Suppositories.eps

This is an essential resource for all those involved in the formulation, development, manufacture and testing of suppositories.The administration of drugs using a suppository base formulation is particularly useful in paediatrics, debilitated patients and 'non-oral' patients. Depending on the excipient used, it is possible to control the release of the active pharmaceutical ingredient, thus offering some advantages in specific drug regimens over other dosage forms.Many suppository formulations have been developed for a number of therapeutic aims, however comprehensive reliable information on suppository formulation is not always readily available. "Suppositories" resolves this situation by providing up-to-date, comprehensive information in one point of reference." Suppositories" provides a detailed review of suppository dosage forms with chapters covering: the history and development of the suppository; suppository bases and their characteristics; pharmaceutical, biopharmaceutical and pharmacokinetic factors; formulation considerations; manufacturing and compounding suppositories; special types of suppositories; quality control; packaging and labelling; stability and storage; and clinical considerations.This book is an essential resource for all those involved in the formulation, development, manufacture and testing of suppositories. Cover 1 Prelims 2 Contents 6 Preface 10 About the author 11 Chapter 1 - Introduction to suppositories 12 What is a suppository? 13 Uses and applications 14 Advantages of suppositories 15 Disadvantages of suppositories 15 Background 16 Synonyms/definitions/descriptions 17 Extemporaneous compounding 22 References 22 Chapter 2 - History and development of the suppository 24 Definitions: Suppository, pessary, bougie 24 Early history 24 Modern period 26 Suppository molds 27 Official status 30 Commercial manufacturing 30 Summary 35 References 35 Chapter 3 - Suppository bases and their characteristics 38 Classification of suppository bases 38 Development of suppository bases 57 References 59 Chapter 4 - Pharmaceutic, biopharmaceutic, and pharmacokinetic factors involving suppositories 62 Anatomical and physiological considerations 62 Bioavailability of rectal suppositories 65 Physicochemical factors 65 Bioequivalence 68 Contemporary studies on the bioavailability of suppositories 69 Miscellaneous 80 References 80 Chapter 5 - Formulation considerations 88 Drug selection 89 Base selection 89 Formulation variables 91 Formulation studies of suppositories in the literature 92 Absorption enhancers 97 References 104 Chapter 6 - Manufacturing suppositories 110 Melt–fusion method 110 Cold compression method 113 General controls relative to manufacturing all suppositories 113 Chapter 7 - Compounding suppositories 116 Physicochemical considerations 116 Bases 118 Preparation 119 Preparation by compression 127 Special problems 128 Summary 130 References 130 Chapter 8 - Special types of suppositories 132 Non-rectal suppositories – vaginal suppositories 132 Non-rectal suppositories – urethral suppositories 134 Controlled-release suppositories 134 Coated microsphere/microcapsule suppositories 134 Emulsion and emulsion–gel suppositories 135 Hollow-type suppositories 135 Hydrogel suppositories 137 Layered double or triple suppositories 138 Matrix–agar suppositories 139 Matrix–wax suppositories 139 Mucoadhesive suppositories 139 Nanoparticle suppositories 140 Osmotic suppositories 140 Prolonged-release suppositories 140 Sectile or bisected suppositories 140 Reversed micellar solution suppositories 141 Sustained-release suppositories 141 Thermo-reversible-liquid suppositories 143 Xerogel suppositories 144 Miscellaneous suppositories and bases 144 References 145 Chapter 9 - Quality control of suppositories 150 Physical analysis 150 Chemical testing 158 Content uniformity testing 163 Conductivity 164 Chemical testing procedures 164 Aging and aging tests 167 References 167 Chapter 10 - Packaging and labeling of suppositories 170 Packaging 170 Labeling 175 References 176 Chapter 11 - Stability and storage of suppositories 178 Physical stability 178 Chemical stability 179 Factors affecting stability 179 Microbiological stability 180 Stability studies for suppositories 180 Beyond-use dating for compounded suppositories 181 Expiry dating for manufactured suppositories 181 Storage of suppositories 181 Holding and distribution 182 Transportation 182 Responsibility of pharmacists 182 Drug-specific stability studies 184 References 186 Chapter 12 - Clinical considerations 188 Clinical response factors 188 Patient counseling 188 General toxicity 189 Local toxicity 190 Adverse reactions to suppositories 190 Contemporary studies of clinical effectiveness 191 References 209 Appendix I - Glossary 224 Appendix II - Compounding formulas 226 ABHR suppository (Ativan–Benadryl–Haldol–Reglan suppository) 226 Acetaminophen 650mg suppository 226 5-Aminosalicylic acid 500mg compound suppository 226 Amitriptyline hydrochloride suppository 226 Ampicillin 250mg suppository 227 Antiemetic suppository 227 Antiemetic–antispasmodic suppository 227 Antinauseant suppositories #1 227 Antinauseant suppositories #2 227 Antinauseant suppositories, pediatric 228 Belladonna and opium suppository (modified) 228 Bismuth subgallate suppository 228 Boric acid 600mg vaginal suppository 228 Carbamazepine suppository 228 Chloral hydrate 500mg suppository 228 Chloroquine 300mg suppository 229 Clindamycin phosphate 150mg vaginal suppository 229 Clotrimazole 250mg suppository 229 Diazepam 10mg suppository 229 Dihydroergotamine 2mg suppository 229 Droperidol 1.25mg suppository 229 Ergotamine tartrate-PB suppositories 230 Etodolac 200mg suppository 230 Glycerin suppositories 230 Hydrocortisone acetate 25mg suppository 230 Hydrocortisone 100mg mucoadhesive suppository 230 Indometacin 50mg suppository 230 Lorazepam 1mg suppository 231 Metoclopramide hydrochloride 10mg suppository 231 Metronidazole 500mg vaginal suppository 231 Miconazole nitrate 100mg vaginal suppository 231 Migraine headache suppository 231 Misoprostol 1mg suppository 231 Morphine sulfate 10–100mg suppository 232 Morphine sulfate 25mg or 50mg slow-release suppository 232 Nifedipine, lidocaine, and nitroglycerin suppositories 232 Nitrofurantoin urethral inserts 232 Nitrofurazone urethral inserts 232 Ondansetron hydrochloride 8mg suppository 232 Phenytoin (dilantin) 200mg suppository 233 Polyethylene glycol suppository bases 233 Prochlorperazine maleate 25mg suppository 233 Progesterone 25–400mg suppository 233 Promethazine hydrochloride 25mg suppository 233 Tetracycline 250mg suppository 233 Trimethobenzamide 100mg suppository 234 Verapamil hydrochloride 40mg suppository 234 Appendix III - Manufacturing formulas 236 Acetaminophen 125mg suppository 236 Acetaminophen 250mg suppository 236 Acetaminophen 500mg suppository 236 Acetylsalicylic acid suppository 236 Antihemorrhoidal suppositories 237 Betamethasone and cinchocaine suppository 237 Bisacodyl 10mg suppository 237 Clotrimazole and clindamycin vaginal suppository (glycerinated gelatin base) 237 Clotrimazole and clindamycin vaginal suppository (Macrogol base) 237 Diclofenac sodium suppository 237 Ephedrine sulfate and zinc oxide suppository 238 Glycerin suppository 238 Indometacin 50mg suppository 238 Laxative suppository 238 Lidocaine and tribenoside suppository 238 Mesalamine 500mg suppository 239 Metoclopramide suppository 239 Miconazole nitrate suppository 239 Povidone-iodine vaginal ovule 239 Pramoxine suppository 239 Pramoxine suppository (alternate) 240 Vitamin A 150000 IU suppository 240 Zinc oxide suppository 240 Appendix IV - Calculations involving suppositories 242 Density (dose replacement) calculations for suppositories 242 Dosage replacement factor method 242 Density factor method 242 Occupied volume method 244 Displacement value method 244 Index 246 "This reference book is an essential resource for all those involved in the formulation, development, manufacture and testing of suppositories. Many suppository formulations have been developed for a number of therapeutic aims. However, comprehensive reliable information on suppository formulation is not always readily available. Suppositories resolves this situation by providing up-to-date, comprehensive information in one point of reference. Suppositories provides a detailed review of suppository dosage forms with chapters covering: the history and development of the suppository; suppository bases and their characteristics; pharmaceutical, biopharmaceutical and pharmacokinetic factors; formulation considerations; manufacturing and compounding suppositories; special types of suppositories; quality control; packaging and labelling; stability and storage; and clinical considerations."--Publisher's website This reference book is an essential resource for all those involved in the formulation, development, manufacture and testing of suppositories. The book provides a detailed review of suppository dosage forms with chapters covering: the history and development of the suppository; the history and development of the suppository; pharmaceutical, biopharmaceutical and pharmacokinetic factors; formulation considerations; manufacturing and compounding suppositories; special types of suppositories; quality control; packaging and labelling; stability and storage; and clinical considerations. Offering information on suppository formulation, this book provides a review of suppository dosage forms. It contains chapters which cover: the history and development of the suppository; suppository bases and their characteristics; pharmaceutical, biopharmaceutical and pharmacokinetic factors; and special types of suppositories.