利培酮有机原位凝胶的制备及其体外评价
Preparation and in vitro release analysis of in situ organogel of Risperidone
作者:苏玉春;姚举;于小玉;徐睿超;康蓉;
Author:
收稿日期: 年卷(期)页码:2016,31(06):-556-558
期刊名称:华西药学杂志
Journal Name:WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字:利培酮;有机原位凝胶;抗凝剂;凝胶因子;体外释放;体内释放;炎症反应
Key words:
基金项目:
中文摘要
目的以利培酮为模型药物,制备利培酮有机原位凝胶。方法通过考察凝胶因子和抗凝剂对药物在体内外的释放及相关性的影响,确定最佳的制剂处方。结果注射用大豆油为凝胶基质,12.5%的硬脂酸为凝胶因子,NMP为抗凝剂制备的液态载药有机原位凝胶,在37℃下的体外释放周期约为72 h,体内结果与体外的基本一致。注射予大鼠,无明显的炎症反应。结论利培酮有机原位凝胶是可以延长药物释放周期的新剂型。
参考文献
[1]齐鹏,任丽莉,陈国广,等.利培酮经皮给药系统的研制[J].华西药学杂志,2011,26(2):112-114.
[2]Byerly MJ,Devane CL.Pharamacokinetics of clozapine and risperidone:A review of recent literature[J].Clin Psychopharmacol Copyright,1995,26:177-187.
[3]Hatefi A,Amsden B.Biodegradable injectable in situ forming drug delivery systems[J].J Control Releas,2002,80:9-28.
[4]Moder K,Bittner B,Li Y,et al.Monitoring microviscosity and microacidity of the albumin microenvironment inside degrading microparticles from poly(lactideco-glycolide)(PLG)or ABA-triblock polymers containing hydrophobic poly(lactideco-glycolide)A blocks and hydrophilic poly(ethyleneoxide)B blocks[J].Pharm Res,1998,15:787-793.
[5]Abdallah DJ,Weiss RG.Organogels and low molecular mass organic gelators[J].Advanced Materials,2000,12(17):1237-1247.
[6]Motulsky A,Lafleur M,Couffin-hoarau A-C,et al.Characterization and biocompatibility of organogels based on L-alanine for parenteral drug delivery implants[J].Biomaterials,2005,26(31):6242-53.
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