PHARMACEUTICAL DOSAGE FORMS Tablets SECOND EDITION, REVISED AND EXPANDED In Three Volumes VOLUME 1 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 MARCEL DEKKER, INC. New York and Basel
Contents Preface Contributors Pharmaceutical Dosage Forms: Tablets, Second Edition Volumes 2 and 3 Pharmaceutical Dosage Forms: Parenteral Medications, Volumes 1 and 2 Pharmaceutical Dosage Forms: Disperse Systems, Volumes 1 and 2 iii xi xiii xv XXX Chapter 1. Chapter 2. Preformulation Testing Deodat; t A. Wadke, Abu T. M. Serajuddin, and Harold Jacobson II. Organoleptic Properties III. Purity IV. Particle Size, Shape, and Surface Area V. Solubility VI. Dissolution VII. Parameters Affecting Absorption VIII. Crystal Properties and Polymorphism IX. Stability X. Miscellaneous Properties XI. Examples of Preformulation Studies Tablet Formulation and Design Garnet E. Peck, George J. Baley, Vincent E. McCurdy, and Gilbert S. Banker II. Preformulation Studies III. A Systematic and Modern Approach to Tablet Product Design IV. Tablet Components and Additives V. Recrulatorv Reauirements for Excipients in the United States VI. 1 1 2 3 5 12 18 24 34 42 53 57 69 75 75 77 79 88 121 128 vu
Vlll Chapter 3. Compressed Tablets by Wet Granulation Fred J. Bandelin I. Properties of Tablets II. Formulation of Tablets III. Tablet Manufacture IV. Granulation V. Excipients and Formulation VI. Multilayer Tablets VII. Prolonged Release Tablets VIII. Manufacturing Problems Contents 131 132 133 135 148 151 179 181 188 190 Chapter 4. Compressed Tablets by Direct Compression 195 Ralph F. Shangraw and History 195 II. Advantages and Disadvantages of the Wet Granulation Process 197 III. The Direct-Compression Process 198 IV. Direct-Compression Filler Binders 203 V. Factors in Formulation Development 214 VI. Morphology of Direct-Compression Fillers 220 VII. Coprocessed Active Ingredients 225 VIII. Modification and Integration of Direct- Compression and Granulation Processes 227 IX. Future of Direct-Compression Tableting 228 X. Formulations for Direct Compression 229 Glossary of Trade Names and Manufacturers 243 245 Chapter 5. Compression-Coated and Layer Tablets William C. Gunsel and Robert G. Dusel I. Compression Coating II. Formulations (Compression Coating) III. Inlay Tablets IV. Layer Tablets V. Formulations (Layer) 247 247 260 273 274 278 284 Chapter 6. Effervescent Tablets Raymond Mohrle II. Raw Materials III. Processing IV. Manufacturing Operations V. Tablet Evaluation 285 285 286 294 300 302
Contents ix VI. Effervescent Stability 304 VII. Effervescent Formulations 320 VIII. 326 Chapter 7. Special Tablets 329 James W. Conine and Michael J. Pikal I. Drug Absorption Through the Oral Mucosa 329 II. Molded Sublingual Tablets 334 III. Special Problems with Molded Nitroglycerin Tablets 340 IV. Compressed Sublingual Tablets 354 V. Buccal Tablets 356 VI. Vaginal Tablets 359 VII. Rectal Tablets 360 VIII. Dispensing Tablets 362 IX, Tablets for Miscellaneous Uses 363 364 Chapter 8. Chewable Tablets 367 Robert W. Mendes, Aloysius O. Anaebonam, and Jahan B. Darwwala 367 II. Formulation Factors 368 III. Formulation Techniques 371 IV. Excipients 382 V. Flavoring 387 VI. Colorants 392 VII. Manufacturing 396 VIII. Evaluation of Chewable Tablets 406 IX. Summary 415 415 Chapter 9. Medicated Lozenges 419 David Peters I. Hard Candy Lozenges 419 II. Processing 445 III. Formulations (Hard Candy Lozenges) 497 IV. Center-Filled Hard Candy Lozenges 501 V. Formulations (Center Filled Lozenges) 509 VI. Packaging 511 VII. Chewy or Caramel Base Medicated Tablets 520 VIII. Formulations (Chewy Based Confections) 541 IX. Compressed Tablet Lozenges 543 X. Manufacturing: Compression Sequence 558 XI. Typical Formulations (Compressed-Tablet Lozenges) 565
x Contents XII. Quality Control Procedures 567 576 Suggested Reading 580 Index 583