Transdermal Controlled Systemic Medications

Transcription

1 Transdermal Controlled Systemic Medications edited by YIEW.CHIEN Controlled Drug-Delivery Research Center Rutgers-The State University of New Jersey Piscataway, New Jersey MARCEL DEKKER, INC. New York and Basel

2 Contents Preface Contributors Hi v 1. Advances in Transdermal Systemic Medication 1 Yie W. Chien I. Introduction 1 II. The Skin: Site of Transdermal Drug Administration 2 III. Early Development of Transdermal Drug Delivery 6 IV. Recent Developments in Transdermal Drug Delivery 14 References 21 DEVELOPMENT AND PRECLINICAL ASSESSMENTS OF. TRANSDERMAL THERAPEUTIC SYSTEMS \ 2. Developmental Concepts and Practice in Transdermal Therapeutic Systems 25 Yie W. Chien I. Introduction 25 II. Fundamentals of Rate-Controlled Transdermal Drug Delivery 26 III. Approaches to the Development of Transdermal Therapeutic Systems 31 IV. Kinetic Evaluations of Transdermal Therapeutic Systems 44 V. Formulation Design and Optimization 56 XI

3 xii I Contents VI. VII. Enhancement of Transdermal Controlled Drug Delivery 59 Generic Program for Transdermal Drug Delivery System Development 75 References Alterations in Skin Permeability 83 Eugene R. Cooper I. Introduction 83 II. Enhancement Recognition 84 III. Membrane Alterations 86 IV. Reduction of Penetration 90 V. Summary 90 References Pressure-Sensitive Adhesives: Science and Engineering 93 Martin C. Musolf I. II. III. IV. Introduction Pressure-Sensitive Adhesives Pressure-Sensitive Adhesives for Transdermal Applications Summary References 5. Polymeric Materials: Assessment of Skin Biocompatibility 113 Kevin S. Weadock, James M. Pachence, Richard A. Berg, and Frederick H. Silver I. Introduction 113 II. Biocompatibility Testing of Polymers 114 III. Cellular Response to Polymers \ 117 IV. Polymer Degradation 118 V. Conclusions 120 References Design and Calibration of In Vitro Permeation Apparatus 127 Kakuji Tojo I. Introduction 127 II. Design of In Vitro Skin Permeation Apparatus 129 III. Method for Characterizing the Hydrodynamics of In Vitro Systems 137 IV. Correlation Equation for Mass Transfer Coefficient 141

4 Contents I xiii V. Effect of the Diffusion Boundary Layer on Drug Permeation 143 VI. Calculation of Intrinsic Rate of Permeation 151 VII. Effect of Temperature on Drug Permeation 154 VIII. Conclusion 156 References In Vitro Evaluations of Transdermal Drug Delivery 159 Yih-Chain Huang I. Introduction 159 II. In Vitro Skin Permeation Kinetics 160 III. Conclusion 177 References In Vivo Evaluations of Transdermal Drug Delivery 179 Richard H. Guy, Jonathan Hadgraft, Robert S. Hinz, Kathleen V. Roskos, and Daniel A. W. Bucks I. Introduction 179 II. Animal Models 181 III. Human Experimentation 192 IV. Kinetic Modeling of Transdermal Drug Delivery 204 V. Summary 215 References 216 CLINICAL ASSESSMENTS OF TRANSDERMAL THERAPEUTIC SYSTEMS 9. Transdermal Delivery of Nitroglycerin I 227 Nathaniel Reichek I. Introduction ; 227 II. History of Transdermal Nitroglycerin v 228 III. Problems in Assessment of Long-Acting Nitrates for Angina Prophylaxis 229 IV. Antianginal Effect of Nitroglycerin Ointment 231 V. Antianginal Effect of Nitroglycerin Patches 233 VI. Attenuation of Antianginal Effects of Other Nitrates 238 VII. Studies in Progress 240 VIII. Future Directions 241 IX. Conclusions 241- References 242

5 xiv I Contents 10. Transdermal Delivery of Nitroglycerin II 245 v - Dzenana E. Rezakovic I. Introduction 245 II. Clinical Trials of Nitroglycerin Patches in Coronary Artery Disease 246 III. Hemodynamic Trials of Nitroglycerin Patches 284 IV. Multicenter Studies of the Nitroglycerin Patch in Europe 295 V. Old and New Data About Nitroglycerin Patch Efficacy 301 VI. Conclusions 309 References Transdermal Delivery of Clonidine 321 G. S. Perlmutter, Ester Paran, Bonita Falkner, Carol M. Bies, T. Fagan, Robert R. Chase, and David T. Lowenthal I. Introduction 321 II. Mechanism of Action 322 III. Pharmacokinetics 322 IV. Pharmacological Effects 323 V. Adverse Effects 326 VI. Conclusions 329 References Transdermal Delivery of Bupranolol 333 Inge Weiss, Hans-Michael Wolff, Gunter Cordes, and Willi Cawello I. Introduction 333 II. Transdermal Absorption of Bupranolol in Rabbits 334 III. Pharmacokinetic and Pharmacodynamic Studies in Human Volunteers v 339 IV. Evaluation of Pharmacodynamic Effects Compared to Peroral Propranolol 343 V. Summary 345 References 345 ENGINEERING AND MANUFACTURING OF TRANSDERMAL THERAPEUTIC SYSTEMS 13. Development of Processes and Equipment for Rate-Controlled Transdermal Therapeutic Systems 349 John W. Dohner I. Introduction 349 II. Transdermal Products Developed at Alza 349

6 Contents I xv III. Manufacturing Processes and Equipment 351 IV. Engineering Development of Transdermal Systems 354 V. Commercial Production of Transdermal Systems 362 VI. Summary 363 References Development of Processes and Technology for Adhesive- Type Transdermal Therapeutic Systems 365 Hans-Michael Wolff, Hans Rainer Hoffmann, and Gunter Cordes I. Introduction 365 II. Galenical Structure of the Deponit System 366 III. Manufacturing Process 368 IV. Comments on Galenical Design 373 References Product Development and Technology Transfer for Transdermal Therapeutic Systems 379 David J. Bova, Valerie N. Ahmuty, Robert L. Cirrito, Karen O'Toole Holmes, K. Kasper, Caroline LaPrade, R. LaPrade, Gustav A. Maag, Juan A. Mantelle, John A. MeCarty, J. Miranda, Frankie A. Morton, and Steven Sablotsky I. Introduction 379 II. Research Phase 380 III. Product Development and Technology Transfer 381 IV. Conclusion 396 REGULATORY REQUIREMENTS AMONG INTERNATIONAL HEALTH AUTHORITIES 16. Regulatory Considerations in Transdermal Drug Delivery Systems in the United States 399 Vinod P. Shah and Jerome P. Skelly I. Introduction 399 II. Biopharmaceutic Considerations 401 III. Regulatory Requirements 408 IV. Generic Versions of Transdermal Drug Products Regulatory Approval of Transdermal Therapeutic Systems in the United Kingdom 411 Paul Adams I. Introduction 411 II. Product License Applications 412

7 xvi I Contents III. Abridged Applications 412 IV. Conclusion Regulatory Approval of Transdermal Therapeutic Systems in Japan 419 Tsuneji Nagai and Yoshiharu Machida I. Introduction 419 II. Application Requirements for Approval of New Prescription Drugs in Japan 420 III. Scientific Data Required for Approval of Transdermal Therapeutic Systems 423 IV. Procedure and Time Needed for Approval 429 V. Regulatory Policy in Other Asian Countries 429 Reference 430 Index 431