Pharmaceutical Dosage Forms Capsules
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Pharmaceutical Dosage Forms Capsules Edited by Larry L. Augsburger Stephen W. Hoag 9781841849768_C000.indd 3 6/15/2017 3:04:58 PM CRC Press Taylor & Francis Group 6000 Broken Sound Parkway NW, Suite 300 Boca Raton, FL 33487-2742 © 2017 by Taylor & Francis Group, LLC CRC Press is an imprint of Taylor & Francis Group, an Informa business No claim to original U.S. Government works Printed on acid-free paper International Standard Book Number-13: 978-1-84184-976-8 (Hardback) This book contains information obtained from authentic and highly regarded sources. Reasonable efforts have been made to publish reliable data and information, but the author and publisher cannot assume responsibility for the validity of all materi- als or the consequences of their use. The authors and publishers have attempted to trace the copyright holders of all material reproduced in this publication and apologize to copyright holders if permission to publish in this form has not been obtained. If any copyright material has not been acknowledged please write and let us know so we may rectify in any future reprint. Except as permitted under U.S. Copyright Law, no part of this book may be reprinted, reproduced, transmitted, or utilized in any form by any electronic, mechanical, or other means, now known or hereafter invented, including photocopying, micro- filming, and recording, or in any information storage or retrieval system, without written permission from the publishers. For permission to photocopy or use material electronically from this work, please access www.copyright.com (http://www .copyright.com/) or contact the Copyright Clearance Center, Inc. (CCC), 222 Rosewood Drive, Danvers, MA 01923, 978-750- 8400. CCC is a not-for-profit organization that provides licenses and registration for a variety of users. For organizations that have been granted a photocopy license by the CCC, a separate system of payment has been arranged. Trademark Notice: Product or corporate names may be trademarks or registered trademarks, and are used only for identifi- cation and explanation without intent to infringe. Visit the Taylor & Francis Web site at http://www.taylorandfrancis.com and the CRC Press Web site at http://www.crcpress.com 9781841849768_C000.indd 4 6/15/2017 3:04:58 PM Contents Preface...............................................................................................................................................ix Editors ...............................................................................................................................................xi Contributors ................................................................................................................................... xiii Chapter 1 Advances in Capsule Formulation Development and Technology ...............................1 Larry L. Augsburger and Stephen W. Hoag Chapter 2 An Introduction to Two-Piece Hard Capsules and Their Marketing Benefits ...........15 Dennis Murachanian Chapter 3 Hard Shell Capsules in Clinical Trials ....................................................................... 31 Moji Christianah Adeyeye and Amusa Adebayo Chapter 4 Capsule Shell Manufacture ........................................................................................ 75 Brian E. Jones, Fridrun Podczeck, and Paul Lukas Chapter 5 Non–Gelatin-Based Capsules .................................................................................. 111 Sven Stegemann Chapter 6 Hard Shell Capsule Filling Machines ...................................................................... 131 Donald K. Lightfoot Chapter 7 Instrumented Automatic Capsule Filling Machines and Filling Machine Simulation ................................................................................................................ 191 Larry L. Augsburger and Vikas Moolchandani Chapter 8 Dry-Fill Formulation and Filling Technology ......................................................... 211 Pavan Heda, Vikas Agarwal, and Shailesh K. Singh Chapter 9 Plug Formation .........................................................................................................237 Fridrun Podczeck Chapter 10 Modeling Powder Filling during Encapsulation ......................................................283 Ammar Khawam, PhD Chapter 11 Scale-Up and Transfer of Hard Shell Formulations across Machine Types ............307 Larry L. Augsburger and Michael Levin vii 9781841849768_C000toc.indd 7 6/15/2017 6:37:45 PM viii Contents Chapter 12 Modified-Release Delivery Systems: Extended-Release Capsule Platform............. 317 Reza Fassihi, PhD, AAPS Fellow Chapter 13 Analytical Testing and Evaluation of Capsules ........................................................345 Stuart L. Cantor and Asish K. Dutta Chapter 14 Rheological Aspects of Capsule Shell Excipients and the Manufacture of Encapsulated Formulations .................................................................................. 373 Lawrence H. Block Chapter 15 Quality-by-Design (QbD) for Capsule Formulation and Process Development: Regulatory Science Relevance, Scientific Case Studies, and Future Challenges .... 393 Huiquan Wu, Lin Xie, Stephen W. Hoag, Larry L. Augsburger, and Mansoor Khan Index .............................................................................................................................................. 415 9781841849768_C000toc.indd 8 6/15/2017 6:37:45 PM Modified-Release 12 Delivery Systems Extended-Release Capsule Platform Reza Fassihi, PhD, AAPS Fellow CONTENTS Introduction .................................................................................................................................... 317 Capsules as a Carrier Platform for Oral Extended-Release Drug Delivery ................................... 319 Modified-Release Dosage Forms ..............................................................................................320 Terminology and Definition of Modified-Release Dosage Forms ................................................. 323 Dissolution Rate of Drug from Drug Particles, Pellets, or from Various Modified-Release Formulations and Delivery Systems Encapsulated in a Capsule Shell as a Delivery Carrier ........326 Operating Release Mechanisms Associated with Different Encapsulated Modified-Release Dosage Forms ................................................................................................................................ 327 Mathematical Models to Describe Release Kinetics from Extended-Release Capsules Containing Formulated Delivery Systems .....................................................................................328 Types of Blood Levels for Different Therapeutic Effects .............................................................. 332 Examples of Commercially Available Hard Shell Extended-Release Capsule Delivery Systems .....332 Encapsulated Matrix Tablets for Extended Drug Release ......................................................... 332 Encapsulated Coated and Uncoated Pellets for Extended Drug Release .................................. 335 Encapsulated Enteric-Coated Pellets and Enteric-Coated Mini-tablets for Delayed Release and/or Delayed Extended Release ............................................................................... 336 Encapsulated Beads of a Polypeptide Linaclotide for Once-a-Day Oral Administration ......... 338 Encapsulated Drug Formulation for Time-Delayed and Targeted Delivery during Drug Development Phases and Research to Assess Drug Absorption .................................................... 338 Port System ............................................................................................................................... 339 Egalet ......................................................................................................................................... 339 Electronic Capsule Devices for Site-Specific Determination of the Drug Absorption ............. 339 IntelliCap Device.......................................................................................................................340 Endoscopy Camera Capsules .........................................................................................................342 Summary ........................................................................................................................................342 References ...................................................................................................................................... 343 INTRODUCTION Pharmaceutical drug delivery embraces a range of delivery carriers and constructs that have dimen- sions ranging from several nanometers (nanotechnology) to numerous millimeters (conventional dosage forms, i.e., pellets, tablets, and capsules). Such delivery systems spawn a whole array of assemblies for delivery of highly potent active drugs through different routes of administrations to numerous sites and targets in the human or animal body to treat disease conditions. Such delivery types and carrier systems, with their relative sizes together with some molecules and bacterial cells, are shown in Figure 12.1. 317 9781841849768_C012.indd 317 6/15/2017 9:24:45 PM 318 Pharmaceutical Dosage Forms Water GlucoseAntibodyVirus Bacteria Cancer cellsPellets, capsules, tablets 10−1 110102 103 104 105 NanometerMicrometer Dendrimers Solid nanopartickes Nanosuspensions stealth liposomes (SL) Paclitaxel Imaging and biosensors Suspensions Quantum dots Albumin-bound Emulsions