壳聚糖包覆左旋多巴脂质体冻干制剂的制备及大鼠口服药动学  

Preparation of freeze-dried chitosan-liposome containing L-dopa and pharmacokinetics in rats after oral administration

作　　者：李赛[1] 侯冬枝[1] 孙敏捷[1] 平其能[1] 徐岩[2] 

机构地区：[1]中国药科大学药剂学教研室,南京210009 [2]华中科技大学同济医学院附属协和医院神经内科,武汉430022

出　　处：《中国药科大学学报》2009年第5期406-411,共6页Journal of China Pharmaceutical University

基　　金：国家自然科学基金资助项目(No.30700881)~~

摘　　要：目的:制备壳聚糖包覆的左旋多巴脂质体以增加左旋多巴生物利用度,减少血药浓度波动;研究冻干的最佳处方及工艺。方法:逆相蒸发法制备左旋多巴脂质体并以壳聚糖包覆,采用冷冻干燥法制备脂质体冻干制剂,单因素实验考察不同因素对冻干后包封率的影响;高效液相色谱法研究大鼠口服壳聚糖包覆的左旋多巴脂质体的药动学。结果:最佳冻干处方为:磷脂浓度50mg/mL,药脂比1∶10,壳聚糖浓度0.17%,冻干保护剂蔗糖用量2%。其包封率为(34.34±0.65)%(n=6)。与溶液组相比,大鼠口服壳聚糖包覆的左旋多巴脂质体后血药浓度达峰时间后延,且长时间维持在较高水平,生物利用度提高到溶液组的400%以上。结论:选用合适冻干工艺可以得到包封率大于30%的左旋多巴脂质体冻干制剂。壳聚糖包覆脂质体能够提高左旋多巴生物利用度,减少血药浓度波动。Aim:To prepare chitosan-coated L-dopa liposomes,and to optimize the formulation and freeze-drying processing parameters of L-dopa liposomes.Methods:The liposomes were prepared by using reverse phase evaporation followed by freeze-drying,and effects of the factors on the entrapment efficiency of L-dopa liposome were studied.Pharmacokinetics of L-dopa in rats receiving oral dosing of L-dopa solution and chitosan-coated liposomes were investigated after HPLC determination of L-dopa levels in rats plasma.Result...

关 键 词：左旋多巴 壳聚糖 脂质体 冻干技术 药动学 

分 类 号：R944[医药卫生—药剂学]