Analytical Profiles of Drug Substances, Excipients, and Related Methodology

360 Pages·2009·7.25 MB·English

by  Harry G. Brittain (Eds.)

Profiles of
DRUG
SUBSTANCES,
EXCIPIENTS, AND
RELATED
METHODOLOGY
34
VOLUME
CONTRIBUTING EDITORS
ABDULLAH A. AL-BADR
ALEKHA K. DASH
FOUNDING
EDITOR
KLAUS FLOREY
Profiles of
DRUG
SUBSTANCES,
EXCIPIENTS, AND
RELATED
METHODOLOGY
34
VOLUME
Edited by
HARRY G. BRITTAIN
Center for Pharmaceutical Physics,
Milford, New Jersey 08848
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CONTENTS
Preface ix
1. CreatineMonohydrate 1
SomnathSinghandAlekhaK.Dash
1. HistoryandTherapeuticAspects 2
2. Description 4
3. Synthesis 5
4. PhysicalProperties 8
5. MethodsofAnalysis 23
6. StabilityandDegradation 27
7. Pharmacokinetics,Metabolism,andToxicity 28
Acknowledgments 32
References 32
2. Cytarabine 37
HusseinI.El-SubbaghandAbdullahA.Al-Badr
1. Description 38
2. MethodsofPreparation 41
3. PhysicalCharacteristics 47
4. MethodsofAnalysis 54
5. Radioimmunoassay 95
6. BiologicalAnalysis 98
7. Stability 100
8. Pharmacokinetics,Metabolism,andExcretion 102
9. Pharmacology 104
Acknowledgments 110
References 110
3. Famotidine 115
MohamedA.Al-Omarand AbdullahM.Al-Mohizea
1. GeneralInformation 116
2. PhysicalCharacteristics 117
3. StabilityandStorage 125
v
vi Contents
4. AnalyticalProfilesofFamotidine 126
5. DrugMetabolismandPharmacokineticProfilesofFamotidine 144
References 150
4. FexofenadineHydrochloride 153
LokeshKumar,Md.ShahnwajAlam,ChhuttanLalMeena,RahulJain,
andArvindK.Bansal
1. Description 154
2. MethodsofPreparation 156
3. PhysicalProperties 161
4. MethodsofAnalysis 175
5. Stability 188
6. DrugMetabolismandPharmacokinetics 189
Acknowledgments 190
References 190
5. Itraconazole:ComprehensiveProfile 193
AbdullahA.Al-BadrandHusseinI.El-Subbagh
1. Description 194
2. PhysicalCharacteristics 196
3. UsesandApplications 205
4. MethodsofChemicalSynthesis 205
5. MethodsofAnalysis 217
6. FoodandDrugInteraction 251
7. Stability 253
8. Pharmacokinetics 254
9. Absorption,Metabolism,andExcretion 260
Acknowledgment 261
References 261
6. Ofloxacin 265
MohammedA.Al-Omar
1. PhysicalProfilesofOfloxacin 266
2. AnalyticalProfilesofOfloxacin 276
3. DrugMetabolismandPharmacokineticProfilesofOfloxacin 293
References 296
7. Paclitaxel 299
SaurabhJauhari,SomnathSingh,andAlekhaK.Dash
1. Introduction 301
2. Description 307
3. MethodsofPreparation 309
Contents vii
4. PhysicalProperties 312
5. MethodofAnalysis 321
6. Stability 324
7. PharmacokineticsandMetabolism 328
Acknowledgment 339
References 339
CumulativeIndex 345
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PREFACE TO VOLUME 34
The comprehensive profiling of drug substances and pharmaceutical
excipients as to their physical and analytical characteristics remains at
thecoreofpharmaceuticaldevelopment.Asaresult,thecompilationand
publication ofcomprehensivesummaries ofphysical and chemical data,
analytical methods, routes of compound preparation, degradation path-
ways,usesandapplications,etc.,havealwaysbeenavitalfunctiontoboth
academiaandindustry.
As the science of pharmaceutics grows and matures, the need for
information similarly expands along new fronts and causes equivalent
growth in the vehicles where investigators find the information they
need. The content of the Profiles series has expanded to meet this need,
withchaptersfallingintooneormoreofthefollowingmaincategories:
1. Comprehensiveprofilesofadrugsubstanceorexcipient
2. Physicalcharacterizationofadrugsubstanceorexcipient
3. Analyticalmethodsforadrugsubstanceorexcipient
4. Detailed discussions of the clinical uses, pharmacology, pharmaco-
kinetics,safety,ortoxicityofadrugsubstanceorexcipient
5. Reviews of methodology useful for the characterization of drug
substancesorexcipients
6. Annualreviewsofareasofimportancetopharmaceuticalscientists
Asitturnsout,allofthechaptersinthecurrentvolumearecomprehen-
sive in nature, and provide detailed profiles of the drug substances
involved.Volumesintherecentpasthavecontainedreviewsofmethod-
ology,anditisanticipatedthatfuturevolumesintheoftheProfilesseries
willcontainsimilarreviews,aswellasothertypesofreviewarticlesthat
summarize the current state in a particular field of pharmaceutics. As
always, I welcome communications from anyone in the pharmaceutical
communitywhomightwanttoprovideanopinionoracontribution.
HarryG.Brittain
Editor,ProfilesofDrugSubstances,
Excipients,andRelatedMethodology
[email protected]
ix