Controlled-Release Technology

353

INDEX Royal Danish School of Pharmacy, 201 Rutgers—The State University of New Jersey, 281 SRI International, 172 Sandoz Research Institute, 214 State University of Ghent, 188 UMIST, 100 University of California—San Francisco, 84,267

University of Keele, 188 University of Manchester, 128 University of Nottingham, 100,201 University of Strathclyde, 158 University of Toronto, 341 University of Utah, 232,241 Upjohn Company, 301,324 Welsh School of Pharmacy, 84 Youngstown State University, 120

Downloaded by 80.82.77.83 on May 6, 2018 | https://pubs.acs.org Publication Date: September 4, 1987 | doi: 10.1021/bk-1987-0348.ix002

Subject Index A Absorption enhancement strategies, peptides and proteins, 303-305 ionizable drugs from topical dosage form, 273-279 transbuccal, diclofenac sodium in a dog model, 310-321 Activation, dextran and inulin, 189-195 Activation energy of diffusion, 50-52 Additives, effect on percutaneous absorption of drugs in rabbits, 275 Agarose gel, use in liposomal drug delivery system, 267-270 Albumin microspheres intramuscular and intraarticular drug delivery, 204,206,211 preparation, 204,207/ Aldehydes, introduction in polysaccharides, 189-190 Aligned fiber moderators, flow rate, 346/ Amine functions, effect on pH sensitivity of poly(ortho esters), 176-178 Aminobenzoate esters, correlations of partition coefficients for solvent pairs, 62,63/

Β Barrier function, stratum corneum general discussion, 241-242 ways to decrease for enhanced drug delivery, 283 Base, use in microencapsulation process, 214-229 Basket technique, controlled release of bioactive agents, 121,124,125/ Binary image, drug delivery system, 24/ Bioadhesive agents, use to enhance intranasal absorption of peptides and proteins, 304

Bioadhesive properties, microspheres, use in nasal drug administration, 209,212 Biodégradation of dextran derivatives, 196 Bioerodible drug delivery systems, 2-3 Bioerodible polymers, use in self-regulated drug delivery systems, 172-186 Biopharmaceutical considerations, controlled-release drug delivery, 9-11 Block copolymer, gelation characteristics after exposure to irradiation, 128-138 Buccal administration of drugs, advantages, 310 Buccal mucosa histology, 311-315 Burst period, frustum array drug delivery device, 332 Butanol, permeability coefficients in hairless mouse skin, 246,247/ C Capric acid effect on progesterone skin permeation, 292,296-299 use to enhance skin permeation of progesterone, 289/ Carbamate content, activation of dextran with 4-nitrophenyl chloroformate, 193,194/ Carbamate derivatives of dextran, preparation, 196 Carboxylic groups, introduction in polysaccharides, 190-191,192/ Carboxymethylcellulose effect on nasal blood flow response, 306-308 use to enhance intranasal absorption of peptides and proteins, 305 Chemically controlled drug delivery systems, 2-4 Chitin hydrogels, partially deacetylated, degradation, 182-184 Chloroformâtes, reaction with polysaccharides, 191,193-195

Lee and Good; Controlled-Release Technology ACS Symposium Series; American Chemical Society: Washington, DC, 1987.


354

CONTROLLED-RELEASE TECHNOLOGY

Clinical results, morphine hydrogel suppositories, 166-169 Computer-generated images application to drug delivery systems, 27,29/,30 obtained from random structures, 23 verification of methods, 25-27,28/ Concentration determination, drug delivery systems, 18 distribution, matrix drug delivery system, 8-9 gradients, drug release from polymer beads, 151-154 profiles oil-water multilaminate, 38/ steady-state diffusion process, 43/ solutions effect on light-scattering ratio, 131,135 effect on micellar diffusion coefficient, 130-131,134 effect on viscosity, 131-132,135-136 steady-state diffusion process, 42 Conformational alterations, keratinized protein components of hairless mouse skin, 263 Constant-release configurations, drug dispersed in a permeable matrix, 326 Constant-release diffusion systems, rate control by means of geometric configuration, 324-340 Controlled-release device description, 267 disposable, use for drug infusion, 341-350 preparation, 268 Controlled-release drug delivery benefits, 1 classification, 2 frustum array device, 326-340 overview, 1-11 parenteral and nasal drug administration, 201-212 theory, 17-22 use of liposomal delivery system, 267-272 See also Drug delivery systems Controlled-release kinetics of 5-fluorouracil from copolymer system, measurement, 120-125 Copolymer, block, gelation characteristics after exposure to irradiation, 128-138 Copolymer systems, measurement of controlled-release kinetics of 5-fluorouracil, 120-125 Corner flow function, steady-state diffusion process, 42 Crystallinity of polymers, relation to drug release from hydrogels, 162,164 Cylindrical design, comparison with slab design for hydrogels, 164

D Decylmethyl sulfoxide, effect on progesterone skin permeation, 292,296-299 Degradation of dextran derivatives by dextranases, 196-199 Delipidization of skin, effect on progesterone permeation, 292,294-299 Desmopressin, effect on nasal blood flow response, 306-308 Desorption from oil-water multilaminates, 39-40,41/ Dextran, activation, 189-195 Dextran derivatives biodégradation, 196 degradation by dextranases, 196-199 Dialdehyde derivatives of dextran, preparation, 196 Diclofenac sodium absorption from hydrogel discs, 320 characterization of the buccal permeability, 311 comparison with oxprenolol hydrochloride, 153-156 disposition kinetics in dogs, 312-313 in vitro delivery from a transbuccal drug delivery device, 314,316/ in vivo absorption studies, 314-321 partial extraction and release from polymer beads, 145-156 release as a function of water content of drug-free polymer, 141,143/ release from beads of very low water content, 141,144/ Differential scanning calorimetry (DSC) hairless mouse skin and components, 245-246,247/ use to study thermal transitions of stratum corneum, 242 Diffusion comparison of theoretical results with experimental electrical values, 46,47/ drugs in polymers, estimation of rates, 49-69 drugs through human skin, measurement, 113-119 heterogeneous media, 34-47 steady-state, in a hollow sphere, theory, 328-331 water-filled phase, effect on drug release, 30 Diffusion cells comparison of variability, 117 flow-through, description, 114-115,116/ study of ^-estradiol transport in hairless mouse skin, 233 use to monitor controlled release of progesterone, 268


355


INDEX

Diffusion coefficients drug delivery systems, 18 hydrogels, 162 matrix drug delivery systems, 6 methods of estimation, 50 micellar, effect of radiation dose, 130-131,134 Diffusion-controlled drug delivery system, 4-5 Diffusion kinetics, absorption of drugs through human skin, 115,116/ Diffusion systems, rate control by means of geometric configuration, 324-340 Diffusive transport in porous polymers, 16-32 Digital images, drug delivery system, 21/ Diltiazem hydrochloride, percutaneous absorption from polymeric film bases, 273-279 Discontinuous surface coatings, steady-state permeation, 40-47 Discrete models of release behavior, drug delivery systems, 18-19,21/ Disodium cromoglycate, percutaneous absorption from polymeric film bases, 273-279 Disposable controlled-release device for drug infusion, 341-350 Dissolution rate of a solid, influence of geometry, 325 Dissolution test procedure, enhanced drug release from microspheres, 215-216 Dog, buccal mucosa, 314,315/ Drug(s) advantages of intranasal delivery, 301-302 ionizable, enhanced absorption from topical dosage form, 273-279 transdermal delivery, chemical structure and skin permeation rate, 284/ transport across biological membranes, factors affecting, 311 Drug carriers, activation procedures and biodégradation studies, 188-199 Drug delivery, controlled-release—See Controlled-release drug delivery Drug delivery systems liposomal, use of controlled drug release, 267-272 pH-sensitive, 172-179,180/ schematic, 21/ self-regulated, use of bioerodible polymers, 172-186 surface chemical analysis, 100-111 transbuccal, preparation, 312 transdermal, with enhanced skin permeability, 281-299 Drug delivery systems—See also Controlled-release drug delivery

Drug diffusion in polymers, estimation of rates, 49-69 through human skin, measurement, 113-119 Drug dispersed in a permeable matrix, constant-release configurations, 326 Drug infusion disposable controlled-release device, 341-350 in vivo test of device, 348-349 Drug loading percentage of microspheres, effect on drug release, 217,219,222/ Drug-polymer conjugates, controlled-release drug delivery, 3-4 Drug release by partial extraction, 145-156 enhanced, polylactide microspheres, 214-229 from microspheres, factors affecting, 217 from polymer beads, 141-145,146/, 148/ Drug solubilities in polymers determination using partition coefficients, 61-68 estimation, 57-61

Ε Egg phosphatidylcholine liposomes, multi lamellar, associated with progesterone, effect on controlled drug release, 268-272 Electrolytes combined with nonelectrolytes, effect on percutaneous absorption of drugs in rabbits, 275,278 weak, solubilities, 64,67/ Emulsifiers, effect on thioridazine release from microspheres, 219,221/ Emulsion characteristics, effect on porosity of thioridazine microspheres, 226-227 Enhanced absorption of ionizable drugs from topical dosage form, 273-279 Enhanced drug release from polylactide microspheres, 214-229 Enhanced intranasal peptide delivery, 301-308 Enhanced skin permeability, transdermal drug delivery, 281-299 Enhancement factor enhanced permeation of progesterone across various skin structures, 297-299 skin permeation of progesterone, factors affecting, 285,290/ Enzymatic degradation, dextran and derivatives, 196-199 Enzyme-degradable hydrogel, triggered drug delivery system, 182-184 Enzyme-substrate reactions, effect on drug delivery systems, 172-179,180/



356


Enzyme-triggered drug delivery system, reversibly inactivated, 182,184-186 Erosion matrix drug delivery systems, 7 modulated drug delivery systems, 172-179,180/ ^-Estradiol effects of ethanol on transport in hairless mouse skin, 232-240 enhancement of skin permeability by different enhancers, 285,291/ solubility in various ethanol-water solutions, 234-235,236/ transport across skin, 234,236/ Ethanol concentration-distance profile, 234 effects on the transport of ^-estradiol in hairless mouse skin, 232-240 swelling of polymers for drug release, 141,142/ l-(N-2-Ethylmethacrylcarbamoyl)5-fluorouracil (EMCF), controlled release of 5-fluorouracil, 120-125 Extent of orientation, particle, drug delivery systems, 20 Extraction lipids from hairless mouse skin, 243-244 mechanism, drug release from polymer beads, 151-153,154/

F Fabrication, drug delivery systems, 22 Fatty acids, use to enhance skin permeation of progesterone, 285,290/ Fatty matrix pathway, contribution to enhancement of progesterone skin permeation, 297-299 Fiber flow moderator, aligned, preparation, 342 Fick's first law, determination of diffusion rates, 50 Fick's second law, solute concentration, 35 Film continuity, role in steady-state diffusion processes, 46 Flow diagram, steady-state diffusion process, 45/ Flow moderators, disposable controlled-release device for drug infusion, 346-347 Flow rate aligned fiber moderators, 346/ infusion devices, assembly for testing, 343 Flow-through diffusion cells, description, 114-115,116/ 5-Fluorouracil, measurement of controlled-release kinetics from copolymer systems, 120-125

Flux membrane-dispersed monolith, 317 permeants through hairless mouse skin, thermal dependence, 258 solute across a membrane or stratum corneum, 238 Fourier transform IR spectroscopy (FTIR), hairless mouse skin and components, 245-246,248-261 Fractional drug release, matrix drug delivery systems, 6 Frustum array device application of hollow sphere concept of diffusion, 329-331 construction, 331 controlled drug release, 326-340 schematic, 327/ zero-order release phase, 329 Frustum-shaped cell, partially depleted, schematic, 327/

G Gas dispersion tube, use to study controlled release of 5-fluorouracil from copolymer systems, 121-125 Gastrointestinal residence time, effect on oral drug delivery, 9-10 Gel permeation chromatograms, dextran derivatives, 197/ Gelation characteristics, block copolymer after exposure to irradiation, 128-138 Geometric configuration, use for rate control of drug release, 324-340 Geometric considerations, drug delivery systems, 7,30 Glass hollow fibers effect of internal diameter on flow rate, 347-348 flow moderation, 342-343 Glass transition temperature copolymer system, effect on release rate of a bioactive agent, 124 guidelines for predicting changes, 52,57 Glucose-glucose oxidase modulated drug delivery, 174-179,180/ Glutaraldehyde stabilization, albumin microspheres, 206,208/

H Heat stabilization, albumin microspheres, 204-208 Hemispheric configuration, drug release system, 326 Heparin infusion device, in vivo test, 348-349 microvolume infusion of rodents, 344,346


357


INDEX

Heterogeneous media, diffusion, 34-47 High-performance liquid chromatography, rabbit plasma after administration of diltiazem hydrochloride, 278-279 Higuchi equation, drug release kinetics, 6 Histamine effect on nasal blood flow response, 306-308 intranasal administration, 301-308 Histology, buccal mucosa, 311-315 Homogeneous enzyme immunoassay, principle, 184/ Human beings, measurement of in vitro drug diffusion, 113-119 Human oral mucosa, description, 320 Hydration, micellar effect of radiation dose, 132 effect of temperature, 136 Hydrocortisone effect of urea concentration on release rate, 174,175/ enhancement of skin permeability by different enhancers, 285,291/ permeability coefficients in hairless mouse skin, 246,247/ Hydrogel(s) description, 159-160 enzyme-degradable, 182-184 for sustained drug release, cross sections of different designs, 160,161/ Hydrogel beads, advantages for oral drug delivery, 139 Hydrogel discs, absorption of diclofenac sodium, 320 Hydrogel suppositories, morphine device design, scale-up, and evaluation, 158-170 photograph, 169/ Hydrogel systems, properties affecting the mechanism of drug release, 159 Hydrolysis studies, controlled release of 5-fluorouracil from copolymer systems, 121-125 Hydrophobic polymers, controlled-release drug delivery, 17 Hydroxypropylcellulose, SSIMS spectra, 103,104/ Hydroxypropylmethylcellulose, SSIMS spectra, 103,105/

Image processing, drug delivery systems, 22-23 Images obtained from computer-generated random structures, estimation of three-dimensional properties, 23 Immunoassay, homogeneous enzyme, 184/

Immunogenic effects, microspheres, 203 In vitro delivery of diclofenac sodium from a transbuccal drug delivery device, 314,316/ In vitro diffusion of drugs through human skin, measurement, 113-119 In vitro drug release from transbuccal disc devices, determination, 312 / In vivo absorption studies, diclofenac sodium, 314-321 In vivo test, drug infusion device, 348-349 Indomethacin enhancement of skin permeability by different enhancers, 285,291/ permeability enhancement by a combination of enhancers, 293/ SSIMS spectra, 106,107/ Indomethacin-loaded polymer beads, SSIMS spectra, 106,108/ Infrared spectrum, activated dextran, 195/ Infusion drugs, use of a disposable controlled-release device, 341-350 heparin in rodents, 344,346 Infusion device for controlled drug release fabrication, 343-344 factors affecting flow rate, 347-348 flow-rate testing, 343 preparation and running, 344,345/ Insulin delivery system, schematic, 175/ enhancement of intranasal delivery, 304 release rate, modulation in response to glucose concentration, 174-179,180/ Intraarticular delivery of drugs, use of albumin microspheres, 204,206-211 Intramuscular delivery of drugs, use of albumin microspheres, 204,206-211 Intranasal delivery of drugs, advantages, 301-302 Intranasal peptide delivery, enhancement, 301-308 Intravenous delivery of drugs advantages, 281-299 use of microspheres, 203-204,205/ Inulin activation, 189-195 succinoylation, 190-191,192/ Ion-exchange microspheres, uptake in the lung region, 203,205/ Ionizable drugs, enhanced absorption from topical dosage form, 273-279 Irradiation, effect on gelation characteristics of a block copolymer, 128-138 Κ Keratinized protein components of hairless mouse skin, C - H stretching vibration, 262-263


358



Keratinized striated epithelia, inner cheek of rodents, 313-314,315/ Kinetics of diffusion, absorption of drugs through human skin, 115,116/

Membrane-reservoir drug delivery systems, 4-5 Membranization, drug release from polymer beads, 145,146/, 148/ Metabolism of diltiazem hydrochloride by rabbits L effect of delivery route, 278-279 study methods, 274 Lag time, oil-water multilaminate, 39 Methanol extraction, effect on FTIR spectra Laplace's equation, steady-state diffusion of hairless mouse skin, 256/,260-261/ process, 40 Micellar properties, effect of Laser Doppler flow probe, measurement of temperature, 134-138 nasal blood flow, 305 Microencapsulation process, use of Laurocapram, effect on progesterone skin base, 214-229 permeation, 292,296-299 Microscopic sample preparation, drug Light-scattering ratio, solutions exposed to delivery systems, 22 radiation, 131,135 Microspheres Linked suppositories, release profile of as controlled-release systems for morphine hydrochloride, 166,167/ parenteral and nasal drug Lipids administration, 201-212 drug delivery systems barrier model, permeability limitations, 202 coefficient, 235 possible materials, 202 extraction from hairless mouse requirements, 202 skin, 243-244, 262 polylactide, enhanced drug mobility within the stratum corneum, correlation to enhanced release, 214-229 permeability, 262 use in nasal administration of mouse stratum corneum, DSC and FTIR drugs, 209,212 studies, 245-261 use in parenteral administration of removal from skin, effect on progesterone drugs, 203-211 permeation, 292-299 Microstructural models for diffusive stratum corneum, thermal transitions, 242 transport in porous polymers, 16-32 Lipophilic molecules, enhancement of Modifications, hydrogel suppository, 166-168 permeability through hairless mouse Modulated drug delivery skin, 258 systems, 172-179,180/ Liposomal delivery system for controlled Molar water solubilities, correlations to drug release, 267-272 partition coefficients, 64 Lung retention, microspheres after Mole fraction solubility of a drug, relation intravenous administration, 203 to melting point, 58-61 Lysozyme-catalyzed degradation, Molecular weight, relation to diffusion hydrogels, 182-184 coefficient, 52,56/ Lysozyme-morphine conjugation scheme, Monosuccinate ester of dextran, 185/ preparation, 196 Morphine antibodies added to a M lysozyme-morphine conjugate, effect on glucose oxidase release, 186/ Morphine hydrochloride release from hydrogel slabs into Mass conductance, drug delivery systems, 19 Mathematical simulations, experimental water, 160,161/ studies of constant-release diffusion release from outer surface of dispersions in hollow cylindrical systems, 322,337,339/ hydrogels, 162,163/ Matrix drug delivery systems, 5-9 Morphine hydrogel suppositories, device Matrix inversion algorithm, use to predict design, scale-up, and particle size distributions, 27 evaluation, 158-170 Mechanisms, skin permeation Morphine impregnation in hydrogels, 160-166 enhancement, 292-299 Morphine-lysozyme conjugation scheme, 185/ Melting point of a drug, relation to Mouse skin, hairless solubility, 58 Membrane function, drug release from polymei effect of ethanol on the transport of ^-estradiol, 232-240 beads, 156


359

INDEX

Mouse skin, hairless—Continued probing the structure on the molecular level, 241-264 transdermal delivery rate of progesterone, 270-272 Mucosa, human oral, description, 320 Mucosal membrane, nasal, description, 302-303 Multilamellar egg phosphatidylcholine liposomes, associated with progesterone, effect on controlled drug release, 268-272

Organic solvents, effects on the intrinsic permeability of the stratum corneum, 232 Osmotic pumping mechanism, drug-release from reservoir systems, 4-5 Oxprenolol hydrochloride comparison with diclofenac sodium, 153-156 partial extraction and release from polymer beads, 145-156 release as a function of water content of drug-free polymer, 141,143/


Ν

Paracetamol-loaded polymer beads, SIMS image, 109,110/ Parenteral administration of drugs, use of Naltrexone microsphere systems, 201-212 delivery system, schematic, 180/ Partial extraction, drug release from solubility, 68/ Nasal administration of drugs, use of polymer beads, 145-156 microsphere systems, 201-212 Particle size distributions, obtained from Nasal blood flow, measurement, 305 computer-generated images, 26/,29/ Nasal mucosal membrane, description, 302-30 Partition coefficients Nasal peptide absorption, factors correlations for solvent pairs, 62-64 affecting, 303 permeability coefficient, 235 Negative-ion SSIMS spectra, use to determine drug solubilities in polymers, 61-68 hydroxypropylcellulose, 103,104/ Peptide drugs Nitrocellulose acetate membrane plug, advantages of intranasal ethanol-water concentration-distance delivery, 301-302 profile, 238,239/ intranasal delivery, Nitrogen bases, correlations between enhancement, 301-308 partition coefficients and Percolation theory, evaluation of transport solubilities, 64-66 phenomena in heterogeneous Nitroglycerin, transdermal delivery, 11 environments, 32 4-Nitrophenyl chloroformate activation, Percutaneous absorption of drugs in rabbits, dextran, 191,193-195 intact versus stripped skin, 275-277 Nonelectrolytes, solubilities, 64,67/ Percutaneous administration of diltiazem Non-steady-state permeation through hydrochloride, comparison with oral oil-water multilaminates, 35-39 administration, 278-279 Periodate oxidation, dextran, 189-190 Permeability, enhanced skin, transdermal Ο drug delivery, 281-299 Permeability coefficients Octanol, permeability coefficients in calculation, 233 hairless mouse skin, 246,247/ determination, 245 Oil-water multilaminates desorption, 39-40,41/ lipid barrier model, 235 non-steady-state permeation, 35-39 solute across a membrane or stratum Oleic acid, effect on progesterone skin corneum, 235 Permeability studies, hairless mouse permeation, 292,296-299 Opiate addiction, application of triggered skin, 233,244-246,247/ Permeation drug delivery systems, 179-186 through discontinuous surface Optimal transport, oil-water multilaminate, 36,38/,39 coatings, 40-47 Oral administration of diltiazem through oil-water multilaminates, 35-39 hydrochloride, comparison with pH-sensitive polymers, drug delivery percutaneous administration, 278-279 systems, 172-182 Oral delivery systems, controlled-release Pharmaceutical compounds, diffusion through drug delivery, 9-10 human skin, variability, 118



360


Pharmacokinetic model, analysis of plasma concentration-time profiles after intravenous dosing, 313 Photomicrographs, drug-loaded beads during extraction, 150/ Physiological modifying agents, use to enhance intranasal absorption of peptides and proteins, 304 Plasma concentration profiles, transbuccal administration of diclofenac sodium, 316/,318/ Plasma levels, drugs after application on stripped rabbit skin, 275-277 Poloxamer, gelation characteristics after exposure to irradiation, 128-138 Polyacrylic acid gel, effect on intranasal absorption of insulin, 307 Polydispersity of micellar sizes in poloxamer solutions effect of radiation dose, 133 effect of temperature, 137 Polylactide microspheres, enhanced drug release, 214-229 Polymer(s) beads low water swelling, 139-156 synthesis, 140 erosion, mechanisms of control, 3 estimation of drug diffusion rates, 49-69 estimation of drug solubility, 57-61 for drug release, composition, swelling, and release data, 142/ matrices, advantages as drug delivery systems, 341 monoliths, slowing the initial rate of drug release, 140 porous, diffusive transport, 16-32 solubility parameters, 65/ swelling, matrix drug delivery system, 7-8 Polymer-drug conjugates, controlled-release drug delivery, 3-4 Polymeric drug delivery systems, surface chemical analysis, 100-111 Poly(ortho esters) effect of pH on erosion rate, 177-178/, 180/ use in modulated drug delivery systems, 174-179,180/ Poly(oxyethylene)-poly(oxypropylene) block copolymer, gelation characteristics, 128-138 Polypropylene molds, use to make suppositories, 164 Polysaccharides as drug carriers, 188-199 introduction of aldehydes, 189-190 introduction of carboxylic groups, 190-191,192/ reaction with chloroformâtes, 191,193-195

Porosity estimates, obtained from computer-generated images, 26/,29/ hairless mouse skin, effect of ethanol, 235-240 particle, drug delivery systems, 20 Porous network, drug delivery systems, 19 Porous polymers, diffusive transport, 16-32 Positive-ion SSIMS spectra hydroxypropylcellulose, 103,104/ hydroxypropylmethylcellulose, 103,105/ indomethacin, 106,107 indomethacin-loaded polymer beads, 106,108/ Posttreatment of polylactide microspheres with NaOH, effect on drug release, 223,225/ Prednisolone, release from heat-stabilized albumin microspheres, 207/ Pretreatment of polylactide microspheres with NaOH, effect on drug release, 219,223,224/ Progesterone effect of enhancers on permeation rate across various skin structures, 292,296-299 enhancement of skin permeability by different enhancers, 285,291/ permeability enhancement, effect of location of enhancer, 291/ permeation across a delipidized skin, 292,294-299 permeation across a stripped skin, 292,295-299 release kinetics from controlled-release device, 268-271 solubilities, 68/ transdermal delivery rate across hairless mouse skin, 270-272 use of capric acid to enhance skin permeation, 289/ use of fatty acids to enhance skin permeation, 290/ Prostaglandin, diffusion coefficients, 54-55/ Protein components, keratinized, hairless mouse skin, C - H stretching vibration, 262-263 Protein gel pathway, contribution to enhancement of progesterone skin permeation, 297-299 Protein residue sheets extraction from hairless mouse skin, 244 mouse stratum corneum, DSC and FTIR studies, 245-261 Pumping mechanism, infusion pumps, 349 R Rabbit skin, enhanced absorption of ionizable drugs, 273-279



INDEX

361

Skin—Continued Radiation dose, effect on micellar permeation enhancement properties, 130-133 mechanisms, 292-299 Rats transdermal drug delivery, 281-299 buccal mucosa, 313-314,315/ permeation enhancers, examples, 286 use to test heparin infusion device, 349 rabbit, enhanced absorption of ionizable Rectal administration of drugs, advantages drugs, 273-279 and disadvantages, 159 Skin-permeation-enhancing transdermal drug Release kinetics, zero-order, frustum delivery system array drug delivery device, 332-340 Release mechanism, drug release from polymer development, 283-292 structural components, 286/ beads, 145,146/, 148/ Slab design for hydrogels, comparison with Release profiles microspheres prepared with cylindrical design, 164 NaOH-posttreated polymers, 223,225/ Sodium hydroxide, effect on drug release microspheres prepared with NaOH-pretreated from polylactide microspheres, 214-229 polymers, 223 Solid dissolution rate, influence of morphine hydrochloride from geometry, 325 hydrogels, 160-166,167/ Solubility Release rates, drugs from polymer diclofenac sodium and oxprenolol beads, 141-145,146/ hydrochloride, 153/ Reservoir-membrane drug delivery ^-estradiol, 234-235,236/ systems, 4-5 Solubility parameters, polymers, 65/ Reticuloendothelial system, removal of Solution-diffusion mechanism, drug release microspheres, 203 from membrane-reservoir systems, 4-5 Reversibility of erosion rates, poly(ortho Sphere, hollow, theory of steady-state esters), 176,180/ diffusion, 328-331 Reversibly inactivated enzyme, triggered Spring-type diffusion cell, variability, 117 drug delivery system, 182,184-186 Static secondary ion mass spectrometry Rodents, microvolume infusion of description, 101-102 heparin, 344,346 surface analysis of polymers, 101 Rose bengal surface chemical analysis of polymeric clearance from normal and arthritic rabbit drug delivery systems, 100-111 knee joints, 209,210/ Steady-state diffusion in a hollow sphere, release from the lung region of a theory, 328-331 rabbit, 203,204,205/ Steady-state permeation through discontinuous surface coatings, 40-47 Stereological analysis of three-dimensional Sample size, effect on controlled release of materials, 20-22 5-fluorouracil from E M C F Steroids monomer, 122,123/ correlations of solubilities with Scanning electron microscopy partition coefficients, 62,63/ microspheres, 216 diffusion coefficients, 54,55/ thioridazine microspheres, 228-229/ relation of melting point to Scopolamine, transdermal delivery, 11 solubility, 58-61 Screw-type diffusion cell, variability, 117 use of compounds to enhance skin Secondary ion mass spectrometric imaging permeation, 285,291/ description, 102 use of microspheres for controlled surface chemical analysis of polymeric release, 204,206,207/ drug delivery systems, 100-111 Stratum corneum Self-regulated drug delivery systems, use effect of removal on progesterone permeation, 292,295-299 of bioerodible polymers, 172-186 effect on transdermal drug delivery, 10-11 Size distribution of microspheres, effect on hypothesized structure, 258 drug release, 217 modeling as a hydrophilic protein gel Skin dispersing in a continuous lipid hairless mouse, effect of ethanol on the matrix, 292,293/ transport of ^-estradiol, 232-240 mouse human, measurement of in vitro drug DSC and FTIR studies, 245-261 diffusion, 113-119 permeability studies, 244-246,247/ permeation cell, hydrodynamically separation from the epidermis, 243 calibrated, 288/



362


Stratum corneum—Continued probing the structure on the molecular level, 241-264 thermal transitions, 242 Succinic anhydride activation, inulin, 190-191,192/ Suppositories clinical evaluation, preparation, 164,166 composition, 160 joining with a hydrogel rod, 166,167/ morphine hydrogel, device design, scale-up, and evaluation, 158-170 Surface area, effect on solid dissolution rate, 325 Surface chemical analysis, polymeric drug delivery systems, 100-111 Surface coatings, discontinuous, permeation, 40-47 Surface distribution of drugs, polymeric drug delivery systems, 106-109 Surface-to-volume ratio of drug particles, 20 Surfactant agents, use to enhance intranasal absorption of peptides and proteins, 304 Swelling ethanol and water, polymers for drug release, 141,142/ keratinized protein components of hairless mouse skin, 263 matrix drug delivery systems, 7

Transbuccal drug delivery device general discussion, 314,316/ modeling of drug release, 317 preparation, 312 Transdermal drug delivery rate, progesterone across hairless mouse skin, 270-272 Transdermal drug delivery systems benefits, 282 controlled-release drug delivery, 10-11 potential, 283 uses, 282 with enhanced skin permeability, 281-299 Transmission FTIR spectra, hairless mouse skin and components, 246-261 Transport ^-estradiol in hairless mouse skin, effects of ethanol, 232-240 oil-water multilaminate, 35-36 Triggered drug delivery systems, 179-186 Tritiated triamcinolone intraarticular administration, 209,211/ release from an intramuscular site, 206,208/

Τ

U Urea-urease modulated drug delivery system, 173-174,175/ V Viscosity, solutions exposed to radiation, 131-132,135-136 Volume expansion, drug release from polymer beads, 141-145,146/ W

Temperature effects barrier function of stratum corneum, 242 FTIR spectra of hairless mouse skin and components, 246-261 micellar properties, 134-138 Theophylline, structure, 109 Theophylline bead, polymer-coated, SIMS image, 109,110-111/ Thermal dependence, flux of permeants through hairless mouse skin, 258 Thermal transitions, stratum corneum, 242 Thermograms, DSC, hairless mouse skin and components, 246,247/ Thioridazine microspheres preparation, 215 scanning electron micrographs, 228-229/ Thioridazine release from polylactide microspheres, effect of NaOH, 217-229 Three-dimensional materials, stereological analysis, 20-22 Topical dosage form of ionizable drugs, enhanced absorption, 273-279 Tortuosity, drug delivery systems, 18 Transbuccal absorption of diclofenac sodium in a dog model, 310-321

Water diffusion rates across a sealed hollow hydrogel, 162 Water-oil multilaminates, desorption, 39-40,41/ non-steady-state permeation, 35-39 Water solubilities, correlations to partition coefficients, 64 Water-soluble drugs, release from polymer beads with low swelling, 139-156 Wavenumber versus temperature plots C - H stretching band of hairless mouse skin and components, 252/,255/,257/ N - H stretching and bending bands of hairless mouse skin, 255/,259/ Weak electrolytes, solubilities, 64,67/ X X-ray photoelectron spectroscopy, surface analysis of polymers, 100-101

Ζ Zero-order release kinetics, frustum array drug delivery device, 332-340


Controlled-Release Technology

Recommend Documents