Biopharmaceutics and Pharmacokinetics—A Treatise
  by D.M. Brahmankar  &   S.B. Jaiswal
 
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   ISBN 978-81-85731-93-3; 3rd Ed. 2015, Rpt 2016; pp.xvi+544;

   Delhi price: 320      Outside Delhi price: 335      Overseas price : 960

 About The Book  

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.

 Content


1. 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

3. Distribution of Drugs
Steps in drug distribution
Factors affecting distribution of drug
Tissue permeability of drugs
Organ/tissue size and perfusion rate
Binding of drugs to tissue components
Miscellaneous factors
Volume of distribution
Questions

4. Protein Binding of Drugs
Mechanisms of protein-drug binding
Binding of drugs to blood components
Tissue binding of drugs
Determination of protein-drug binding
Factors affecting protein-drug binding
Drug-related factors
Protein/tissue-related factors
Drug interactions
Patient-related factors
Significance of protein/tissue binding of drugs
Kinetics of protein-drug binding
Questions

5. 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

 
8. 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

10. Nonlinear Pharmacokinetics
Causes of nonlinearity
Michaelis Menten equation
Questions

11. 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

12. Applications of Pharmacokinetic Principles
Design of dosage regimens
Individualization
Monitoring drug therapy
Questions

13. Drug Concentration and Pharmacological Response
Problems in developing PK-PD relationship
Concentration-response relationships—
Pharmacodynamic models,
Questions

14. Controlled Release Medication
Factors in the design of controlled release
drug delivery systems
Pharmacokinetic principles in the design of
controlled-release drug delivery systems
Drug release patterns of controlled delivery dosage forms
Classification of CRDDS
Rate-programmed DDS
Stimuli-activated/stimuli-responsive DDS
Site-targeted DDS
Mathematical models for controlled-release systems
Oral controlled-release systems
Oral mucosal/buccal drug delivery
Ocular drug delivery systems
Intranasal drug delivery systems
Pulmonary drug delivery systems
Parenteral controlled-release systems
Transdermal drug delivery systems
Intravaginal and intrauterine drug delivery systems
Intrauterine DDS (IUDs)
Bioavailability testing of controlled-release formulations
Questions