Topical Drug Bioavailability, Bioequivalence, and Penetration PDF
Preview Topical Drug Bioavailability, Bioequivalence, and Penetration
Topical Drug Bioavailability, Bioequivalence, and Penetration Topical Drug Bioavailability, Bioequivalence, and Penetration Edited by Vinod P. Shah Foodand DrugAdministration Rockville.Maryland and Howard I. Maibach UniversityofCalifornia SanFrancisco.California Springer Science+Business Media, LLC LLLL1lllbbbbrrrraaaarrrryyyy ooooffff CCCCoooonnnnggggrrrreeeessssssss CCCCaaaattttaaaallllooooggggllllnnnngggg----1lllnnnn----PPPPuuuubbbbllllllllccccaaaatttt1llloooonnnn DDDDaaaattttaaaa TTTTooooppppIiiieeecaaaallll ddddrrrruuuugggg bbbbiliiooooaaaavvvvaaaailiillllaaaabbbbllii1lllliiittttyyyy,,,. bbbbiliiooooeeeeqqqquuuuiliivvvvaaaalllleeeennnneceeeeee,.,, aaaannnndddd ppppeeeennnneeeettttrrrraaaattttIiiioooonnnn IIII eeeeddddiIiitttteeeedddd bbbbyyyy VVVVliiinnnnoooodddd PPPP.... SSSShhhhaaaahhhh aaaannnndddd HHHHoooowwwwaaaarrrrdddd IIII.... MMMMaaaaliiibbbbaaaaceeehhhh.... pppp.... eeecmmm~.... 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Anderson • Department of Pharmaceutics and Pharmaceutical Chemistry, University ofUtah,Salt Lake City, Utah 84112 B.W.Barry. PostgraduateStudiesinPharmaceuticalTechnology,TheSchool ofPharmacy, University ofBradford, Bradford BD7 IDP, United Kingdom E. Dennis Bashaw • Center for Drug Evaluation, Food and Drug Administra tion, Rockville, Maryland 20857 Charan R. Behl • Pharmaceutical R&D, Hoffmann-La Roche, Inc., Nutley, NewJersey07110 Robert L. Bronaugh • Cosmetic Toxicology Branch, Food and Drug Admin istration, Laurel, Maryland 20708 Daniel A. W. Bucks. Penederm Incorporated, FosterCity, California 94404 Annette Bunge • Department of Chemical Engineering, Colorado School of Mines,Golden, Colorado 8040I Hing Char • Pharmaceutical R&D, Hoffmann-La Roche, Inc., Nutley, New Jersey 071IO GaryW.Cleary • CygnusTherapeuticSystems,RedwoodCity,California94063 ShrikantV.Dighe • CenterforDrug Evaluationand Research,Foodand Drug Administration, Rockville, Maryland 20857 C.Carnot Evans,Jr.• OfficeofOrphan Products Development,Food and Drug Administration, Rockville, Maryland 20857 v vi CONTRIBUTORS Gordon L. Flynn. College of Pharmacy, The University of Michigan, Ann Arbor, Michigan 48109-1065 Suneel K.Gupta • AlzaCorporation, Palo Alto, California 94303 John M.Haigh • SchoolofPharmaceutical Sciences,Rhodes University,Gra hamstown 6140, South Africa Donald Hare • Centerfor Drug Evaluation and Research,Food and Drug Ad ministration, Rockville, Maryland 20857 StephenS. Hwang. AlzaCorporation, Palo Alto, California 94303 J. C.Jamoulle • ALGOVITAL Laboratory, 06400 Cannes, France Joseph Kost • Department of Chemical Engineering, Ben-Gurion University, Beer-Sheva 84105, Israel Gerald G. Krueger. Division of Dermatology, University ofUtah, Salt Lake City, Utah 84132 RobertLanger. DepartmentofChemical Engineering, MassachusettsInstitute ofTechnology, Cambridge, Massachusetts 02139 C.Lotte. L'Oreal Research, 93601 Aulnay sous Bois, France Thomas M. Ludden • Center for Drug Evaluation and Research, Food and Drug Administration, Rockville, Maryland 20857 Howard I. Maibach • Department of Dermatology, School of Medicine, Uni versityofCalifornia, San Francisco, California 94143 A.WaseemMalick • PharmaceuticalR&D,Hoffmann-La Roche,Inc.,Nutley, NewJersey 07110 Deepak B.Mehta • PharmaceuticalR&D, Hoffmann-LaRoche, Inc., Nutley, NewJersey 07110 Eric Meyer. Pharmacy Department, The University ofSydney,Sydney, Aus tralia Gabriela Nicolau • Innapharma Inc., Suffern, New York 1090I CONTRIBUTORS Vll Greg E. Parry • Norwich Eaton Pharmaceutics, Norwich, New York 13815 Sunil B. Patel • Pharmaceutical R&D, Hoffmann-La Roche, Inc., Nutley, NewJersey 07110 Lynn K. Pershing. Division of Dermatology, University of Utah, Salt Lake City, Utah 84132 DavidPiemontese • Pharmaceutical R&D,Hoffmann-LaRoche,Inc.,Nutley, NewJersey 07110 J. Edmond Riviere. Cutaneous Pharmacology and ToxicologyCenter, North Carolina State University, Raleigh, North Carolina 27606 A.Rougier • L'Oreal Research, 9360I Aulnay sous Bois, France H.Schaefer. L'Oreal,Centre CharlesZviak,92583ClichyCedex,Paris,France Vinod P. Shah • Center for Drug Evaluation and Research, Food and Drug Administration, Rockville, Maryland 20857 Jerome P.Skelly • Jerome P. Skelly, Ltd., Alexandria, Virginia 22309 Eric W. Smith. School of Pharmaceutical Sciences, Rhodes University, Gra hamstown 6140,South Africa SolomonSobel • Division ofMetabolism and Endocrine Drug Products,Food and Drug Administration, Rockville, Maryland 20857 Ronald C. Wester. Department of Dermatology, School of Medicine, Uni versityofCalifornia,San Francisco, California 94143 RogerL. Williams • CenterforDrug Evaluationand Research,Food and Drug Administration, Rockville, Maryland 20857 Avraham Yacobi • Medical Research Division, American Cyanamid Company, Lederle Laboratories, Pearl River, New York 10965 Preface Topical drugdeliveryhasbecome one ofthe mostexcitingand challengingareas of pharmaceutical research in the last decade. Topical drugs encompass both dermal and transdermal products, which are used forlocaland systemiceffects, respectively. This volume succinctly discusses different aspects ofdermal and transdermaldrugdeliveryand represents the state ofthe art and sciencein mea suring percutaneous penetration and in determining biological relevance. The topics covered are ofimportance for both basic research and clinical applications, forexample, cutaneousbioavailabilityand bioequivalence. Signif icant areasdiscussedinclude dermal and transdermal drugdelivery,in vitroand in vivomethodology to assessbioavailabilityand bioequivalenceoftopical drug products, in vitro and in vivo correlations, and pharmacokinetic and pharma codynamic modeling. Also covered are regulatory considerations for the drug approval process and requirements for all topical drug products. Many ofthe complexissuesinvolvedintheevaluation ofboth innovatorand genericproducts are identified and explained as well.This reference guide willbe a useful basic workingtool forinvestigators, and willbea valuable assetto allpharmaceutical scientistsinvolved in the development oftopical drug products. Vinod P. Shah Howard I. Maibach ix Contents Part I Topical Drug Delivery Chapter I Percutaneous Absorption Ronald C. Wester andHowardI. Maibach I. Introduction 3 2. Powdered Human Stratum Corneum 4 3. In Vitro Percutaneous Absorption Method 5 4. In VitroIndividual and Regional Variation ................... 7 5. In VitroShort-Term Skin Exposure 9 6. In VivoPercutaneous Absorption Methods 10 6.1. Skin Stripping: Short-Term Exposure 10 6.2. Skin Flaps II 6.3. Systemic Bioavailability(Blood and Excreta) 12 6.4. Surface Disappearance 13 6.5. Biological Response 13 References 14 Chapter 2 Transdermal Delivery Systems: A Medical Rationale Gary W.Cleary I. Introduction 17 2. Pharmacokinetic Interpretation 21 3. Selection ofSuitable Drug Candidates 28 4. Pharmaceutics Considerations 30 4.1. Design ofTransdermal Delivery Systems ................ 30 4.2. Regulatory Considerations 34 XI XII CONTENTS 5. Commercial Transdermal Drug DeliverySystems 35 5.1. Scopolamine Transdermal Systems 35 5.2. Nitroglycerin Transdermal Systems 37 5.3. Clonidine Transdermal Systems ....................... 44 5.4. Estradiol Transdermal Systems 47 5.5. Fentanyl Transdermal Systems ........................ 50 5.6. Nicotine Transdermal Systems ........................ 52 6. How Transdermal Drug Delivery Has Performed 57 6.1. Different Therapeutic Areas 57 6.2. Advantage over Current DosageForms 57 6.3. Different Ratios of Metabolites and Lipids: Estradiol Trans- dermal versusOral 58 6.4. Drugs with Difficult-to-Formulate Properties 58 6.5. Different Blood-LevelProfilesfrom Other DosageForms .. 58 6.6. Linear Relation ofBlood Levelto Area ofSystem 59 6.7. Different Deliveryand Wearing Time 59 6.8. Same Blood Levelswith Different Designs 59 6.9. Same Blood Levelswith Different Mechanisms 59 6.10. Other Drugs ....................................... 60 6.11. Intermittent Delivery 61 6.12. ElectricallyEnhanced Permeation 62 References 63 Chapter 3 Prodrugs and TheirTopical Use Bradley D.Anderson 1. Introduction 69 2. Selectivityofthe Stratum Corneum to Permeant Structure 71 2.1. Polar Pathway 72 2.2. Lipid Pathway 73 3. DesignofProdrugs to Optimize Maximum Flux 80 References 87 Chapter4 Ultrasound-Mediated Transdermal Drug Delivery Joseph Kost andRobert Langer 1. Introduction 91 2. Ultrasound Characteristics 92
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