Advanced Drug Formulation Design to Optimize Therapeutic Outcomes

532 Pages·2007·13.503 MB·English

by  Robert O. Williams, David R. Taft, Jason T. McConville

Advanced Drug Formulation Design
to Optimize
Therapeutic Outcomes
Williams_978-1420043877_TP.indd 1 8/28/07 3:51:21 PM
DRUGS AND THE PHARMACEUTICAL SCIENCES
A Series of Textbooks and Monographs
Executive Editor
James Swarbrick
PharmaceuTech, Inc.
Pinehurst, North Carolina
Advisory Board
Larry L. Augsburger Harry G. Brittain
UniversityofMaryland CenterforPharmaceuticalPhysics
Milford,NewJersey
Baltimore,Maryland
Anthony J. Hickey
Jennifer B. Dressman
UniversityofNorthCarolinaSchoolof
JohannWolfgangGoetheUniversity
Pharmacy
Frankfurt,Germany
ChapelHill,NorthCarolina
Jeffrey A. Hughes
Ajaz Hussain
UniversityofFloridaCollegeofPharmacy Sandoz
Gainesville,Florida Princeton,NewJersey
Trevor M. Jones Stephen G. Schulman
TheAssociationofthe UniversityofFlorida
BritishPharmaceuticalIndustry Gainesville,Florida
London,UnitedKingdom
Elizabeth M. Topp
Vincent H. L. Lee UniversityofKansasSchoolof
Pharmacy
UniversityofSouthernCalifornia
Lawrence,Kansas
LosAngeles,California
Peter York
Jerome P. Skelly
UniversityofBradfordSchoolof
Alexandria,Virginia
Pharmacy
Bradford,UnitedKingdom
Geoffrey T. Tucker
UniversityofSheffield
RoyalHallamshireHospital
Sheffield,UnitedKingdom
1. Pharmacokinetics,Milo Gibaldi and DonaldPerrier
2. GoodManufacturing Practices forPharmaceuticals: APlanfor
Total QualityControl, SidneyH. Willig, MurrayM.Tuckerman, and
William S. Hitchings IV
3. Microencapsulation, editedbyJ.R. Nixon
4. DrugMetabolism: Chemicaland Biochemical Aspects,Bernard Testa
and Peter Jenner
5. NewDrugs:DiscoveryandDevelopment,editedbyAlanA. Rubin
6. Sustained andControlled ReleaseDrugDelivery Systems,editedby
JosephR. Robinson
7. ModernPharmaceutics, editedbyGilbertS.Banker and
Christopher T.Rhodes
8. Prescription Drugs inShortSupply: CaseHistories,Michael A.Schwartz
9. Activated Charcoal:Antidotal andOtherMedical Uses, DavidO. Cooney
10. ConceptsinDrugMetabolism(intwoparts),editedbyPeterJennerand
BernardTesta
11. PharmaceuticalAnalysis:ModernMethods(intwoparts),editedby
JamesW.Munson
12. TechniquesofSolubilizationofDrugs,editedbySamuelH.Yalkowsky
13. OrphanDrugs,editedbyFredE.Karch
14. Novel Drug Delivery Systems: Fundamentals, Developmental Concepts,
BiomedicalAssessments,YieW.Chien
15. Pharmacokinetics:SecondEdition,Revisedand Expanded,
MiloGibaldiandDonaldPerrier
16. GoodManufacturingPracticesforPharmaceuticals:APlanforTotalQuality
Control,SecondEdition, RevisedandExpanded,SidneyH. Willig,
MurrayM.Tuckerman,andWilliamS.Hitchings IV
17. FormulationofVeterinary DosageForms,editedbyJackBlodinger
18. DermatologicalFormulations:PercutaneousAbsorption,BrianW.Barry
19. TheClinicalResearchProcessinthePharmaceuticalIndustry,editedby
GaryM.Matoren
20. MicroencapsulationandRelatedDrugProcesses,PatrickB.Deasy
21. DrugsandNutrients: TheInteractiveEffects,editedbyDaphneA.Roe
andT.ColinCampbell
22. BiotechnologyofIndustrial Antibiotics,ErickJ.Vandamme
23. PharmaceuticalProcessValidation, editedbyBernardT.Loftusand
RobertA. Nash
24. Anticancer and Interferon Agents: Synthesis and Properties, edited by
RaphaelM.OttenbriteandGeorgeB.Butler
25. PharmaceuticalStatistics:PracticalandClinicalApplications,
SanfordBolton
26. DrugDynamicsforAnalytical,Clinical,andBiological Chemists,
BenjaminJ.Gudzinowicz,Burrows T.Younkin,Jr.,and
MichaelJ.Gudzinowicz
27. ModernAnalysisofAntibiotics,editedbyAdjoranAszalos
28. SolubilityandRelatedProperties,KennethC.James
29. Controlled Drug Delivery: Fundamentals and Applications, Second Edition,
RevisedandExpanded,editedbyJosephR. Robinsonand
VincentH. Lee
30. NewDrugApprovalProcess:ClinicalandRegulatoryManagement,
editedbyRichardA.Guarino
31. TransdermalControlledSystemicMedications,editedbyYieW.Chien
32. DrugDeliveryDevices:FundamentalsandApplications,editedby
PraveenTyle
33. Pharmacokinetics:RegulatoryoIndustrialoAcademicPerspectives,
editedbyPeterG.WellingandFrancisL.S.Tse
34. ClinicalDrugTrials andTribulations,editedbyAllen E.Cato
35. TransdermalDrugDelivery:DevelopmentalIssuesandResearchInitiatives,
editedbyJonathanHadgraftandRichardH.Guy
36. AqueousPolymericCoatingsforPharmaceuticalDosageForms,
editedbyJamesW.McGinity
37. PharmaceuticalPelletizationTechnology,editedbyIsaacGhebre-Sellassie
38. GoodLaboratory PracticeRegulations,editedbyAllenF.Hirsch
39. NasalSystemicDrugDelivery,YieW.Chien,KennethS.E.Su,
andShyi-FeuChang
40. ModernPharmaceutics:SecondEdition, RevisedandExpanded, editedby
GilbertS.Banker andChristopherT.Rhodes
41. SpecializedDrugDeliverySystems:Manufacturingand
ProductionTechnology,editedbyPraveenTyle
42. TopicalDrugDeliveryFormulations,editedbyDavid W.Osborneand
AntonH.Amann
43. DrugStability:Principles andPractices,JensT.Carstensen
44. PharmaceuticalStatistics:PracticalandClinicalApplications,
SecondEdition, RevisedandExpanded,SanfordBolton
45. BiodegradablePolymersasDrugDeliverySystems,editedby
MarkChasinandRobertLanger
46. PreclinicalDrugDisposition:ALaboratory Handbook,
FrancisL.S.TseandJamesJ.Jaffe
47. HPLCinthePharmaceuticalIndustry,editedbyGodwinW.Fong
andStanleyK.Lam
48. PharmaceuticalBioequivalence,editedbyPeterG.Welling,
FrancisL.S.Tse,andShrikant V.Dinghe
49. PharmaceuticalDissolution Testing,Umesh V.Banakar
50. NovelDrugDeliverySystems:SecondEdition, RevisedandExpanded,
YieW.Chien
51. ManagingtheClinicalDrugDevelopmentProcess,DavidM.Cocchettoand
RonaldV.Nardi
52. GoodManufacturingPracticesforPharmaceuticals:APlanforTotalQuality
Control,ThirdEdition,editedbySidney H.Willig andJames
R.Stoker
53. Prodrugs:TopicalandOcularDrugDelivery,editedbyKennethB.Sloan
54. PharmaceuticalInhalationAerosolTechnology,editedby
AnthonyJ.Hickey
55. Radiopharmaceuticals: ChemistryandPharmacology,editedby
AdrianD. Nunn
56. New Drug Approval Process: Second Edition, Revised and Expanded,
editedbyRichardA.Guarino
57. PharmaceuticalProcessValidation:SecondEdition,RevisedandExpanded,
editedbyIraR. BerryandRobertA.Nash
58. OphthalmicDrugDeliverySystems,editedbyAshim K.Mitra
59. PharmaceuticalSkinPenetrationEnhancement,editedby
KennethA.Walters andJonathanHadgraft
60. ColonicDrugAbsorption andMetabolism,editedbyPeterR. Bieck
61. PharmaceuticalParticulateCarriers:TherapeuticApplications,editedby
AlainRolland
62. DrugPermeationEnhancement:TheoryandApplications,editedby
DeanS.Hsieh
63. Glycopeptide Antibiotics,editedbyRamakrishnanNagarajan
64. AchievingSterilityin MedicalandPharmaceuticalProducts,NigelA.Halls
65. MultiparticulateOralDrugDelivery,editedbyIsaacGhebre-Sellassie
66. ColloidalDrugDeliverySystems,editedbyJo¨rgKreuter
67. Pharmacokinetics: Regulatory o Industrial o Academic Perspectives,
SecondEdition, editedbyPeterG. Wellingand FrancisL.S.Tse
68. DrugStability:Principles andPractices,SecondEdition,Revisedand
Expanded,JensT.Carstensen
69. GoodLaboratory PracticeRegulations: SecondEdition,Revised
andExpanded,editedbySandyWeinberg
70. Physical CharacterizationofPharmaceuticalSolids,editedby
HarryG.Brittain
71. PharmaceuticalPowderCompactionTechnology,editedbyGo¨ranAlderborn
andChristerNystro¨m
72. ModernPharmaceutics:ThirdEdition, RevisedandExpanded,editedby
GilbertS.Banker andChristopherT.Rhodes
73. Microencapsulation:MethodsandIndustrial Applications,editedby
SimonBenita
74. OralMucosalDrugDelivery,editedbyMichaelJ.Rathbone
75. ClinicalResearchinPharmaceuticalDevelopment,editedby
BarryBleidtandMichaelMontagne
76. TheDrugDevelopmentProcess:IncreasingEfficiencyand
CostEffectiveness,editedbyPeterG.Welling,LouisLasagna,
andUmeshV.Banakar
77. Microparticulate Systems for the Delivery of Proteins and Vaccines, edited
bySmadarCohenandHowardBernstein
78. GoodManufacturingPracticesforPharmaceuticals:APlanforTotalQuality
Control,FourthEdition, RevisedandExpanded,SidneyH.Willig and
JamesR. Stoker
79. AqueousPolymericCoatingsforPharmaceuticalDosageForms:
SecondEdition, RevisedandExpanded,editedbyJamesW.McGinity
80. PharmaceuticalStatistics:PracticalandClinicalApplications,ThirdEdition,
SanfordBolton
81. HandbookofPharmaceuticalGranulationTechnology,editedby
DilipM.Parikh
82. BiotechnologyofAntibiotics:SecondEdition, RevisedandExpanded,
editedbyWilliamR.Strohl
83. Mechanisms of Transdermal Drug Delivery, edited by Russell O. Potts and
RichardH.Guy
84. PharmaceuticalEnzymes,editedbyAlbertLauwersandSimonScharpe´
85. Development of Biopharmaceutical Parenteral Dosage Forms, edited by
JohnA.Bontempo
86. PharmaceuticalProjectManagement,editedbyTonyKennedy
87. DrugProductsforClinicalTrials:AnInternationalGuidetoFormulation
ProductionoQualityControl,editedbyDonaldC.Monkhouseand
ChristopherT.Rhodes
88. DevelopmentandFormulationofVeterinaryDosageForms:SecondEdition,
RevisedandExpanded,editedbyGregoryE.HardeeandJ.Desmond
Baggot
89. Receptor-Based DrugDesign,editedbyPaulLeff
90. Automation and Validation of Information in Pharmaceutical Processing,
editedbyJosephF.deSpautz
91. Dermal Absorption and Toxicity Assessment, edited by Michael S. Roberts
andKennethA.Walters
92. PharmaceuticalExperimentalDesign,GarethA.Lewis,DidierMathieu,and
RogerPhan-Tan-Luu
93. PreparingforFDAPre-ApprovalInspections,editedbyMartinD. HynesIII
94. PharmaceuticalExcipients:CharacterizationbyIR,Raman,and
NMRSpectroscopy,DavidE.BugayandW.PaulFindlay
95. PolymorphisminPharmaceuticalSolids,editedbyHarryG.Brittain
96. Freeze-Drying/LyophilizationofPharmaceuticalandBiologicalProducts,
editedbyLouisRey andJoanC.May
97. Percutaneous Absorption: Drugs-Cosmetics-Mechanisms-Methodology,
ThirdEdition, RevisedandExpanded,editedbyRobertL.Bronaughand
HowardI.Maibach
98. BioadhesiveDrugDeliverySystems:Fundamentals,NovelApproaches,and
Development,editedbyEdithMathiowitz,DonaldE.ChickeringIII,and
Claus-MichaelLehr
99. ProteinFormulationandDelivery,editedbyEugeneJ.McNally
100. NewDrugApproval Process:ThirdEdition, TheGlobalChallenge,
editedbyRichardA.Guarino
101. PeptideandProteinDrugAnalysis,editedbyRonaldE.Reid
102. TransportProcessesinPharmaceuticalSystems,editedby
GordonL.Amidon, PingI. Lee,andElizabeth M.Topp
103. ExcipientToxicityandSafety,editedbyMyraL.Weinerand
LoisA.Kotkoskie
104. TheClinicalAuditinPharmaceuticalDevelopment,editedby
MichaelR.Hamrell
105. Pharmaceutical Emulsions and Suspensions, edited by Francoise Nielloud
andGilberteMarti-Mestres
106. OralDrugAbsorption:PredictionandAssessment,editedby
JenniferB.Dressmanand HansLennerna¨s
107. DrugStability: PrinciplesandPractices,ThirdEdition, Revised
andExpanded,editedbyJensT.CarstensenandC. T.Rhodes
108. ContainmentinthePharmaceuticalIndustry,editedbyJamesP.Wood
109. GoodManufacturingPracticesforPharmaceuticals:APlanforTotalQuality
ControlfromManufacturer toConsumer,Fifth Edition,Revisedand
Expanded,SidneyH.Willig
110. AdvancedPharmaceuticalSolids,JensT.Carstensen
111. Endotoxins:Pyrogens,LALTesting,andDepyrogenation,
SecondEdition,Revisedand Expanded,KevinL.Williams
112. PharmaceuticalProcessEngineering, AnthonyJ.Hickeyand
DavidGanderton
113. Pharmacogenomics,editedbyWernerKalow,UrsA.Meyerand
RachelF.Tyndale
114. HandbookofDrugScreening,editedbyRamakrishnaSeethala
andPrabhavathiB.Fernandes
115. DrugTargetingTechnology:PhysicaloChemicalo
BiologicalMethods,editedbyHansSchreier
116. Drug-DrugInteractions,editedbyA.DavidRodrigues
117. HandbookofPharmaceuticalAnalysis,editedbyLenaOhannesian
andAnthonyJ.Streeter
118. PharmaceuticalProcessScale-Up,editedbyMichaelLevin
119. DermatologicalandTransdermalFormulations,editedby
KennethA.Walters
120. ClinicalDrugTrials andTribulations:SecondEdition, Revisedand
Expanded,editedbyAllenCato,LyndaSutton,andAllenCatoIII
121. ModernPharmaceutics:FourthEdition, RevisedandExpanded,
editedbyGilbertS.Banker andChristopherT.Rhodes
122. SurfactantsandPolymersinDrugDelivery,MartinMalmsten
123. TransdermalDrugDelivery:SecondEdition,RevisedandExpanded,edited
byRichardH. GuyandJonathanHadgraft
124. GoodLaboratoryPracticeRegulations:SecondEdition,Revised
andExpanded,editedbySandyWeinberg
125. Parenteral Quality Control: Sterility, Pyrogen, Particulate, and Package
IntegrityTesting:ThirdEdition, RevisedandExpanded,MichaelJ.Akers,
DanielS.Larrimore,andDanaMortonGuazzo
126. Modified-ReleaseDrugDeliveryTechnology,editedbyMichaelJ.Rathbone,
JonathanHadgraft,and MichaelS.Roberts
127. SimulationforDesigningClinicalTrials:
APharmacokinetic-PharmacodynamicModelingPerspective,
editedbyHuiC. KimkoandStephenB.Duffull
128. Affinity Capillary Electrophoresis in Pharmaceutics and Biopharmaceutics,
editedbyReinhardH. H.NeubertandHans-Hermann Ru¨ttinger
129. Pharmaceutical Process Validation: An International Third Edition, Revised
andExpanded,editedbyRobertA.NashandAlfredH. Wachter
130. OphthalmicDrugDeliverySystems:SecondEdition, Revisedand
Expanded,editedbyAshimK.Mitra
131. Pharmaceutical Gene Delivery Systems,edited by Alain Rolland and Sean
M.Sullivan
132. BiomarkersinClinicalDrugDevelopment,editedbyJohnC.Bloom
andRobertA.Dean
133. PharmaceuticalExtrusionTechnology,editedbyIsaacGhebre-Sellassieand
CharlesMartin
134. PharmaceuticalInhalationAerosolTechnology:SecondEdition,
RevisedandExpanded,editedbyAnthonyJ.Hickey
135. PharmaceuticalStatistics:PracticalandClinicalApplications,FourthEdition,
SanfordBoltonandCharles Bon
136. ComplianceHandbookforPharmaceuticals,MedicalDevices,andBiologics,
editedbyCarmenMedina
137. Freeze-Drying/Lyophilization of Pharmaceutical and Biological Products:
SecondEdition,Revisedand Expanded,editedbyLouisReyand
JoanC.May
138. Supercritical Fluid Technology for Drug Product Development, edited by
PeterYork, UdayB.Kompella, andBorisY.Shekunov
139. NewDrugApproval Process:FourthEdition,Accelerating
GlobalRegistrations,editedbyRichardA.Guarino
140. MicrobialContaminationControlinParenteralManufacturing,
editedbyKevinL.Williams
141. New Drug Development: Regulatory Paradigms for Clinical Pharmacology
andBiopharmaceutics,editedbyChandrahasG. Sahajwalla
142. MicrobialContaminationControlinthe PharmaceuticalIndustry,
editedbyLuisJimenez
143. GenericDrugProductDevelopment:Solid OralDosageForms,
editedbyLeonShargelandIzzyKanfer
144. IntroductiontothePharmaceuticalRegulatoryProcess,edited
byIraR.Berry
145. DrugDeliverytotheOral Cavity:MoleculestoMarket,editedby
TapashK.GhoshandWilliam R.Pfister
146. GoodDesign PracticesforGMPPharmaceuticalFacilities,editedby
AndrewSignoreandTerryJacobs
147. DrugProductsforClinicalTrials,SecondEdition,editedby
DonaldMonkhouse,CharlesCarney,andJimClark
148. PolymericDrugDeliverySystems,editedbyGlenS.Kwon
149. InjectableDispersedSystems:Formulation,Processing,and
Performance,editedbyDianeJ.Burgess
150. LaboratoryAuditingforQualityandRegulatoryCompliance,DonaldSinger,
Raluca-IoanaStefan,and JacobusvanStaden
151. ActivePharmaceuticalIngredients:Development,Manufacturing,
andRegulation, editedbyStanleyNusim
152. PreclinicalDrugDevelopment,editedbyMarkC. RoggeandDavidR.Taft
153. PharmaceuticalStress Testing:Predicting DrugDegradation,
editedbyStevenW.Baertschi
154. HandbookofPharmaceuticalGranulationTechnology:
SecondEdition,editedbyDilipM.Parikh
155. Percutaneous Absorption: Drugs-Cosmetics-Mechanisms-Methodology,
FourthEdition, editedbyRobertL.Bronaugh andHowardI.Maibach
156. Pharmacogenomics:SecondEdition, editedbyWernerKalow,
UrsA.Meyer andRachelF.Tyndale
157. PharmaceuticalProcessScale-Up,SecondEdition,editedbyMichaelLevin
158. Microencapsulation: Methods and Industrial Applications, Second Edition,
editedbySimonBenita