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

发布时间：2018-09-13 08:30

【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。
[Abstract]:OBJECTIVE: To prepare fluoxetine hydrochloride ethosome gel and investigate its transdermal permeability in vitro. METHODS: Fluoxetine hydrochloride ethosome was prepared by ethanol injection method. The encapsulation efficiency and particle size were taken as the index. The formulation and preparation technology were optimized by orthogonal design. The particle size, encapsulation efficiency and Zeta potential of the gel were evaluated. Carbomer 940 was used as the matrix to prepare the gel. Preparation of ethosome gel. In vitro transdermal test was carried out on rat skin by transdermal diffusion apparatus. The drug concentration was determined by HPLC and the cumulative penetration and steady-state transdermal rate were calculated. The transdermal permeation rate in vitro was (5.13+0.78) UG cm 2 h 1, which was 1.31 and 4.31 times higher than that of normal gel and control gel.
【作者单位】：南京中医药大学药学院;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;江苏省中药高效给药系统工程技术研究中心;南京市中药微丸产业化工程技术研究中心;中国人民解放军第102医院药剂科;
【基金】：江苏高校优势学科建设工程资助项目
【分类号】：R943

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