ACUTE PHARMACODYNAMICS

EFFECT?
 Maximum pharmacodynamics effect (E max)
 Time for maximum pharmacodynamics effect
 Area under the pharmacodynamics effect time curve
 Onset time for pharmacodynamics effect
20. WHAT DOES IN VITRO IN VIVO CORRELATION (IVIVC) MEAN?

It means that the in-vitro drug dissolution rate should correlate with in-vivo drug bioavailability.
21. EXPLAIN IMPORTANCE OF ACUTE PHARMACODYNAMICS MODEL?
The use of an acute pharmacodynamics effect is to determine bioavailability. Bioavailability is

determined by characterization of the dose response curve. For bioequivalence determination,
pharmacodynamics parameters including the total area under the acute pharmacodynamics
effect time curve, peak pharmacodynamics effect, and time for peak pharmacodynamics effect
are obtained from the pharmacodynamics effect time curve. The onset time and duration of the
pharmacokinetic effect may also be included in the analysis of the data. The use of
pharmacodynamics endpoints for the determination of bioavailability and bioequivalence is
much more variable than the measurement of plasma or urine drug concentrations.
22. WHAT IS CROSSOVER STUDY?
Ten individuals are selected and given a test drug product, then collect blood samples and
calculate AUC. Then after washout period of two weeks when the drug is completely eliminated
from body, reference product is given to same individuals and collect blood samples and
calculate AUC to compare test product with reference one.
23. WHAT IS BIOEQUIVALENT DRUG PRODUCTS?
Pharmaceutical equivalent or pharmaceutical alternative products that display comparable

bioavailability when studied under similar experimental conditions is called Bioequivalent drug
products.
24. WHAT IS A GENERIC NAME? (Chap no.15, pg 441)

The established, nonproprietary, or common name of the active drug in the drug product is
called as generic name.
25. ABBREVIATED NEW DRUG APPLICATION (ANDA)
Drug manufacturers must file an ANDA for approval to market a generic drug product.
The generic manufacturer is not required to perform clinical efficacy studies or nonclinical
toxicology studies for the ANDA. ( pg no.441)
26. DIFFERENCE BETWEEN BIOEQUIVALENCE AND SAFETY/EFFICACY

STUDIES? Page 405
Ans: Bioequivalence studies must be performed on drug formulation proposed for marketing as
a generic drug product. Clinical safety and efficacy studies are not generally performed on
generic drug products.
27. What are the limitations of multi dose administration over single dose? (Page
421)
 Requires more time to complete.
 More difficult and costly to conduct(requiring prolonged monitoring of subjects)
 Greater problems with compliance control.
 Greater exposure of subjects to the test drug, increasing the potential for adverse
reactions.
28. . What are the important considerations to determine the urinary drug
excretion? (Pg#410)
1. Atleast 20% of a dose must be excreted unchanged in urine.
2. Fraction of drug entering the blood and being excreted intact must remain constant.
3. Collection of urine continues until all drug has been completely excreted.
29. Write the advantages of multi dose administration over single dose? (Page
420)
1) It eliminates the need to extrapolate the plasma concentration profiles to obtain the total
AUC after a single dose.
2) Eliminates the need for a long wash-out period between doses.
3) More closely reflects the actual clinical use of the drug.
4) Allows blood levels to be measured at the same concentration s encountered
therapeutically.
FILL IN THE BLANKS:
1. Bioavailability means the rate and extent to which the active ingredient or active
moiety is absorbed from a drug product and becomes available at the site of action
2. Bioavailability and bioequivalence can be considered as measure of drug product

performance in-vivo
Bioavailability and Bioequivalence , page (pg 403)
3. A generic drug product is a multisource drug product that has been approved by
FDA as therapeutic equivalent to innovator drug product.
4. Ideally, the in-vitro drug dissolution rate should correlate with in-vivo drug
bioavailability.
5. Bioequivalence studies are used to compare the bioavailability of the same drug from
various drug products.
6. The area under the drug concentration time curve (AUC) is used as a measure of the
total amount of unaltered drug that reaches the systemic circulation.
7. After IV administration of drug, F is equal to 1 0r 100 %
8. After oral administration of a drug, F may not exceed 100 % F>1(no drug absorption)
to 1 (complete drug absorption).

9. T max corresponds to the time required to reach maximum drug concentration after
drug administration.
10. At t max, peak drug absorption occurs and the rate of drug absorption exactly equals
the rate of drug elimination.
11. AUC is a measurement of the extent of drug bioavailability.
12. Pharmaceutical equivalent or pharmaceutical alternative products that display

comparable bioavailability when studied under similar experimental conditions is called
Bioequivalent drug products
13. The process of choosing or selecting the drug product in a specified dosage form is
Drug product selection.
14. A drug substance is the active pharmaceutical ingredient (API) or component in the
drug product that furnishes the pharmaco-dynamic activity.
15. Relationship in terms of bioavailability, therapeutic response, or a set of established

standards of one drug product to another is Equivalence.
16. The established, nonproprietary, or common name of the active drug in a drug product
is Generic name.
17. Drug products in identical dosage forms that contain the same active ingredient(s), ie,
the same salt or ester, are of the same dosage form, use the same route of
administration, and are identical in strength or concentration is Pharmaceutical
equivalents.
18. Drug products that contain the same therapeutic moiety but as different salts, esters,
or complexes is Pharmaceutical alternatives.
19. Different dosage forms and strengths within a product line by a single manufacturer
are pharmaceutical alternatives.
20. The process of dispensing a pharmaceutical alternative for the prescribed drug product
is Pharmaceutical substitution.
21. Pharmaceutical substitution generally requires the physician's approval.
22. Drug products containing different active ingredients that are indicated for the same
therapeutic or clinical objectives is Therapeutic alternatives.
23. Active ingredients in therapeutic alternatives are from the same pharmacologic class
and are expected to have the same therapeutic effect when administered to patients
for such condition of use.

24. Drug products are considered to be therapeutic equivalents only if they are
pharmaceutical equivalents and if they can be expected to have the same clinical
effect and safety profile when administered to patients under the conditions specified
in the labeling.
25. The process of dispensing a therapeutic alternative in place of the prescribed drug
product is Therapeutic substitution.
26. Bioavailability studies are performed for both approved active drug ingredients and
therapeutic moieties not yet approved for marketing by the FDA.
27. New formulations of active drug ingredients must be approved by the FDA before
marketing.
28. In approving a drug product for marketing, the FDA ensures that the drug product is
safe and effective for its labeled indications for use.
29. The drug product must meet all applicable standards of identity, strength, quality,
and purity.
30. The units of Cmax are concentration units (e.g., mg/mL, ng/mL).
31. Cmax is used as a surrogate measure for the rate of drug bioavailability. (Pg#408)
32. AUC is independent of route of administration. (Pg#409)
33. The changes to the marketed drug products are known as post approval changes.
(Pg#404)
34. Single-source drug products are usually brand-name (innovator) drug products. (403)
35. A drug substance is considered highly soluble when the highest dose strength is
soluble in 250ml of medium. (Pg#432)
36. A highly permeable drug should have extent of absorption >90%. (Pg#432)
37. An immediate release drug is considered rapidly dissolving when not less than 85% of
drug dissolves within 30 minutes. (Pg#432)
38. An objective of BCS is to determine pH-solubility profiles over a pH range of 1 to 8.
(Pg#431)
39. Comparative drug release/dissolution studies under certain conditions may give an
indication of drug bioavailability and bioequivalence. page.412
40. A non-replicate, parallel design is used for drug products that contain drugs that have
a long elimination half-life.
41. Bioequivalence studies are performed to compare the bioavailability of the generic
drug product to the brand-name product. (Page 414)
MULTIPLE CHOICE QUESTIONS:
1. Pharmaceutical equivalent or pharmaceutical alternative products that display

comparable bioavailability when studied under similar experimental conditions is called
a) Bioequivalent drug products c) Pharmaceutical drug products
b) Bioavailable drug products d) Therapeutic drug products
Bioavailability and Bioequivalence , page440)
2. A drug substance is the active pharmaceutical ingredient (API) or component in

the drug product that furnishes the .
a) Pharmacokinetic activity c) Drug product selection
b) Pharmacodynamic activity d) Bioequivalent drug product
3. Relationship in terms of bioavailability, therapeutic response, or a set of established

standards of one drug product to another is .
a) Generic name c) Similarity
b) Equivalence d) Substitution
4. The established, nonproprietary, or common name of the active drug in a drug product is
a) Generic name c) Similarity
b) Equivalence d) Substitution
5. Drug products in identical dosage forms that contain the same active ingredient(s), ie,
the same salt or ester, are of the same dosage form, use the same route of
administration, and are identical in strength or concentration is.
a) Pharmaceutical equivalents c) Therapeutic equivalent
b) Pharmaceutical alternatives d) Therapeutic alternative
6. Different dosage forms and strengths within a product line by a manufacturer

are pharmaceutical alternatives.
a) Single c) Double
b) Multiple d) none of these
7. The process of dispensing a pharmaceutical alternative for the prescribed drug product
is
a) Pharmaceutical substitution c) Therapeutic equivalent
b) Pharmaceutical alternatives d) Therapeutic alternative
8. Drug products containing different active ingredients that are indicated for the same
therapeutic or clinical objectives is.
a) Therapeutic alternatives c) Pharmaceutical alternatives
b) Pharmaceutical substitution d) Therapeutic equivalent
9. Active ingredients in therapeutic alternatives are from the same pharmacologic class and
are expected to have the therapeutic effect when administered to patients for such
condition of use.
a) Equal c) Different
b) Same d) None
10. Drug products are considered to be only if they are pharmaceutical

equivalents and if they can be expected to have the same clinical effect and safety
profile when administered to patients under the conditions specified in the labeling.
b) Pharmaceutical substitution d) Therapeutic equivalent
11. The process of dispensing a therapeutic alternative in place of the prescribed drug
product is .
b) Pharmaceutical substitution d) Therapeutic substitution
12. Are performed for both approved active drug ingredients and therapeutic
moieties not yet approved for marketing by the FDA.
a) Bioavailability studies c) Pharmaceutical studies
b) Bioequivalence studies d) None
13. New formulations of active drug ingredients must be approved by the FDA
marketing.
a) After c) Before
b) None
14. In approving a drug product for marketing, the FDA ensures that the drug product is
and effective for its labeled indications for use.
a) Pure c) Filtered
b) Safe d) none
15. The drug product must meet all applicable standards of identity, strength, quality, and
a) Purity c) accuracy
b) Safety d) None
16. studies are also performed for new formulations of active drug ingredients
or therapeutic moieties that have full NDA approval and are approved for marketing.
a) In-vitro bioavailability c) Both
b) In-vivo bioavailability d) None
Bioavailability and Bioequivalence, page405)
17. Purpose of is to characterize the pharmacokinetics of the new

formulation, new dosage form, or new salt or ester relative to a reference formulation
a) Bioavailability Studies c) Both
b) Bioequivalence Studies d) None
18. studies are used to compare the bioavailability of the same drug (same
salt or ester) from various drug products.
a) Bioavailability c) both
b) Bioequivalence d)none
19. Bioavailability and bioequivalence can also be considered as performance measures of

the drug product .
a) In-vivo c) none
b) None d) both
20. The drug is considered to be completely available after ____.

a) SC administration b) IV administration c) IM administration d) IA administration
21. “F” is the fraction of the.

a) Drug eliminated c) Drug absorbed
b) Drug excreted d) None
22. Each urine specimens is analyzed for free drug using a specific _____. (Page 410)
a) Formula b) Method c) Assay d) None of the above

23. The cumulative amount of drug excreted in urine is _________ to the total amount of
drug absorbed.
a) Inversely proportional b) Indirectly proportional c) Directly proportional d) All of the

above
24. Urinary drug excretion data is an indirect method for estimating _______
a) Bioavailability b) Bioinformatics c) Biotransformation d) Biopharmaceutics
25. ______________ is the availability of the drug from a drug product as compared to
recognized standard
A. Bioavailability
B. Absolute availability
C. Relative availability
D. Both b and c
26. Plasma drug concentration is ------------ for estimation of bioavailability…page.408

A. Direct method
B. Indirect method
C. False
D. All Above
27. Post approval changes are often termed as Page 404

A. SUPAC
B. SUPAK
C. SOP
D. none
28. Comparator brand name product must be …….. Equivalent with generic drug product
(Page 404)
A. Pharmaceutically
B. bioequivalent
C. Therapeutically
D. All of the above
29. The area under the curve is used as measure of the total amount of___________ that
reaches systemic circulation.
A. Metabolized drug
B. Altered drug
C. Unaltered drug
D. None
30. When AUC is not directly proportional to _____, bioavailability is difficult to evaluate.
(Page: 410)
A. Time
B. Temperature
C. Dose
D. AUC
CHAPTER 4
BIOPHARMACEUTIC CONSIDERATIONS IN DRUG PRODUCT DESIGN

& IN-VITRO DRUG PRODUCT PERFORMANCE
Q. Short answers.
1. Define biopharmaceutics. Pg# 361
The study of the physicochemical properties of the drug and the drug product, in vitro, on the
bioavailability of the drug, in vivo to produce a desired therapeutic effect.
2. What are the steps for oral drug absorption? Pg# 361
Oral drug absorption involves at least three distinct steps:
I. Drug release and dissolution from the drug product

II. Permeation of drug across the gIT lining
III. Drug disposition during gIT transit.
3. What are the aims and objectives of biopharmaceutics? Pg# 361
The aim of biopharmaceutics is to adjust the delivery of the drug from the drug products in such
a manner as to provide optimal therapeutic activity and safety for the patient.
4. What are the factors that influence the systemic absorption of a drug? Pg# 363
The systemic absorption of a drug from an extravascular site is influenced by the anatomic and
physiological properties of the site and the physicochemical properties of the drug and the drug
product.
5. How the bioavailability of the drug changes by changing the route of its
administration? Pg# 363
By choosing the route of the drug administration carefully and properly designing the drug
product, the bioavailability of the active drug can be varied from rapid and complete absorption
to slow, sustained rate of absorption or even virtually no absorption, depending on the
therapeutic objective.
6. What is meant by rate limiting step? Pg# 363
The slowest step in a series of kinetic processes is called the rate limiting step.
7. Which solid drug products are exempted from disintegration testing? Pg# 364
Solid drug products exempted form disintegration testing include troches, tablets that are
intended to be chewed and drug products intended for sustained release or prolonged or repeat
action.
8. Define complete disintegration. Pg# 364
According to USP-NF:
“The state in which any residue of the tablet, except fragments of insoluble coating,
remaining on the screen of test apparatus in the soft mass have no palpably firm core is known
as complete disintegration.”
9. Why we add buffering agents in the controlled release formulations? Pg# 366
Buffering agents may be added in the controlled release formulations to slow or modify the
release rate of a fast dissolving drug.
10. Write some functional properties of excipients. Pg# 368
Some of the functional properties of the excipients are:
I. to improve the compressibility of the active drug

II. to stabilize the drug against degradation
III. to decrease gastric irritation
IV. to control the rate of drug absorption from absorption site
V. to increase drug bioavailability
11. What is meant by “sink conditions”? Pg# 373
Sink conditions is the term referring to an excess volume of medium that allows the solid drug to
dissolve continuously.
12. What is the main disadvantage of USP apparatus 1(Rotating basket)? Pg# 374
A disadvantage of the rotating basket is that the formulation may clog to 40 mesh screen.
13. What is the function of sinker in apparatus 2? Pg# 375

A sinker such as a few turns of platinum wire may be used to prevent a capsule or tablet from
floating. It may also be used for the film coated tablets that stick to the vessel walls or to help
position the tablet or capsule under the paddle.
14. Define intrinsic dissolution. Pg# 377
The dissolution of a drug powder by maintaining a constant surface area is called intrinsic
dissolution. It is usually expressed as mg/cm2/min.
15. What are the causes for poor disintegration of the compressed tablets? Pg# 369
Poor disintegration of a compressed tablet may be due to high compression of tablets without
sufficient disintegration.
16. What is disadvantage of basket type dissolution apparatus? Pg# 379
Basket type apparatus is sensitive to clogging due to gummy materials. Pieces of small particles
can also clog the basket screen and create local non-sink condition for dissolution.
17. Which type of dissolution method is used in absence of In-vivo data? Pg# 379
In absence of In-vivo data selection of dissolution method is based on type of drug product to be
tested.
18. On what factors in vitro dissolution characteristics depend upon? Pg# 384
Dissolution characteristics depend upon physical properties of active pharmaceutical ingredient,

drug formulation, hydrodynamics of dissolution apparatus and dissolution medium.
19. What are three components of dissolution system? Pg# 378
Dissolution is a complex system that mainly comprises of 3 components
I. analyst
II. dissolution apparatus
III. analytical procedure
20. What does the term “shelf life” means? Pg# 387
Shelf life is the time period during which a drug product is expected to remain within the
specifications under specified storage conditions.
21. What is IVIVC? Pg#380
An in- vitro in vivo correlation establishes a relationship between a biological property of drug
i.e. pharmacodynamics effect or plasma drug concentration and physicochemical property of
drug product containing a drug substance I.e. dissolution rate.
22. What does therapeutic considerations mean? Pg# 387
Therapeutic considerations include the desired pharmacodynamics and pharmacologic

properties of drug, including desired therapeutic response and type and frequency of adverse
reactions to drug.
23. Which formulation is preferred for acute illness? Pg# 387
Oral formulations having quick release, absorption and onset. If more rapid absorption is
needed injectable formulations are preferred.
24. What does therapeutic window determines? Pg# 388
Therapeutic window determines desired or target plasma drug concentration that will be
effective with minimal adverse effects. Drug concentration higher than minimum toxic
concentration may cause more intense pharmacodynamics and/or adverse events. Drug
concentration below minimum effective concentration may be sub therapeutic.
25. Why dosing frequency is necessary? Pg#389
Dosing frequency is related to clearance of drug and the target plasma drug concentration. If
pharmacokinetics show that drug has short duration of action due to short elimination half-life or
rapid clearance from body, drug must be given more frequently or given in extended release
drug product.
26. What is level A Invitro Invivo correlation? (pg.380)
It is highest level of correlation and represents a point to point correlation between Invitro
dissolution and Invivo absorption rate of drug from the dosage form.
27. What is class 1 drug according to BCS system? (pg.383)

According to biopharmaceutics drug classification system class 1 drugs are those drugs that are
highly soluble and highly permeable.
28. What are factors that cause poor patient drug compliance? (pg.389)
Poor patient compliance result due to poor product attributes such as difficulty in swallowing,
disagreeable odor, bitter medicine taste, or two frequent and/or unusual dosage requirements.
29. How total size of drug product is determined? (pg.388)

Total size of drug product is determined by dose of the drug and any additional excipients
needed to manufacture desired dosage form.
30. How drug degradation at low PH could be avoided? (pg.388)

The addition of buffering in formulation or use of enteric coating on dosage form will protect drug
from degradation at low PH.
31. What are important physicochemical properties of drug? (pg.387)

Important physicochemical properties of drug are solubility, stability, chirality, impurity/purity
profile.
32. What are some biopharmaceutical considerations in drug product design?

Following are some biopharmaceutical considerations
 Pharmacodynamics considerations
 Therapeutic objective
 Toxic effects
 Adverse reactions
 Physicochemical properties of drug
 Drug product considerations
 Pharmacokinetics of drug
 Bioavailability of drug
 Route of administration
 Desired drug dosage form
 Desired dose of drug
 Compliance and acceptability of drug product
 Cost
 Manufacturing considerations
 Availability of raw material
 Stability
 Quality control
 Method of manufacturing
33. Enlist some common excipients used in solid dosage forms. (Page:368)
Ans: Common Excipients Used in Solid Drug Products
 Lactose -Diluent
 Dibasic calcium phosphate - Diluent
 Starch – Disintegrant, diluent
 Microcrystalline cellulose - Disintegrant, diluent
 Magnesium stearate - Lubricant
 Stearic acid - Lubricant
 Hydrogenated vegetable oil - Lubricant
 Talc – Lubricant
34. Enlist Dissolution Apparatus mentioned in Pharmacopoeia. (Page:372)

Ans: These include:
 Apparatus 1 - Rotating basket – Tablets

 Apparatus 2 – Paddle - Tablets, capsules, modified drug products, suspensions
Apparatus 3 - Reciprocating cylinder - Extended-release drug products
 Apparatus 4 - Flow cell - Drug products containing low-water-soluble drugs
Apparatus 5 - Paddle over disk - Transdermal drug products
 Apparatus 6 – Cylinder - Transdermal drug products
 Apparatus 7- Reciprocating disk - Extended-release drug products
 Rotating bottle (Non-USP-NF) - Extended-release drug products (beads) Diffusion
cell (Franz) (Non-USP-NF)- Ointments, creams, transdermal drug products
35. What are the biopharmaceutical considerations for eye medication?

(Page:362)
An eye medication may require special biopharmaceutical considerations, including appropriate
pH, isotonicity, sterility, local irritation to the cornea, draining by tears, and concern for systemic
drug absorption.
Fill in the blanks.
1. A primary concern in biopharmaceutics is the bioavailability of drugs. (Pg #361)

2. The aim of biopharmaceutics is to adjust the delivery of drug from the drug product in
such a manner as to provide optimal therapeutic activity and safety for the patient.
(Pg #361)
3. Drug products include the active drug substance combined with excipients that
make up the dosage form. (Pg# 362)
4. For many commercial drug products, the dose is determined based on average body
weight. (Pg #363)
5. Biopharmaceutic considerations determine the ultimate dose and dosage form of
the drug product. (Pg# 363)
6. The slowest step in the series of kinetic processes is called rate limiting step. (Pg#
363)
7. The drugs with poor aqueous solubility, dissolution is the rate limiting step. (Pg
#364)
8. The drugs with high aqueous solubility, dissolution is rapid and permeability is the
rate limiting step. (Pg# 364)
9. Dissolution is the process by which a solid drug substance becomes dissolved in a
solvent. (Pg#364)
10. Solubility is the mass of solute that dissolves in a specific mass or volume at a
given temperature. (Pg #364)
11. By increasing the thickness of the stagnant layer, dissolution of the drug decreases.
(Pg# 365)
12. Noyes and Whitney studied the rate of dissolution of solid drugs. (Pg # 365)
13. The dissolved drug in the saturated solution, known as the stagnant layer. (Pg
#365)
14. The increase in temperature will increase the kinetic energy of the molecules and
increase the diffusion constant. (Pg# 365)
15. Intravenous solution are difficult to prepare with drugs that have poor aqueous
solubility (pg 366)
16. A basic drug is more soluble in an acidic medium, forming a soluble salt (Pg# 366)
17. pKa and pH profile are necessary for optimal stability and solubility of the final
product. (Pg# 366)
18. The stability pH profile is a plot of the reaction rate constant for drug degradation
versus pH (Pg #366)
19. Amorphous forms are non-crystalline forms. (Pg# 367)
20. Polymorphs have same chemical structure but different physical properties. (Pg
#367)
21. Some drugs may interact with solvent during preparation to form a crystal called a
solvate. (Pg# 368)
22. Sucrose solution may act as a granulating agent in the dosage form. (Pg# 368)
23. Larger drug particles have a smaller surface area and dissolve more slowly than
smaller particles. (Pg# 369)
24. Drug dissolution studies are often use for monitoring drug product stability and
manufacturing process control (Pg#371)
25. The choice of apparatus and dissolution medium are based on physiochemical
characteristics of API and the type of dosage form. (Pg #371)
MCQs.
1. Excipients are considered -------------- with respect to pharmacodynamics activity:
a) Inert
b) Reactive
c) Partial Inert
d) None of these
(Page No: 362)
2. For many commercial drug product, the dose is determined based on average
------------.
a) Body surface area
b) Body weight
c) Condition of patient
d) Both A & C
(Page No: 363)

3. For drugs that have poor aqueous solubility, the rate limiting step is:
a) Permeation
b) Disintegration
c) Dissolution
d) None of these
(Page No: 364)
4. The USP disintegration apparatus, the beaker used has-------- capacity of fluid.
a) 500mL
b) 700mL
c) 800mL
d) 1000mL
(Page No: 364)
5. Solubility is ----------- property.
a) Static
b) Dynamic
c) Partial Dynamic
d) May be static or dynamic
(Page No: 365)
6. The stability of solution is often affected by ----------- of vehicle.
a) Formulation
b) pH
c) Temperature
d) All of these
(Page No: 366)
7. Turbulence can create increased agitation resulting in a higher:
a) Absorption rate
b) Dissolution rate
c) Elimination rate
d) None of the above
(Page No: 379)
8. The _______ method is less sensitive to the tilting effect:
e) Paddle method
f) Oscillating method
g) Basket method
h) All of above
(Page No: 379)
9. __________ correlation is the highest level of correlation and represents a point to point
relationship between an in vitro dissolution and the in vivo input rate of the drug from the
dosage form:
a) Level C
b) Level A
c) Level B
d) Level D
(Page No: 380)
10. Solubilization of aspirin may be increased by addition of -----------------:
a) Acidic buffer
b) Basic buffer
c) Partial acidic
d) Partial basic
(Page No: 366)

11. In a study on aspirin absorption, dissolution medium selected was:
e) Simulated intestinal fluid
f) Distilled water
g) Simulated gastric juice
h) None
(Page No: 383)
12. Erythromycin tablets are ---------------- coated protect against degradation in stomach.
a) Film coated
b) Sugar coated
c) Enteric coated
d) None of these
(Page No: 367)
13. The dissolution test is important ----------------- procedure used to confirm batch to batch
reproducibility:
a. Chemical test
b. Physical test
c. Quality control test
d. Both A & B
(Page No: 370)
14. Some polymorphs are --------------- & may convert into more stable state over time:
a. Unstable
b. Already Stable
c. Metastable
d. Partial Unstable
(Page No: 368)

15. Excipient is added for formulation to enhance -------- & ----------of drug absorption.
a. Stability and strength
b. Stability and extent
c. Rate and extent
d. None
(Page No: 369)
16. In vitro drug dissolution studies are often used to monitor --------------- and manufacturing
process control:
a. Drug reproducibility
b. Drug product stability
c. Drug chemical properties
d. Rate of dissolution
(Page No: 371)
17. A sinker is used in -------------- type of tablets
a. Enteric coated
b. Film coated
c. Sugar coated
d. None
(Page No: 375)
18. Intrinsic dissolution is expressed as:
a) g/cm2/min
b) mg/cm3/min
c) mg/cm2/min
d) All
` (Page No: 377)
19. The reciprocating frequency in reciprocating disk apparatus is ---------:
a) 20 cycles per min
b) 25 cycles per min
c) 30 cycle per min
d) 37 cycles per min
(Page No: 376)
20. Level C correlation is:
e) Not statistical
f) Useful in formulation selection
g) Useful in formulation development
h) All of above
(Page No: 381)
21. _________ is a predictive approach to relate certain physicochemical characteristics of a

drug substance and drug product to in vivo bioavailability:
a) DCS
b) BCS
c) MCS
d) Both A and B
(Page No: 383)
22. In vitro dissolution characteristics are dependent on:
a) Physical properties of API

b) Drug formulation
c) Dissolution medium
d) All of above
(Page No: 384)
23. __________ is a logarithmic reciprocal square root transformation of the sum of squared
error:
a) Difference factor
b) Similarity factor
c) Both
d) None
(Page No: 386)
24. The prime considerations in the design of drug are:

a) Therapeutic objective
b) Safety
c) Efficacy
d) All of above
(Page No: 387)
25. The size of dose in drug product is based on:
a) Potency of drug
b) Apparent volume of distribution
c) Both a and b
d) None
(Page No: 388)
26. A primary concern in Biopharmaceutics is the ______ of drugs. (Page :361)
a) Toxicity
b) Response
c) Mechanism of Action
d) Bioavailability
27. The slowest step in series of kinetic processes is called _____. (Page :363)
a) Rate limiting step
b) Slowest step
c) Fastest step
d) % yield
28. Solid drug products exempted from disintegration tests includes : (Page :364)
a) Troches
b) Chewable tablets
c) Sustained release
d) All
29. The dissolved drug in the saturated solution is known as __________. (Page:365)
a) Condensate layer
b) Stagnant layer
c) Surface Tension
d) None
30. In dissolution test, agitation or stirring rate is held to ____ RPM. (Page: 365)
a) 70
b) 75
c) 47
d) 82
31. __________ has several crystal forms when given orally as a suspension. (Page:367)
a) Cephalosporin
b) Macrolides
c) Chloramphenicol
d) Penicillin
32. ______ agents may be added to slow or modify the release rate of fast dissolving drugs.
(Page:366)
a) Suspending
b) Emulsifying
c) Buffering
d) Surface active
33. The geometric shape of the particles also affects ______. (Page:367)
a) Particle size
b) Surface area
c) pH
d) disintegration
34. Reduction of particle size by _____ to micronized form has improved the oral absorption of
drugs. (Page:367)
a) Milling
b) Grinding
c) Sieving
d) Agitation
35. ________ are added to the formulation to provide certain functional properties to the
dosage form. (Page:368)
a) Lubricants
b) Glidants
c) Excipients
d) Disintegrants
36. Coatings particularly ___________ will crosslink upon aging and decrease the dissolution
rate. (Page :369)
a) Shellac
b) Enteric
c) Film
d) Sugar
37. Tetracycline is formulated with calcium carbonate, an insoluble complex of _______ is
formed. (Page:369)
a) Calcium carbonate
b) Calcium salicylate
c) Calcium phosphate
d) Calcium hydroxide
38. Poor disintegration of a compressed tablet may be due to ________ of tablets without
sufficient disintegrant. (Page:369)
a) Low compression
b) High compression
c) High temperature
d) Low temperature
39. For transdermal drug products, the recommended temperature is ____’C. (Page:373)
a) 37
b) 35
c) 32
d) 30

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BIOPHARMACEUTICS-I

OBJECTIVES OF CHAPTER 1, 2, 3 & 4

2. How can you define drug product performance?

Biopharmaceutics is the science that examines this interrelationship of the physicochemical

Bioavailability is a measure of systemic availability of a drug.

5. What are the major factors discussed in biopharmaceutics?

Biopharmaceutics involves following factors that influence

 The design of drug product.

8. Define drug disposition?

9. What are the important biopharmaceutical considerations in drug product design?

Following are the important biopharmaceutical considerations in drug product design:

4-Drug dosage and dosage regimens

5-type of drug product

10. Define pharmacodynamics

11. What is the drug response?

12. What is the difference between invasive and non-invasive methods?

13. What is clinical toxicology?

14. What is the significance of pharmacokinetic models?

Pharmacokinetic models are used to:

2. Calculate the optimum dosage regimen for each patient individually

3. Estimate the possible accumulation of drugs and/or metabolites

4. Correlate drug concentrations with pharmacologic or toxicologic activity

5. Evaluate differences in the rate or extent of availability between formulations (bioequivalence)

7. Explain drug interactions

15. What is a compartment?

A compartment is not a real physiologic or anatomic region but is considered as a tissue or

16. Define bioequivalence:

17. Define generic equivalence.

18. What are therapeutic equivalent drugs?

19. What does MEC and MTC represents ?

20. Define drug delivery systems.

21. Differentiate between mammillary and catenary model…….(ch:1, page:13)

Answer: Mammillary model consists of one or more compartments around a central

23. How does the pharmacokinetics change from linear to non-linear?

24. Define pharmaceutical equivalents.

25. What is clinical pharmacokinetics?

Clinical pharmacokinetics is the application of pharmacokinetic methods to the drug therapy.

26. What is meant by toxicokinetics?

Toxicokinetics is the application of pharmacokinetic principles to the design, conduct and

27. What is a model?

FILL IN THE BLANKS:

5. Biopharmaceutics examines the interrelationship of the physical/ chemical properties of

7. Bioavailability is a measure of systemic availability of a drug.

11. elimination of the drug involves excretion and metabolism

19. Pharmacokinetic-pharmacodynamics models are constructed to relate plasma drug level

20. Toxicokinetics is the application of pharmacokinetic principles to the design, conduct,

23. The AUC is related to the amount of drug absorbed systemically.

24. The therapeutic window is concentration between MEC and MTC

28. Drug concentration can be correlated to pharmacological/toxicological activity by

MULTIPLE CHOICE QUESTIONS:

a) Minimum effective concentration (MEC)

a-dosage form C-drugs

A-drug product performance C-pharmacokinetics

5. Biopharmaceutics involves the factors that influence:

a) Design of the drug product

7. ______ a measure of systemic availability of a drug.

a-bioavailabilty c-drug concentration

8. bioavailability may differ from ____________________

a- one drug product to another containing b-one drug product to another

9. drug distribution and elimination are often termed _____

10. elimination of the drug involves _____________

a-excretion and metabolism c-metabolism

11. methods involving human subjects or laboratory animals are _____