JAWAHARLAL NEHRU TECHNOLOGICAL UNIVERSITY HYDERABAD

Course Objectives

The student shall know about bioavailability, bioequivalence and factor affecting

bioavailability. They also know the pharmacokinetic parameter like drug disposition, absorption, non- linear and time dependant pharmacokinetics. They also know about the drug interactions & problems associated in pharmacokinetic parameters calculations.

Course Outcomes

students will be able to tell factors affecting the bioavailability and stability of

dosage form; they also know the bioequivalence studies and protocols for bioequivalent studies. They also know the parameters for the disposition, absorption and Michaelis-Menton constants for non- linear kinetics.

UNIT - I

• a. Biological and metabolic factors affecting bioavailability, complexation, dissolution - techniques of enhancing dissolution.
• b. Formulation factors affecting bioavailability of drugs in dosage forms of tablets, capsules, parenterals, liquid orals and topical dosage forms.
• c. Bioavailability: Importance, dose dependency, AUC, rate and extent, assessment, blood and urine samples, single dose and multiple dose studies, Invitro- Invivo Correlation analysis and Levels of Correlations.
• d. Bioequivalence: Importance equivalency concepts, biowaivers, study designs, protocol, transformation of data, Statistical Criteria as per the Regulations.

UNIT - II

Pharmacokinetics – Drug Disposition: compartment models: One, two and non-compartmental approaches to pharmacokinetics. Recent trends, merits and limitations of these approaches. Application of these models to determine the various pharmacokinetic parameters pertaining to:

• a. Distribution: Apparent volume of distribution and its determination, factors affecting.
• b. Metabolism: Metabolic rate constant, Factors affecting Metabolism
• c. Elimination: Over all apparent elimination rate constant, and half life. All the above under the following conditions:
• 1. Intravenous infusion
• 2. Multiple dose injections
• d. Non-invasive methods of estimating pharmacokinetics parameters with emphasis on salivary and urinary samples.
• e. Concept of clearance: organ, total clearance, hepatic clearance, lung clearance and renal clearance.

UNIT - III

Pharmacokinetics – Absorption: Rate constants – Zero order, first order,Models of experimental study of absorption (in silico, in vitro, in situ and in vivo) – Absorption half lives, method of residuals, Wagner – Nelson method, Loo - Reigleman method, Analysis of kinetics from urine samples. Pharmacokinetic parameters determination pertaining to: Multiple dosage oral administration.

UNIT - IV

Non-linear pharmacokinetics: Concepts of linear and non-linear pharmacokinetics, Michaelis- Menton kinetics characteristics. Basic kinetic parameters, possible causes of non-induction, non- linear binding, and non-linearity of pharmacological responses.

R19 M.PHARM INDUSTRIAL PHARMACY

Clinical Pharmacokinetics: Altered kinetics in pregnancy, child birth, infants and geriatrics. kinetics in GI disease, malabsorption syndrome, liver, cardiac, renal and pulmonary disease states.

UNIT - V

Time dependent pharmacokinetics: Introduction, classification, physiologically induced time dependency: Chronopharmacokinetics - principles, drugs– (amino glycosides, NSAIDS, antihypertensive drug) chemically induced dependency. Drug Interactions: Kinetics of drug interaction, study of drug-drug interaction mediated through absorption, distribution, metabolism and elimination, mechanisms of interaction and consequence.

• Numerical problems associated with all units, if any.

TEXT BOOKS

• 1. Biopharmaceutics and Clinical Pharmacokinetics by Milo Gibaldi.
• 2. Learn Shargel and ABC yu, Applied Biopharmacokinetics and Pharmacokinetics
• 3. Biopharmaceutics and Pharmacokinetics by C.V.S. Subrahmanyam, Vallabh Prakashan.2010.
• 4. Basic biopharmaceutics, Sunil S. Jambhekar and Philip J Brean.
• 5. Text book of Biopharmaceutics and Clinical Pharmacokinetics by NiaziSarfaraz

REFERENCE BOOKS

• 1. Bio-Pharmaceutics and Pharmacokinetics by V. Venkateshwarlu.
• 2. Pharmacokinetics, Biopharmaceutics and Clinical pharmacy by Robert E. Notari.
• 3. Biopharmaceutics and Clinical Pharmacokinetics - An Introduction by Robert E. Notari.
• 4. Drug drug interactions, scientific and regulatory perspectives by Albert P. G R19 M.PHARM INDUSTRIAL PHARMACY M.Pharm I Year I Sem (Industrial Pharmacy)