It is the study of factors influencing the rate (Kinetics) & amount of drug that reaches the systemic circulation

and the use of this information to optimize the efficacy of the drug products.

Bioavailability is the rate (Kinetics) and extent (amount) of drug absorption. Any alteration in the drugs bioavailability is reflected in its pharmacological effects.

Pharmacokinetics is the study of time course of drug ADME and their relationship with its therapeutic and toxic effects of the drugs.
OR Pharmacokinetics is the kinetics of ADME or KADME

Pharmacokinetic processes

Four Phases of Drug administration and Therapy:

1. 2.

3.
4.

Pharmaceutical Phase Pharmacokinetic Phase Pharmacodynamic Phase Therapeutic Phase.

1. Pharmaceutical Phase: Concerned with

Physicochemical properties of drugs, and Design and manufacture of effective drug product for administration by a suitable means.

2. Pharmacokinetic Phase:

ADME of drugs and its relationship with

Dose, Dosage form, Dosing frequency and Route of administration.

3. Pharmacodynamic Phase:

Concerned with Biochemical and Physiological effects of drugs, and its mechanism of action. Concentration of drug at the site of action and its relation to the magnitude of effects observed. Pharmacokinetics is the study of what the body does to the drug, whereas, Pharmacodynamics is the study of what the drug does to the body.

In comparison

4. Therapeutic Phase:

Concerned with the pharmacological effects of the drug.

Drug in dosage form

Release Drug particles in body fluids Dissolution Drug in solution

Processes involved in Drug Therapeutics

Pharmacologic effect

Degradation

Peripheral Tissues Distribution Central Compartment

GI

Absorption

Liver Excretion

Free Bound

Pharmaceutics
Drug in dosage form
Release

Therapeutic Phase
Pharmacologic effect

Drug particles in body fluids

Dissolution

Pharmacodynamics
Peripheral Tissues

Drug in solution

Degradation

GI

Absorption

Distribution

Central Compartment

Liver
Excretion

Free Bound

Pharmacokinetics

Relationship between drug Product and its Pharmacological action

Drug Release & Dissolution Absorption Drug in Systemic Circulation Elimination Pharmacological or Clinical Effects Drug in Tissues

Excretion & Metabolism

Different Transport Mechanisms

Anatomical & Functional differences between important regions of GIT

Stomach
pH range Length (cm) Diameter (cm)

Small Intestine 5-7.5 300-500 2.5

Large Intestine 6-8 110 5

Rectum 6-8 20 2.5

1-3 20 15

Surface area (sq.m)

Blood flow (L/min.) Transit time (hrs) Absorptive role

0.1-0.2
0.15 1-5 Lipophilic, acidic & neutral drugs

200
1.0 3-6 All types of drugs

0.15
0.02 6-12 Some drugs, water & electrolytes

0.02
6-12 All types of drugs

Absorption mechanism

Passive diffusion, convective transport

All absorption mechanisms

Passive diffusion, convective transport

Passive diffusion, convective transport, Endocytosis

 Systemic distribution:
1. Plasma 3L 2. Extra-cellular 15 L 3. Intra-cellular 4L

Drug Distribution

Binding to blood proteins Uneven distribution in body organs:

1. Deposition in fat tissue 2. Deposition in liver/kidneys 3. Deposition in target organ

Internal barriers-Blood brain barrier/Placenta

Amount of drug adsorption

20%

80%

Influenced by: Release of the active substance from the formulation Solubility of the active component Enzymatic degradation prior to adsorption Transport over the biological barrier