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PHARMACEUTICAL MANUFACTURING HANDBOOK Production and Processes SHAYNE COX GAD, PH.D., D.A.B.T. Gad Consulting Services Cary, North Carolina A JOHN WILEY & SONS, INC., PUBLICATION PHARMACEUTICAL MANUFACTURING HANDBOOK Production and Processes PHARMACEUTICAL MANUFACTURING HANDBOOK Production and P...

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PHARMACEUTICAL MANUFACTURING HANDBOOK Production and Processes

SHAYNE COX GAD, PH.D., D.A.B.T. Gad Consulting Services Cary, North Carolina

A JOHN WILEY & SONS, INC., PUBLICATION

PHARMACEUTICAL MANUFACTURING HANDBOOK Production and Processes

PHARMACEUTICAL MANUFACTURING HANDBOOK Production and Processes

SHAYNE COX GAD, PH.D., D.A.B.T. Gad Consulting Services Cary, North Carolina

A JOHN WILEY & SONS, INC., PUBLICATION

Copyright © 2008 by John Wiley & Sons, Inc. All rights reserved Published by John Wiley & Sons, Inc., Hoboken, New Jersey Published simultaneously in Canada No part of this publication may be reproduced, stored in a retrieval system, or transmitted in any form or by any means, electronic, mechanical, photocopying, recording, scanning, or otherwise, except as permitted under Section 107 or 108 of the 1976 United States Copyright Act, without either the prior written permission of the Publisher, or authorization through payment of the appropriate percopy fee to the Copyright Clearance Center, Inc., 222 Rosewood Drive, Danvers, MA 01923, (978) 750-8400, fax (978) 750-4470, or on the web at www.copyright.com. Requests to the Publisher for permission should be addressed to the Permissions Department, John Wiley & Sons, Inc., 111 River Street, Hoboken, NJ 07030, (201) 748-6011, fax (201) 748-6008, or online at http://www.wiley.com/go/permission. Limit of Liability/Disclaimer of Warranty: While the publisher and author have used their best efforts in preparing this book, they make no representations or warranties with respect to the accuracy or completeness of contents of this book and specifically disclaim any implied warranties of merchantability or fitness for a particular purpose. No warranty may be created or extended by sales representatives or written sales materials. The advice and strategies contained herein may not be suitable for your situation. You should consult with a professional where appropriate. Neither the publisher nor author shall be liable for any loss of profit or any other commercial damages, including but not limited to special, incidental, consequential, or other damages. For general information on our other products and services or for technical support, please contact our Customer Care Department within the United States at (800) 762-2974, outside the United States at (317) 572-3993 or fax (317) 572-4002. Wiley also publishes its books in a variety of electronic formats. Some content that appears in print may not be available in electronic formats. For more information about Wiley products, visit our web site at www.wiley.com. Library of Congress Cataloging-in-Publication Data is available. ISBN: 978-0-470-25958-0

Printed in the United States of America 10 9 8 7 6 5 4 3 2 1

CONTRIBUTORS

Susanna Abrahmsén-Alami, AstraZeneca R&D Lund, Lund, Sweden, Oral Extended-Release Formulations James Agalloco, Agalloco & Associates, Belle Mead, New Jersey, Sterile Product Manufacturing Fakhrul Ahsan, Texas Tech University, Amarillo, Texas, Nasal Delivery of Peptide and Nonpeptide Drugs James Akers, Akers Kennedy & Associates, Kansas City, Missouri, Sterile Product Manufacturing Raid G. Alany, The University of Auckland, Auckland, New Zealand, Ocular Drug Delivery; Microemulsions as Drug Delivery Systems Monique Alric, Université d’Auvergne, Clermont-Ferrand, France, Recombinant Saccharomyces Cerevisiae as New Drug Delivery System to Gut: In Vitro Validation and Oral Formulation Sacide Alsoy Altinkaya, Izmir Institute of Technology, Urla-Izmir, Turkey, Controlled Release of Drugs from Tablet Coatings Maria Helena Amaral, University of Porto, Porto, Portugal, Vaginal Drug Delivery Anil Kumar Anal, Living Cell Technologies (Global) Limited, Auckland, New Zealand, Controlled-Release Dosage Forms Gavin Andrews, Queen’s University Belfast, Belfast, Northern Ireland, Effects of Grinding in Pharmaceutical Tablet Production Sophia G. Antimisiaris, School of Pharmacy, University of Patras, Rio, Greece, Liposomes and Drug Delivery

vi

CONTRIBUTORS

Robert D. Arnold, The University of Georgia, Athens, Georgia, BiotechnologyDerived Drug Product Development C. Scott Asbill, Samford University, Birmingham, Alabama, Transdermal Drug Delivery Maria Fernanda Bahia, University of Porto, Porto, Portugal, Vaginal Drug Delivery Bernard Bataille, University of Montpelier 1, Montpellier, France, Tablet Design Gerald W. Becker, SSCI, West Lafayette, Indiana, Biotechnology-Derived Drug Product Development; Regulatory Considerations in Approval of Follow-On Protein Drug Products B. Wayne Bequette, Rensselaer Polytechnic Institute, Troy, New York, From Pilot Plant to Manufacturing: Effect of Scale-Up on Operation of Jacketed Reactors Erem Bilensoy, Hacettepe University Faculty of Pharmacy, Ankara, Turkey, Cyclodextrin-Based Nanomaterials in Pharmaceutical Field Stéphanie Blanquet, Université d’Auvergne, Clermont-Ferrand, France, Recombinant Saccharomyces Cerevisiae as New Drug Delivery System to Gut: In Vitro Validation and Oral Formulation Gary W. Bumgarner, Samford University, Birmingham, Alabama, Transdermal Drug Delivery Isidoro Caraballo, University of Sevilla, Seville, Spain, Tablet Design Stephen M. Carl, Purdue University, West Lafayette, Indiana, BiotechnologyDerived Drug Product Development; Regulatory Considerations in Approval of Follow-On Protein Drug Products Sudhir S. Chakravarthi, University of Nebraska Medical Center, College of Pharmacy, Omaha, Nebraska, Biodegradable Nanoparticles D.F. Chowdhury, University of Oxford, Oxford, United Kingdom, Pharmaceutical Nanosystems: Manufacture, Characterization, and Safety Barbara R. Conway, Aston University, Birmingham, United Kingdom, Solid Dosage Forms José das Neves, University of Porto, Porto, Portugal, Vaginal Drug Delivery Osama Abu Diak, Queen’s University Belfast, Belfast, Northern Ireland, Effects of Grinding in Pharmaceutical Tablet Production Brit S. Farstad, Instititue for Energy Technology, Isotope Laboratories, Kjeller, Norway, Radiopharmaceutical Manufacturing Dimitrios G. Fatouros, School of Pharmacy and Biomedical Sciences, Portsmouth, England, Liposomes and Drug Delivery Jelena Filipoviç-Grčič, Faculty of Pharmacy and Biochemistry, University of Zagreb, Zagreb, Croatia, Nasal Powder Drug Delivery

CONTRIBUTORS

vii

Eddy Castellanos Gil, Center of Pharmaceutical Chemistry and University of Havana, Havana, Cuba; University of Sevilla, Seville, Spain; University of Montpelier 1, Montpellier, France, Tablet Design Anita Hafner, Faculty of Pharmacy and Biochemistry, University of Zagreb, Zagreb, Croatia, Nasal Powder Drug Delivery A. Atilla Hincal, Hacettepe University Faculty of Pharmacy, Ankara, Turkey, Cyclodextrin-Based Nanomaterials in Pharmaceutical Field Michael Hindle, Virginia Commonwealth University, Richmond, Virginia, Aerosol Drug Delviery Bhaskara R. Jasti, University of the Pacific, Stockton, California, Semisolid Dosages: Ointments, Creams, and Gels Yiguang Jin, Beijing Institute of Radiation Medicine, Beijing, China, Nanotechnology in Pharmaceutical Manufacturing David Jones, Queen’s University Belfast, Belfast, Northern Ireland, Effects of Grinding in Pharmaceutical Tablet Production Anne Juppo, University of Helsinki, Helsinki, Finland, Oral Extended-Release Formulations Paraskevi Kallinteri, Medway School of Pharmacy, Universities of Greenwich and Kent, England, Liposomes and Drug Delivery Gregory T. Knipp, Purdue University, West Lafayette, Indiana, BiotechnologyDerived Drug Product Development; Regulatory Considerations in Approval of Follow-On Protein Drug Products Anette Larsson, Chalmers University of Technology, Göteborg, Sweden, Oral Extended-Release Formulations Beom-Jin Lee, Kangwon National University, Chuncheon, Korea, Pharmaceutical Preformulation: Physiochemical Properties of Excipients and Powders and Tablet Characterization Xiaoling Li, University of the Pacific, Stockton, California, Semisolid Dosages: Ointments, Creams, and Gels David J. Lindley, Purdue University, West Lafayette, Indiana, BiotechnologyDerived Drug Product Development Roberto Londono, Washington State University, Pullman, Washington, Liquid Dosage Forms Ravichandran Mahalingam, University of the Pacific, Stockton, California, Semisolid Dosages: Ointments, Creams, and Gels Kenneth R. Morris, Purdue University, West Lafayette, Indiana, BiotechnologyDerived Drug Product Development; Regulatory Considerations in Approval of Follow-On Protein Drug Products Erin Oliver, Rutgers, The State University of New Jersey, Piscataway, New Jersey, Biotechnology-Derived Drug Product Development; Regulatory Considerations in Approval of Follow-On Protein Drug Products

viii

CONTRIBUTORS

Iván Peñuelas, University of Navarra, Pamplona, Spain, Radiopharmaceutical Manufacturing Omanthanu P. Perumal, South Dakota State University, Brookings, South Dakota, Role of Preformulation in Development of Solid Dosage Forms Katharina M. Picker-Freyer, Martin-Luther-University Halle-Wittenberg, Institute of Pharmaceutics and Biopharmaceutics, Halle/Saale, Germany, Tablet Production Systems Satheesh K. Podaralla, South Dakota State University, Brookings, South Dakota, Role of Preformulation in Development of Solid Dosage Forms Dennis H. Robinson, University of Nebraska Medical Center, College of Pharmacy, Omaha, Nebraska, Biodegradable Nanoparticles Arcesio Rubio, Caracas, Venezuela, Liquid Dosage Forms Maria V. Rubio-Bonilla, Research Associate, College of Pharmacy, Washington State University, Pullman, Washington, Liquid Dosage Forms Ilva D. Rupenthal, The University of Auckland, Auckland, New Zealand, Ocular Drug Delivery Maria Inês Rocha Miritello Santoro, Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, São Paulo, Brazil, Packaging and Labeling Helton M.M. Santos, University of Coimbra, Coimbra, Portugal, Tablet Compression Raymond K. Schneider, Clemson University, Clemson, South Carolina, CleanFacility Design, Construction, and Maintenance Issues Anil Kumar Singh, Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, São Paulo, Brazil, Packaging and Labeling João J.M.S. Sousa, University Compression

of

Coimbra,

Coimbra,

Portugal,

Tablet

Shunmugaperumal Tamilvanan, University of Antwerp, Antwerp, Belgium, Progress in Design of Biodegradable Polymer-Based Microspheres for Parenteral Controlled Delivery of Therapeutic Peptide/Protein; Oil-in-Water Nanosized Emulsions: Medical Applications Chandan Thomas, Texas Tech University, Amarillo, Texas, Nasal Delivery of Peptide and Nonpeptide Drugs Gavin Walker, Queen’s University Belfast, Belfast, Northern Ireland, Effects of Grinding in Pharmaceutical Tablet Production Jingyuan Wen, The University of Auckland, Auckland, New Zealand, Microemulsions as Drug Delivery Systems Hui Zhai, Queen’s University Belfast, Belfast, Northern Ireland, Effects of Grinding in Pharmaceutical Tablet Production

CONTENTS

PREFACE SECTION 1 1.1

xiii MANUFACTURING SPECIALTIES

Biotechnology-Derived Drug Product Development

1 3

Stephen M. Carl, David J. Lindley, Gregory T. Knipp, Kenneth R. Morris, Erin Oliver, Gerald W. Becker, and Robert D. Arnold

1.2

Regulatory Considerations in Approval on Follow-On Protein Drug Products

33

Erin Oliver, Stephen M. Carl, Kenneth R. Morris, Gerald W. Becker, and Gregory T. Knipp

1.3

Radiopharmaceutical Manufacturing

59

Brit S. Farstad and Iván Peñuelas

SECTION 2 ASEPTIC PROCESSING

97

2.1

99

Sterile Product Manufacturing James Agalloco and James Akers

SECTION 3 3.1

FACILITY

From Pilot Plant to Manufacturing: Effect of Scale-Up on Operation of Jacketed Reactors

137

139

B. Wayne Bequette ix

x

3.2

CONTENTS

Packaging and Labeling

159

Maria Inês Rocha Miritello Santoro and Anil Kumar Singh

3.3

Clean-Facility Design, Construction, and Maintenance Issues

201

Raymond K. Schneider

SECTION 4 4.1

NORMAL DOSAGE FORMS

Solid Dosage Forms

233 235

Barbara R. Conway

4.2

Semisolid Dosages: Ointments, Creams, and Gels

267

Ravichandran Mahalingam, Xiaoling Li, and Bhaskara R. Jasti

4.3

Liquid Dosage Forms

313

Maria V. Rubio-Bonilla, Roberto Londono, and Arcesio Rubio

SECTION 5 5.1

NEW DOSAGE FORMS

345

Controlled-Release Dosage Forms

347

Anil Kumar Anal

5.2

Progress in the Design of Biodegradable Polymer-Based Microspheres for Parenteral Controlled Delivery of Therapeutic Peptide/Protein

393

Shunmugaperumal Tamilvanan

5.3

Liposomes and Drug Delivery

443

Sophia G. Antimisiaris, Paraskevi Kallinteri, and Dimitrios G. Fatouros

5.4

Biodegradable Nanoparticles

535

Sudhir S. Chakravarthi and Dennis H. Robinson

5.5

Recombinant Saccharomyces cerevisiae as New Drug Delivery System to Gut: In Vitro Validation and Oral Formulation

565

Stéphanie Blanquet and Monique Alric

5.6

Nasal Delivery of Peptide and Nonpeptide Drugs

591

Chandan Thomas and Fakhrul Ahsan

5.7

Nasal Powder Drug Delivery

651

Jelena Filipović-Grčić and Anita Hafner

5.8

Aerosol Drug Delivery

683

Michael Hindle

5.9

Ocular Drug Delivery

729

Ilva D. Rupenthal and Raid G. Alany

5.10

Microemulsions as Drug Delivery Systems Raid G. Alany and Jingyuan Wen

769

CONTENTS

5.11

Transdermal Drug Delivery

xi

793

C. Scott Asbill and Gary W. Bumgarner

5.12

Vaginal Drug Delivery

809

José das Neves, Maria Helena Amaral, and Maria Fernanda Bahia

SECTION 6 TABLET PRODUCTION 6.1

Pharmaceutical Preformulation: Physicochemical Properties of Excipients and Powers and Tablet Characterization

879

881

Beom-Jin Lee

6.2

Role of Preformulation in Development of Solid Dosage Forms

933

Omathanu P. Perumal and Satheesh K. Podaralla

6.3

Tablet Design

977

Eddy Castellanos Gil, Isidoro Caraballo, and Bernard Bataille

6.4

Tablet Production Systems

1053

Katharina M. Picker-Freyer

6.5

Controlled Release of Drugs from Tablet Coatings

1099

Sacide Alsoy Altinkaya

6.6

Tablet Compression

1133

Helton M. M. Santos and João J. M. S. Sousa

6.7

Effects of Grinding in Pharmaceutical Tablet Production

1165

Gavin Andrews, David Jones, Hui Zhai, Osama Abu Diak, and Gavin Walker

6.8

Oral Extended-Release Formulations

1191

Anette Larsson, Susanna Abrahmsén-Alami, and Anne Juppo

SECTION 7 7.1

ROLE OF NANOTECHNOLOGY

Cyclodextrin-Based Nanomaterials in Pharmaceutical Field

1223 1225

Erem Bilensoy and A. Attila Hincal

7.2

Nanotechnology in Pharmaceutical Manufacturing

1249

Yiguang Jin

7.3

Pharmaceutical Nanosystems: Manufacture, Characterization, and Safety

1289

D. F. Chowdhury

7.4

Oil-in-Water Nanosized Emulsions: Medical Applications

1327

Shunmugaperumal Tamilvanan

INDEX

1367

PREFACE

This Handbook of Manufacturing Techniques focuses on a new aspect of the drug development challenge: producing and administering the physical drug products that we hope are going to provide valuable new pharmacotherapeutic tools in medicine. These 34 chapters cover the full range of approaches to developing and producing new formulations and new approaches to drug delivery. Also addressed are approaches to the issues of producing and packaging these drug products (that is, formulations). The area where the most progress is possible in improving therapeutic success with new drugs is that of better delivery of active drug molecules to the therapeutic target tissue. In this volume, we explore current and new approaches to just this issue across the full range of routes (oral, parenteral, topical, anal, nasal, aerosol. ocular, vaginal, and transdermal) using all sorts of forms of formulation. The current metrics for success of new drugs in development once they enter the clinic (estimated at ranging from as low as 2% for oncology drugs to as high as 10% for oral drugs) can likely be leveraged in the desired direction most readily by improvements in this area of drug delivery. The Handbook of Manufacturing Techniques seeks to cover the entire range of available approaches to getting a pure drug (as opposed to a combination product) into the body and to its therapeutic tissue target. Thanks to the persistent efforts of Michael Leventhal, these 34 chapters, which are written by leading practitioners in each of these areas, provide coverage of the primary approaches to these fundamental problems that stand in the way of so many potentially successful pharmacotherapeutic interventions.

xiii

SECTION 1 MANUFACTURING SPECIALTIES

1.1 BIOTECHNOLOGY-DERIVED DRUG PRODUCT DEVELOPMENT Stephen M. Carl,1 David J. Lindley,1 Gregory T. Knipp,1 Kenneth R. Morris,1 Erin Oliver,2 Gerald W. Becker,3 and Robert D. Arnold4 1

Purdue University, West Lafayette, Indiana Rutgers, The State University of New Jersey, Piscataway, New Jersey 3 SSCI, West Lafayette, Indiana 4 The University of Georgia, Athens, Georgia 2

Contents 1.1.1 Introduction 1.1.2 Formulation Assessment 1.1.2.1 Route of Administration and Dosage 1.1.2.2 Pharmacokinetic Implications to Dosage Form Design 1.1.2.3 Controlled-Release Delivery Systems 1.1.3 Analytical Method Development 1.1.3.1 Traditional and Biophysical Analytical Methodologies 1.1.3.2 Stability-Indicating Methodologies 1.1.3.3 Method Validation and Transfer 1.1.4 Formulation Development 1.1.4.1 Processing Materials and Equipment 1.1.4.2 Container Closure Systems 1.1.4.3 Sterility Assurance 1.1.4.4 Excipient Selection 1.1.5 Drug Product Stability 1.1.5.1 Defining Drug Product Storage Conditions 1.1.5.2 Mechanisms of Protein and Peptide Degradation 1.1.5.3 Photostability 1.1.5.4 Mechanical Stress 1.1.5.5 Freeze–Thaw Considerations and Cryopreservation 1.1.5.6 Use Studies 1.1.5.7 Container Closure Integrity and Microbiological Assessment 1.1.5.8 Data Interpretation and Assessment Pharmaceutical Manufacturing Handbook: Production and Processes, edited by Shayne Cox Gad Copyright © 2008 John Wiley & Sons, Inc.