BIOPHARMACEUTICS 2

Distribution
Metabolism
Excretion
 Bioavailability
• Refers to the rate and extent at which the active moiety (drug or
metabolite) enters circulation and thereby accesses the site of action
• Is the rate at which the drug becomes available to the body and the
extent to which the dose is ultimately absorbed after administration of
a particular pharmaceutical form.
• Is dependent upon the properties of dosage form; i.e. the design and
manufacture of the formulation from which the drug is released
– Poor or inappropriate formulation results in a product that releases drug too
slow or fails to release a portion of the drug or leads to undesired variations in
performance of individual units
 excipient -components greatly influence rate of release of drug from a
formulation: both slow and fast rates of absorption can be desirable
depending on specific therapeutic goals
– The factors that influence the process of dissolution of drug in a dosage form
especially for particulate drug affect bioavailability
Differences in bioavailability between formulations of the same drug can have
clinical significance
Biopharmaceutics 2
 Bioequivalence
• Bioequivalence indicates that the two or more drug
products under comparison, when given to the same
patient in the same dosage regimen, result in equivalent
concentrations of drug in plasma and tissues
– Bioequivalent products are expected to be therapeutically
equivalent
• Chemical equivalence: indicates that drug products
contain the same active compound in the same amount
and meet current official standards; although, the
inactive ingredients in drug products may differ.
 Pharmaceutical Equivalence
Pharmaceutical products with similar
bioavailability, include active
ingredients drug amounts dosage
form although they may NOT have
the same inactive ingredients
• What is clinical equivalence?
 Key Parameters
• Minimum Effective Concentration(MEC):
• Onset of drug action:
• Onset time: t0
• Cmax = Peak concentration
• tmax = peak time
• Intensity of action
• Area under curve (AUC)

Biopharmaceutics 5
 Key Parameters ctd.
• Duration of therapeutic action
• Therapeutic range: sub-therapeutic, toxic levels
• Maximum Safe Therapeutic Concentration:
(MSC)
• Absorption Phase
• Elimination phase
• Absorption process in equilibrium with
elimination process

Biopharmaceutics 6
A typical blood plasma drug concentration-
time curve (oral admin)
https://1.bp.blogspot.com/-gb1DRJlFUKM/UmBMmZ5FLAI/AAAAAAAAAes/ktF967EFlOs/s1600/Screen+shot+2013-10- 17+at+4.45.57+PM.png

Biopharmaceutics 7
Blood plasma drug –time concentration curve
following IV and 3 oral dosage forms https://www.boomer.org/c/p4/c20/Fig2012.jpg

Biopharmaceutics 8
 PHARMACOKINETICS
Is the study of the quantitative
changes of absorption,
distribution, metabolism and
excretion of a drug with time,
following its administration to
man or animals.

Biopharmaceutics 9
Multiple dosing regimen
http://www.thebody.com/content/art875.html

Biopharmaceutics 10
 Drug half-life
Is the amount of time it takes for the
blood concentration of a drug to
decline to one half of the an initial
concentration value