纳洛酮微乳的制备及其透皮吸收作用  

Optimized Preparation of Naloxone Microemulsion and Its Transdermal Delivery Effect

作　　者：李天傲[1] 章晔[2,3] 冯璇[2] 徐翔[2] 许东航[2] 

机构地区：[1]浙江大学城市学院医学与生命科学院,杭州310015 [2]浙江大学医学院附属第二医院,杭州310009 [3]浙江中医药大学,杭州310053

出　　处：《中国药学杂志》2009年第9期688-691,共4页Chinese Pharmaceutical Journal

摘　　要：目的探讨水溶性药物纳洛酮微乳的制备以及作为载体促进药物的透皮吸收。方法以肉豆蔻酸异丙酯(IPM)-水-卵磷脂-正丙醇作为微乳的组成部分,制备纳洛酮-卵磷脂油包水型微乳。采用效应面优化法,对微乳处方进行星点设计,筛选出最佳处方。采用Franz扩散池,SD雄性大鼠离体皮肤作为透皮模型,HPLC测定药物含量。结果最佳处方条件为卵磷脂:29%,正丙醇:25%,IPM:35%。按此最优条件制备的纳洛酮微乳稳态渗透速率为4.33μg·h-1·cm-2,大大高于水溶液稳态渗透速率(0.20μg·h-1·cm-2)。结论微乳对纳洛酮的经皮渗透具有促进作用。OBJECTIVE To prepare W/O microemulsion formulation containing naloxone and to investigate its transdermal delivery effect in vitro. METHODS The microemulsion was prepared with the system contained of isopropyl myristate-water-lecithin-propanol according to the central composite design （CCD） . The steady permeation rate of naloxone hydrochloride was determined in vitro using Franz diffusion cell with the skin of SD male rats. The concentration of naloxone hydrochloride was measured by HPLC. RESULTS The optimal formulation contained lecithin （29 % ）, propanol （25%） and IPM （35%）. The steady permeation rate ofnaloxone microemulsion was 4.33 μg·h^-1·cm^-2, much higher than that of the aqueous solution （0.20 μg.h^-1.cm^2） . CONCLUSION Microemulsion enhanced the permeation of naloxone hydrochloride across the skin of SD male rats.

关 键 词：透皮 微乳 纳洛酮 星点设计 

分 类 号：R944[医药卫生—药剂学]