BIOPHARMACEUTICS AND PHARMACOKINETICS BY D.M.BRAHMANKAR PDF

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ISBN ; 3rd Ed. About The Book. Related Books. The science and technology associated with pharmacy has progressed enormously over the past few decades. Significant advances in the understanding of diseases have necessitated the need to optimize drug therapy. The concern today is not just to produce elegant and accurate dosage forms but also to ensure that optimum amount of drug reaches the target site at an optimal rate and its concentration is maintained for the entire duration of therapy.

A thorough background of the fate of drug after its administration; the rate processes to which it is subjected in the body and its behavior after biotransformation, are thus very essential in addition to the knowledge about its pharmacodynamics.

The twin disciplines of Biopharmaceutics and Pharmacokinetics have, therefore, been developed with the objective of learning how drugs can be utilized optimally in the treatment of diseases—through design and development of new and better therapeutic moieties, new dosage forms and appropriate dosage regimens.

Significant expansion of the chapter on controlled release medication has been made to cover in a broader perspective, the principles employed in the design of such dosage forms, their classification and brief description of the technologies and products delivered by various routes.

The concerted attempt was to collectively address the several modern approaches adopted to design the modified drug delivery systems, which is an exciting and highly dynamic area of pharmaceutical research. The chapter on Absorption of Drugs has been dealt with comprehensively as most of its principles also form the basis of drug distribution and elimination. Elaborate treatment of text on Biotransformation of Drugs in chapter 5 is justified since a pharmacy student is well versed with the basic chemistry and enzymology.

A brief mention about Bioactivation and Tissue Toxicity has been included at the end of this chapter so that after understanding the mechanisms of drug metabolism, a student will be better placed to appreciate their significance. Prodrugs discussed in chapter 6 give insight into the manner in which chemical formulation techniques can be utilized to overcome some of the inherent biopharmaceutic and pharmacokinetic problems of the active principles.

Mathematical treatment of chapters on pharmacokinetics has been kept to at modest level in order not to overburden the students with the complexities of equations and formulae. A brief description of methods usually employed to enhance the bioavailability of a drug from its formulation has been included.

In addition to covering various aspects of design of dosage regimens and application of pharmacokinetic principles in clinical situations, the text contains a chapter on Controlled Release Medication to familiarize the students with the principles involved in the design of innovative formulations.

Introduction 2. Absorption of Drugs Gastrointestinal Absorption of Drugs Mechanisms of drug absorption Phases and routes of drug transfer from GI absorption site GI epithelium into systemic circulation Factors influencing drug absorption and bioavailability Pharmaceutical factors Patient-related factors Methods for studying drug uptake Absorption of drugs from non-per os extravascular routes Questions.

Need for drug biotransformation Drug metabolising organs Drug metabolising enzymes Chemical pathways of drug biotransformation Phase I reactions Oxidative reactions Reductive reactions Hydrolytic reactions Phase II reactions Conjugation with glucuronic acid Conjugation with sulphate moieties Conjugation with alpha amino acids Conjugation with glutathione and mercapturic acid formation Acetylation Methylation Miscellaneous conjugation reactions Fate of metabolites following biotransformation in liver Presystemically formed vs systemically formed metabolites Methods for the study of drug biotransformation Factors affecting biotransformation of drugs Physicochemical properties of the drug Chemical factors Biological factors Bioactivation and tissue toxicity Biopharmaceutics drug disposition classification system Questions.

Renal excretion of drugs Concept of clearance Factors affecting renal excretion or renal clearance Renal function and renal failure Dose adjustment in renal failure Dialysis and haemoperfusion Non-renal routes of drug excretion Questions.

Factors contributing to drug interactions Mechanisms of drug interactions Reducing the risk of drug interactions Questions. Pharmacokinetics: Basic Considerations Plasma drug concentration time profile Pharmacokinetic parameters Pharmacodynamic parameters Rate, rate constants and order of reactions Pharmacokinetic analysis of mathematical data: Pharmacokinetic models Questions. One-compartment open model Intravenous bolus administration Intravenous infusion Extravascular administration Urinary excretion data Multicompartment models Two compartment open model Intravenous bolus administration Intravenous infusion Extravascular administration Questions.

Causes of nonlinearity Michaelis Menten equation Questions. Considerations in in vivo bioavailability study design Measurement of bioavailability In vitro drug dissolution testing models Dissolution acceptance criteria Methods for dissolution profile comparison In vitro-in vivo correlation IVIVC Biopharmaceutics classification system and IVIVC Bioequivalence studies Types of bioequivalence studies Bioequivalence experimental study design Bioequivalence study protocol Statistical interpretation of bioequivalence data Methods for enhancement of bioavailability Bioavailability enhancement through enhancement of drug solubility or dissolution rate, Bioavailability enhancement through enhancement of drug permeability across biomembrane Bioavailability enhancement through enhancement of drug stability Bioavailability enhancement through gastrointestinal retention Questions.

Design of dosage regimens Individualization Monitoring drug therapy Questions. Order Now by Email. Absorption of Drugs Gastrointestinal Absorption of Drugs Mechanisms of drug absorption Phases and routes of drug transfer from GI absorption site GI epithelium into systemic circulation Factors influencing drug absorption and bioavailability Pharmaceutical factors Patient-related factors Methods for studying drug uptake Absorption of drugs from non-per os extravascular routes Questions 3.

Biotra0nsformation of Drugs Need for drug biotransformation Drug metabolising organs Drug metabolising enzymes Chemical pathways of drug biotransformation Phase I reactions Oxidative reactions Reductive reactions Hydrolytic reactions Phase II reactions Conjugation with glucuronic acid Conjugation with sulphate moieties Conjugation with alpha amino acids Conjugation with glutathione and mercapturic acid formation Acetylation Methylation Miscellaneous conjugation reactions Fate of metabolites following biotransformation in liver Presystemically formed vs systemically formed metabolites Methods for the study of drug biotransformation Factors affecting biotransformation of drugs Physicochemical properties of the drug Chemical factors Biological factors Bioactivation and tissue toxicity Biopharmaceutics drug disposition classification system Questions 6.

Excretion of Drugs Renal excretion of drugs Concept of clearance Factors affecting renal excretion or renal clearance Renal function and renal failure Dose adjustment in renal failure Dialysis and haemoperfusion Non-renal routes of drug excretion Questions 7. Pharmacokinetic Drug Interactions Factors contributing to drug interactions Mechanisms of drug interactions Reducing the risk of drug interactions Questions.

Pharmacokinetics: Basic Considerations Plasma drug concentration time profile Pharmacokinetic parameters Pharmacodynamic parameters Rate, rate constants and order of reactions Pharmacokinetic analysis of mathematical data: Pharmacokinetic models Questions 9.

Compartment Modelling One-compartment open model Intravenous bolus administration Intravenous infusion Extravascular administration Urinary excretion data Multicompartment models Two compartment open model Intravenous bolus administration Intravenous infusion Extravascular administration Questions Bioavailability and Bioequivalence Considerations in in vivo bioavailability study design Measurement of bioavailability In vitro drug dissolution testing models Dissolution acceptance criteria Methods for dissolution profile comparison In vitro-in vivo correlation IVIVC Biopharmaceutics classification system and IVIVC Bioequivalence studies Types of bioequivalence studies Bioequivalence experimental study design Bioequivalence study protocol Statistical interpretation of bioequivalence data Methods for enhancement of bioavailability Bioavailability enhancement through enhancement of drug solubility or dissolution rate, Bioavailability enhancement through enhancement of drug permeability across biomembrane Bioavailability enhancement through enhancement of drug stability Bioavailability enhancement through gastrointestinal retention Questions Applications of Pharmacokinetic Principles Design of dosage regimens Individualization Monitoring drug therapy Questions History of Pharmacy in India Autobiography Industry.

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