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PHARMACEUTICAL DOSAGE FORMS PHARMACEUTICAL DOSAGE FORMS Tablets SECOND EDITION, REVISED AND EXPANDED In Three Volumes VOLUME 3 EDITED BY Herbert A. Lieberman H. H. Lieberman Associates, Inc. Consultant Services Livingston, New Jersey Leon Lachman Lachman Consultant Services Westbury, New York Josep...

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PHARMACEUTICAL DOSAGE FORMS

PHARMACEUTICAL DOSAGE FORMS Tablets SECOND EDITION, REVISED AND EXPANDED In Three Volumes

VOLUME 3 EDITED BY

Herbert A. Lieberman H. H. Lieberman Associates, Inc. Consultant Services Livingston, New Jersey

Leon Lachman Lachman Consultant Services Westbury, New York

Joseph B. Schwartz Philadelphia College of Pharmacy and Science Philadelphia, Pennsylvania

n

MARCEL

DEKKER

MARCEL DEKKER, INC.

NEW YORK· BASEL· HONG KONG

ISBN: 0-8247-8300-X

This book is printed on acid- free paper. Copyright 0 1990 by MARCEL DEKKER. INC.

All Rights Reserved

Neither this book nor any part may be reproduced or transmitted in any form or by any means. electronic or mechanical, including photocopying, microfilming, and recording. or by any information storage and retrieval system, without permission in writing from the pubttsher , MARCEL DEKKER. INC. 270 Madison Avenue. New York. New York 10016 Current printing (last digit): 10 9 8 7 6 5 PRINTED IN THE UNITED STATES OF AMERICA

Preface

Tablets are the most commonly prescribed dosage form. The reason for this popularity is that tablets offer a convenient form of drug administration, provide dosage uniformity from tablet to tablet. are stable over extended and diverse storage conditions, and can be produced on high -speed compression, labeling, and packaging equipment. As a result, tablet production technology is constantly undergoing improvements that enhance their ability to deliver, with precision. a desired drug in a dosage form intended for immediate or extended therapeutic effect. In addition. the growth of the generic industry as well as increased competition from both foreign and domestic markets require that a tablet manufacturer have greater concern regarding the economics of tablet production by introducing less labor-intensive, higher-productivity manufacturing methods for making the increasing number of tablet products available today. The changes in the science and technology of tablet formulation, production, and quality assurance to accomplish the above are reflected in the second edition of the three-volume series Pharmaceutical Dosage Forms: Tablets. The first volume in this series describes the many types of tablet products, giving specific updated examples of typical formulations and methods of manufacture. These include single- and multilayered tablets, buccal and sublingual tablets, effervescent tablets. and diverse methods for manufaeturtng them by wet and dry granulations and by direct compression. In addition, medicated candy products are a form of drug delivery that has appeared in the marketplace; no complete chapter on this technology has been printed in any pharmacy text other than both editions of this series on tablets. To manufacture tablets a number of unit processes are required, such as mixing, drying, size reduction, and compression. The economics of tablet production today require an update of the technologies for each of these pharmaceutical operations. The granulations and tablets produced iii

iv

Preface

have particular characteristics that must be analyzed and understood in order to produce superior tablets, particularly when new and sometimes faster methods of manufacture are introduced. No drug dosage form would be meaningful to the patient without the drug being bioavailable. The chapter on bioavailability in tablet technology is updated in the second edition of Volume 2. Finally, many advances in the specifications and care of tablet tooling and problem solving caused by faulty compression tools are expertly covered in the second volume. Volume 3 in the series on tablets updates the special characteristics that should be considered for optimizing tablet production. Particular emphasis is given to design methods that should be considered when formuIattng a tablet product. Discussions of specialized granule and tablet-coating equipment are presented. discussing improvements or presenting new equipment developed since the publication of the first edition. Aqueous film coating is now firmly established in pharmaceutical coating processes, and thus, a shift in emphasis on coating procedures has been made in the revised chapter on coating. New coating pans and automation of aqueous film- and sugar-coating methods are covered. Fluid-bed processes and particle-coating methods, including theoretical considerations, are updated to reflect current practices. No text on tablet technology eould be considered complete without a full theoretical and practical updated description of current methods for formulating, manufacturing, and controlling the release of drug from sustained-release tablet and particle dosage forms. A chapter on sustained drug release through coating provides an updated and authoritative discussion of this popular form of drug delivery. There is an enhanced emphasis on the various polymers and their combinations used to attain sustained drug activity. Pilot operations must reflect production methods in order to minimize difficulties in transferring a product from preproduction to production. Granules prepared by precompression, wet and dry granulation, fluidized-bed granulation, and spray drying are compared. A new method for preparing a granulation, namely the moisture-activated dry granulation (MADG), is also suggested for more widespread pilot evaluation. With the increasing emphasis on product uniformity from one tablet to another. or from one batch to another, whether the product is made sequentially or with long lag periods between batches, or whether the raw material source is from several different manufacturers, the concept of process validation is essential. An extensive chapter descrfbing the essential considerations that should be evaluated in process validation has been added to the revised edition of this volume. Although the chapter presents a complete detailed description of many validation methods, it also shows how less detailed approaches, some of which are commonly used in the industry, are useful. Current tablet production methods are described with sample control charts to help the readers improve their tablet production methods. The importance of the several different functions of production departments, their particular skills, and the need for coordinated and cooperative work relationships are stressed in the chapter "Tablet Production" so that the combined, partnership efforts of all production personnel can lead to superior tablet production. Automation of tablet compression and coating is also part of the chapter concerned with the production of tablets. In the discussion of stability, updated stability protocols to comply with recent FDA guidelines are presented. A new covariance analysis and

Preface

v

statistical method for expiration date prediction are described. The chapter "Quality Assurance" upgrades tablet testing for uniformity. dissolution, assay limit, test methods, and compendia! requirements for tablets to comply with current USP/NF requirements. Included are instructive figures for new schematic sampling plans. an update of the restrictions on the use of colors, and a recommended sampling method for raw materials. Thus, with this third volume on tablets. all the parameters currently concerned with the production of superior tablets are made current and discussed extensively. An updated and full coverage of the many topics concerned with tablets requires highly knowledgeable authors for each of the many areas that must be covered. To compile and update the pertinent information needed for the various chapters in this book required a multiauthored text of technologists with specific expertise and experience in their chosen subject matter. Each of the authors was charged with teaching their subject in such a fashion that the novice as well as the experienced reader will profit. They were to offer basic scientific facts and practical information so that all readers can learn theory and apply it toward the knowledge that each needs to formulate, produce, and control tablet operations in a scientific rather than an empirical manner. With this third volume. the editors have finished their task of updating the second edition on tablets. The editors are grateful to the authors for their fine contributions and. particularly. their patient response to the editors' suggestions for changes. The choice of the chapter topics, the authors. and the format are the responsibilities of the editors. It is hoped that these choices will prove fruitful to our readers by helping them solve their tablet technology problems and thereby advance industrial pharmacy's contribution toward improving both quality and efficiency in the manufacture of tablets. Herbert A. Lieberman Leon Lachman Joseph B. Schwartz

Contents

Preface Contributors Contents of Pharmaceutical Dosage Forms: Volumes 1 and Contents of Pharmaceutical Volumes 1 and Contents of Pharmaceutical Volumes 1 and

Tablets, Second Edition

iii xi xiii

Parenteral Medications.

xv

2 Dosage Forms: 2 Dosage Forms: 2

Disperse Systems.

Chapter 1. Principles of Improved Tablet Production System Design

xvii

1

Garnet E. Peck. Neil R. Anderson. and Gilbert S. Banker

I. 11. III. IV.

Introduction Benefits of Improved Tablet Production Systems Production Process Design Considerations Validation Appendix: List of Manufacturers References

Chapter 2. Coating of Pharmaceutical Solid -Dosage Forms

1 3 3 64 73 74

77

Stuart C. Porter and Charles H. Bruno

I. II. III.

Introduction Sugar Coating Film Coating

77

78 93

vii

viii

Contents

IV. V.

Coating Equipment Automated Coating Procedures References

Chapter 3. Particle-Coating Methods

125 155 158

161

Dale E. WUr'ster

I.

II. III. IV.

V. VI. VII.

Chapter 4.

Introduction Wurster Process Centrifugation Spray Drying Aqueous- Phase Separation. Coacervation Nonaqueous-Phase Separation In terfacial Polymerization References

Sustained Drug Release from Tablets and Particles Through Coating

161 162 184 187 189 193 194 195

199

Hong-Run Chang and Joseph R. Robinson I.

II. III. IV. V. VI.

Chapter 5.

Introduction Requirements for Sustained Drug Release Fabrication of Sustained - Release Products Sustained-Release Products Through Coating Coating Materials Summary References

The Pharmaceutical Pilot Plant

199 201 208 241 282 287 287

303

Charles I. Jarowski

I. II. III. IV. V. VI. VII.

VIII. IX. X.

Introduction Selected Factors to Be Considered During Development Types of Organizational Structures Responsible for Pilot Operations Educational Backgrounds of Pilot Plant Personnel Pilot Plant Design for Tablet Development Paper Flow Between Research. Quality Control, and Production Use of the Pilot Plant Scale-Up to Select the Optimal Procedure for the Preparation of Dexamethasone Tablets Problem Caused by a Change in Excipient Supplier Friability Related to Particle Size Distribution Effect of Disintegrant Viscosity on Disintegration Rate

303 304 305 310 311 315

320 344 345 346

Contents

XI.

Influence of Ingredient Moisture Content on Friability XII. Drug and Dye Migration in Wet Granulation XIII. Effect of Aged Simple Syrup on Smoothing and Rounding Steps in the Sugar Coating of Tablets XIV. Effect of Film-Former Viscosity on Disintegration Rate XV. Tablet Binding XVI. Picking and Sticking XVII. Selected Tablet Problems; Suggested Solutions XVJII. Selected Process Development Projects of Current Interest XIX. Additional Pilot Plant Responsibilities References Chapter 6

Tablet Production

347 347 350 351 352 352 353 354 355 365 369

Robert J. Connolly, Frank A. Berstler , and David Cofnn-Beach I. II. III.

IV.

V. VI. VII. VIII. IX.

Introduction Four Basic Requirements for Successful Tablet Production Overview of the Process Design of the Product Design of the Facility Equipment Selection Personnel Role of Manufacturing Industry Outlook Appendix: List of Suppliers Suggested Readings References

Chapter 7. The Essentials of Process Validation

369 369 370 390 392 403 410 411

413 414 415 415 417

Robert A. Nash I. II.

III. IV.

V. VI. VII. VIII. IX. X.

XI. XII. XIII.

Introduction Total Approach to Pharmaceutical Process Validation Organizing for Validation Process Validation -Order of Priority Pilot - Scale- Up and Process Validation Process Capability Design and Testing Cause-and-Effect or "Fishbone" Diagram Constraint Analysis Qualification Trial Options Process Validation Prospective Process Validation Strategy for Process Validation Concurrent Validation

417 418 421 423 423 426 431 431 433 442

443 444 445

Contents

XIV. XV. XVI.

Chapter 8

Retrospective Validation Control Charting Conclusions Glossary of Terms References

Stability Kinetics

447 448 450 451 453 457

Samir A. Hanna

Introduction Current Good Manufacturing Practices Requirements III. Compendia! Requirements IV. U • S. Food and Drug Administration Requirements V. Reaction Kinetics in Solid-Dosage Forms VI. Kinetic Studies VII. Solid-Drug Degradation VIII. Solid -Solid Degradation IX. Solid-Dosage Form Degradation X. Mechanisms that Affect Tablet Stability XI. Container-Closure System XII. Expiration Dating References

457 457 458 458 464 477 477 478 478 482 485 495

Quality Assurance

497

I. II.

Chapter 9

457

Samir A. Hanna I. II.

III. IV.

V. VI. VII. VIII. IX.

X. XI. XII. XIII.

Index

Introduction Quality Assurance System Good Manufacturing Practices Requirements Compendia! Requirements Raw Materials Active or Therapeutic Materials Inactive or Inert Materials Container In -Process Quality Assurance Quality Assurance Before Start Checking After Start Checking Qualification/Validation Finished Product

497 497 499 499 507 511 515 518 522 522 537 548 548

555

Contributors

Neil R. Anderson Department Head. Pharmacy Research Department. Merrell Dow Pharmaceuticals. Inc .• Indianapolis, Indiana Gilbert S. Banker Dean, College of Pharmacy, University of Minnesota Health Sciences Center. Minneapolis, Minnesota Frank A. Berstler Manager, Technical Service, Superpharm Corporation, Central Islip, New York Charles H. Bruno Director, Pharmaceutical Technical Services, Colorcon, West Point, Pennsylvania Rong-Kun Chang Principle Scientist, Formulation Development. Schering Research, Miami, Florida David Coffin-Beach Manager, Process Development, Schering-Plough, Inc., Kenilworth, New Jersey Robert J. Connolly Vice President, Manufacturing, 8uperpharm Corporation, Central Islip, New York Samir A. Hanna Vice President, Quality Assurance, Industrial Division, Bristol-Myers Squibb Company, Syracuse. New York Charles I. Jarowski Professor, Department of Pharmacy, St. John's University, Jamaica, New York Robert A. Nash Associate Professor. College of Pharmacy and Allied Health Professions, 8t. JOhn's University, Jamaica, New York xi

xii

Contributors

Garnet E. Peck Professor, Department of Industrial and Physical Pharmacy, Purdue University, West Lafayette, Indiana Stua rt C. Porter Vice President, Scientific Services, Colorcon, West Point, Pennsylvania Joseph R. Robinson Professor of Pharmacy, Madison Center for Health Sciences, University of Wisconsin-Madison, Madison, Wisconsin Professor and Dean Emeritus, College of Pharmacy, Da leE. Wu rster University of Iowa, Iowa City, Iowa

Contents of Pharmaceutical Dosage Forms: Tablets, Second Edition, Revised and Expanded, Volumes 1 and 2 edited by Herbert A. Lieberman, Leon Lachman, and Joseph B. Schwartz

VOLUME 1

1.

Preformulation Testing, Deodatt A. Wadke, Abu T. M. Serajuddin, and Harold Jacobson

2.

Tablet Formulation and Design. Garnet E. Peck, George J. Bailey, Vincent E. McCurdy, and Gilbert S. Banker

3.

Compressed Tablets by Wet Granulation, Fred J. Bandelin

4.

Compressed Tablets by Direct Compression, Ralph F. Shangraw

5.

Compression-Coated and Layer Tablets, William C. Gunsel and Robert G. Dusel

6.

Effervescent Tablets, Raymond Mohrle

7.

Special Tablets, James W. Conine and Michael J. Pikal

8.

Chewable Tablets, Robert W. Mendes, Aloysius O. Anaebonam, and Johan B. Daruwala

9.

Medicated Lozenges, David Peters

xiii

Contents

xiv

of

Other Volumes

VOLUME 2

1.

Mixing,

Russell J. Lantz, Jr., and Joseph B. Schwartz

2.

Drying,

Kurt G. Van Scoik, Michael Zoglio, and Jens T. Carstensen

3.

Size Reduction.

4.

Compression.

5.

Granulation Technology and Tablet Characterization, Roger E. Gordon, Thomas W. Rosanaske, Dale E. Fonner. Neil R. Anderson. and Gilbert S. Banker

6.

Russell J. Lantz. Jr. Eugene L. Parrott

Bioavailability in Tablet Technology.

Solomon A. Stavchansky and

James W. McGinity

7.

Pharmaceutical Tablet Compression Tooling, Glen C. Ebey

George F. Loeffler and

Contents of Pharmaceutical Dosage Forms: Parenteral Medications, Volumes 1 and 2 edited by Kenneth E. Avis, Leon lachman, and Herbert A. Lieberman

VOLUME 1.

The Dosage Form and Its Historical Development, Kenneth E. Avis and Beth G. Morris

2.

Parenteral Drug Administration: Routes, Precautions, Problems, and Complications, Richard J. Duma and Michael J. Akers

:3.

Biopharmaceutics of Injectable Medication, Sol Motola

4.

Preformulation of Parenteral Medications, Sol Motola and Shreeram A gharkar

5.

Formulation of Small Volume Parenterals , Patrick P. DeLuca and James C. Boylan

6.

The Processing of Small Volume Parenterals and Related Sterile Products, Joel Benton Portnoff. Richard J. Harwood, and Edward William Sunbery

7.

Manufacturing of Large Volume Parenterals, Nicholas J. KarUnos and Michale J. Groves

8.

Records and Reports. David C. Fry

9.

Environmental Factors in the Design of a Parenteral Production Facility, A. Michael Keller

10.

Personnel:

The Key Factor in Clean Room Operations, Cecelia J. Luna

xv...