Introduction to

Biopharmaceutics &
Pharmacokinetics
Louie Fernand Legaspi, RPh
Instructor, DLSHSI

Objectives

At the end of the session, the student should be able

to:

Define biopharmaceutics and pharmacokinetics

Understand the concept of bioavailability
Enumerate the factors affecting bioavailability
Describe plasma level-time curve
Identify the pharmacokinetic parameters

Outline
Definition
Drug Product
Drug Delivery System
Biopharmaceutics
Pharmacokinetics
Pharmacodynamics
Concept of bioavailability
Routes of Administration
Factors affecting bioavailability
Plasma Level-Time Curve
Pharmacokinetic Parameters

Drug Product

finished dosage form (e.g., tablet, capsule,

solution) that contains the active drug ingredient in
association
with
nondrug
(usually
inactive)
ingredients (excipients) that make up the vehicle or
formulation matrix.

Drug Delivery System

Often used interchangeably with drug product

or dosage form
Includes the drug formulation and the
dynamic interactions among the drug, its
formulation matrix, its container, and the
patient.

Drug in dosage form

Pharmacological Effect
Liberation
Drug particles in
body fluids/cavities

Site of action

Dissolution
Drug in solution

Degradation

Peripheral
Tissues
Distribution

Absorption

Central Compartment =
Circulatory System
(Blood/Plasma)
Free
Metabolism
Excretion

Bound

Biopharmaceutics
Biopharmaceutics is the study of the

interrelationship between 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.

Applications of Biopharmaceutics

Explain difference in drug effect

Explain generic drug controversy
Design drug delivery system

The concentration of drug in

blood plasma

Depends on numerous factors:

the amount of an administered dose that is absorbed and

reaches the systemic circulation;

the extent of distribution of the drug between the systemic

circulation and other tissues and fluids (which is usually a
rapid and reversible process); and

the rate of elimination of the drug from the body.

The drug can either be eliminated unchanged or be

enzymatically cleaved or biochemically transformed, in which
case it is said to have been metabolized.

Pharmacokinetics

What the body does to the drug

The study and characterization

of the time
course of drug absorption, distribution,
metabolism and excretion (ADME)
Application of mathematical principles to
quantify drug movements in an organism

Pharmacodynamics

What the drugs does to the body

The study of the relation of

the drug
concentration or amount at the site of action
(receptor) and its pharmacologic response as
a function of time.

Applications of Pharmacokinetics

Pharmacological testing
Relationship between drug concentration and activity

How much and how often

Toxicological testing
Relation of tissue accumulation and toxicity
Evaluation of organ function
Eliminating organs
Dosage Regimen Design
Dose and dosing interval
Maximum therapeutic effect with minimal toxicity

Drug Absorption
The

rate and extent at which drugs reach the

systemic circulation from the site of drug
administration.
Thus, a drug is said to be absorbed if it has reached
the systemic absorption.
Drugs directly administered into the bloodstream are
assumed to be 100% absorbed.

Concept of Bioavailability
Bioavailability

is a measurement of the rate and

extent (amount) of systemic absorption of the
therapeutically active drug.

The fraction of drug dose of unchanged drug that reaches

the systemic circulation

The rate and extent to which the API is absorbed from the
drug product and becomes available at the site of action

For a drug to be 100%

bioavailable
The drug must be:

completely released from the dosage form

pass through the liver into the systemic circulation

unchanged

fully dissolved in the gastrointestinal fluids

stable in solution in the gastrointestinal fluids
pass through the gastrointestinal barrier into the mesenteric
circulation without being metabolized

Routes of Administration
Administration route

Dosage forms

Oral

Solutions, syrups, suspensions, emulsions, gels,

powders, granules, capsules, tablets

Rectal

Suppositories, ointments, creams, powders,

solutions

Topical

Ointments, creams, pastes, lotions, gels, solutions,

topical aerosols

Parenteral

Injections (solution, suspension, emulsion forms),

implants, irrigation and dialysis solutions

Respiratory

Aerosols (solution, suspension, emulsion, powder

forms), inhalations, sprays, gases

Nasal

Solutions, inhalations

Eye

Solutions, ointments, creams

Ear

Solutions, suspensions, ointments, creams

Factors affecting bioavailability

Food
Effect of the disease state on drug absorption
Age of the patient
Site(s) of absorption of the administered drug
Co-administration of other drugs
Physical and chemical properties of the administered drug
Type of dosage form
Composition and method of manufacture of the dosage
form
Size of the dose and the frequency of administration.

Plasma Level-Time Curve

generated

by obtaining the drug

concentration in plasma samples taken at
various time intervals after a drug is
administered.

Figure. A typical blood plasma concentration-time curve obtained following the

per oral administration of a single dose of a drug in a tablet.

Plasma Level-Time Curve

Onset time
corresponds to the time required for
the drug to reach the MEC.

Plasma Level-Time Curve

Intensity
The intensity

of the pharmacologic effect is

proportional to the number of drug receptors
occupied.
Higher plasma drug concentrations produce a
greater pharmacologic response, up to a
maximum pharmacological effect.

Plasma Level-Time Curve

Duration of drug action

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

Plasma Level-Time Curve

Therapeutic window
Drug concentration between the MEC and
the MTC.

Plasma Level-Time Curve

Pharmacokinetic parameters

peak plasma level/concentration

time for peak plasma level
area under the curve (AUC)

Plasma Level-Time Curve

Peak plasma level

maximum drug concentration
related to the dose, the rate

constant for
absorption, and the elimination constant of
the drug.

Plasma Level-Time Curve

Time for peak plasma level

the time of maximum drug concentration in

the plasma
a rough marker of average rate of drug
absorption.

Plasma Level-Time Curve

Area under the curve (AUC)

Related to the total amount

of drug
absorbed into the systemic circulation
following the administration of a single
dose.

What can you conclude on the

following drug concentration profile?

Thank you for

your kind attention!