Pharmaceutics: Basic Principles and Application to Pharmacy Practice

394 Pages·2013·26.52 MB·English

by  Alekha Dash

PHARMACEUTICS
We dedicatethis text to our teachersand professors who inculcated inus a love of scientificprinciples and pharmaceutics.
PHARMACEUTICS
Basic Principles and
Application to Pharmacy Practice
Edited by
A K. D , RP , P D
LEKHA ASH H H
CreightonUniversity,Nebraska,USA
S S , P D
OMNATH INGH H
CreightonUniversity,Nebraska,USA
J T , P D, P D
USTIN OLMAN HARM H
CreightonUniversity,Nebraska,USA
AMSTERDAM(cid:129)BOSTON(cid:129)HEIDELBERG(cid:129)LONDON
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14 15 16 17 10 9 8 7 6 5 4 3 2 1
Contents
Preface ix 3. Physical Properties, Their Determination,
Acknowledgments xi and Importance in Pharmaceutics
List of Contributors xii SOMNATHSINGHANDALEKHAK.DASH
3.1. Introduction 51
I 3.2. SurfaceandInterfacialTension 52
3.3. Adsorption 53
PHYSICAL PRINCIPLES AND 3.4. Solubilization 59
3.5. Rheology 61
PROPERTIES OF PHARMACEUTICS
3.6. ColligativeProperties 65
3.7. OsmolarityandOsmolality 68
3.8. SolubilityandSolutionsofNonelectrolytes 71
1. Introduction: Terminology, Basic
3.9. Spectroscopy 73
Mathematical Skills, and Calculations
3.10. Conclusions 83
EMANATEFANDSOMNATHSINGH CaseStudies 82
References 84
1.1. Introduction 3
1.2. ReviewofBasicMathematicalSkills 3
1.3. GraphicalRepresentation 11 4. Equilibrium Processes in Pharmaceutics
1.4. DimensionsandUnits 12
SUNILS.JAMBHEKAR
1.5. Conclusions 14
CaseStudies 14 4.1. Introduction 85
References 15 4.2. GastrointestinalPhysiology 87
4.3. Ionization 90
4.4. PartitionCoefficient:Lipophilicity 93
2. Physical States and Thermodynamic
4.5. EquilibriumSolubility 96
Principles in Pharmaceutics 4.6. TheEffectofpH 98
4.7. UseofCo-solvents 99
VIVEKS.DAVE,SEONHEPBURN
ANDSTEPHENW.HOAG 4.8. DrugDissolutionandDissolutionProcess 100
4.9. FactorsInfluencingtheDissolutionRate 102
2.1. Introduction 17 4.10. PassiveDiffusion 104
2.2. CompositionofMatter 17 4.11. BiopharmaceuticsClassificationSystem(BCS) 105
2.3. ForcesofAttractionandRepulsion 18 4.12. Conclusions 106
2.4. StatesofMatter 22 CaseStudies 106
2.5. Thermodynamics 33 References 107
2.6. BasicConceptsandDefinitions 35 SuggestedReadings 108
2.7. TheFirstLawofThermodynamics 37
2.8. EnthalpyandHeatCapacity 39
5. Kinetic Processes in Pharmaceutics
2.9. TheSecondLawofThermodynamics 41
2.10. TheThirdLawofThermodynamics 44 RAMPRAKASHGOVINDARAJAN
2.11. FreeEnergyandThermodynamicFunctions 44
2.12. ChemicalEquilibrium 46 5.1. Introduction 109
2.13. OpenSystems 46 5.2. Thermodynamicsvs.Kinetics 109
2.14. Conclusions 47 5.3. ChemicalReactionKineticsandDrugStability 110
CaseStudies 47 5.4. Diffusion 127
Appendix2.1CalculusReview 48 5.5. Dissolution 130
References 49 5.6. Conclusions 136
v
vi
CONTENTS
CaseStudies 136 9. Liquid Dosage Forms
References 137
HARIR.DESU,AJITS.NARANG,LAURAA.THOMA
ANDRAMI.MAHATO
6. Biopolymers
9.1. Introduction 181
SOMNATHSINGHANDJUSTINTOLMAN 9.2. SelectionofLiquidDosageForms 181
9.3. TypesofLiquidDosageForms 183
6.1. IntroductiontoPolymers 139
9.4. GeneralAspectsofLiquidDosageForms 207
6.2. IntroductiontoPeptidesandProteins 142
9.5. ManufacturingProcessesandConditions 210
6.3. IntroductiontoOligonucleotides 146
9.6. Packaging 214
6.4. Conclusions 149
9.7. Labeling 217
CaseStudies 149
9.8. QualityAssuranceandQualityControl 217
References 150
9.9. RegulatoryConsiderations 219
SuggestedReadings 150
9.10. Conclusions 221
ListofAbbreviations 221
II CaseStudies 221
References 222
PRACTICAL ASPECTS OF
PHARMACEUTICS 10. Aerosol Dosage Forms
JUSTINA.TOLMANANDMEGANHUSLIG
7. Drug, Dosage Form, and
10.1. Introduction 225
Drug Delivery Systems
10.2. LungAnatomy 226
ALEKHAK.DASH 10.3. LungPhysiology 227
10.4. PulmonaryDrugTargets 228
7.1. Introduction 153 10.5. PulmonaryDrugDeposition 228
7.2. PharmaceuticalIngredients 154 10.6. TherapeuticGases 230
7.3. PreformulationStudies 154 10.7. InhaledAerosols 232
7.4. PhysicalDescription 154 10.8. Conclusions 237
7.5. LiquidDosageForms 154 CaseStudies 238
7.6. SolidDosageForms 156 Acknowledgments 238
7.7. PartitionCoefficientandpKa 157 References 238
7.8. Solubility 157
7.9. Dissolution 157
7.10. Polymorphism 157 11. Semisolid Dosage Forms
7.11. Stability 158 SHAILENDRAKUMARSINGH,KALPANANAGPAL
7.12. Conclusions 158 ANDSANGITASAINI
CaseStudies 158
11.1. Introduction 241
References 159
11.2. ClassificationofSemisolidDosageForms 243
11.3. PercutaneousAbsorption 249
8. Solid Dosage Forms 11.4. TheoryofSemisolidDosageForms 253
ALEKHAK.DASH 11.5. MethodsofEnhancementofPercutaneous
Absorption 255
8.1. Introduction 161 11.6. CharacterizationandEvaluationofSemisolid
8.2. Powders 161 DosageForms 260
8.3. Capsules 165 11.7. ProcedureandApparatusforDiffusionExperiment 263
8.4. Tablets 168 11.8. Conclusions 269
8.5. ManufactureofCompressedTablets 170 CaseStudies 269
8.6. MethodsUsedforManufactureofCompressed References 270
Tablets 172
8.7. TabletCompressionandBasicFunctionalUnits
12. Special Dosage Forms and
ofaTabletPress 173
8.8. QualityControlofTabletDosageForm 175 Drug Delivery Systems
8.9. TabletCoating 178
SARATK.MOHAPATRAANDALEKHAK.DASH
8.10. Conclusions 179
CaseStudies 179 12.1. Introduction 273
References 180 12.2. SpecialDosageForms 274
vii
CONTENTS
12.3. ParenteralDrugDelivery 275 14.5. EvaluationofOralAbsorption 324
12.4. OsmoticDelivery 277 14.6. DrugDisposition 325
12.5. NanotechnologyforDrugDelivery 280 14.7. Conclusions 327
12.6. ImplantableDrugDelivery 292 CaseStudies 327
12.7. Prodrugs 299 References 329
12.8. Conclusions 301
CaseStudies 302
15. Routes of Drug Administration
References 303
MOHSENA.HEDAYAANDJUSTINA.TOLMAN
III
15.1. Introduction 333
15.2. ParenteralDrugAdministration 334
BIOLOGICAL APPLICATIONS
15.3. TransdermalDrugAdministration 337
OF PHARMACEUTICS 15.4. OphthalmicDrugAdministration 338
15.5. Auricular(Otic)DrugAdministration 340
15.6. NasalDrugAdministration 341
13. Membrane Transport and Permeation
15.7. PulmonaryDrugAdministration 341
JUSTINA.TOLMANANDMARIAP.LAMBROS 15.8. OralDrugAdministration 342
15.9. RectalDrugAdministration 346
13.1. Introduction 307 15.10. VaginalDrugAdministration 347
13.2. CellMembranes 307 15.11. Conclusions 347
13.3. MembraneTransport 309 References 348
13.4. PharmacologicallyRelevantMembrane
TransportProcesses 311
13.5. Conclusions 315 16. Bioavailability and Bioequivalence
CaseStudies 315
AJITS.NARANGANDRAMI.MAHATO
References 315
16.1. Introduction 349
16.2. Bioavailability 349
14. Factors Affecting Drug Absorption
16.3. FactorsAffectingBioavailability 352
and Disposition
16.4. Bioequivalence 359
CHONG-HUIGU,ANUJKULDIPKUMAR 16.5. Conclusions 362
ANDHARSHCHAUHAN CaseStudies 362
References 362
14.1. Introduction 317
14.2. DrugAbsorption 317
14.3. OralDrugAbsorptionProcesses 318
Index 365
14.4. FoodEffectsonOralDrugAbsorption 323
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