A Guide to Pharmaceutical Particulate Science

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<p>Boca Raton London New York Washington, D.C.Interpharm/CRCTimothy M. CrowderAnthony J. HickeyMargaret D. LoueyNorman OrrA Guide toPharmaceuticalParticulateScience</p> <p>This book contains information obtained from authentic and highly regarded sources. Reprinted materialis quoted with permission, and sources are indicated. A wide variety of references are listed. Reasonableefforts have been made to publish reliable data and information, but the author and the publisher cannotassume responsibility for the validity of all materials or for the consequences of their use.Neither this book nor any part may be reproduced or transmitted in any form or by any means, electronicor mechanical, including photocopying, microlming, and recording, or by any information storage orretrieval system, without prior permission in writing from the publisher.The consent of CRC Press LLC does not extend to copying for general distribution, for promotion, forcreating new works, or for resale. Specic permission must be obtained in writing from CRC Press LLCfor such copying.Direct all inquiries to CRC Press LLC, 2000 N.W. Corporate Blvd., Boca Raton, Florida 33431. Trademark Notice: Product or corporate names may be trademarks or registered trademarks, and areused only for identication and explanation, without intent to infringe.Visit the CRC Press Web site at www.crcpress.com 2003 by Interpharm/CRCNo claim to original U.S. Government worksInternational Standard Book Number 1-57491-142-2Library of Congress Card Number 2002152626Printed in the United States of America 1 2 3 4 5 6 7 8 9 0Printed on acid-free paperLibrary of Congress Cataloging-in-Publication DataCrowder, Timothy M. [et al.]A guide to pharmaceutical particulate science / Timothy M. Crowder, et al.p. cm.Includes bibliographical references and index.ISBN 1-57491-142-21. Powders (Pharmacy) 2. Particles.[DNLM: 1. Pharmaceutical Preparationschemistry. 2. Powderschemistry. 3. DrugAdministration Routes. 4. Drug Compounding. QV 785 G946 2003] I. Crowder, Timothy M.RS201.P8 G85 2003615d.43dc21 2002152626</p> <p>Contents iiiDr. Norman OrrPowder technology is the foundation of dosageform design and particle engineering is the futureof efficient, reproducible, and effective drugdelivery.This was Normans view of the justification for a book on pharma-ceutical particulate science. His vision, enthusiasm, encouragement,and early contributions are its basis. This publication representsone small addition to Normans list of achievements as a pharma-ceutical scientist, educator, industrialist, colleague, family man, andfriend. He is missed by all who knew him.2003 by Interpharm/CRC Press LLC</p> <p>iv ContentsThe AuthorsAnthony J. Hickey, Ph.D., C. Biol. F.I.Biol., is Professor of Drug Deliveryand Disposition and Biomedical Engineering and Mathematics at the Uni-versity of North Carolina in Chapel Hill. In addition to his academic posi-tion, he is President and CEO of Cirrus Pharmaceuticals, Inc. and founderof Oriel Therapeutics, Inc.Dr. Hickey received his Ph.D. in Pharmaceutical Sciences from theUniversity of Aston in Birmingham, United Kingdom (1984), and thenworked at the University of Kentucky before joining the faculty inParmaceutics at the University of Illinois/Chicago. In 1990, he receivedthe Young Investigator Award in Pharmaceutics and Pharmaceutical Tech-nology from the American Association of Pharmaceutical Scientists. Heaccepted a faculty position in 1993 in the School of Pharmacy at the Uni-versity of North Carolina. In 2000, he was elected a Fellow of the Instituteof Biology of the United Kingdom.Dr. Hickey has published over 100 papers and chapters in the pharma-ceutical and biomedical literature and co-authored a text on pharmaceuti-cal process engineering, as well as editing two volumes on the subject ofpharmaceutical inhalation aerosols.Margaret D. Louey, Ph.D., graduated with a Bachelor of Pharmacy (Hon-ors) and a Ph.D. in Pharmaceutics from the Victorian College of Pharmacy,Monash University (Australia). She completed a postdoctoral fellowshipat the School of Pharmacy at the University of North Carolina/Chapel Hill.Her research has primarily involved particle interactions within dry pow-der aerosols and their formulations. Dr. Louey is a registered pharmacistwith clinical experience in Australia and the United Kingdom.Timothy M. Crowder, Ph.D., graduated with a B.S. in Physics fromDavidson College, Davidson, North Carolina and a Masters in Physicsfrom North Carolina State University. He completed his Ph.D. in Biomedi-cal Engineering from the University of North Carolina. Dr. Crowders re-search concerns the physics of powder flow and its application to disper-sion in dry powder inhalers. He is a founder and the Chief TechnologyOfficer of Oriel Therapeutics.2003 by Interpharm/CRC Press LLC</p> <p>Contents vContentsPreface1. Introduction and OverviewSituation AnalysisQuality of Published Data on Particle Size inPharmaceuticalsThe Future of Crystal EngineeringChemistry and Pharmacy Regulatory SubmissionsMisconceptions and Misunderstandings ofParticulate SciencePowerful Methods Complementary to ParticleSizingIntegration of Particle Sizing Methods withTheir In-Use SituationAdjacencies and Interactions Between ParticlesLessons from Other IndustriesPharmaceutical Particulate Science as a CoreEducational RequirementParticle Characterization and Its Impact onRegulatory Submissions from Formulationthrough Toxicology and EfficacyConclusion2. Particulate Systems: Manufacture andCharacterizationStates of MatterCrystalline SolidsCrystal SymmetryEulers RelationshipCrystal Systems2003 by Interpharm/CRC Press LLC</p> <p>Miller IndicesSpace LatticesSolid State BondingIsomorphs and PolymorphsEnantiomorphs and RacematesCrystal HabitCrystal ImperfectionsMethods of Particle ProductionParticulate SystemsConclusion3. Sampling and Measurement BiasesSampling StrategiesStatistical AnalysesSampling TechniquesSegregationSamplingSampling ErrorsPreparation ErrorsParticle Size Measurement ErrorsConclusions4. Particle Size Descriptors and StatisticsParticle Size DescriptorsParticle Size StatisticsMathematical DistributionsApplicationsConclusion5. Behavior of ParticlesPhysical PropertiesParticle AdhesionParticle Motion in Bulk PowdersParticle Motion in Gaseous DispersionsParticle Motion in Liquid MediaConclusion2003 by Interpharm/CRC Press LLC</p> <p>6. Instrumental AnalysisDirect ImagingIndirect ImagingPhysical Methods of Particle Size SeparationApproaches to CalibrationConclusions7. Methods of Particle Size Measurement andTheir Importance for Specific Applications(Instrument Synergy)An Essay on Measures of DiametersConclusion8. Particle Size and Physical Behavior of a PowderSelection of the Appropriate Particle Size ExpressionPowder Flow and MixingDispersionGranulation and CompressionConclusion9. Clinical Effect of Pharmaceutical Particulate SystemsOral DeliveryParenteral DeliveryRespiratory DeliveryNasal DeliveryTransdermal and Topical DeliveryOcular DeliveryOtic DeliveryBuccal and Sublingual DeliveryRectal DeliveryVaginal DeliveryConclusions10. General ConclusionsReferences2003 by Interpharm/CRC Press LLC</p> <p>Preface ixPreface</p> <p>Numerous texts focus on aspects of powder formation and be-havior, notably the contributions of Rumpf, Rietema, and Allen. Inaddition, the pharmaceutical application of powder technology andparticle science has long been recognized. Examples of books onthis subject are those by Carstensen, Groves, and Barber. In recentyears, some very thorough texts have addressed pharmaceuticalpowders and their properties. The present volume is intended to bea guide to some key principles and their practical applications. Nu-merous references throughout the text are listed alphabetically atthe back of the book to direct the reader to sources for greater detailon elements of this exposition.The idea for this book was conceived in 1993 by Norman Orr,then of SmithKline Beecham; Amy Davis, formerly of InterpharmPress; and me. Norman felt strongly that this need not be a compre-hensive volume because many excellent texts were already avail-able, such as those mentioned above. Instead, he suggested, and Iagreed, that the importance of particle technology in the pharma-ceutical sciences was understated, and that in particular the poten-tial for error, misuse, or abuse of data should be addressed in a guideto the field. If this initiates some debate, I am sure Norman wouldhave been very pleased.2003 by Interpharm/CRC Press LLC</p> <p>In the intervening years, some quite dramatic developments haveoccurred. Most significantly, the driving force for the production ofthis book was lost. Norman Orr passed away prematurely after arelatively short illness in 1997. In addition, the level of understand-ing of particle properties and their importance for the performanceof a pharmaceutical dosage form have increased substantially. Thisgrowth in knowledge was accompanied by a variety of technologi-cal advances in particle manufacture and characterization. Fortu-nately, these events occurred in time for Norman to see many of hisaspirations realized. In the face of these changes, the incentive toproduce such a volume waned. However, through the encourage-ment and support of Amy Davis and Tom Waters, of InterpharmPress, I continued to muse over the possibility of finishing this project.Finally, I was fortunate in that two enthusiastic and knowledgeablecolleagues, Timm Crowder and Margaret Louey, joined me in thepreparation of the manuscript that was the basis for this book.Largely through their persistence and hard work, this volume wascompleted.Normans major written contribution to the text is the introduc-tion. It includes many of his comments, and their clarity and direct-ness convey his commitment to this subject. His overriding view,expressed in early correspondence with me, was that there is nocurrent text that enables the pharmaceutical scientist to sensibly ex-ploit the power of particulate science in the design, manufacture,and control of quality medicines. To the extent that this text helpsin this endeavor, the credit can be given to Norman who, withoutdoubt, was a visionary in this field. If it deviates from this goal, Iaccept the responsibility because Timm and Margaret have laboredunder my representations of Normans objectives without the plea-sure of having known him. I hope that you, the reader, find the finalproduct of value in your day-to-day activities.Anthony J. HickeyChapel Hill, NC, 20022003 by Interpharm/CRC Press LLC</p> <p>References 207References</p> <p>Aguiar, A. J., J. E. Zelmer, and A. W. Kinkel. 1967. Deaggregation behavior of arelatively insoluble substituted benzoic acid and its sodium salt. J. Pharm. Sci.56:12431252.Alderborn, G. 1996. Particle dimensions. In Pharmaceutical powder compaction tech-nology, eds. G. Alderborn and C. Nystrm. New York: Marcel Dekker. 245282.Allen, L. V, V. A. Yanchick, and D. D. Maness. 1977. Dissolution rates of corticoster-oids utilizing sugar glass dispersions. J. Pharm. Sci. 66:494497.Allen, T. 1968. Particle size measurement. London: Chapman and Hall.Allen, T. 1975. Particle size, shape and distribution. In Particle size measurement, ed.T. Allen. London: Chapman and Hall. 74112.Allen, T. 1990a. Particle size measurement. London: Chapman and Hall.Allen, T. 1990b. Sampling of dusty gases in gas streams. In Particle size measurement,ed. T. Allen. London: Chapman and Hall. 4171.Allen, T. 1990c. Sampling of powders. In Particle size measurement, ed. T. Allen. Lon-don: Chapman and Hall. 140.Amidon, G. 1992. Report and recommendation of the USP Advisory Panel on physi-cal test methodsfunctionality. I: General chapter on particle characterizationby optical microscopy. Pharm. Forum 18:40894092.Amidon, G. E. 1995. Physical and mechanical property characterization of pow-ders. In Physical characterization of pharmaceutical solids, ed. H. G. Brittain. NewYork: Marcel Dekker. 281319.Anderberg, E. K., M. Bisrat, and C. Nystrm. 1988. Physicochemical properties ofdrug release. Part 7: Effect of surfactant concentration and drug particle sizeon solubility and dissolution rate of felodipine, a sparingly soluble drug. Int. J.Pharm. 47:6777.2003 by Interpharm/CRC Press LLC</p> <p>208 A Guide to Pharmaceutical Particulate ScienceAntal, E. J., C. F. Dick, C. E. Wright, I. R. Welshman, and E. M. Block. 1989. Com-parative bioavailability of two medroxyprogesterone acetate suspensions. Int.J. Pharm. 54:3339.Aoyagi, N., H. Ogata, N. Kaniwa, M. Koibuchi, and T. Shibazaki. 1982a. Bioavail-ability of griseofulvin from tablets in beagle dogs and correlation with disso-lution rate and bioavailability in humans. J. Pharm. Sci. 71:11691172.Aoyagi, N., H. Ogata, N. Kaniwa, M. Koibuchi, and T. Shibazaki. 1982b. Bioavail-ability of griseofulvin from tablets in humans and correlation with dissolutionrate. J. Pharm. Sci. 71:11651169.ASTM (American Society for Testing and Materials). 1973. Recommended Practicefor Analyses by Microscopial Methods. Philadelphia: ASTM.Avnir, D., and M. Jaroniec. 1989. An isotherm equation for adsorption on fractalsurfaces of heterogeneous porous materials. Langmuir 5:14311433.Bapatia, K. M., and G. Hecht. 1996. Ophthalmic ointments and suspensions. In Phar-maceutical dosage forms: Disperse systems, eds. H. A. Lieberman, M. M. Rieger,and G. S. Banker. New York: Marcel Dekker. 357397.Barker, G., and M. Grimson. 1990. The physics of muesli. New Scientist 126:3740.Bastian, P., R. Bartkowski, H. Kohler, and T. Kissel. 1998. Chemo-embolization ofexperimental liver metastases. Part I: Distribution of biodegradablemicrospheres of different sizes in an animal model for the locoregional therapy.Eur. J. Pharm. Biopharm. 46:243254.Behl, C. R., H. K. Pimplaskar, A. P. Sileno, J. deMeireles, and V. D. Romeo. 1998.Effects of physicochemical properties and other factors on systemic nasal drugdelivery. Adv. Drug Deliv. Rev. 29:89116.Bennema, P. 1992. Growth forms of crystals: Possible implications for powder tech-nology. Kona Powder Particle. 10:2540.Bentejac, R. 1994. Freeze-drying. In Powder technology and pharmaceutical processes,eds. D. Chulia, M. Deleuil, and Y. Pourcelot. Amsterdam: Elsevier. 257271.Berglund, R. N., and B. Y. H. Liu. 1973. Generation of monodisperse aerosol stan-dards. Environ. Sci. Tech. 7:147153.Berman, J., A. Schoeneman, and J. T. Shelton. 1996. Unit dose sampling: A tale oftwo thieves. Drug Dev. Ind. Pharmacy 22:11211132.Berman, J., and J. A. Planchard. 1995. Blend uniformity and unit dose sampling.Drug Dev. Ind. Pharmacy 21:12571283.Binnig, G., C. F. Quate, and C. Gerber. 1986. Atomic force microscope. Phys. Rev.Lett. 56:930933.Bisrat, M., M. Glazer, O. Camber, and P. Edman. 199...</p>

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