Physico-Chemical Aspects of Dosage Forms and Biopharmaceutics

Recent and Future Trends in Pharmaceutics, Volume 2

1st Edition - August 9, 2024
Imprint: Academic Press
Editors: Amit Kumar Nayak, Kalyan Kumar Sen
Language: English
Paperback ISBN:
9 7 8 - 0 - 3 2 3 - 9 1 8 1 8 - 3
eBook ISBN:
9 7 8 - 0 - 3 2 3 - 9 7 2 4 7 - 5

Physico-Chemical Aspects of Dosage Forms and Biopharmaceutics: Recent and Future Trends in Pharmaceutics, Volume Two explores aspects of pharmaceutics with an original approach… Read more

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Physico-Chemical Aspects of Dosage Forms and Biopharmaceutics: Recent and Future Trends in Pharmaceutics, Volume Two explores aspects of pharmaceutics with an original approach that focuses on technology, novelties and future trends. The field of pharmaceutics is highly dynamic and rapidly expanding day-by-day, so it demands a variety of amplified efforts for designing and developing pharmaceutical processes and formulation strategies. Readers will find practical information for conducting research in pharmaceutics that is ideal for researchers in academia and industry as well as advanced graduate students in pharmaceutics.

In addition, the book discusses the most recent developments in biopharmaceutics, including important and exciting areas such as solubility of drugs, pharmaceutical granulation, routes of drug administration, drug absorption, bioavailability and bioequivalence.

Cover image
Title page
Table of Contents
Copyright
List of contributors
Preface
Section I: Physico-chemical aspects of dosage forms
Chapter 1. Physio-chemical factor influencing drug degradation
Abstract
1.1 Introduction
1.2 Conclusion
References
Chapter 2. Stability and accelerated stability studies of dosage forms
Abstract
2.1 Introduction
2.2 Significance of stability studies
2.3 Stability study to identify potential instability issues
2.4 Stability-indicating quality parameters
2.5 Functional changes in dosage form with time
2.6 Reaction kinetics and drug product stability
2.7 Factors influencing stability of pharmaceutical dosage form
2.8 Prevention of pharmaceutical products from thermal degradation
2.9 Control of product degradation by oxidation
2.10 Prevention from photolytic degradation
2.11 Carper and Garrett method
2.12 Stability protocols
2.13 ICH stability guidelines
2.14 ICH Q1A(R2) (stability testing of new drug substances and products)
2.15 ICH Q1B (photostability testing of new drug substances and products)
2.16 ICH Q1C (stability testing for new dosage forms)
2.17 ICH Q1D (bracketing and matrixing designs for stability testing of new drug substances and products)
2.18 ICH Q1E (evaluation of stability data)
2.19 ICH Q1F (for registration applications in climatic zones III and IV)
2.20 Conclusion
References
Chapter 3. Solubility of drugs
Abstract
3.1 Introduction
3.2 Solubility expressions
3.3 Interactions between solutes and solvents: mechanisms
3.4 Ideal solubility parameters
3.5 Solvation and association
3.6 Factors influencing the solubility of drugs
3.7 Phase-solubility analysis
3.8 Diffusion principles in biological systems
3.9 Solubility of gas in liquid
3.10 Solubility of liquids in liquids
3.11 Partially miscible liquids
3.12 Distribution phenomenon
3.13 Determination of solubility
3.14 Solubility enhancement techniques
3.15 Conclusion
References
Chapter 4. Drug dissolution studies of pharmaceutical formulations
Abstract
4.1 Introduction
4.2 Mechanism of dissolution
4.3 Noyes–Whitney equation
4.4 Dissolution method development
4.5 Dissolution test
4.6 Dissolution test apparatus
4.7 Discriminative dissolution
4.8 Dissolution testing for immediate and control release formulation
4.9 Method to enhance the rate of dissolution and the bioavailability of a poorly soluble drug
4.10 In vitro–in vivo correlation
4.11 Biowaiver
4.12 Conclusion
References
Chapter 5. Pharmaceutical granulation: engineering perspective and futuristic trends
Abstract
5.1 Introduction
5.2 Advantages and disadvantages of granulation
5.3 Factors affecting granulation process selection
5.4 Wet granulation
5.5 Granulating media and binder solution
5.6 Mechanism of granules formation
5.7 Factors associated with granulating media
5.8 Media volume
5.9 Solid content
5.10 Addition time
5.11 Types of equipment used for wet granulation
5.12 Rapid mixer granulator (RMG)
5.13 RMG bowl
5.14 Impeller
5.15 Chopper
5.16 RMG bowl, impeller, and chopper geometry
5.17 Scale up in RMG
5.18 Top spray wet granulation
5.19 Scale-up of top spray process
5.20 Calculation of fluidization air flow
5.21 Calculation of spray rate
5.22 Dry granulation
5.23 Futuristic trend
5.24 Conclusion
References
Chapter 6. Tablet compression and consolidation: theory and applications
Abstract
6.1 Introduction
6.2 Compression and theory of compression
6.3 Formulation factors and processing parameters that have an impact on compression
6.4 Manufacturing problems
6.5 Compaction simulation
6.6 Guided formulation and process development using dynamic compaction analysis
6.7 Development strategies and compression classification systems/preformulation tools
References
Section II: Biopharmaceutics
Chapter 7. Introduction to biopharmaceutics
Abstract
7.1 Introduction
7.2 Pharmacokinetics
7.3 Pharmacodynamics
7.4 Drug absorption
7.5 Drug absorption mechanism via the gastrointestinal tract
7.6 Structure of gastrointestinal tract membrane
7.7 Intracellular (transcellular) transport
7.8 Active transport
7.9 Passive transport
7.10 Intercellular (paracellular) transport
7.11 Active transport
7.12 Ion pair transport
7.13 Passive diffusion
7.14 Pore transport
7.15 Carrier-mediated transport
7.16 Facilitated diffusion
7.17 Factors affecting drug absorption through gastrointestinal tract
7.18 Non-per oral extravascular drug absorption
7.19 Distribution of drugs
7.20 Steps in drug distribution
7.21 Tissue permeability of drugs
7.22 Physiological hurdle to drug distribution
7.23 Organ/Tissue size and perfusion rate
7.24 Apparent distribution volume
7.25 Binding of drug
7.26 Protein binding of drug
7.27 Mechanism of protein–drug binding
7.28 Hemoglobin
7.29 Cell membrane
7.30 Factors influencing protein binding of drugs
7.31 Protein binding and kinetics of protein binding
7.32 Conclusion
References
Chapter 8. Gastrointestinal absorption of drugs
Abstract
8.1 Introduction
8.2 Physiology of gastrointestinal tract
8.3 Mechanism of drug absorption
8.4 Models for oral absorption of drug
8.5 Factor affecting gastrointestinal absorption of a drug
8.6 Conclusion
Acknowledgment
Conflict of interest
Consent for publication
References
Chapter 9. Routes of drug administration and their impact in biopharmaceutics
Abstract
9.1 Introduction
9.2 General consideration for drug administration
9.3 Important routes of drug administration
9.4 Pharmaceutical concern and novel manipulation on routes of drug administration
9.5 Conclusion
References
Chapter 10. Drug elimination and renal excretion of drugs
Abstract
10.1 Introduction
10.2 General consideration on drug elimination
10.3 Organ function and drug elimination
10.4 Organ impairment and dose adjustment for drug elimination
10.5 Conclusion
References
Chapter 11. Membrane transport and permeation of drugs
Abstract
11.1 Introduction
11.2 Membrane transport mechanism
11.3 Membrane permeation tool
11.4 Model for assessment of drug permeation across the gastro-intestinal tract
11.5 Model for assessment of drug permeation across blood–brain barrier
11.6 Model for assessment of drug permeation across skin
11.7 Model for assessment of ocular drug permeation
11.8 Model for assessment of pulmonary drug permeation
11.9 Conclusion
References
Chapter 12. Factors affecting drug absorption and disposition
Abstract
12.1 Introduction
12.2 Drug absorption
12.3 Drug distribution
12.4 Factors affecting drug distribution
12.5 Physiological barriers
12.6 Drug metabolism
12.7 Factors affecting drug metabolism
12.8 Drug excretion
References
Chapter 13. Bioavailability and bioequivalence
Abstract
13.1 Introduction
13.2 Objective of bioavailability studies
13.3 Absolute and relative bioavailability
13.4 Factors affecting the bioavailability
13.5 Methods for determination of bioavailability
13.6 In vitro in vivo correlation
13.7 Protocol design for bioavailability assessment
13.8 Bioequivalence studies
13.9 Methods utilized for enhancement of solubility/dissolution rate
13.10 Biowaivers
13.11 Biosimilars
13.12 BA, BE, and biowaiver modeling
References
Chapter 14. Contribution of biopharmaceutics and pharmacokinetics to improve drug therapy
Abstract
14.1 Introduction
14.2 Significance of pharmacokinetics and biopharmaceutics
14.3 Drug–drug interaction and its impact in drug therapy
14.4 Drug food interaction
14.5 Therapeutic drug monitoring: optimizing drug therapy across patient populations
14.6 Regulatory aspects on the absorption, bioavailability, and bioequivalence of drugs
References
Chapter 15. Dosage regimen
Abstract
15.1 Choice of a drug, its dose, and frequency of administration
15.2 Some considerations before designing a dosage regimen
15.3 Factors affecting dosage regimen design
15.4 Definition of dosage regimen
15.5 Factors that affects pharmacokinetic parameters and the design of drug dosage regimens
15.6 Preclinical drug investigation
15.7 Development of dosage regimen
15.8 Single dosage
15.9 Multiple dosing
15.10 The use of a nomogram in determining dosage regimen
15.11 Multiple dosage and plasma drug concentration
15.12 Drug accumulation
15.13 Multiple-oral-dose regimen of an oral or extravascular route of administration
15.14 Loading dose
15.15 Individualization of dosage regimen
15.16 Determination of total body surface area
Further reading
Chapter 16. Multicompartment model
Abstract
16.1 Introduction
16.2 Two compartmental modeling following IV bolus administration
16.3 Two-compartment model following IV infusion
16.4 Two-compartment open model with extravascular administration
16.5 Three-compartment model with IV bolus injection
16.6 Multiple dosing regimen
Appendix 1 Basics of compartment modeling
Appendix 2 Laplace transformation
Further reading
Chapter 17. Nonlinear pharmacokinetics
Abstract
17.1 Introduction
17.2 Factors causing nonlinearity
17.3 Michaelis–Menten equation
17.4 One compartment open model-intra venous bolus injection-drug elimination by saturated kinetics
17.5 Determination of Km and Vm
17.6 Estimation of Vm and Km following multiple dose administration
17.7 Direct estimation of Km at two dose levels of multiple dosing
17.8 Determination of clearance, half-life, and volume of distribution
17.9 Relationship between the area under the curve and the administered dose when drug follows nonlinear kinetics
17.10 Inhibition of drug metabolism
17.11 Detection of nonlinearity
17.12 Simulation of nonlinear pharmacokinetics in physiologically based pharmacokinetic models
17.13 The case of phenytoin
17.14 Conclusion
Further reading
Chapter 18. Computer-aided biopharmaceutical model development
Abstract
18.1 Introduction
18.2 Computational biopharmaceutics
18.3 Computer-aided biopharmaceutical model development
18.4 Concluding remarks
Acknowledgments
Consent for publication
Conflict of interest
References
Chapter 19. Computer simulations in pharmacokinetics
Abstract
19.1 Introduction
19.2 Noncompartmental pharmacokinetic analysis
19.3 Compartmental pharmacokinetic models
19.4 Physiologically based-pharmacokinetic models
19.5 Applications of pharmacokinetic model simulations in drug development and therapeutics
19.6 Additional pharmacokinetic example. Dermato-pharmacokinetics
19.7 Summary
References
Chapter 20. World Health Organization and International Council for Harmonization guidelines for “Good Manufacturing Practices”
Abstract
20.1 Introduction
20.2 Objectives of good manufacturing practices
20.3 Infrastructural requirements
20.4 Storage area
20.5 Machinery and equipments
20.6 Health and hygiene
20.7 Standard operating procedure (SOP)
20.8 Reference standard
20.9 Documentation and records
20.10 Recording information in the document
20.11 Labels
20.12 Records
20.13 Basic aspects of current good manufacturing practice regulations in pharmaceutical industry
20.14 Current good manufacturing practices general provisions and quality control
20.15 Significance of current good manufacturing practices
20.16 Conclusion
Abbreviations
References
Chapter 21. Pilot plant scale-up techniques in pharmaceutical product development
Abstract
21.1 Introduction
21.2 Pilot plant scale-up considerations for solids
21.3 Pilot plant scale-up considerations for liquid
21.4 Pilot plant scale-up considerations for semisolids
21.5 Conclusion
References
Chapter 22. Advances in solid dosage forms
Abstract
22.1 Introduction
22.2 Tablet
22.3 Capsule
22.4 Pellet
References
Index

Amit Kumar Nayak

Dr. Amit Kumar Nayak (MPharm, PhD) is working as a professor, at the Department of Pharmaceutics, School of Pharmaceutical Sciences, Siksha ‘O' Anusandhan (Deemed to be University), Odisha, India. He has earned his PhD from IFTM University, Moradabad, Uttar Pradesh, India. He has over 14 years of research experiences in the field of pharmaceutics, especially in the development and characterization of novel biopolymeric and nanostructured drug delivery systems. Till date, he has authored more than 138 research and review publications in various high-impact peer-reviewed journals and 135 book chapters. He has edited/authored 23 international books to his credit. Dr. Nayak has presented his research work at several conferences. He has received University Foundation Day Research Award, 2019 and 2022 by Biju Patnaik University of Technology, Odisha. Dr. Nayak is a life member of the Association of Pharmaceutical Teachers of India (APTI) and a registered pharmacist.

Affiliations and expertise

Professor, Department of Pharmaceutics, School of Pharmaceutical Sciences, Siksha 'O' Anusandhan (Deemed to be University), Bhubaneswar, Odisha, India

Kalyan Kumar Sen

Dr. Kalyan Kumar Sen (MPharm, PhD) has over 38 years of teaching and industrial and research experience in the field of pharmaceutics, especially in the development and characterization of novel drug delivery systems. He has earned his PhD in pharmacy from Jadavpur University, India. Currently, Dr. Sen is working as a principal and professor of Gupta College of Technological Sciences, Asansol, India. Till date, he has authored several publications in various journals of international repute. He has authored several book chapters. He already has edited two books and co-authored one book. He has been the permanent reviewer of many international journals of high repute. Dr. Sen has participated and presented his research work at several conferences in India. Dr. Sen is a life member of the APTI and several professional bodies.

Affiliations and expertise

Department of Pharmaceutics, Principal of Gupta College of Technological Sciences, Asansol, W.B, India

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