水杨酸异辛酯促进雌二醇喷雾剂透皮吸收的体外研究

发布时间：2018-01-28 23:53

本文关键词： 水杨酸异辛酯雌二醇透皮喷雾剂透皮渗透体外　出处：《中国新药杂志》2015年04期 　论文类型：期刊论文

【摘要】：目的:通过对雌二醇喷雾剂中水杨酸异辛酯的用量研究,初步评价其体外透皮渗透特性。方法:以离体鼠皮为渗透屏障,采用Franz扩散池进行体外透皮渗透试验,运用HPLC法测定接受液中雌二醇的含量,分别与参比制剂和阴性对照进行体外透皮渗透参数的对比研究。结果:与阴性对照相比,处方3和4的稳态渗透速率和累积透过百分率均有增大,且都存在显著性差异(P0.05),而处方2无显著性差异(P0.05);与参比制剂相比,处方2、处方3和处方4的渗透参数均无显著性差异(P0.05),但在整个渗透特性趋势上处方3与参比制剂相似度最高。结论:水杨酸异辛酯对雌二醇的透皮渗透有着明显的促进作用,含水杨酸异辛酯8.5%的处方3与参比制剂在体外透皮渗透特性上具有较高的相似性。
[Abstract]:Objective: to study the content of isooctyl salicylate in estradiol spray and evaluate its permeation characteristics in vitro. Methods: the isolated rat skin was used as the permeation barrier. The transdermal permeation test in vitro was carried out by Franz diffusion cell, and the content of estradiol in the receiving solution was determined by HPLC method. Results: compared with the negative control, the steady-state osmotic rate and cumulative penetration percentage of prescription 3 and 4 were increased. There were significant differences in P0.05P, but there was no significant difference in prescription 2 (P0.05A). The osmotic parameters of prescription 2, prescription 3 and prescription 4 were not significantly different from those of reference preparation (P 0.05). Conclusion: isooctyl salicylate can promote transdermal permeation of estradiol. Prescription 3 containing isooctyl salicylate 8.5% is similar to the reference preparation in transdermal permeability in vitro.
【作者单位】：济川药业集团有限公司;
【分类号】：R965
【正文快照】： 雌二醇临床上主要用于改善更年期血管舒缩症状和防治骨质疏松症等,其常用给药方法有口服、阴道给药和透皮给药[1-2]。由于雌二醇口服给药存在肝脏首过效应,生物利用度很低[3-5],而阴道给药具有子宫放大反应,患者适应性差,故雌二醇的透皮给药被广泛应用于更年期血管舒缩症(如潮

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