盐酸氟西汀醇质体凝胶剂的制备及其体外经皮渗透性研究  

Preparation of fluoxetine hydrochloride ethosome gel and its transdermal penetration in vitro

作　　者：孙杏华 李圣惠[1] 丁青龙[2] 狄留庆[1,3,4] 黄家富[5] 李俊松[1,3,4] 祖强[1] 

机构地区：[1]南京中医药大学药学院,南京210046 [2]中国人民解放军第102医院全军心理疾病防治中心药物研究室,常州213003 [3]江苏省中药高效给药系统工程技术研究中心,南京210046 [4]南京市中药微丸产业化工程技术研究中心,南京210029 [5]中国人民解放军第102医院药剂科,常州213003

出　　处：《中国新药杂志》2015年第24期2843-2847,2864,共6页Chinese Journal of New Drugs

基　　金：江苏高校优势学科建设工程资助项目

摘　　要：目的:制备盐酸氟西汀醇质体凝胶剂并考察其体外经皮渗透特性。方法:采用乙醇注入法制备盐酸氟西汀醇质体,以包封率和粒径为指标,利用正交设计优化处方和制备工艺,对其粒径及包封率、Zeta电位进行评价,并以卡波姆940为基质制备醇质体凝胶。采用透皮扩散仪,大鼠离体皮肤进行体外透皮实验,HPLC测定药物浓度并计算药物累积渗透量、稳态透皮速率。结果:制得的盐酸氟西汀醇质外观呈淡蓝色,平均粒径为(77.3±1.49)nm,包封率为(60.4±1.76)%,盐酸氟西汀醇质体凝胶体外经皮渗透速率为(5.13±0.78)μg·cm-2·h-1,是普通凝胶剂和对照凝胶的1.31和4.31倍。结论:盐酸氟西汀醇质体凝胶剂制备工艺简单可行,质量稳定可控,能明显促进盐酸氟西汀的经皮渗透。Objective： To prepare fluoxetine hydrochloride ethosome gel and to investigate its transdermal penetration in vitro. Methods： Fluoxetine hydrochloride ethosomes were prepared by an ethanol injection method.The formulation and the preparation method of ethosomes were optimized by orthogonal experiment using entrapment efficiency（ EE） and particle size as indexes. The particle size,zeta potential and entrapment efficiency were evaluated,and the carbomer was added as the base for preparation of the ethosome gel. The penetration of fluoxetine hydrochloride ethosome gel through rat skin was evaluated by Franz＇s cell. The concentration of fluoxetine hydrochloride was determined by HPLC. The accumulated permeation amounts and steady permeation rate of fluoxetine hydrochloride were calculated. Results： The color of fluoxetine hydrochloride ethosome was light blue,the average diameter was（ 77. 3 ± 1. 49） nm,and the EE was（ 60. 4 ± 1. 76） %. The permeation rate of fluoxetine hydrochloride ethosome gel [（ 5. 13 ± 0. 78） μg·cm- 2·h- 1]was 1. 31 and 4. 31 times higher than those of general gel and control gel,respectively. Conclusion： The preparation technique of fluoxetine hydrochloride ethosome gel is feasible with stable and controllable quality,and can improve transdermal penetration.

关 键 词：盐酸氟西汀 醇质体 凝胶剂 经皮渗透 

分 类 号：R943.43[医药卫生—药剂学] R971.43[医药卫生—药学]