Transdermal and topical drug delivery systems:
Gespeichert in:
| Weitere Verfasser: | |
|---|---|
| Format: | Buch |
| Sprache: | English |
| Veröffentlicht: |
Buffalo Grove, Ill.
Interpharm Press
1997
|
| Online-Zugang: | Inhaltsverzeichnis |
| Beschreibung: | XX, 713 S. graph. Darst. |
| ISBN: | 1574910418 |
Internformat
MARC
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| 245 | 1 | 0 | |a Transdermal and topical drug delivery systems |c Tapash K. Ghosh ... ed.-in-chief |
| 264 | 1 | |a Buffalo Grove, Ill. |b Interpharm Press |c 1997 | |
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| 700 | 1 | |a Ghosh, Tapash K. |4 edt | |
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Datensatz im Suchindex
| _version_ | 1804145138716377088 |
|---|---|
| adam_text | CONTENTS
PREFACE xv
DEDICATION xix
1. TRANSDERMAL AND TOPICAL DELIVERY SYSTEMS:
AN OVERVIEW AND FUTURE TRENDS 1
Tapash K. Ghosh and William R. Pfister
Transdermal Drug Transport 3
Skin Anatomy 3
Mechanism of Drug Transport 6
Types of Dermal Drug Delivery 7
Topical Delivery 7
Transdermal Delivery 8
Future Trends 1 4
Transdermal Therapeutic Products in Research and Development 14
Dermal Therapeutic Systems in Research and Development 20
Permeation Enhancement 21
Device Designs 22
Transmucosal Drug Delivery Systems 22
Summary 23
Acknowledgments 25
References 25
Hi
iv Contents
2. TRANSDERMAL AND DERMAL THERAPEUTIC
SYSTEMS: CURRENT STATUS 33
William R. Pfister
Transdermal and Dermal Therapeutic Systems 34
Product Market 34
Product Characteristics 38
Transdermal Drug Delivery Products 56
Treatment of Motion Sickness 5 7
Treatment of Hypertension 64
Treatment of Pain 64
Treatment of Angina Pectoris 65
Female Hormone Replacement Therapy 6 7
Male Hormone Replacement Therapy 71
Smoking Cessation Therapy 73
Dietary Aids 75
Dermal Therapeutic Systems 76
Product Attributes 76
Historical Developments 77
Dermal Drug Delivery Products 78
Treatment of Calluses, Corns, and Warts 86
Treatment of Pain 87
Treatment of Rheumatism 89
Treatment of Inflammation 89
Topical Local Anesthesia 93
Antimicrobial Agents 94
Wound Dressings 95
Dermal Cosmetic and Diagnostic Patches 95
Cosmetic Patches 95
Noninvasive Diagnostic Patches 95
Therapeutic Drug Monitoring 97
Summary 99
Acknowledgments 100
References 100
3. THE PREDICTION OF TRANSDERMAL
PERMEATION: MATHEMATICAL MODELS 113
Kakuji Tojo
Drug Transport Across the Stratum Corneum 115
Homogeneous Model 115
Random Brick Model 116
Contents v
Nonsteady State Diffusion Model 1I9
Effect of Microcirculation 121
Effect of Binding 121
Skin Metabolism 122
Prediction of Blood Concentration 125
In Vitro Method of Evaluation for Model Parameters 126
Prediction of Penetration Rate Under Iontophoresis 128
Effect of Ultrasound 132
Effect of Temperature 134
Conclusions 135
References 135
4. PREFORMULATION ASPECTS OF
TRANSDERMAL DRUG DELIVERY SYSTEMS 139
Samir D. Roy
Prediction of Transdermal Permeation and
Mathematical Modeling 140
Shin Structure and Barrier Function 140
Physicochemical Properties of Drugs and Skin Permeation 143
Influence of pH on Drug Permeability 152
Selection of Drug Candidates 156
Drug Release from Transdermal Devices 158
Transdermal Devices 158
Release Kinetics from Matrix Devices 159
Summary 163
References 164
5. PRECLINICAL ASSESSMENT OF TRANSDERMAL
DRUG DELIVERY SYSTEMS 167
Thomas S. Spencer
In Vitro Skin Permeation Techniques 168
Donor Compartment 169
Permeation Membrane 173
Receptor Compartment I 77
In Vivo Evaluation in Different Animal Models 179
Evaluation of Skin Toxicity, Skin Binding, and Skin Metabolism 181
Pharmacokinetics Following Transdermal Administration 183
vi Contents
Mass Balance Following Transdermal Administration 185
In Vitro/In Vivo Correlation 186
Summary 188
References 188
6. SAFETY ASSESSMENT OF TRANSDERMAL
AND TOPICAL DERMATOLOGICAL PRODUCTS 191
John Ademola and H.I. Maibach
Evaluation of Skin Irritation and Sensitization 193
Mechanisms of Dermal Hypersensitivity, Allergic Contact
Dermatitis, and Atopic Dermatitis 194
In Vivo Methods to Evaluate Dermal Sensitization 198
In Vitro Methods for Assessing Skin Irritancy of Transdermal
Therapeutic Systems 201
Toxicology and Shin Irritation 201
Toxicological Evaluation of Transdermal and Topical Products 202
Factors Affecting the Shin Toxicity of Topical Products 203
Systemic Toxicity and Adverse Shin Reactions 205
Clinical Pharmacological Considerations of Skin Penetration
Enhancement 206
Regulatory Considerations 208
Summary 209
References 210
7. CLINICAL ASSESSMENT OF TRANSDERMAL
DRUG DELIVERY SYSTEMS 215
Suneel K. Gupta, Gayatri Sathyan, and Stephen S. Hwang
Pharmacokinetic and Pharmacodynamic Characterization 216
Pharmacokinetic Characterization 216
Examples of Pharmacokinetic Modeling 225
Pharmacodynamic Characterization 237
Efficacy and Safety Characterization 239
Efficacy Studies 239
Safety Studies 240
Conclusions 242
References 242
Contents vii
8. DESIGN, DEVELOPMENT, MANUFACTURING, AND
TESTING OF TRANSDERMAL DRUG DELIVERY
SYSTEMS 249
Timothy A. Peterson, Stephen M. Wick, and Chan Ko
Transdermal System Design Alternatives 250
Reservoir-Type Product Design 253
Matrix Product Design 254
Drug-in-Adhesive Product Design 256
Multilaminate Drug-in-Adhesive Product Design 258
Patient Preference Among Product Designs 259
Patch Design Selection Process 259
Materials Selection for Transdermal Drug Delivery Systems 263
Pressure Sensitive Adhesives for TDD Systems 263
Packaging Components 2 76
Membranes 281
Manufacturing Technology in TDD 283
Unit Operations 284
Sample Manufacturing Process for a DIA Design 286
Scale-Up from Laboratory to Production 288
Information Data Package 288
Process Validation 290
Testing of Transdermal Drug Delivery Systems 291
Chemical Tests 292
Physical Tests 292
Summary 293
References 294
9. TRANSDERMAL DELIVERY OF p-ADRENERGIC
THERAPEUTICS 299
Tapash K. Ghosh, John Ademola, and William R. Pfister
Skin Irritation/Sensitization of p-Adrenergic Therapeutics 301
Transdermal Delivery of p-Adrenergics 304
^-Agonists 305
^-Antagonists 309
Transdermal Feasibility Assessment 312
Development of a Metoprolol Transdermal Delivery System 314
Patch Preparation 315
In Vitro Study 315
viii Contents
Pharmacokinetic Study 31 7
Pharmacodynamic Study 318
Conclusion 320
Summary 321
Acknowledgment 321
References 322
10. SKIN ABSORPTION ENHANCEMENT BY PHYSICAL
MEANS: HEAT, ULTRASOUND, AND ELECTRICITY 327
Ying Sun
Chemical Physical Drug Permeation Enhancement 327
Permeation Enhancement by Thermal Energy 329
Temperature Effects on Drug Diffusion 329
Skin Temperature Site Variations 330
Effect of Temperature on In Vitro Drug Permeation 330
Effect of Exercise and Temperature on In Vivo Drug Absorption 333
Use of Thermal Energy for Skin Absorption Enhancement 336
Permeation Enhancement by Ultrasonic Energy 337
Phonophoresis (Sonophoresis) 337
Effect of Ultrasound Frequency on Phonophoresis 341
Permeation Enhancement by Electric Energy 344
Iontophoresis 344
Electroporation 346
Reverse Iontophoresis and Noninvasive Diagnostic Applications 34 7
Combination of Different Enhancement Methods 349
Future Directions 349
Summary 351
Acknowledgment 352
References 352
11. CHEMICAL MEANS OF TRANSDERMAL DRUG
PERMEATION ENHANCEMENT 357
Nadir Buyuktimkin, Servet Buyuktimkin, and J. Howard Rytting
Properties of Permeation Enhancers 358
Ideal Properties 359
Contents ix
Mechanisms of Action 360
Instrumental Assessment of Enhancer Interactions 361
Development of New Permeation Enhancers 363
Permeation Enhancers: Formulation Considerations 363
Selection Criteria 363
Formulation/Compatibility Assessment 364
Quantitative Assessment of Permeation Enhancement
and Techniques for Optimization 367
In Vitro Techniques 366
In Vivo Techniques 371
Classification of Permeation Enhancers 371
Review of the Literature 3 71
Chemical Classification 372
Conclusions and Future Perspectives 442
Acknowledgments 446
References 447
12. OXAZOLIDINONES: A NEW CLASS OF
PERMEATION ENHANCER 477
Vithal J. Rajadhyaksha, Kuldeepak Sharma, and
William R. Pfister
Permeation Enhancers 478
Oxazolidinones: Rationale and Chemistry 479
Conceptual Development 4 79
Chemical Structure and Properties 482
SR-38 Permeation Enhancer 485
Physicochemical Properties 485
Formulation Guidelines 487
Mechanisms of Action 489
SR-38 Safety Evaluation 490
Preclinical Safety Studies 490
Skin Permeability and Pharmacokinetics 492
Targeted and Enhanced Absorption with SR-38 493
Targeted Local Topical Delivery 493
Enhanced Percutaneous Absorption 499
Summary 502
x Contents
Acknowledgments 502
References 503
13. DRUG DELIVERY FROM TOPICAL FORMULATIONS 511
John Ademola
Characteristics of Topical Formulations 512
Theory of Drug Release from Topical Formulations 513
Kinetic Factors Affecting Drug Release 513
Thermodynamic Determinants of Drug Release 514
Formulation Optimization 517
The Selection of Ingredients 517
Mutual Solubility/Compatibility 518
Experimental Design 519
Modeling and Optimization 520
Nontraditional Topical Drug Delivery Formulations 520
Permeation Enhancers 521
Liposomes in the Delivery of Topical Drugs 522
Factors Affecting Drug Delivery from Topical Formulations 523
Assessment of Drug Delivery from Topical Formulations 526
In Vitro Drug Release Studies 526
In Vivo Drug Release Studies 528
Bioavailability and Bioequivalence of Topical Formulations 530
Quantitation of Drug Molecules in Different Skin Layers 531
Summary 534
Acknowledgment 534
References 534
14. FORMULATION OF TOPICAL DRUG DELIVERY
SYSTEMS 539
Monica Ramchandani and Rohinton Toddywala
Design of Topical Products 542
Emulsions and Microemulsions 542
Ointments 546
Gels 54 7
Liposomes 547
Aerosols 549
Others 549
Contents xi
Excipients Used in Topical Products 550
Oil-Based Excipients 550
Aqueous-Based Excipients 550
Surfactants 550
Emulsion Stabilizers 554
Solubilizers 554
Humectants and Emollients 554
pH Adjusters 555
Skin Penetration Enhancers 555
Shin Protectants 555
Viscosity Imparting Agents 555
Preservatives 556
Antioxidants 556
Propellants 557
Evaluation of Topical Products 557
Physicochemical Testing 55 7
In Vitro Studies 559
Rheology of Topical Formulations 560
Preservative Challenge Test 560
Testing of Topical Formulations on the Shin 561
Toxicology of Topical Formulations 562
In Vivo Evaluation 562
In Vitro Evaluation 564
Clinical Testing of Topical Formulations 565
Clinical Evaluation 565
Bioavailability 567
Shin Stripping Studies 567
Manufacture and Scale-Up of Topical Formulations 568
Mixing or Blending Equipment 568
Dispersion Equipment 568
Emulsification Equipment 569
Vacuum Processors 569
Stability Testing of Topical Formulations 571
Preformulation Stage 5 71
Product Development Stage 5 71
Post-NDA Stage 574
Summary 574
References 574
xii Contents
15. TOPICAL FORMULATION DEVELOPMENT OF
LEUKOTRIENE B4 RECEPTOR ANTAGONISTS
FOR PSORIASIS 579
Donald J. Fretland, Rajeev Gokhale, and James Truelove
The Arachidonic Acid Cascade and Leukotriene B^ 580
Formulation Development 582
Solubility 582
Initial Formulations 583
Final Formulations 583
Models of Skin Inflammation 586
Animal Models 586
Chemically Induced Models 587
Results 587
Conclusion 588
Acknowledgments 589
References 590
16. RECENT ADVANCES IN TOPICAL DRUG DELIVERY
SYSTEMS 593
Jue-Chen Liu and Stephen J. Wisniewski
Topical Delivery Systems 593
Liposomes 594
Dermal Membrane Structure (DMSj 598
Glycospheres 598
Microsponge System 599
Cyclodextrins 601
Strategies for Irritation Reduction 603
Drug Delivery Approach 603
Irritation Mitigants 604
Compound Modification 605
Topical Formulation Assessment Methodologies 606
Formulation Characterization 606
Drug Deposition and Delivery Pathway 606
Additional Shin Measurement Techniques 607
Noninvasive Irritation Measurement 607
Summary 607
Acknowledgment 608
References 608
Contents xiii
17. TOPICAL PROTECTIVE AND COSMETIC PRODUCTS 613
Joel L. Zatz and David C. Steinberg
Moisturizers 615
Formulation 617
Testing 618
Sunscreens 619
Formulation 619
Testing 621
Insect Repellants 622
Formulation 622
Testing 623
Lip and Skin Protectants 623
Formulation 624
Testing 625
Barrier Creams 626
Summary 626
References 626
18. BIOPHARMACEUTICAL CONSIDERATIONS
FOR TOPICAL AND TRANSDERMAL
DRUG DELIVERY SYSTEMS 629
Vijay K. Tammara, Raman K. Baweja, Angelica Dorantes,
John P. Hunt, Francis R. Pelsor, He Sun, Vinod P. Shah,
and Jonathan K. Wilkin
Topical (Dermatological) Products 631
Transdermal Drug Delivery Systems 631
Regulatory Issues and Considerations 632
Investigational New Drug Application 632
New Drug Application 636
Abbreviated New Drug Application 637
Regulatory Considerations for Topical and Transdermal
Products 638
Overall Summary Information 639
Background Information 640
Metabolism and Elimination 640
Bioavailability/Bioequivalence 640
Single- and Multiple-Dose Pharmacokinetics 642
Dose Proportionality 642
Special Populations 642
xiv Contents
Drug-Drug Interactions 643
Pharmacokinetics/Pharmacodynamics Relationships 643
Population Analyses 643
In Vitro Testing 643
In Vitro In Vivo Correlation 644
Residual Drug and Product Drug Delivery Characteristics 644
Adhesion Information 644
Analytical Methodology 644
Drug Formulation 645
Protein Binding 645
Labeling 645
Present Regulatory Considerations and Waiver Requirements 645
Generic Versions of Topical/Transdermal Drug Products 647
In Vitro Release Technology for Topical Drug Products 649
In Vitro Release Methods for Transdermal Patches 650
In Vitro Release Method for Dermatological (Topical)
Creams, Ointments, and Gels 651
Summary 651
Acknowledgments 652
Glossary 652
Symposia/Workshops 655
References 656
INDEX 659
|
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