Based on a training course developed by Dr. Joseph T. Piechocki and other experts in this field whose contributions appear in this book for two International Meetings on the Photostability of Drugs and Drug Products, this text clarifies the guidelines set by the International Conference on Harmonization (ICH) and provides a comprehensive background in the scientific principles involved in photostability testing. Presenting the advantages and disadvantages of various procedures so the reader can select and utilize the most appropriate technique best-suited to their needs, this source includes references to current literature in the field and offers an opinion on future opportunities and challenges.
Author(s): T. Piechocki Joseph, Karl Thoma
Series: Drugs and the Pharmaceutical Sciences
Edition: 1
Publisher: Informa Healthcare
Year: 2006
Language: English
Pages: 439
Pharmaceutical Photostability
and Stabilization Technology......Page 10
Table of Contents......Page 15
DRUGS AND THE PHARMACEUTICAL SCIENCES A Series of Textbooks and Monographs......Page 2
Preface......Page 13
REFERENCES......Page 14
Contributors......Page 20
Bordier......Page 22
Table of Contents......Page 0
Coebergh......Page 23
Arny......Page 26
Blythe......Page 31
Lachman et al.......Page 32
Reisch......Page 34
Thoma......Page 35
Kerker......Page 36
Gauglitz......Page 37
Tønnesen......Page 38
Moore......Page 39
Beaumont......Page 41
Piechocki......Page 43
Matsuda......Page 44
Matsuo......Page 45
Lachman et al.......Page 47
Alsante et al.......Page 48
Japanese......Page 49
Draft 1......Page 50
Draft 2......Page 51
Draft 4......Page 52
Final Document......Page 53
REFERENCES......Page 54
Forced Degradation Studies......Page 67
Irradiation Sources......Page 68
Source Selection......Page 69
Exposure Level......Page 70
Irradiance Level and Temperature Effects......Page 72
Sample Cooling......Page 73
Calibration......Page 74
Meter Calibration......Page 75
Presentation of Samples......Page 76
Interpretation of Data......Page 77
REFERENCES......Page 79
Light......Page 81
Einstein......Page 83
Equivalency......Page 84
Inner Filter Effect......Page 85
Room Light......Page 86
Lux (lx)......Page 87
Photochromism......Page 88
Photometer......Page 89
Radiometer......Page 90
D65......Page 91
Xenon Lamps......Page 92
Metal-Halide Lamps......Page 93
Cool White......Page 95
REFERENCES......Page 96
BASIC CONCEPTS......Page 99
Direct Drug Photoreactivity......Page 100
Indirect Photoreactivity......Page 101
ACTINOMETRY......Page 102
Solid Tablets......Page 103
INTERNATIONAL COMMITTEE FOR HARMONIZATION GUIDELINE......Page 104
CONCLUSIONS......Page 105
REFERENCES......Page 106
EMISSION SPECTRA......Page 107
Arc Lamps......Page 108
INCIDENT RADIATION......Page 109
ABSORPTION SPECTRA......Page 110
Activation Spectra......Page 111
Action Spectra......Page 112
Pseudo-Action Spectrum......Page 114
SPECTRAL POWER DISTRIBUTIONS......Page 115
SUMMARY......Page 116
REFERENCES......Page 117
INTERNATIONAL CONFERENCE ON HARMONIZATION OPTIONS......Page 119
Fluorescent Lamps......Page 120
Ultraviolet Lamps......Page 124
Visible Lamps......Page 125
Xenon Lamps......Page 126
SOURCE SELECTION CRITERIA......Page 130
LAMP STUDIES......Page 135
CONCLUSION......Page 136
REFERENCES......Page 137
GLASSES......Page 140
Quartz......Page 143
Aging......Page 144
Window (Plate) Glass......Page 145
Self-Cleaning Glass......Page 146
FILTERS......Page 147
Absorption......Page 148
Dichroic......Page 149
Plastic......Page 150
CONTAINERS......Page 151
SUMMARY......Page 153
REFERENCES......Page 155
INTRODUCTION......Page 158
Chemical Methods......Page 159
Basic Photokinetic Equations......Page 160
Amount of Radiation Absorbed......Page 161
Monitoring of Actinometer Response: Spectrophotometric Analysis......Page 163
SELECTED CHEMICAL ACTINOMETERS......Page 164
The Azobenzene Actinometer......Page 165
The Meso-diphenylhelianthrene Actinometer......Page 167
The Aberchrome 540 Actinometer......Page 168
The Potassium Reineckate Actinometer......Page 169
The Quinine Actinometer......Page 170
SPECIAL APPLICATIONS......Page 172
Laser Actinometry with Ferrioxalate......Page 173
Laser Intensity Measurements with the Azobenzene Actinometer......Page 174
Laser Intensity Measurements with a Photooxygenation Actinometer......Page 175
Chemical Actinometry of Polychromatic Light Sources......Page 176
The Matsuura Method for Approximate Estimates of Solid-State Quantum Yields......Page 178
The First Actinometric Reaction on a Solid Support......Page 179
REFERENCES......Page 180
Radiant Flux (Power) and Luminous Flux (Lumen)......Page 183
Radiant and Luminous Intensity......Page 184
Radiance and Luminance......Page 185
QUALITY OF MEASUREMENT......Page 186
Spatial Response......Page 187
Spectral Response......Page 188
Absolute Calibration......Page 191
PHOTOSTABILITY......Page 192
REFERENCES......Page 194
Forced Degradation......Page 195
Sources......Page 196
Chambers......Page 197
Mapping......Page 200
Chamber Temperature and Lamp Intensity......Page 204
Temperature Control......Page 206
CONTAINERS......Page 207
Cross-Contamination of Samples......Page 208
Greenhouse Effect......Page 209
Shading......Page 211
DRUG SUBSTANCE......Page 212
DRUG PRODUCTS......Page 216
CONCLUSION......Page 217
REFERENCES......Page 218
REACTION KINETICS AND PHOTOSTABILITY......Page 220
Derivation of the Photochemical Rate Equation......Page 223
Experimental Examples......Page 225
Deviations from First-Order Kinetics......Page 226
KINETICS OF PHOTOSENSITIZED REACTIONS......Page 228
APPLICATION OF KINETIC MEASUREMENTS TO REACTION MECHANISM DETERMINATION IN PHOTOSTABILITY......Page 229
Initial Mechanism Studies......Page 230
Singlet Oxygen Detection......Page 231
Free-Radical Formation......Page 232
Laser Flash Photolysis......Page 234
Detection of Free Radicals......Page 235
Photodehalogenation Reactions......Page 236
REFERENCES......Page 237
INTRODUCTION......Page 239
DILUENT MEDIATED PHOTOCHEMISTRY......Page 241
EXCIPIENT MEDIATED PHOTOCHEMISTRY......Page 243
PRODUCT COMPONENT MEDIATED PHOTOCHEMISTRY......Page 260
REFERENCES......Page 264
TESTING APPARATUS/CHAMBERS......Page 268
FLUORESCENT LAMP CHAMBERS......Page 271
Binder GmbH......Page 272
Caron......Page 273
Environmental Specialties (LUWA)......Page 274
Hotpack (SP Industries)......Page 275
Nagano Science......Page 276
Percival Scientific, Inc.......Page 277
Powers Scientific, Inc.......Page 278
Q-Lab Corporation......Page 279
Termaks......Page 280
Weiss Gallenkamp......Page 281
Atlas Material Testing Technology LLC......Page 284
Luzchem Research Inc......Page 286
Q-Lab......Page 287
Atlas Material Testing Technology LLC......Page 288
Dr. Hönle......Page 289
Rumed® (Rubarth Apparate GmbH)......Page 291
MAPPING......Page 292
Brumfield......Page 294
Clapham and Sanderson......Page 298
Baertschi......Page 304
REFERENCES......Page 305
Selection of a Suitable Photostability Testing Cabinet......Page 308
Measurement of the Photon Exposure......Page 310
Selection of a Suitable Photon Dose......Page 311
Spectrophotometry......Page 312
High Performance Liquid Chromatography......Page 313
Liquid Chromatography-Mass Spectrometry......Page 315
Particle Beam......Page 316
CONCLUSION......Page 317
REFERENCES......Page 318
Brown Glass......Page 319
Other Colors......Page 322
Layer Thickness......Page 323
Immediate Containers for Liquid Dosage Forms......Page 324
Blisters......Page 325
Blisters......Page 326
Colored......Page 327
Foils......Page 331
Cartons......Page 332
REFERENCES......Page 333
Influence of Concentration......Page 336
Influence of Sample Geometry......Page 337
Influence of the Sample Surface and Volume......Page 338
Influence of the Drug Physical Form......Page 339
Influence of Humidity......Page 341
Ultraviolet Absorbers......Page 342
Food Colorants......Page 344
Film Coatings......Page 345
Photoinstability of Dyes......Page 346
Shell Additives......Page 347
Microencapsulation......Page 348
Testing of Dermal Preparations......Page 349
Formulation Factors......Page 350
Photostabilization by Spectral Overlay......Page 351
Photostabilization by Opacification......Page 352
Photostabilization by Cyclodextrin and Liposome Inclusion......Page 353
CONCLUSION......Page 354
REFERENCES......Page 355
Change of Potency......Page 357
Photocarcinogenicity......Page 358
Photosensitized Degradation......Page 359
PHOTOSTABILITY TESTING......Page 361
Buffer Species......Page 363
Ionic Strength (µ)......Page 365
Additives......Page 367
Drug Concentration......Page 369
Source, Intensity, and Wavelength Effects......Page 370
Temperature......Page 373
Type of Packaging......Page 374
Addition of Light Absorbers......Page 377
Incorporation of Antioxidants......Page 380
Complex Formation......Page 383
CONCLUSION......Page 384
REFERENCES......Page 385
INTRODUCTION......Page 391
Photostability and the Sun-Protection Factor......Page 392
PHOTOSTABILITY OF SUNSCREENS......Page 394
Reversible Transformations......Page 395
Nonreversible Transformations......Page 398
Alpha-Cleavage (Norrish I) of Dibenzoylmethane......Page 399
Single Ultraviolet Filters......Page 400
Sunscreen Preparations......Page 401
The Inner Filter Effect......Page 402
Triplet–Triplet Energy Transfer......Page 403
SYNOPSIS......Page 405
REFERENCES......Page 407
INTRODUCTION......Page 409
PHOTODEGRADATION AND PHOTOPROTECTION DURING ADMINISTRATION......Page 410
Infusions......Page 411
Length and Diameter of Intraluminal Tubing......Page 412
Oral......Page 413
Topicals......Page 414
Amphotericin B......Page 415
Doxycycline......Page 416
Quinolones......Page 417
Anthracyclines......Page 418
Cisplatin......Page 419
Dacarbazine......Page 420
Fluorouracil......Page 422
Irinotecan, Topotecan......Page 423
Methotrexate......Page 424
Molsidomine......Page 425
Nimodipine......Page 426
Sodium Nitroprusside......Page 428
Catecholamines......Page 429
Diuretics......Page 430
TOTAL PARENTERAL NUTRITION SOLUTIONS......Page 431
Multivitamins......Page 432
Vitamin K 1 (Phytomenadione)......Page 433
Ascorbic Acid......Page 434
REFERENCES......Page 435
