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Samanta / 2005 1
CHAPTER – 1
Introduction to biopharmaceutics and pharmacokinetics
Syllabus:
Introduction to biopharmaceutics and pharmacokinetics and their role in information development and clinical setting.
Definition of Biopharmaceutics
Biopharmaceutics can be defined as the study of 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 (amount) of systemic drug absorption.
Drug release
Elimination
Drug in extravascular tissues Metabolism DISPOSITION
Drug at site of action Excretion
PHARMACODYNAMICS
In normal body
Pharmacologic response
THERAPEUTICS
In diseased body
Therapeutic effect at therapeutic dose
Toxic effect at toxic dose
Pharmacokinetics is defined as the study of rate processes involved in absorption, distribution, metabolism and
excretion (ADME).
Pharmacokinetics
The study of pharmacokinetics involves both
experimental and theoretical approaches. Absorption Disposition
The experimental approach involves
1. the development of biological sampling Distribution Elimination
techniques
2. analytical methods development for the
measurement of drugs and metabolites Excretion Metabolism
3. and the procedures for data collection and manipulation.
The theoretical aspect of pharmacokinetics involves the development of pharmacokinetic models that predicts drug
disposition after drug administration.
The application of statistics is an integral part of pharmacokinetic models top determine data errors, deviation of
models and correlation.
Population pharmacokinetics is the study of pharmacokinetic differences of drug in various population groups.
Pharmacodynamics deals with the relationship between the drug concentration at the site of action (receptor) and
pharmacologic response, including biochemical and physiological effects that influence the interaction of drug with the
receptor.
Under pharmacodynamics we study the relationship between the plasma concentration of drug (related to the
concentration at the site of action) and the magnitude of biological effect it shows.
Toxicokinetics
Toxicokinetics is the application of pharmacokinetic principles to the design, conduct and interpretation of drug safety
evaluation studies and used in validating dose related exposure in animals. Toxicokinetic studies are conducted in
animals and the result obtained is used to interpret possible toxic reactions in human.
Application of biopharmaceutics
1. A company is going to market a new dosage form of a certain drug. The dose is known. When this dosage form is
administered to a healthy human the drug may not released quickly. In this case the action of the drug will be
delayed. In another case if the drug is released all at a time then the duration of action of the drug will be very
short. So with the knowledge of biopharmaceutics we can change various formulation factors to obtain optimum
onset of action and duration of action.
2. A company is marketing tablets of a certain drug. Now it wants to change a few ingredients or some formulation
factors. The new tablets may not behave similarly as the previous one. So the bioavailability of new tablets are
compared with the old tablets. If it is found that the bioavilability of the newer tablets are equivalent (i.e
bioequivalent) to that of older tablets then the new tablets will be permitted to market (by FDA).
3. A company is marketing the tablets of a certain drug. Now they have planned to make transdermal dosage form of
the same drug. To establish its efficacy the bioavailability of the transdermal dosage form is compared to that of
the established tablet dosage form. If both are found to be closer then the transdermal dosage form will be accepted
by FDA.
Application of pharmacokinetics
1. The bioavailabilty of a dosage form is calculated by pharmacokinetic equations.
2. The frequency of dosing is calculated from pharmacokinetic equations.
3. To calculate the dose of a controlled release dosage form pharmacokinetic equations are required.
4. In case of patients with kidney failure the dose of a drug should be calculated very cautiously. If the rate of
absorption of the drug is greater than the elimination rate of the drug from that patient then the drug will be
accumulated in the body and may show toxic effect. The rate of elimination of the drug from the body of that
patient is calculated with the help of pharmacokinetic equations.
5. When a potent anticancer drug is administered to a patient the plasma concentration of the drug must be very close
to minimum effective concentration. Since the therapeutic index of the drug is very narrow in case of potent drugs
so rate of administration must also be very slow. This rate of administration is calculated by pharmacokinetic
principles.