Ariëns Drug Design

Medicinal Chemistry: A Series of Monographs, Vol. 4
1. Auflage 2013
ISBN: 978-1-4832-1606-5
Verlag: Elsevier Science & Techn.
Format: PDF
Kopierschutz: 1 - PDF Watermark

E-Book, Englisch, 506 Seiten, Web PDF

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.

Autoren/Hrsg.

Ariëns, E. J.

Inhaltsverzeichnis

1;Front Cover;1
2;Drug Design;4
3;Copyright Page;5
4;Table of Contents;6
5;List of Contributors;10
6;Preface;12
7;Contents of Other Volumes;14
8;Chapter 1. Biopharmaceutics as a Basis for the Design of Drug Products;18
8.1;I. Introduction;18
8.2;II. Biopharmaceutics—The Science of Input;20
8.3;III. Bioavailability;23
8.4;IV. Selection of the Route of Administration;25
8.5;V. Getting Drugs into Solution;29
8.6;VI. Gastrointestinal Membrane Transport;41
8.7;VII. Getting Drugs into the Small Intestine;46
8.8;ACKNOWLEDGMENTS;49
8.9;REFERENCES;49
9;Chapter 2. Peroral Solid Dosage Forms with Prolonged Action;54
9.1;I. Introduction;54
9.2;II. Types of Peroral Prolonged Action Dosage Forms;56
9.3;III. Evaluation of Peroral Prolonged Action Dosage Forms;65
9.4;IV. Pharmacokinetics;72
9.5;V. Additives;79
9.6;VI. Manufacturing Process;81
9.7;REFERENCES;88
10;Chapter 3. Parenteral Dosage Forms with Prolonged Action;92
10.1;I. Introduction;92
10.2;II. Types of Parenteral Prolonged Action Dosage Forms;93
10.3;III. Evaluation of Parenteral Prolonged Action Dosage Forms;97
10.4;REFERENCES;107
11;Chapter 4. Design of Topical Drug Products: Pharmaceutics;110
11.1;I. Skin;110
11.2;II. Dermatological Bases;119
11.3;III. Drugs;148
11.4;IV. Testing;153
11.5;REFERENCES;160
12;Chapter 5. Design of Topical Drug Products: Biopharmaceutics;166
12.1;I. Introduction;166
12.2;II. Fundamentals of Drug Diffusion into Human Skin;168
12.3;III. Optimizing Drug Availability from Topical Dosage Forms;176
12.4;IV. Summary;205
12.5;REFERENCES;206
13;Chapter 6. The Design of Sunscreen Preparations;210
13.1;I. Introduction;210
13.2;II. Ultraviolet Radiation;211
13.3;III. Human Reactions to Ultraviolet Radiation;217
13.4;IV. Sunscreen Preparations;224
13.5;V. Multiple Action Products;244
13.6;VI. Evaluation of Sunscreen Preparations;247
13.7;REFERENCES;252
14;Chapter 7. Litholytic Agents: Preventive and Curative Drugs for Nephrolithiasis;254
14.1;I. Introduction;254
14.2;II. Factors Influencing Stone Formation;256
14.3;III. Litholytic Agents;259
14.4;IV. Possibilities for Dissolving the Four Different Types of Kidney Stones;262
14.5;V. Clinical Application of the Litholytic Agents for the Dissolution of Kidney Stones;294
14.6;VI. Summary;297
14.7;ACKNOWLEDGMENTS;298
14.8;REFERENCES;298
15;Chapter 8. The Design of Biologically Active Nucleosides;302
15.1;I. Introduction;303
15.2;II. Functional Considerations;310
15.3;III. Structural Considerations;323
15.4;IV. Approaches toward Enhancing the Biological Activity of Nucleoside Analogs;373
15.5;V. The Mode of Action of Nucleosides in Relation to Their Structure;375
15.6;ACKNOWLEDGMENTS;377
15.7;REFERENCES;377
16;Chapter 9. The Design of Insecticidal Chlorohydrocarbon Derivatives;396
16.1;I. Introduction;396
16.2;II. Physical and Chemical Toxicants;398
16.3;III. Aromatic Chlorohydrocarbon Insecticides: DDT Group;407
16.4;IV. Chlorohydrocarbon Insecticides Derived from Reduced Cyclic Systems;432
16.5;REFERENCES;458
17;Author Index;462
18;Subject Index;488