Pharmaceutical Preformulation and Formulation: A Practical Guide from Candidate Drug Selection to Commercial Dosage Form, Second Edition (Drugs and the Pharmaceutical Sciences, 199) PDF
Preview Pharmaceutical Preformulation and Formulation: A Practical Guide from Candidate Drug Selection to Commercial Dosage Form, Second Edition (Drugs and the Pharmaceutical Sciences, 199)
DRUGS AND THE PHARMACEUTICAL SCIENCES VOLUME 199 S E C O N D E D I T I O N Pharmaceutical Preformulation and Formulation A Practical Guide from Candidate Drug Selection to Commercial Dosage Form edited by Mark Gibson Pharmaceutical Preformulation and Formulation 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 University of Maryland Center for Pharmaceutical Physics Milford, Baltimore, Maryland New Jersey Jennifer B. Dressman Robert Gurny University of Frankfurt Institute Universite de Geneve of Pharmaceutical Technology Geneve, Switzerland Frankfurt, Germany Jeffrey A. Hughes Anthony J. Hickey University of Florida College University of North Carolina of Pharmacy School of Pharmacy Gainesville, Florida Chapel Hill, North Carolina Vincent H. L. Lee Ajaz Hussain US FDA Center for Drug Sandoz Evaluation and Research Princeton, New Jersey Los Angeles, California Joseph W. Polli Kinam Park GlaxoSmithKline Purdue University Research Triangle Park West Lafayette, Indiana North Carolina Jerome P. Skelly Stephen G. Schulman Alexandria, Virginia University of Florida Gainesville, Florida Elizabeth M. Topp University of Kansas Yuichi Sugiyama Lawrence, Kansas University of Tokyo, Tokyo, Japan Peter York Geoffrey T. Tucker University of Bradford University of Sheffield School of Pharmacy Royal Hallamshire Hospital Bradford, United Kingdom Sheffield, United Kingdom For information on volumes 1–149 in the Drugs and Pharmaceutical Science Series, please visit www.informahealthcare.com 150. Laboratory Auditing for Quality and Regulatory Compliance, Donald Singer, Raluca-Ioana Stefan, and Jacobus van Staden 151. Active Pharmaceutical Ingredients: Development, Manufacturing, and Regulation, edited by Stanley Nusim 152. Preclinical Drug Development, edited by Mark C. Rogge and David R. Taft 153. Pharmaceutical Stress Testing: Predicting Drug Degradation, edited by Steven W. Baertschi 154. Handbook of Pharmaceutical Granulation Technology: Second Edition, edited by Dilip M. Parikh 155. Percutaneous Absorption: Drugs–Cosmetics–Mechanisms–Methodology, Fourth Edition, edited by Robert L. Bronaugh and Howard I. Maibach 156. Pharmacogenomics: Second Edition, edited by Werner Kalow, Urs A. Meyer and Rachel F. Tyndale 157. Pharmaceutical Process Scale-Up, Second Edition, edited by Michael Levin 158. Microencapsulation: Methods and Industrial Applications, Second Edition, edited by Simon Benita 159. Nanoparticle Technology for Drug Delivery, edited by Ram B. Gupta and Uday B. Kompella 160. Spectroscopy of Pharmaceutical Solids, edited by Harry G. Brittain 161. Dose Optimization in Drug Development, edited by Rajesh Krishna 162. Herbal Supplements-Drug Interactions: Scientific and Regulatory Perspectives, edited by Y. W. Francis Lam, Shiew-Mei Huang, and Stephen D. Hall 163. Pharmaceutical Photostability and Stabilization Technology, edited by Joseph T. Piechocki and Karl Thoma 164. Environmental Monitoring for Cleanrooms and Controlled Environments, edited by Anne Marie Dixon 165. Pharmaceutical Product Development: In Vitro-In Vivo Correlation, edited by Dakshina Murthy Chilukuri, Gangadhar Sunkara, and David Young 166. Nanoparticulate Drug Delivery Systems, edited by Deepak Thassu, Michel Deleers, and Yashwant Pathak 167. Endotoxins: Pyrogens, LAL Testing and Depyrogenation, Third Edition, edited by Kevin L. Williams 168. Good Laboratory Practice Regulations, Fourth Edition, edited by Anne Sandy Weinberg 169. Good Manufacturing Practices for Pharmaceuticals, Sixth Edition, edited by Joseph D. Nally 170. Oral-Lipid Based Formulations: Enhancing the Bioavailability of Poorly Water-soluble Drugs, edited by David J. Hauss 171. Handbook of Bioequivalence Testing, edited by Sarfaraz K. Niazi 172. Advanced Drug Formulation Design to Optimize Therapeutic Outcomes, edited by Robert O. Williams III, David R. Taft, and Jason T. McConville 173. Clean-in-Place for Biopharmaceutical Processes, edited by Dale A. Seiberling 174. Filtration and Purification in the Biopharmaceutical Industry, Second Edition, edited by Maik W. Jornitz and Theodore H. Meltzer 175. Protein Formulation and Delivery, Second Edition, edited by Eugene J. McNally and Jayne E. Hastedt 176. Aqueous Polymeric Coatings for Pharmaceutical Dosage Forms, Third Edition, edited by James McGinity and Linda A. Felton 177. Dermal Absorption and Toxicity Assessment, Second Edition, edited by Michael S. Roberts and Kenneth A. Walters 178. Preformulation Solid Dosage Form Development, edited by Moji C. Adeyeye and Harry G. Brittain 179. Drug-Drug Interactions, Second Edition, edited by A. David Rodrigues 180. Generic Drug Product Development: Bioequivalence Issues, edited by Isadore Kanfer and Leon Shargel 181. Pharmaceutical Pre-Approval Inspections: A Guide to Regulatory Success, Second Edition, edited by Martin D. Hynes III 182. Pharmaceutical Project Management, Second Edition, edited by Anthony Kennedy 183. Modified Release Drug Delivery Technology, Second Edition, Volume 1, edited by Michael J. Rathbone, Jonathan Hadgraft, Michael S. Roberts, and Majella E. Lane 184. Modified-Release Drug Delivery Technology, Second Edition, Volume 2, edited by Michael J. Rathbone, Jonathan Hadgraft, Michael S. Roberts, and Majella E. Lane 185. The Pharmaceutical Regulatory Process, Second Edition, edited by Ira R. Berry and Robert P. Martin 186. Handbook of Drug Metabolism, Second Edition, edited by Paul G. Pearson and Larry C. Wienkers 187. Preclinical Drug Development, Second Edition, edited by Mark Rogge and David R. Taft 188. Modern Pharmaceutics, Fifth Edition, Volume 1: Basic Principles and Systems, edited by Alexander T. Florence and Juergen Siepmann 189. Modern Pharmaceutics, Fifth Edition, Volume 2: Applications and Advances, edited by Alexander T. Florence and Juergen Siepmann 190. New Drug Approval Process, Fifth Edition, edited by Richard A.Guarino 191. Drug Delivery Nanoparticulate Formulation and Characterization, edited by Yashwant Pathak and Deepak Thassu 192. Polymorphism of Pharmaceutical Solids, Second Edition, edited by Harry G. Brittain 193. Oral Drug Absorption: Prediction and Assessment, Second Edition, edited by Jennifer J. Dressman, hans Lennernas, and Christos Reppas 194. Biodrug Delivery Systems: Fundamentals, Applications, and Clinical Development, edited by Mariko Morista and Kinam Park 195. Pharmaceutical Process Engineering, Second Edition, edited by Anthony J. Hickey and David Ganderton 196. Handbook of Drug Screening, Second Edition, edited by Ramakrishna Seethala and Litao Zhang 197. Pharmaceutical Powder Compaction Technology, Second Edition, edited by Metin Celik 198. Handbook of Pharmaceutical Granulation Technology, Dilip M. Parikh 199. Pharmaceutical Preformulation and Formulation: A Practical Guide from Candidate Drug Selection to Commercial Dosage Form, Second Edition, edited by Mark Gibson Pharmaceutical Preformulation and Formulation Second Edition A Practical Guide from Candidate Drug Selection to Commercial Dosage Form edited by Mark Gibson AstraZeneca R&D Charnwood Loughborough, Leicestershire, UK InformaHealthcareUSA,Inc. 52VanderbiltAvenue NewYork,NY10017 #2009byInformaHealthcareUSA,Inc. InformaHealthcareisanInformabusiness NoclaimtooriginalU.S.Governmentworks PrintedintheUnitedStatesofAmericaonacid-freepaper 10 9 8 7 6 5 4 3 2 1 InternationalStandardBookNumber-10:1-4200-7317-6(Hardcover) InternationalStandardBookNumber-13:978-1-4200-7317-1(Hardcover) This book contains information obtained from authentic and highly regarded sources. Reprinted material is quoted with permission,andsourcesareindicated.Awidevarietyofreferencesarelisted.Reasonableeffortshavebeenmadetopublish reliabledataandinformation,buttheauthorandthepublishercannotassumeresponsibilityforthevalidityofallmaterials orfortheconsequenceoftheiruse. Nopartofthisbookmaybereprinted,reproduced,transmitted,orutilizedinanyformbyanyelectronic,mechanical,or othermeans,nowknownorhereafterinvented,includingphotocopying,microfilming,andrecording,orinanyinformation storageorretrievalsystem,withoutwrittenpermissionfromthepublishers. For permission to photocopy or use material electronically from this work, please access www.copyright.com (http:// www.copyright.com/)orcontacttheCopyrightClearanceCenter,Inc.(CCC)222RosewoodDrive,Danvers,MA01923, 978-750-8400. CCC is a not-for-profit organization that provides licenses and registration for a variety of users. For organizationsthathavebeengrantedaphotocopylicensebytheCCC,aseparatesystemofpaymenthasbeenarranged. Trademark Notice: Product or corporate names may be trademarks or registered trademarks, and are used only for identificationandexplanationwithoutintenttoinfringe. LibraryofCongressCataloging-in-PublicationData Pharmaceuticalpreformulationandformulation:Apracticalguidefromcandidatedrug selectiontocommercialdosageform/editedbyMarkGibson. —2nded. p.;cm.— (Drugsandthepharmaceuticalsciences;199) Includesbibliographicalreferencesandindex. ISBN-13:978-1-4200-7317-1(hb:alk.paper) ISBN-10:1-4200-7317-6(hb:alk.paper) 1. Drugs—Dosageforms. I. Gibson,Mark,1957-II. Series:Drugsandthepharmaceutical sciences;v.199. [DNLM: 1. DrugCompounding. 2. Biopharmaceutics—methods. 3. DosageForms. 4. DrugDiscovery. 5. DrugEvaluation. W1DR893Bv.199 2009/QV778P535352009] RS200.P4252009 6150.1—dc22 2009012458 ForCorporateSalesandReprintPermissionscall212-520-2700orwriteto:SalesDepartment,52VanderbiltAvenue, 16thfloor,NewYork,NY10017. VisittheInformaWebsiteat www.informa.com andtheInformaHealthcareWebsiteat www.informahealthcare.com Preface Thefirsteditionofthisbookpublishedin2001hasbeenmoresuccessfulthanIeverimagined, as indicated by the excellent reviews it has received, the continued demand, and impressive sales! I believe that the main reasons for its popularity are that there was a significant gap in the literature and also that the information presented was based on the extensive experiences of the various contributors who were all actively working in the industry and were willing to share “best practice” from their knowledge and experiences. The book is intended to be a practical guide to pharmaceutical preformulation and formulation to be used as a reference source or a guidance tool to those working in the pharmaceutical industry or related industries, such as biopharmaceuticals or medical devices, or anyone wanting an insight into thesubjectarea.Indeed,thisbookhasalsoprovedtobeavaluabletextforundergraduateand postgraduatecoursesinindustrialpharmacyandpharmaceuticaltechnology.Asecondedition isrequiredbecausepreformulationandformulationtechnologycontinuestodevelopandalso because there are bound to be some gaps and improvements to be filled. The second edition still meets the main objectives of the first edition, that is, to l provide a logical and structured approach to product development, with key stages identified and the preformulation, biopharmaceutics, and formulation activities and typicalissuesateachstagediscussed,whereverpossiblewithrealorworkedexamples, l emphasize what practical studies need to be undertaken for what reasons and during what key stages of the drug development process, and l provide separate chapters on the formulation development of each route and type of dosage forms. The pressure to accelerate the drug development process, shorten the development timelines, and launch new pharmaceutical products is even more intense than before, with fewer registrations year on year. Having a structured approach and doing the right things first time are essential elements for achieving this. The chapters on product design and product optimization are still very relevant but have been updated to include the quality by design (QbD) and International Conference on Harmonisation (ICH) Q8 (product development), ICH Q9 (quality risk management), process analytical technology (PAT), and lean manufacturing principles that aim to link regulatory expectations to good science. Another significant change since the first edition is the growth of biopharmaceuticals, compared with small molecules, that deserves more attention. Pharmaceutical companies are shifting from developing small molecules to developing biopharmaceuticals to treat a wide range of diseases, and today approximately one in four drugs introduced to the market is a biopharmaceutical. Since the majority of biopharmaceuticals will be delivered by injection or infusion, the chapter on parenteral dosage forms has been updated to reflect this. Focus has been given to the steps after purification, formulation, and subsequent fill-finish. Consider- ationhasalsobeengivenintheotherchaptersforhandlinganddevelopingbiopharmaceutical dosage forms where there is some potential for drug delivery, for example, intranasal dosage forms. Elsewhere in the second edition, there are updates throughout the book to reflect on some omissions and developmentssince the first editionand makeit up-to-date; forexample, to reflect emerging “cutting-edge” technologies such as polymorph and salt selection and viii Preface prediction, molecular modeling and automation in preformulation studies, and more consider- ation for packaging technology during development of the various dosage forms. Once again I am indebted to all the contributors for giving up their time and energy in producingthisupdatedversion.Iamalsoindebtedtomywife,Alison,andmyfamilyfortheir support and understanding during the time I have been busy working on this book. Mark Gibson Contents Preface vii Contributors xi 1. Introduction and Perspective 1 Mark Gibson 2. Aiding Candidate Drug Selection: Introduction and Objectives 11 Mark Gibson 3. Preformulation Investigations using Small Amounts of Compound as an Aid to Candidate Drug Selection and Early Development 17 Gerry Steele and Talbir Austin 4. Biopharmaceutical Support in Candidate Drug Selection 129 Anna-Lena Ungell and Bertil Abrahamsson 5. Early Drug Development: Product Design 172 Mark Gibson 6. Preformulation as an Aid to Product Design in Early Drug Development 188 Gerry Steele 7. Biopharmaceutical Support in Formulation Development 247 Bertil Abrahamsson and Anna-Lena Ungell 8. Product Optimization 289 Mark Gibson 9. Parenteral Dosage Forms 325 Joanne Broadhead and Mark Gibson 10. Inhalation Dosage Forms 348 Paul Wright 11. Oral Solid Dosage Forms 367 Peter Davies 12. Ophthalmic Dosage Forms 431 Mark Gibson
The list of books you might like
