Drug Design

Medicinal Chemistry: A Series of Monographs, Vol. 4

1st Edition - January 1, 1973
Editor: E. J. Ariëns
Language: English
eBook ISBN:
9 7 8 - 1 - 4 8 3 2 - 1 6 0 6 - 5

Drug Design, Volume IV covers the pharmaceutical phase of drug action, with emphasis on those aspects that are of importance in the design of optimally effective drug products.… Read more

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Drug Design, Volume IV covers the pharmaceutical phase of drug action, with emphasis on those aspects that are of importance in the design of optimally effective drug products. The book discusses biopharmaceutics as a basis for the design of drug products; the types and pharmacokinetics of peroral prolonged action dosage forms and parenteral prolonged action forms; and the design of topical drug products. The text also describes physical-chemical parameters which affect the bioavailability of topical drug products; the design of sunscreen preparations; as well as the clinical application of litholytic agents, which are preventive and curative drugs for nephrolithiasis. The design of biologically active nucleosides and of insecticidal chlorohydrocarbon derivatives is also encompassed. Chemists, biochemists, pharmacologists, and people involved in drug design will find the book invaluable.

List of Contributors

Preface

Contents of Other Volumes

Chapter 1. Biopharmaceutics as a Basis for the Design of Drug Products

I. Introduction

II. Biopharmaceutics—The Science of Input

III. Bioavailability

IV. Selection of the Route of Administration

V. Getting Drugs into Solution

VI. Gastrointestinal Membrane Transport

VII. Getting Drugs into the Small Intestine

References

Chapter 2. Peroral Solid Dosage Forms with Prolonged Action

I. Introduction

II. Types of Peroral Prolonged Action Dosage Forms

III. Evaluation of Peroral Prolonged Action Dosage Forms

IV. Pharmacokinetics

V. Additives

VI. Manufacturing Process

References

Chapter 3. Parenteral Dosage Forms with Prolonged Action

I. Introduction

II. Types of Parenteral Prolonged Action Dosage Forms

III. Evaluation of Parenteral Prolonged Action Dosage Forms

References

Chapter 4. Design of Topical Drug Products: Pharmaceutics

I. Skin

II. Dermatological Bases

III. Drugs

IV. Testing

References

Chapter 5. Design of Topical Drug Products: Biopharmaceutics

I. Introduction

II. Fundamentals of Drug Diffusion into Human Skin

III. Optimizing Drug Availability from Topical Dosage Forms

IV. Summary

References

Chapter 6. The Design of Sunscreen Preparations

I. Introduction

II. Ultraviolet Radiation

III. Human Reactions to Ultraviolet Radiation

IV. Sunscreen Preparations

V. Multiple Action Products

VI. Evaluation of Sunscreen Preparations

References

Chapter 7. Litholytic Agents: Preventive and Curative Drugs for Nephrolithiasis

I. Introduction

II. Factors Influencing Stone Formation

III. Litholytic Agents

IV. Possibilities for Dissolving the Four Different Types of Kidney Stones

V. Clinical Application of the Litholytic Agents for the Dissolution of Kidney Stones

VI. Summary

References

Chapter 8. The Design of Biologically Active Nucleosides

I. Introduction

II. Functional Considerations

III. Structural Considerations

IV. Approaches toward Enhancing the Biological Activity of Nucleoside Analogs

V. The Mode of Action of Nucleosides in Relation to Their Structure

References

Chapter 9. The Design of Insecticidal Chlorohydrocarbon Derivatives

I. Introduction

II. Physical and Chemical Toxicants

III. Aromatic Chlorohydrocarbon Insecticides: DDT Group

IV. Chlorohydrocarbon Insecticides Derived from Reduced Cyclic Systems

References

Author Index

Subject Index