INTRODUCTION TO

BIOPHARMACEUTICS AND
PHARMACOKINETICS

Milon Kumar Ghosh

Lecturer
Department of Pharmacy
Islamic University, Kushtia-7003
 Biopharmaceutics

• Biopharmaceutics is the science that examines 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. Thus, biopharmaceutics involves factors
that influence
(1) The stability of the drug within the drug product,
(2) The release of the drug from the drug product,
(3) The rate of dissolution/release of the drug at the absorption site, and
(4) The systemic absorption of the drug. A general scheme describing this
dynamic relationship is described in .
Scheme demonstrating the dynamic relationship between the
drug, the drug product, and the pharmacologic effect
• Biopharmaceutics is a major branch in pharmaceutical sciences
which relates between the physicochemical properties of a drug in
dosage form and the pharmacology, toxicology, or clinical response
observed after its administration.
 Pharmacokinetics

Absorption

Distribution
Excretion

Pharmacokinetics ADM
E

Metabolism

What the body does to the drugs?

• Pharmacokinetics is the science of the kinetics of drug absorption,
distribution, and elimination (i.e., excretion and metabolism). The
description of drug distribution and elimination is often termed drug
disposition. Characterization of drug disposition is an important
prerequisite for determination or modification of dosing regimens for
individuals and groups of patients.

• Clinical pharmacokinetics is the application of pharmacokinetic methods

to drug therapy. Clinical pharmacokinetics involves a multidisciplinary
approach to individually optimized dosing strategies based on the patient's
disease state and patient-specific considerations.
 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.

What the drug does to the body?

Relationship of drug concentration to drug effect at the
receptor site
 Some Practical Definitions

• Active pharmaceutical ingredient: The biologically active component of a

drug product, that is, the component directly responsible for the
pharmacological response. It is also usually referred as drug. Some drug
products include more than one active pharmaceutical ingredient. Such
substances can be used in the diagnosis, cure, mitigation, treatment, or
prevention of disease.
• Drug product: Through appropriate manufacturing processes, active
pharmaceutical ingredients are combined with inactive pharmaceutical
ingredients called excipients, which compose the pharmaceutical vehicle,
pharmaceutical carrier, or drug delivery system. Closely related to the dosage
form concept i.e., physical form in which a drug product is produced and
dispensed, e.g., tablet, capsule, syrup, etc.
• Drug target: A biomolecule with which the drug specifically interacts to
elicit its therapeutic response. Most drug targets are proteins, though some
correspond to other types of biomolecules (e.g., DNA, RNA).

• Bioavailability: Bioavailability refers to the extent and rate at which the

drug reaches its site of action. As the determination of drug levels in the
site of action is not feasible in some cases (for instance, the reader may
imagine how invasive would be to measure drug levels in the central
nervous system), bioavailability assessment in the site of action is often
replaced by measuring systemic bioavailability, i.e., the extent and rate at
which the drug reaches systemic circulation. This is more convenient,
since drug levels are more frequently quantified in serum or plasma.
• Biophase: The effect site of a drug. Physical region (environment) in
which the drug target is located.

• Systemic treatment or systemic medication: A pharmacological treatment

in which the therapeutic agent (the drug) reaches its site of action through
the bloodstream. We will consider that a drug molecule has reached
systemic circulation once it has left the left ventricle of the heart at least
once, that is, once it has reached the aorta.

• Topical medication: A medication that is locally applied to the particular

place on or in the body where it is intended to elicit its action. Many
topical medications are applied directly to the skin. Topical medications
may also be inhalational or applied to the surface of tissues other than the
skin, such as eye drops applied to the conjunctiva or ear drops placed in
the ear.
• Therapeutic window: Also known as therapeutic range, it refers to
the range of drug concentrations in a bodily fluid (usually, plasma)
that provides safe and effective therapy. The lower bound of the
therapeutic range is called minimum effective concentration (MEC),
whereas the upper bound is called minimum toxic concentration
(MTC). Below the lowest concentration of the window, it is likely
that the drug will fail to work. If the drug concentration climbs
above the therapeutic window, a detrimental intensification of the
drug’s intended (on-target) and unintended (off-target) actions will
occur.
Generalized plasma level–time curve after oral administration
of a drug
Onset of drug action: The onset time corresponds to the time required
for the drug to reach the MEC.

Duration of drug action: The duration of drug action is the difference

between the onset time and the time for the drug to decline back to the
MEC.

Peak plasma level: The maximum drug concentration in the plasma.

Time for peak plasma level: The time of peak plasma level is the time to
reach of maximum drug concentration in the plasma.

Area under the curve, or AUC: The AUC is related to the amount of
drug absorbed systemically.
 PLASMA LEVEL–TIME CURVE

• The plasma level–time curve is generated by obtaining the drug

concentration in plasma samples taken at various time intervals after a
drug product is administered. The concentration of drug in each plasma
sample is plotted on rectangular-coordinate graph paper against the
corresponding time at which the plasma sample was removed. As the
drug reaches the general (systemic) circulation, plasma drug
concentrations will rise up to a maximum. Usually, absorption of a drug
is more rapid than elimination. As the drug is being absorbed into the
systemic circulation, the drug is distributed to all the tissues in the body
and is also simultaneously being eliminated. Elimination of a drug can
proceed by excretion, biotransformation, or a combination of both.
PHYSICOCHEMICAL NATURE OF THE DRUG
 PHARMACOKINETIC MODELS

• A model is a hypothesis using mathematical terms to describe

quantitative relationships concisely. The key parameters in a process
are commonly estimated by fitting the model to the experimental
data, known as variables.
• A pharmacokinetic function relates an independent variable to a
dependent variable, often through the use of parameters. For
example, a pharmacokinetic model may predict the drug
concentration in the liver 1 hour after an oral administration of a 20-
mg dose.
• Such mathematical models can be devised to simulate the rate processes
of drug absorption, distribution, and elimination to describe and predict
drug concentrations in the body as a function of time. 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
• Apparent volume of distribution:
• Plasma half life: