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Drug Design -

Drug Design (eBook)

Medicinal Chemistry: A Series of Monographs, Vol. 4

E. J. Ariens (Herausgeber)

eBook Download: PDF
2013 | 1. Auflage
506 Seiten
Elsevier Science (Verlag)
978-1-4832-1606-5 (ISBN)
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69,42 inkl. MwSt
(CHF 67,80)
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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.
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.

Front Cover 1
Drug Design 4
Copyright Page 5
Table of Contents 6
List of Contributors 10
Preface 12
Contents of Other Volumes 14
Chapter 1. Biopharmaceutics as a Basis for the Design of Drug Products 18
I. Introduction 18
II. Biopharmaceutics—The Science of Input 20
III. Bioavailability 23
IV. Selection of the Route of Administration 25
V. Getting Drugs into Solution 29
VI. Gastrointestinal Membrane Transport 41
VII. Getting Drugs into the Small Intestine 46
ACKNOWLEDGMENTS 49
REFERENCES 49
Chapter 2. Peroral Solid Dosage Forms with Prolonged Action 54
I. Introduction 54
II. Types of Peroral Prolonged Action Dosage Forms 56
III. Evaluation of Peroral Prolonged Action Dosage Forms 65
IV. Pharmacokinetics 72
V. Additives 79
VI. Manufacturing Process 81
REFERENCES 88
Chapter 3. Parenteral Dosage Forms with Prolonged Action 92
I. Introduction 92
II. Types of Parenteral Prolonged Action Dosage Forms 93
III. Evaluation of Parenteral Prolonged Action Dosage Forms 97
REFERENCES 107
Chapter 4. Design of Topical Drug Products: Pharmaceutics 110
I. Skin 110
II. Dermatological Bases 119
III. Drugs 148
IV. Testing 153
REFERENCES 160
Chapter 5. Design of Topical Drug Products: Biopharmaceutics 166
I. Introduction 166
II. Fundamentals of Drug Diffusion into Human Skin 168
III. Optimizing Drug Availability from Topical Dosage Forms 176
IV. Summary 205
REFERENCES 206
Chapter 6. The Design of Sunscreen Preparations 210
I. Introduction 210
II. Ultraviolet Radiation 211
III. Human Reactions to Ultraviolet Radiation 217
IV. Sunscreen Preparations 224
V. Multiple Action Products 244
VI. Evaluation of Sunscreen Preparations 247
REFERENCES 252
Chapter 7. Litholytic Agents: Preventive and Curative Drugs for Nephrolithiasis 254
I. Introduction 254
II. Factors Influencing Stone Formation 256
III. Litholytic Agents 259
IV. Possibilities for Dissolving the Four Different Types of Kidney Stones 262
V. Clinical Application of the Litholytic Agents for the Dissolution of Kidney Stones 294
VI. Summary 297
ACKNOWLEDGMENTS 298
REFERENCES 298
Chapter 8. The Design of Biologically Active Nucleosides 302
I. Introduction 303
II. Functional Considerations 310
III. Structural Considerations 323
IV. Approaches toward Enhancing the Biological Activity of Nucleoside Analogs 373
V. The Mode of Action of Nucleosides in Relation to Their Structure 375
ACKNOWLEDGMENTS 377
REFERENCES 377
Chapter 9. The Design of Insecticidal Chlorohydrocarbon Derivatives 396
I. Introduction 396
II. Physical and Chemical Toxicants 398
III. Aromatic Chlorohydrocarbon Insecticides: DDT Group 407
IV. Chlorohydrocarbon Insecticides Derived from Reduced Cyclic Systems 432
REFERENCES 458
Author Index 462
Subject Index 488

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