盐酸奥昔布宁醇脂质体的制备及体外透皮吸收研究  

Preparation and in vitro transdermal penetration of oxybutynin hydrochloride ethosome

作　　者：沈丹丹[1,2] 张涛[2,3] 黄华[1] 

机构地区：[1]重庆医科大学药剂学教研室,重庆400016 [2]重庆医药工业研究院有限责任公司,重庆400061 [3]重庆市化学制药工程技术研究中心,重庆400061

出　　处：《中国药科大学学报》2011年第1期48-52,共5页Journal of China Pharmaceutical University

摘　　要：研究采用乙醇注入均质法制备盐酸奥昔布宁醇质体,正交设计优化处方。用动态光散射测定平均粒径及粒径分布;扫描电子显微镜观测其形态;水平透皮扩散试验仪考察其大鼠离体皮肤经皮渗透量。蛋黄卵磷脂、乙醇、盐酸奥昔布宁的质量分数分别为3%,45%和5%时,制备的醇质体平均粒径为(98±12)nm,包封率为(48.1±1.4)%。各种盐酸奥昔布宁制品24 h的经皮渗透量由大到小依次为:醇脂质体(盐酸奥昔布宁5%)、除去游离药物的醇脂质体(盐酸奥昔布宁2.4%)、物理混合物(盐酸奥昔布宁5%)、无水乙醇(盐酸奥昔布宁5%)、质量分数为45%的乙醇溶液(盐酸奥昔布宁5%)。研究表明醇脂质体是盐酸奥昔布宁经皮给药系统的良好载体。Oxybutynin hydrochlorid（oxb） ethosomes were prepared by ethonal infusion and homogenization.Orthogonal method was used to optimize the formulation of the ethosomes preparation.The average size and size distribution were determined by dynamic light scattering,and the shape of ethosomes was observed by the scanning electron microscopy.In vitro transdermal flux of oxb through the separated rat skin was determined by Franz-type diffusion cells.The encapsulation efficiency of the ethosomes was（48.1±1.4）%,and the average size was（98±12）nm,when the ethosomal preparation consisted of 3% egg phospholipids,45% ethanol and 5% oxb.Transdermal flux of oxybutynin hydrochloride in various preparations at 24 h was ranked in the order of： ethosomes（oxb 5%）unencapsulate-oxb-free ethosomes（oxb 2.4%）physical mixture（oxb 5%）ethanol solution（oxb 5%）45%ethanol solution（oxb 5%）.The results suggested that ethosomes could be the ideal carrier in oxb transdermal delivery.

关 键 词：盐酸奥昔布宁 醇脂质体 正交设计 包封率 经皮渗透量 

分 类 号：R944[医药卫生—药剂学]