关于半固体制剂中药物的体外释放研究进展
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摘要
目的综合国内外关于半固体制剂的体外药物释放试验的研究,探讨关于体外药物释放试验各装置特点及试验条件的选择并判断释药模型。方法根据国内外31篇文献,对如何根据所研究半固体制剂的特点选择合适装置及试验条件进行体外药物释放试验进行综述。结果通过药物的体外释放结果判断出药物符合的释药模型并阐明释药机理。结论通过选择合适的试验装置及条件进行体外药物释放试验,根据释药模型阐明释药机理,加深对于半固体制剂体外药物释放的研究。
Objective Based on the study of in vitro drug release test of semisolid preparation at home and abroad, the characteristics of each device and the selection of experimental conditions in vitro drug release test were discussed, and the drug release model was determined. Method According to the characteristics of semisolid preparation, suitable device and experimental conditions were selected for in vitro drug release test. Result According to the results of in vitro drug release test, the drug release model was determined and the mechanism of drug release was elucidated. Conclusion The mechanism of drug release is elucidates according to the model of drug release, and the research on drug release of semisolid preparations in vitro is deepened.
Objective Based on the study of in vitro drug release test of semisolid preparation at home and abroad, the characteristics of each device and the selection of experimental conditions in vitro drug release test were discussed, and the drug release model was determined. Method According to the characteristics of semisolid preparation, suitable device and experimental conditions were selected for in vitro drug release test. Result According to the results of in vitro drug release test, the drug release model was determined and the mechanism of drug release was elucidated. Conclusion The mechanism of drug release is elucidates according to the model of drug release, and the research on drug release of semisolid preparations in vitro is deepened.
引文
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[29]DONG Y,QU H,PAVURALA N,et al.Formulation characteristics and in vitro release testing of cyclosporine ophthalmic ointments[J].Int J Pharm,2018,544:254-264.
[30]XU X,Al-GHABEISH M,KRISHNAIAH Y S,et al.Kinetics of drug release from ointments:Role of transientboundary layer[J].International Journal of Pharmaceutics,2015,494(1):31-39.
[31]BAO Q,NEWMAN B,WANG Y,et al.In vitro ancorrelation of drug release from ophthalmic ointments[J].Journal of Controlled Release,2018,276:93-101.
[2]SHILPA P,BRYAN N,YAN W,et al.Influence of manufacturing process variables on the properties of ophthalmic ointments of tobramycin[J].Pharmaceutical Research,2018,35(9):179.
[3]PETRóé,PAáL T L,ER?S I,et al.Drug release from semisolid dosage forms:a comparison of two testing methods[J].Pharmaceutical Development and Technology,2015,20(3):330-336.
[4]FRANZ T J,LEHMAN P A,RANEY S G.Use of excised human skin to assess the bioequivalence of topical products[J].Intervirology,2008,22(5):276-286.
[5]FDA.Guidance for industry:SUPAC-SS nonsterile semisolid dosage forms:Scale-up and postapproval changes:chemistry,manufacturing,and controls;in vitro release testing and in vivo bioequivalence documentation[EB/OL].(1997-05-03)[2019-02-19].http://www.fda.gov/cder/guidance/index.htm.
[6]UCHIDA T,KADHUM W R,KANAI S,et al.Prediction of skin permeation by chemical compounds using the artificial membrane,Strat-M?[J].European Journal of Pharmaceutical Sciences,2015,67:113-118.
[7]BARBERO A M,FRASCH H F.Pig and guinea pig skin as surrogates for human in vitro,penetration studies:Aquantitative review[J].Toxicology in Vitro,2009,23(1):1-13.
[8]SIMON G A,MAIBACH H I.The pig as an experimental animal model of percutaneous permeation in man:qualitative and quantitative observationsan overview[J].Skin Pharmacology&Applied Skin Physiology,2000,13(5):229-234.
[9]胥洪灿,蒋厚迪,曹礼静,等.对猪皮不同部位药物透皮效果的研究[J].四川畜牧兽医,2004,31(11):29-30.
[10]SCIENCE P.Development and validation of in vitro release testing methods for semisolid formulations[J].Indoor Air,1993,15(5):311-316.
[11]DIAS M,FARINHA A E,HADGRAFT J,et al.Topical delivery of caffeine from some commercial formulations[J].International Journal of Pharmaceutics,1999,182(1):41-47.
[12]SHAH V P,ELKINS J,LAM S Y,et al.Determination of in vitro drug release from hydrocortisone creams[J].International Journal of Pharmaceutics,1989,53(1):53-59.
[13]SHAH V P,ELKINS J S,WILLIAMS R L.Evaluation of the test system used for in vitro release of drugs for topical dermatological drug products[J].Pharmaceutical Development&Technology,1999,4(3):377.
[14]SHAH V P,ELKINS J S.In-vitro release from corticosteroid ointments[J].Journal of Pharmaceutical Sciences,1995,84(9):1139-1140.
[15]关玉晶,丁平田,姜建华.乙氧苯柳胺软膏体外释放方法的研究[J].中国药剂学杂志:网络版,2006,4(4):150-154.
[16]HAIGH J M,SMITH E W.The selection and use of natural and synthetic membranes for in vitro diffusion experiments[J].European Journal of Pharmaceutical Sciences,1994,2(5/6):311-330.
[17]NG S F,ROUSE J J,SANDERSON F D,et al.Validation of a static Franz diffusion cell system for in vitro permeation studies[J].AAPS Pharm Sci Tech,2010,11(3):1432-1441.
[18]CSOKA I,CSANYIE,ZAPANTIS G,et al.In vitro and in vivo percutaneous absorption of topical dosage forms:case studies[J].International Journal of Pharmaceutics,2015,291(1):11-19.
[19]THAKKER K D,CHEM W H.Development and validation of in vitro release tests for semisolid dosage forms-case study[J].Dissolution Technologies,2003,10(2):10-15.
[20]LIEBENBERG W,ENGELBRECHT E,WESSELS A,et al.A comparative study of the release of active ingredients from semisolid cosmeceuticals measured with Franz,enhancer or flow-through cell diffusion apparatus[J].Journal of Food&Drug Analysis,2004,12(1):19-28.
[21]BROWN C,FRIEDELl H,BARKER A,et al.FIP/AAPS joint work shop report:Dissolution/In vitro release testing of novel/special dosage forms[J].AAPS Pharm Sci Tech,2011,12(2):782-794.
[22]KESHARY P R,CHIEN Y W.Mechanisms of transdermal controlled nitroglycerin administration(I):Development of a finite-dosing skin permeation system[J].Drug Development&Industrial Pharmacy,2008,10(6):883-913.
[23]CHIEN Y W,KESHARY P R,HUANG Y C,et al.Comparative controlled skin permeation of nitroglycerin from marketed transdermal delivery systems[J].Journal of Pharmaceutical Sciences,1983,72(8):968-970.
[24]BAO Q,SHEN J,JOG R,et al.In vitro release testing method development for ophthalmic ointments[J].International Journal of Pharmaceutics,2017,526(1/2):145-156.
[25]REGE P R,VILIVALAM V D,COLLINS C C.Development in release testing of topical dosage forms:use of the Enhancer cell with automated sampling[J].Journal of Pharmaceutical and Biomedical Analysis,1998,17(8):1226-1233.
[26]KUMAR P,SANGHVI P,COLLINS C C.Comparison of diffusion studies of hydrocortisone between the Franz cell and the Enhancer cell[J].Drug Development&Industrial Pharmacy,2008,19(13):1573-1585.
[27]ARELLANO A,SANTOYO S,MARTN C,et al.Surfactant effects on the in vitro percutaneous absorption of diclofenac sodium[J].Eur J Drug Metab Pharmacokinet,1998,23(2):307-312.
[28]TANOJO H,ROEMELE P.New design of a flow-through permeation cell for studying in vitro permeation studies across biological membranes[J].Journal of Controlled Release,1997,45(1):41-47.
[29]DONG Y,QU H,PAVURALA N,et al.Formulation characteristics and in vitro release testing of cyclosporine ophthalmic ointments[J].Int J Pharm,2018,544:254-264.
[30]XU X,Al-GHABEISH M,KRISHNAIAH Y S,et al.Kinetics of drug release from ointments:Role of transientboundary layer[J].International Journal of Pharmaceutics,2015,494(1):31-39.
[31]BAO Q,NEWMAN B,WANG Y,et al.In vitro ancorrelation of drug release from ophthalmic ointments[J].Journal of Controlled Release,2018,276:93-101.