Subject: Pharmacology Lab CAGAYAN STATE UNIVERSITY

Topic: Nature, Sources, and Dosage Forms

Lecturer: Dr. Calban  Drug structures are reconfigured to decrease reported
Date: September 7, 2018 drug reactions.
 Ex. Asthma use to be treated with Theophylline, which has
a narrow therapeutic index. Increasing the dose carries the
OUTLINE risk of causing adverse reactions. At present, Salbutamol, a
I. DRUG AND MEDICINE bronchodilator and beta agonist with far fewer adverse
II. HISTORY OF MEDICINE reactions is used. Theophylline is reserved as a third-line
III. FACTORS THAT TRIGGER DRUG DEVELOPMENT asthma medication
IV. FUTURE
o Lower efficacy
V. SOURCES OF DRUGS
A. PLANT DRUGS  Ex. In treating gastric ulcers, proton pump inhibitors
B. ANIMAL DRUGS (Omeprazole, Lansoprazole) are used instead of H2
C. MINERAL DRUGS blockers and antacids because they have a stronger effect.
D. SYNTHETIC DRUGS o Narrow spectrum
VI. DOSAGE FORMS  Ex. Amoxicillin (broad-spectrum antibiotic) vs. Cloxacillin
A. DROPS VS SUSPENSION VS CAPSULE and Penicillin (narrow-spectrum antibiotics)
VII. BIOPHARMACEUTICAL FACTORS o Narrow therapeutic window
VIII. THE NEED FOR DOSAGE FORMS
o Drug Resistance
IX. ROUTES OF ADMINISTRATION
A. CO‐AMOXICLAV VS OFLOXACIN VS CHLORAMPHENICOL  Ex. Streptomycin and quinolones are given to multi-drug
B. ROLE OF EXCIPIENTS resistant case of tuberculosis.
C. SOLID PREPARATIONS
D. SEMISOLID PREPARATIONS II. SOURCES OF DRUGS
E. LIQUID PREPARATIONS  60% of drugs pre-approved are from natural sources
F. AEROSOL
 15% of biologicals (vaccines and antibodies)
G. PARENTERAL PREPARATIONS
H. DOSAGE FROMS WITH LOCAL EFFECTS  80% of antibiotics
 Sources of drugs include:
o Plants
I. HISTORY OF DRUG DEVELOPMENT o Animals
o Microbes
REMEMBER: All medicines are drugs, but not all drugs are o Minerals
medicines.
A. Plants
A. Definition of Terms
 500,000 natural products are from plants
 Drug
o A chemical substance that has known biological effects on  160,000 products are being used worldwide
humans and other animals  Half of the 100,000 new metabolites that are currently being
studied are from plants
 Medicine
o A drug taken to cure and/or ameliorate any symptom of an o The other half of which come from microbes
illness or medical condition, or may be used as preventive  Presently, on a small fraction of plant-derived drugs are utilized in
medicine that has future benefits but does not treat any mainstream or Western medicine.
existing or pre-existing diseases or symptoms  Plant sources that are classified according to their physico-
chemical properties include:
B. History of Drug Development
o ALKALOIDS- basic organic substances containing carbon,
hydrogen, nitrogen, and oxygen; occur in almost all parts of
plants but are most found in seeds, roots and leaves.
- Atropine – for treatment of organophosphate poisoning
and reversal of cholinergic crisis
- Vinblastine or vincristine – chemotherapeutic agents
- Quinine – anti-malarial drug
- Colchicine – used to treat inflammation in gout
- Morphine – used as a pain reliever

o GLYCOSIDES – ether-like combinations of sugar with some

 Potions and mixtures of herbal remedies are still used in Eastern other organic substances mostly used for cardiac disorders,
Medicine (Chinese, Ayurvedic). especially arrythmias.
- Digoxin
- Ouabain
o OILS
Improvements in biotechnology, however, along with evidence- - Castor oil – used as a laxative
based medicine, have ushered in an increase in drug discoveries - Peppermint and spearmint oils – used as antiseptics and
and drug development. gargles
Factors contributing to drug discovery:
o New diseases/new strains of microorganisms o GUMS and RESINS – mixed in ointments for burns; most are
o Adverse reactions used as cathartics
/dokmark
 o Gums
- secretory products from plants
 Carbohydrates that absorb water and swell to form
thick mucilaginous colloid solutions
 A polysaccharide that can cause a large viscosity
increase in solution
 Gum acacia, gum tragacanth
o Resins
- Rosin-like substance usually formed by the oxidation
of volatile oils
- A viscous fluid composed of volatile fluid terpenes
with less components dissolved non-volatile solids
- Produced by most plants
 Pine rosin, franckincense
B. Animals
 Thyroid hormones – extracted from pigs (porcine); used to cure
hypothyroidism
 Insulin – used to be extracted from pigs and horses before human
insulin became available. Human insulin is preferred as it results in
less hypersensitivity reactions
 Cortisone- side effect: Hypersensitivity reactions
C. Microbes
 Penicillium- Penicillin as antibiotic
 Streptomyces- Streptomycin for multi-drug resistant TB
 Cephalosporium- Cephalosporins as antibiotic
D. Minerals
 Iron- for anemic and pregnant women
 Copper
 Iodine- for thyroid disorders
 Magnesium- antacid
 Aluminum - antacid
III. DOSAGE FORMS
 Pharmaceutical products in the form in which they are marketed
for use, typically involving a mixture of active drug components
and excipients along with other non-reusable material that may
not be considered either ingredient or packaging (e.g. capsule
shells)
A. Factors to Consider in Dosage Form Selection
 PHARMACOKINETICS – liberation, absorption, distribution,
metabolism, excretion (what the body does to the drug)
 PHARMACODYNAMICS – effects of drugs in the body or organisms
inside the body, mechanism of drug action and relationship
between concentration and effect (what the drug does to the
body)
 AGE AND SEX- eg. Pediatric patient unable to swallow tablet and
capsules, Vaginal Suppositories and douches, as well as
contraceptive pills are specific for females.
 DISEASE PROCESS – severity and duration, response to treatment,
co-morbid conditions.
 eg. Should I admit this patient because of the progression of the
infection? Is the use of parenteral antibiotic already warranted In
this case? Consider severity and duration of the disease and
response to treatment.
 A px with tonsillitis who find it painful and difficult to swallow may
be able to tolerate a liquid antibiotic better than a capsule or
tablet.
 If a px has malabsorption syndrome or hyperacidity, oral drugs
should not be given due to non-absorption and fast degradation,
respectively.
B. Pharmaceutical Formulation
 Process in which different chemical substances, including the
active drug, are combined to produce a final medicinal product
C. Excipients
 Inactive substances formulated alongside the active ingredient of a
medication, for the purpose of bulking-up formulations that
contain potent active ingredients
o Serves to bulk up substances (eg. Most commonly used fillers
are sugars, CaCo3, and Magnesium
o Therapeutic enhancing purpose
o Useful in the manufacturing of the substance
 Classifications:
o ANTIADHERENTS – so as not to stick to the tablet press (eg.
Magnesium stearate)
o BINDERS – keep the granules together (eg. Saccharides,
sorbitol, gelatin, polyethylene glycols[PEG])
o COATINGS – smoothens the dosage form and makes it more
stable; also increases shelf life (eg. Hydroxypropyl methyl
cellulose[HPMC])
o DISINTEGRANTS – aid in breaking down the medication once
it is in the body (eg. Carboxymethyl cellulose[CMC], sodium
starch glycolate)
o FILLERS – ex. Lactose, sucrose, glucose, mannitol, sorbitol,
calcium carbonate, magnisium stearate
o COLORS– are used for easy identification of tablets and
capsules (eg. Silfenafil- Viagra is a blue tablet in the shape of a
diamond)
o LUBRICANTS – function as anti-adherents, and are helpful in
drug manufacturing ex. Talc, silica fats, stearic acid
o SORBENTS
o PRESERVATIVES– for prolonged shelf life of drugs (eg.
Vitamins A, C, E, selenium, cysteine, methionine, citric acid, Na
citrate)
o FLAVORS/SWEETENERS – are added to tasteless substances,
so children will find the medicine likeble to mask unpleasant
taste. (eg. If drug is bitter: mint, cherry; If drug is salty: peach
or apricot; If drug is sour: raspberry)
D. Routes of Administration
 ENTERAL – oral: most common and easiest to administer
- enteral nutrition (gastric and duodenal feeding tubes via
NGT)
- rectal
 PARENTERAL – intravenous, intraosseous, intramuscular,
intracerebral, intrathecal, subcutaneous, intradermal, intra-
articular, intravitreal (eg. Monoclonal antibodyes are used for
blinding diseases such as diabetic retinopathy and age related
macular degeneration, and are injected into the vitreous body),
intraperitoneal (eg. For px on intraperitoneal dialysis who need
antibiotics; must be administered by trained personnel)
 TOPICAL – dermal, transmucosal, sublingual or buccal (e.g.catapres
or clonidine which are anti-HPN), nasal (decongestant sprays),
eye(opthalmic drops), ear, inhalational(for asthma, or as
anesthesia)
IV. TYPES OF DOSAGE FORMS: SOLIDS
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 Available forms:  Disadvantages:
o Powder- such as those used in inhalers for asthmatics o Not suitable for highly soluble substances like potassium
o Tablets chloride, potassium bromide, ammonium chloride, etc.
o Capsules o Not suitable for highly efflorescent or deliquescent materials
o Lozenges/Pastilles- disintegrates slowly o Special conditions are required for storage
o Suppository o Limited to contain a maximum of 500mg (eg. Co-amoxiclav
 Requirements for use: cannot be found in capsule form since it is comprised of
o Should not have difficulty in swallowing
o Must be old enough to swallow
o Conscious
o No abnormalities in the GIT
o GIT must be able to absorb the drug

Table 1. Advantages and Disadvantages of Solid Drugs. 500mg Amoxicillin plus 125mg Cavulanic Acid-total of 625mg)
Advantages Disadvantages
1. Easy to administer 1. Cannot be given to children Various capsules: hardshell capsule, softshell capsule, spansule
2. Cheap compared to younger than 6 years old who (specially coated for delayed release—not degraded by stomach
parenteral meds cannot swallow tablets or capsules acids, and is able to release its contents in the small intestines),
sustained-release capsules liberate its contents little by little
3. Readily available in (can be pounded using mortal and
the market pestle and mixed with water)
4. Preferred 2. Delays in reaching systemic
preparation for most circulation due to slow absorption B. Tablet
illnesses 3. May not be used in patients with  Different tablet preparations:
5. Delayed absorption- more serious illness whose cases o Multilayer tablet
can be a warrant hospital admission, in
disadvantage in which case parenteral drgs are
emergency used as these go straight to the
situations, since circulationfaster effect (e.g.
delayed absorptions infections)
also delays the effect 4. Not suitable for emergencies o Scored tablet

A. Capsule
 Different capsule preparations:
o For solid substances

 Advantages:
o Easy to administer (for smaller tablets)- especially true of
small ones such as contraceptive pills
o For liquid substances o Can contain larger amounts of ingredients (>500mg) (eg.
Calcium)
o Can be mixed with excipients to alter activity of drug on the
body; make more palatable and pleasant
o Can house multiple ingredients (multilayer tablet) (eg. Alaxan
which contains paracetamol and ibuprofen)
o Can be made with markings at the middle for divided doses
 Advantages: (scored tablet)- can be easily halved, making it economical
o Easy to use, (eg. Amlodipine is usually taken 5mg in the morning and 5mg
o smooth, slippery, easy to swallow in the evening. The 10mg tablet is suitable for this scheme)
o Suitable for substances having bitter taste and unpleasant o Can be made in all shapes and sizes
odor o Retains potency longer than capsules and liquids
o Produced in large quantities; economic, attractive, available in
a wide range of colors  Disadvantages:
o Minimum excipients required o Hard to swallow (larger tablets)
o Little pressure required to compact the material o Need a machine to produce large quantities
o Unit dosage form o Needs multiple excipients
o Easy to store and transport o Not flexible in terms of dosing
o Can contain liquid substances (e.g. vitamin E capsules, ,
Useful analogy: mango juice is to solution, as mango concentrate is
omega 3 capsules, nifedipine)
to extractive.

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 1. Complete and almost immediate
V. TYPES OF DOSAGE FORMS: LIQUIDS absorption; direct to systemic
1. Must be administered by
 Available forms: circulation
o Solution and extractives- mixture of either solid or liquid in 2. Immediate response trained personnel
water (e.g. Iodine solution) 3. Can be given to unconscious and
2. Strict adherence to aseptic
uncooperative patients
o Extractives (e.g. Tincture (least concentrated), Extract, Fluid 4. Suitable for emergencies (eg. techniques
Extract (most concentrated); come mostly from plant Epinephrine given to px
3. Difficult to reverse
material. experiencing anaplyactic
reactions) response (since its effect is
o Aromatic water- aquaeous solution wherein water is mixed 5. Can correct serious disturbances
immediate)
with a volatile substance (can be converted from liquid to such as severe infection or sever
gas). It is used as a gargle inflammations 4. Expensive to manufacture
6. Food cannot alter drug behavior
o Syrups- homogeneous mixture, no precipitate (e.g. (unlike in oral drugs)
Paracetamol which is both flavoured and medicinal)
 Available forms:
o Gargles, Douche (special liquid substances that provide o Vial – contains powder; needs to be mixed with water (eg.
antisepsis to the vagina), and Enema Most parenteral antibiotics; Ceftriaxone even comes with its
own diluent)
o Ophthalmic, Otic, and Nasal medicine- these have excipients o Ampule- liquid form: suspension (eg. Propofol, an anesthetic)
specific to the target area or aqueous solution (eg. Epinephrine)

o Suspensions- a precipitate can be observed to float in water

(eg. Most antibiotics for pediatric patients: amoxicillin, VI. TYPES OF DOSAGE FORMS: SEMI-SOLIDS
cephalexin, co-amoxiclav -are mixtures of granules,  Available forms:
suspending agents and water) o Lotions
 Usually oil mixed with water (more water than oil)
o Decoction and Infusion- ginger root boiled in water is a  Contain less alcohol than solutions (so it can be
decoction; Tea leaves soaked in hot water is a decoction; Tea dehydrating- ideal for use over a short time)
bag steeped in hot water is an infusion  Thicker than solutions
o Creams
o Elixer and Spirits- examples of alcoholic and hydroalcoholic  Emulsions of oil and water in equal proportions
solutions; alcohol serves to prolong the half-life and make the  Thicker than lotion
product more stable (eg. diphenhydramine elixir)  Best topical agent but commercial preparations are
usually small in quantities
Table 2. Advantages and Disadvantages of Liquid Drugs. o Ointments
Advantages Disadvantages  Homogeneous, viscous, semi-solid preparation
1. Easy to swallow 1. Shorter shelf life  Most commonly a greasy, thick oil with high viscosity
2. More difficult to  For external applications to the skin or mucous
2. Dose can be adjusted administer to children membranes
3. Can have variety of dosage forms (because oftentimes bitter  Very moisturizing and good for dry skin
taste)  Good for maintaining drug for prolonged periods
4. Can be absorbed easily compared 3. Harder to measure  80% oil, 20% water
to solids, since its dissolution rates accurately. In the absence  good for hydration but can attract dirt and dust (so is not
of a properly calibrated quite suitable for infections)
is greater medicine glass, for  ideal for us over prolonged periods especiialy since the
5. Can be mixed with volatile instance, an ordinary material doesn’t evaporate easily
teaspoon is used) o Gels
substances to provide antisepsis to 4. May have storage  Semisolid emulsion in an alcohol base
certain areas requirements. Those  Short-term treatment for hydrating any area (for dry
stored in dark brown eyes)
6. Can be given in younger children bottles may be degraded  Contains more alcohols compared to lotions
7. Economical and safe when exposed to heat or
sunlight.  FACTORS AFFECTING THE CHOICE OF SEMI-SOLIDS:
VI. TYPES OF DOSAGE FORMS: PARENTERAL DRUGS o Effect of the vehicle to alter hydration (Oil is hydrating and
alcohol is dehydrating. If long duration of use is anticipated,
Table 3. Advantages and Disadvantages of Parenteral Drugs. an alcohol-based topical drug should not be chosen to avoid
drying of skin)
Advantages Disadvantages
o Effect of the vehicle to promote or prevent collection of dust
and dirt (oil-based topical agents can attract dirt and dust)
o Distribution coefficient of drug to vehicle-water system

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 o Permeability of skin/surface to drug and vehicle

Additional Notes:
-there are different dosage forms for Co-amoxiclav :suspension
for children, tablet for adults, parenteral for px confined in the
hospital and need a stronger route for administration

>Ofloxacin- different dosage forms but same effect

>Cholarmphenicol- the oral form is more effective than the
parenteral form

-More than 50% of drugs available today are from nature. Drug
discovery improves current drug.
-Majority of dosage forms depend on 4 things: Pharmacokinetics,
pharmacodynamics, status of the pts.

-Main advantage of oral drugs: ease of administration

-Parenteral drugs: complete absorption and distribution
-Various semi-solids: useful for their absorptive and maintenance
of hydration properties.

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