水杨酸异辛酯促进雌二醇喷雾剂透皮吸收的体外研究

Promotion effect of 2-ethylhexyl salicylate to transdermal absorption of estradiol spray in vitro

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(P<0.05),而处方2无显著性差异(P>0.05);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(P>0.05),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。

Objective：To screen the formulations of estradiol spray and evaluate the transdermal permeability of estradiol in vitro. Methods： The penetration experiments of different spray formulations and the commercial patch were conducted with isolated rat skin in Franz diffusion cells. The content of estradiol in the receptor solution was determinated by high performance liquid chromatography （HPLC）. The transdermal parameters of different spray prescriptions were compared with the commercial patch and negative control, respectively. Results：Compared with the negative control, the steady-state permeation rates and the cumulative penetration percentages of formulation 3 and formulation 4 were increased significantly （P 〈 0.05 ） ,while formulation 2 was not statistically different（P 〉 0.05 ） ; compared with the commercial patch, the penetration parameters of formulation 2, formulation 3, and formulation 4 had no significant statistical difference （P 〉 0.05 ） , but the similarity in the penetration trend of estradiol was the highest between formulation 3 and the commercial patch. Conclusion： 2-ethylhexyl salicylate has a significant role in promoting the transdermal absorption of estradiol spray, and the formulation 3, which contains 8.5% 2- ethylhexyl salieylate had higher similarity with the commercial patch in the permeability characteristics of estradiol in vitro.