Pharmaceutical Dissolution Testing, Bioavailability, and Bioequivalence: Science, Applications, and Beyond

563 Pages·2022·10.921 MB·English

by  Umesh V. Banakar

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PharmaceuticalDissolutionTesting,
Bioavailability,andBioequivalence
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Pharmaceutical Dissolution Testing,
Bioavailability, and Bioequivalence
Science, Applications, and Beyond
Umesh V. Banakar
BanakarConsultingServices
Westfield,IN,USA
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Thiseditionfirstpublished2022
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Toallthefrontlinehealthcareproviders,firstresponders,serviceproviders,mothers,
fathers,spouses,brothers,sisters,empatheticandcompassionatewell-wishers,gods,
deities,spirits,faiths,andabovealltheloveandaffectionsharedbyeveryoneinthe
combattosurviveandovercometheSARSCOVID-19pandemicof2020.
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vii
Contents
Foreword xvii
Foreword xix
Preface xxi
Acknowledgments xxvii
1 PharmaceuticalDissolutionTesting:Fundamentalsand
EssentialApplications(AnOverview) 1
1.1 IntroductionandObjective(s) 1
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1.2 ScienceofDissolutionOverPast120+Years 3
1.2.1 JourneyfromQualityControl(QC)toDevelopment 5
1.3 FundamentalsofDissolutionTesting(AnOverview) 6
1.4 FactorsInfluencingDissolutionTest(ing) 8
1.5 PharmaceuticalProductLifeCycle:RoleofDissolution
(AnOverview) 12
1.6 DissolutionTest(ing):WhatItIsandWhatItIsNot! 13
1.7 NeedforThisTextbook 14
1.8 SummaryandConcludingRemarks 15
References 16
2 Bioavailability(BA)andBioequivalence(BE):Fundamentals
andApplicationsinDrugProductDevelopment 20
2.1 IntroductionandObjective(s) 20
2.2 Definitions 21
2.3 Bioequivalence(BE)Testing:Basics,Advances,andGlobal
Perspectives 23
2.3.1 BA/BEStudyDesigns 26
2.3.2 SampleSize,n 28
2.3.3 BE(Acceptance)CriteriaandStatisticalConsiderations 31
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viii Contents
2.3.4 Bioequivalence(BE)Studies:Roleof ModelingandSimulations 33
2.3.5 SurrogatestoBE 35
2.3.6 PDEndpoint-BasedandClinicalEndpoint-BasedBEAssessment 37
2.3.7 RegulatoryRequirements 40
2.4 CurrentChallengesandSolutions(InsightintoChapter14) 43
2.5 SummaryandConcludingRemarks 44
References 44
3 Solubility,Dissolution,Permeability,andClassification
Systems 54
3.1 IntroductionandObjective(s) 54
3.2 Definitions 56
3.3 SolubilityVersusSolubilization:WhatIsCriticalinDevelopment? 58
3.3.1 TheoriesofSolubilization 58
3.3.2 Solubility:ChallengesinDrugDevelopment! 63
3.3.3 SolubilityEnhancement:Purpose,TheoreticalandPractical
Considerations! 68
3.4 Dissolution:IntrinsicVersusApparent! 70
3.4.1 TheoriesofDissolution 70
3.4.1.1 Noyes–WhitneyTheory(1897) 70
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3.4.1.2 BrunnerandTolloczkoTheory(1900) 71
3.4.1.3 NernstandBrunnerTheory(1904) 71
3.4.2 IntrinsicVersusApparentDissolution 72
3.5 PermeabilityVersusPermeation(Process):WhatIsCriticalfor
Bioefficacy! 74
3.6 ClassificationSystems:TheoreticalVersusPragmatic
Considerations! 75
3.7 SummaryandConcludingRemarks 78
References 79
4 UnderstandingtheMechanicsofDissolution:Mathematical
ModelsandSimulations 86
4.1 IntroductionandObjective(s) 86
4.2 MechanicsofDissolution:Theories,Presumptions,andReality
Check 87
4.3 DissolutionTheories/Models 91
4.4 DissolutionMechanics(Model-DependentMethods) 92
4.4.1 ZeroOrder 92
4.4.2 First-OrderModel(Gibaldi–FeldmanModel1967) 93
4.4.3 Makoid–BanakarModel(1993) 93
4.4.4 HixsonandCrowellModel(1931) 95
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