NEW AGE
BIOPHARMACEUTICS
AND
PHARMACOKINETICS
of ALL INDIAN UNIVERSITIES
For B.Pharma Degree Sixth Semester Programmes
As Per the Latest Syllabus of Pharmacy Council of India (PCI)
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dney
AKHLESH K JAIN KEERTI MISHRA
U NEW aGE INTERNATIONAL PUBLISHERS
BIOPHARMACEUTICS AND PHARMACOKINETICS
Biopharmaceutics and Pharmacokinetics is one of the key components in understanding the
performance of the drugs and dosage form. In this comprehensive textbook, subject matter
has been explained ina
simple and student firiendly language.
This book is application oriented textbook
especially designed to meet the requirement of
pharmacy students. It brings out the key concepts of Biopharmaceutics and
Pharmacokinetics in a simple and lucid manner as
per the syllabus prescribed by Pharmacy
Council of India for B. Pharma students. The
present book attempts to cover the entire range
ofthe syllabus with most systematic order explaining cach and every topic at desircd length.
Dr. Akhlesh K Jain is
currently working as an Assistant Professor of
Pharmaceutics at School of Pharmacutical Sciences, Guru Ghasidas
Vishwavidyalaya, Bilaspur, India and having 20 years of teaching and rescarch
experience. He has graduated from Dr. H S Gour University and received his
PhD degree in Formulation
Science from Indian Institute of Chemical
Technology, Hyderabad, India (2007) and Postdoctoral training at Dublin City
Dublin, Ireland; University University.
College Cork, Ireland; and National University of Singapore
Singapore (2008-2011). He also worked as Senior Scientist at Central
Institute, Lucknow, India. He is the recipient of many Drug Research
Research Fellowship and CSIR-SRF for research. Dr. reputed fellowships including Junior
Jain has authored more than 35
scientific publications in peer reviewed
journals with total citations of more than 1200 and
h-index 11. He has also authored three book
has
chapters at international level and a textbook. He
successfully investigated two Research projects and guided two PhD students. He is an
inventor of one international patent and three Indian patents. His research focused on
Nanoparticles, Nanocarriers based delivery systems, Mucosal vaccination, Non invasive
protein delivery and Ligand conjugated colloidal carriers for cancer therapy.
Keerti Mishra is working as an Assistant Professor in Shambhunath
Institute of
Pharmacy, Prayagraj, India. She has completed her M. Pharm from School of
Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya,
She has published 5 research and 2 review articles in
Bilaspur, India.
reputed international
journals. She was a recipient of Junior Research Fellowship for her master's
programme. Mainly her research interests are Nanoparticles based drug delivery system for
the cancer treatment and diabetes.
Readership: Undergraduate students and faculties of Pharmacy and Medical Sciences
University and college libraries Researchers and professionals
MRP:225.00
SBN: 978-93-89802-33-7
NEW AGE INTERNATIONAL (P) LIMITED, PUBLISHERS
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DIUriANMAGEUTIGJ
AND
PHARMACOKINETICS
For B.Pharma Degree Sixth Semester Programmes of ALL INDIAN UNIVERSITIES
As Per the Latest Syllabus of Pharmacy Council of India (PCI)
AKHLESH KJAIN
Assistant Professor
School of Pharmaceutical Sciences
Guru Ghasidas Vishwavidyalaya, Bilaspur
Chhattisgarh, India
KEERTI MISHRA
Assistant Professor
Shambhunath Institute of Pharmacy
Prayagraj, UP, India
NEC
An mprint of
NEW AGE INTERNATIONAL (P) LIMITED, PUBLISHERS
LONDON NEW DELHI NAIROBI
Bangalore Chennai Cochin Guwahati Hyderabad Kolkata Lucknow Mumbai
Visit us at
www.newagepublishers.com
Preface
As majority of students find Biopharmaceutics and Pharmacokinetics subject most
difficult and unapproachable, we have tried to solve their problems by writing this
book. We have presented each topic in very easy-going manner with more generous
way. While writing this book, the key focus of authors is to present the basic concepts of
biopharmaceutics and pharmacokinetics in-depth to the students to help them grasp
and understand the subject in the easiest possible way. Over decades, the students of
pharmacy have been searching for a concise handbook of experiments to fulfil their
needs, thus this book is compiled as a single document providing entire required
information.
The book deals with the principles of biopharmaceutics and pharmacokinetics
including the action of drug in the body along with the basics of absorption, distribution,
metabolism and excretion. The entire book is divided into five chapters, namely:
Chapter 1: Introduction to Biopharmaceutics
Chapter 2: Elimination, Bioavailability and Bioequivalence
Chapter 3: Pharmacokinetics
Chapter 4: Multicompartment Models
Chapter 5: Non-linear Pharmacokinetics
Each chapter in the book forms a unique chain of understanding with an attempt
to make the topics interesting. Theoretical definitions, brief description/explanation,
discussions and derivations are furnished, with informatory examples and diagrams
for the clarification of concepts in every chapter. Few additive exercise problems
are also enclosed at the end of every chapter to help the student in gaining skills in
problem solving. In keeping the mind of every type of student, practice questions are
given ranging from very easy to somewhat difficult in order to be solved fairly by each
student. After completion of the book, the student would be able to:
1. Understand the basic concepts of biopharmaceutics and pharmacokinetics.
2 Derive the various models and estimate their pharmacokinetic parameters.
3. Design and evaluate dosage regimens of drugs, using pharmacokinetic and
biopharmaceutics parameters.
Contents
Preface ()
Syllabus (vi)
1. INTRODUCTION TO BIOPHARMACEUTICS 1-43
A. Absorption
1.1 Mechanisms of Drug Absorption through Git
12 Factors influencing Drug Absorption through GIT 7
1.3 Absorption of Drugs from Non-Per Oral Extra-vascular Routes 17
B. Distribution 20
14 Distribution of Drugs 20
1.5 Factors Affecting Distribution of Drugs 22
1.6 Tissue Permeability of the Drug 22
1.7 Volume of Distribution 26
1.8 Plasma and Tissue Protein Binding of Drugs 27
1.9 Factors Affecting Protein-Drug Binding 31
1.10 Kinetics of Protein Binding 33
1.11 Clinical Significance of Protein Binding of Drugs 35
Exercises 36
Multiple Choice Questioms 36
Review Questions 42
Numerical Questions 43
Answers 43
2. ELIMINATION, BIOAVAILABILITY AND BIOEQUIVALENCE 44-76
2.1 Drug Metabolism and Basic Understanding Metabolic Pathways 44
2.2 Factors Influencing Drug Metabolism 48
ix
CHAPTERI
Introduction to Biopharmaceutics
Biopharmaceutics isa leadirg brench in pharmaceutical sciences which relates between
5cochemical properties of a drug in dosage form and the pharmacoiog
O r cinical response observed ater its administration. It is the study of
s aeting the rate and amount of drug that reaches the systemic circulation
an he utilization of this intormation in optimizing the therapeutic efficacy of drug
u s . in easy words, hioriarmaceutics is the study of the physical and chemical
opeies of a drug and its dosage form in which the drug is administered. and the
oute of administration on the rate and extent of systemic drug absorption. It is also
haracteriz i as the study of inter-relationship among the physiochemical properties
o a drug in a dosage form and the biological response determine. Biopharmaceutics is
a distinct discipline which accounts all the various factors infuencing the therapeutic
eeciveness of drug. Biopharmaceutics is an integral component of the overall drug
dere.opment cycle.
A. ABSORPTION
Absorption is the process of movement of unchanged drug from its site of
dministration to the systemic circulation. It refers to the passage of drug molecules
rom the site of administration into the circulation. Bioavailability is the rate and
extent of drug absorption. It is the extent to which an active moiety is absorbed from
pharmaceutical dosage form and becomes available in the systemic cirulation.
Tne movement of drug from one compartment to another is called distribution.
Distribution provides information on the extent and time course of tissue accumulation
and the elimination of drug and/or its metabolites. Elimination is the process that
removes the drug from the body and stops its action. It takes place by two processes:
Biotransformation (metabolism), which normally inactivates the drug and excretion,
which tends to exit the drug/metabolites from the body. Metabolism is the enzyme-
catalyzed conversion of drugs to their metabolites. Metabolism makes the drug less
polar; lipid-soluble substance makes it more polar as well as water soluble, thus
facilitating their excretion by the kidney.
from the mechanism of absorption, distribution, metabolism and
Apart
Excretion, it is also essential to understand the kinetics through which they happen
