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范雅婷

作品数:2 被引量:8H指数:1
供职机构:北京大学药学院药剂学系更多>>
发文基金:全球变化研究国家重大科学研究计划国家科技重大专项国家重点基础研究发展计划更多>>
相关领域:医药卫生化学工程更多>>

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Preparation and property of mPEG-PLA/pluronic mixed micelles and their role in solubilization of propofol被引量:1
2012年
Novel mixed polymeric micelles formed by biocompatible polymers,mPEG-PLA and Pluronic P105,were fabricated and used as a nanocarrier to solubilize the poorly soluble anesthetic drug propofol.Propofol was added directly to an aqueous solution of mPEG-PLA/Pluronic P105 mixed micelles and stirred into a micellar solution.The average particle size and size distribution of micelles were evaluated by the dynamic light scattering technology.Drug loading content,encapsulation efficiency and free drug concentration were determined by using ultracentrifugation and lyophilization.In vitro release characteristic of propofol formulation was investigated by dialysis method.The physical stability of mixed micelles was also assessed under storage condition(4 oC) after six months.Sleep-recovery studies in male Sprague-Dawley rats,at a dose of 10 mg/kg were performed to compare the pharmacodynamic profiles of propofol in mixed micelles with that of commercial lipid emulsion(CLE).The results indicated that solubilization of propofol in the mixed micelles was more efficient than that in mPEG-PLA alone.Micelles with the optimized composition of mPEG-PLA/Pluronic P105/Propofol(10:4:5,w/w/w) had particle size of about 90 nm with narrow distribution(polydispersity index of about 0.2).The content of free propofol in the aqueous phase of mixed micelles was significantly lower than that in CLE(P〈0.05).There was no remarkable differences for particle size,polydispersity index,and free drug concentration when the mix micelles were stored at 4 oC for six months,suggesting that the propofol-loaded mixed micelles were stable for at least six months.The accumulative release of mixed micelles was significantly higher than that of CLE at the corresponding time points,suggesting that quick release rate for mixed micelles might produce favorable pharmacological effect.No significant differences in the unconsciousness time and recovery time of righting reflex were observed between the mixed micelles and CLE(P〉0.05).In
李桂玲李馨儒范雅婷张燕惠李眉刘艳
关键词:PROPOFOLPLURONIC
醋柳黄酮自微乳化给药系统的体内外评价被引量:7
2012年
本文的目的在于对醋柳黄酮自微乳化给药系统进行评价,该给药系统用于提高难溶性药物醋柳黄酮的口服生物利用度。评价指标包括自微乳化时间、粒径及多分散指数、形态学特征、体外分散性、稳定性、在体小肠吸收及生物利用度。结果表明,该自微乳化给药系统在3 min内即形成微乳,平均粒径低于40 nm,多分散指数低于0.2,电镜下观察粒子形态为球形;20 min时体外累积释放百分率(以槲皮素计)接近90%,显著高于普通胶囊剂;加速试验条件下放置6个月,自微乳化给药系统的所有指标均未发生明显改变;该自微乳化给药系统的在体小肠吸收速率常数(以槲皮素计)显著高于醋柳黄酮乙醇溶液(P<0.05);以醋柳黄酮的混悬液为参比制剂,自微乳化给药系统的大鼠灌胃给药相对生物利用度(以槲皮素计)为518%。
李桂玲范雅婷张燕惠李艳芳李馨儒刘艳李眉
关键词:醋柳黄酮自微乳化给药系统分散性小肠吸收生物利用度
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