Drug formulation:
Gespeichert in:
1. Verfasser: | |
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Format: | Buch |
Sprache: | English Hungarian |
Veröffentlicht: |
Chichester u.a.
Wiley
1989
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Schlagworte: | |
Online-Zugang: | Inhaltsverzeichnis |
Beschreibung: | IX, 416 S. graph. Darst. |
ISBN: | 0471905178 |
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adam_text | O DRUG FORMULATION BY I. RACZ, C. SC. (CHEM.) PROFESSOR OF
PHARMACEUTICAL TECHNOLOGY AND PHARMACOKINETICS SEMMELWEIS UNIVERSITY
MEDICAL SCHOOL BUDAPEST, HUNGARY JOHN WILEY AND SONS, CHICHESTER * NEW
YORK * BRISBANE * TORONTO * SINGAPORE 1989 CONTENTS PREFACE . . V
CHAPTER 1 PRINCIPLES OF PRE-FORMULATION AND FORMULATION TESTING OF
PHARMACEUTICAL PRODUCTS . 1 PRE-FORMULATION STUDIES 2 CONVENTIONAL
PHARMACEUTICAL PREPARATIONS 4 .1. HOMOGENEOUS LIQUID-PHASE
PHARMACEUTICAL PREPARATIONS 4 .2. HETEROGENEOUS SOLID-PHASE
PHARMACEUTICAL PRODUCTS 6 .3. HETEROGENEOUS FLUID- AND SEMI-SOLID-PHASE
PHARMACEUTICAL PRODUCTS 9 1.1.1.4. OTHER PHARMACEUTICAL PRODUCTS 10
1.1.2. NON-CONVENTIONAL LONG-ACTING PHARMACEUTICAL PRODUCTS 11 1.2. DRUG
FORMULATION 13 1.3. MATHEMATICAL DESIGN OF PRE-FORMULATION AND
FORMULATION EXPERIMENTS 13 1.3.1. ESTABLISHING THE LEVEL OF SIGNIFICANCE
13 1.3.2. DETERMINING THE NUMBER OF EXPERIMENTS 14 1.3.3. RANDOMIZED
EXPERIMENTAL GROUPS AND LATIN SQUARES 15 1.3.4. FACTORIAL DESIGN OF
EXPERIMENTS 15 1.4. THE ROLE OF SCALE-UP IN DRUG FORMULATION 25 1.5.
CONCLUSIONS 27 LITERATURE . 27 CHAPTER 2 DRUG STABILITY 2 8 2.1.
IMPORTANT CONCEPTS IN DRUG STABILITY 28 2.2. FACTORS INFLUENCING DRUG
STABILITY 31 2.2.1. PHYSICAL AND COLLOIDAL-PHYSICAL CHANGES 32 2.2.2.
CHEMICAL CHANGES . 33 2.2.3. MICROBIOLOGICAL CHANGES 34 2.3.
STABILITY-INDICATING ASSAY METHODS 35 2.4. INTERPRETATION OF THE
CHEMICAL DECOMPOSITION OF DRUGS IN HOMOGENEOUS LIQUID PHASES USING
REACTION KINETICS 47 2.4.1. ORDERS OF THE DECOMPOSITION REACTIONS 47
2.4.1.1. MOLECULARITY AND ORDER OF THE REACTION 47 2.4.1.2. ZERO ORDER
REACTIONS 48 2.4.1.3. FIRST ORDER REACTIONS 50 2.4.1.4. HIGHER REACTION
ORDERS AND FRACTIONAL REACTION ORDERS 53 VII 2.4.1.5. DETERMINATION OF
THE REACTION ORDER AND CALCULATION OF THE RATE CONSTANTS 57 2.4.2.
COMPLEX REACTIONS 61 2.4.2.1. CONSECUTIVE REACTIONS 61 2.4.2.2.
SIMULTANEOUS REACTIONS 65 2.5. CORRELATION BETWEEN CHEMICAL STRUCTURE
AND DRUG STABILITY 69 2.5.1. REACTION KINETICS 69 2.5.1.1. HAMMETT S
EQUATION 70 2.5.1.2. TAFT S EQUATION 72 2.5.2. ASPECTS TO BE CONSIDERED
IN THE FORMULATION OF DRUGS 72 2.6. KINETICS OF THE DECOMPOSITION OF
SOLID PHARMACEUTICAL PREPARATIONS 77 2.7. CHANGES IN THE REACTION RATE
WITH TEMPERATURE. DETERMINATION OF THE EXPIRATION DATE - 95 2.7.1.
ISOTHERMAL PROCESSES 95 2.7.1.1. KINETIC DETERMINATION OF THE PREDICTED
EXPIRATION DATE 98 2.7.2. NON-ISOTHERMAL PROCESS 104 2.7.3. CLIMATIC
ZONES 108 2.8. THE INFLUENCE OF LIGHT ON THE RATE OF DECOMPOSITION
REACTIONS 108 2.9. DECOMPOSITION MECHANISMS OF DRUGS 117 2.9.1. REDOX
DECOMPOSITION PROCESSES 118 2.9.1.1. STABILIZATION POSSIBILITIES 118
2.9.1.2. EXAMPLES OF DRUG FORMULATION 121 2.9.2. SOLVOLYTIC
DECOMPOSITION PROCESSES 128 2.9.2.1. STABILIZATION METHODS 128
2.9.2.1.1. ROLE OF THE HYDROGEN ION CONCENTRATION 128 2.9.2.1.2. THE
ROLE OF IONIC STRENGTH . 132 2.9.2.1.3. THE ROLE OF THE SOLVENT . 134
2.9.2.2. EXAMPLES OF DRUG FORMULATION 135 2.9.3. OTHER DRUG DEGRADATION
PROCESSES 155 2.9.3.1. EXAMPLES OF OTHER DRUG FORMULATION AND
STABILIZATION PROBLEMS 156 2.9.4. BIOCHEMICAL PATHWAYS OF DRUG
DECOMPOSITION 166 2.10. CONCLUSIONS 168 LITERATURE 169 CHAPTER 3
PHYSICOCHEMICAL INTERACTIONS ENCOUNTERED IN THE COURSE OF DRUG PRODUCT
PRE- PARATION 176 3.1. GENERAL ASPECTS, BASIC PRINCIPLES AND DEFINITIONS
176 3.2. DRUG-DRUG INTERACTIONS 183 3.3. DRUG-ADDITIVE AND
ADDITIVE-ADDITIVE INTERACTIONS 212 3.3.1. INTERACTIONS OF ANION-ACTIVE
(NEGATIVELY CHARGED) ADDITIVES 213 3.3.2. INTERACTIONS OF CATION-ACTIVE
ADDITIVES 219 3.3.3. INTERACTIONS OF AMPHOTERIC ADDITIVES 219 3.3.4.
INTERACTIONS OF NON-IONIC ADDITIVES 220 3.3.4.1. POLYVINYL PYRRBLIDONE
220 3.3.4.2. CELLULOSE DERIVATIVES 226 3.3.4.2.1. METHYLCELLULOSE 226
3.3.4.2.2. METHYLHYDROXYETHYL CELLULOSE 227 3.3.4.2.3. HYDROXYETHYL AND
HYDROXYPROPYL CELLULOSE 228 3.3.4.3. POLYETHYLENE AND POLYPROPYLENE
GLYCOLS AND THEIR DERIVATIVES 228 3.3.4.4. POLYVINYL ALCOHOL 239 VIII
3.3.4.5. STARCHES 240 3.3.4.6. CYCLODEXTRINES 241 3.4. CONCLUSIONS 242
LITERATURE - 243 CHAPTER 4 BIOPHARMACEUTICAL ASPECTS OF DESIGNING AND
EVALUATING DRUG PRODUCTS 251 4.1. FUNDAMENTAL DEFINITIONS 251 4.2.
APPLIED PHARMACOKINETIC PROCEDURES 253 4.2.1. FUNDAMENTALS 253 4.2.2.
THE KINETICS OF ABSORPTION AND ELIMINATION 258 4.2.2.1. THE BIOLOGICAL
HALF-LIFE 258 4.2.2.1.1. THE INFLUENCE OF AGING OF THE ORGANISM ON THE
BIOLOGICAL HALF-LIFE 278 4.2.2.1.2. THE BIOLOGICAL HALF-LIFE IN
MULTICOMPARTMENT SYSTEMS 284 4.2.3. THE DOSAGE REGIMEN 287 4.2.4.
COMPUTERIZED PROCESSING OF PHARMACOKINETIC DATA 292 4.3. BIOAVAILABILITY
OF DRUG PRODUCTS 293 4.3.1. TEST METHODS 295 4.3.2. LIMITATIONS OF THE
VARIOUS TEST METHODS 296 4.4. FACTORS WHICH INFLUENCE ABSORPTION 299
4.4.1. PHYSIOLOGICAL FACTORS AND TRANSPORT PROCESSES 299 4.4.2. MODES OF
ADMINISTRATION AND DOSAGE REGIMEN 305 4.4.2.1. PARENTERAL ADMINISTRATION
306 4.4.2.2. PULMONARY ABSORPTION 307 4.4.2.3. RECTAL ABSORPTION 308
4.4.2.4. PERCUTANEOUS ABSORPTION 309 4.4.2.5. GASTROINTESTINAL
ABSORPTION 316 4.4.3. DISTRIBUTION OF THE ACTIVE INGREDIENT 321 4.4.4.
PHYSICOCHEMICAL FACTORS OF DRUG FORMULATION 323 4.4.4.1. SOLUBILITY AND
PARTICLE DIAMETER 323 4.4.4.2. DISSOLUTION RATE 327 4.4.4.3. IN VITRO
ABSORPTION RATE 342 4.4.4.4. ADJUVANTS AND EXCIPIENTS USED IN DRUG
COMPOUNDING 345 4.4.4.5. COMPLEXATION 351 4.5. ORAL DOSAGE FORMS 352
4.5.1. POSSIBLE METHODS FOR DEVELOPMENT OF PROLONGED DRUG ACTION 353
4.5.1.1. CHEMICAL PROCEDURES 354 4.5.1.2. PHYSIOLOGICAL METHODS 359
4.5.1.3. PHARMACEUTICAL TECHNOLOGY PROCEDURES 360 4.5.2. PHARMACOKINETIC
PRINCIPLES IN THE DESIGN OF ORAL CONTROLLED RELEASE DRUG PREPARATIONS
376 4.5.2.1. DESIGN OF DOSAGE FORMS WITH ZERO ORDER DISSOLUTION RATE 377
4.5.2.2. DESIGN OF DOSAGE FORMS WITH A FIRST ORDER DISSOLUTION RATE 381
4.5.3. THE BIOAVAILABILITY AND BIOEQUIVALENCE OF ACTIVE INGREDIENTS IN
ORAL SUSTAINED RELEASE DRUG PRODUCTS 386 4.5.3.1. BLOOD LEVEL
CONCENTRATION DATA 386 4.5.3.2. THE APPLIED STANDARD 387 4.5.3.2.1.
COMMERCIAL SUSTAINED RELEASE PREPARATIONS AS STANDARDS 387 4.5.3.2.2.
NON-SUSTAINED RELEASE ACTIVE INGREDIENTS AS STANDARDS 387 4.5.3.3.
BIOAVAILABILITY AND BIOEQUIVALENCE 388 4.5.3.3.1. INDEXES OF
BIOEQUIVALENCE 388 IX 4.5.3.3.2. INTERPRETATION OF BIOAVAILABILITY IN
THE CASE OF REPEATED ADMINISTRATION OF THE STANDARD . 389 4.5.3.3.3.
INDEXES OF BIOAVAILABILITY IN THE CASE WHERE THE STANDARD PREPARATION IS
ADMINISTERED AS A SINGLE DOSE 389 4.6. CONCLUSIONS 391 LITERATURE 392
SUBJECT INDEX 400
|
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author | Rácz, I. |
author_facet | Rácz, I. |
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dewey-sort | 3615 219 |
dewey-tens | 610 - Medicine and health |
discipline | Chemie / Pharmazie Medizin |
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institution | BVB |
isbn | 0471905178 |
language | English Hungarian |
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physical | IX, 416 S. graph. Darst. |
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spelling | Rácz, I. Verfasser aut Gyogyszerformulálás Drug formulation Chichester u.a. Wiley 1989 IX, 416 S. graph. Darst. txt rdacontent n rdamedia nc rdacarrier Pharmaceutical chemistry Pharmazeutische Technologie (DE-588)4045699-7 gnd rswk-swf Pharmakokinetik (DE-588)4115557-9 gnd rswk-swf Biopharmazie (DE-588)4006890-0 gnd rswk-swf Arzneiform (DE-588)4068874-4 gnd rswk-swf Arzneiform (DE-588)4068874-4 s DE-604 Pharmakokinetik (DE-588)4115557-9 s Biopharmazie (DE-588)4006890-0 s Pharmazeutische Technologie (DE-588)4045699-7 s GBV Datenaustausch application/pdf http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=005032371&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA Inhaltsverzeichnis |
spellingShingle | Rácz, I. Drug formulation Pharmaceutical chemistry Pharmazeutische Technologie (DE-588)4045699-7 gnd Pharmakokinetik (DE-588)4115557-9 gnd Biopharmazie (DE-588)4006890-0 gnd Arzneiform (DE-588)4068874-4 gnd |
subject_GND | (DE-588)4045699-7 (DE-588)4115557-9 (DE-588)4006890-0 (DE-588)4068874-4 |
title | Drug formulation |
title_alt | Gyogyszerformulálás |
title_auth | Drug formulation |
title_exact_search | Drug formulation |
title_full | Drug formulation |
title_fullStr | Drug formulation |
title_full_unstemmed | Drug formulation |
title_short | Drug formulation |
title_sort | drug formulation |
topic | Pharmaceutical chemistry Pharmazeutische Technologie (DE-588)4045699-7 gnd Pharmakokinetik (DE-588)4115557-9 gnd Biopharmazie (DE-588)4006890-0 gnd Arzneiform (DE-588)4068874-4 gnd |
topic_facet | Pharmaceutical chemistry Pharmazeutische Technologie Pharmakokinetik Biopharmazie Arzneiform |
url | http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=005032371&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA |
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