渗透促进剂对蛇床子素透皮吸收的影响

Studies on effects of enhancers on percutaneous absorption of osthol across excised full thickness rat skin

目的 研究渗透促进剂对蛇床子素的体外经皮渗透的影响。方法 将蛇床子有效部位制成饱和生理盐水溶液 ,采用Valia Chien扩散池考察了土荆芥油、薄荷醇和月桂氮酮 (Azone) 3种渗透促进剂对蛇床子素经离体鼠皮渗透性的影响。结果 应用土荆芥油、薄荷醇和Azone为渗透促进剂 ,药物的稳态流量与对照组比较均有提高 ,增渗倍数分别为 3.0 9,3.4 1及4 .38;药物的表观扩散系数分别提高为 1.10 ,2 .18及 6 .30倍 ,但表观分配系数却分别降低为 0 .30 9,0 .341及 0 .4 38倍。结论 3种渗透促进剂的作用机制主要为改变角质层的通透性 ,减低了药物经皮肤渗透的阻力 ,提高了药物在皮肤角质层的扩散系数。

OBJECTIVE: To study the in vitro permeability of osthol across full thickness rat skin treated with enhancers. METHODS: The modified Valia-Chien diffusion cells was used. RESULTS: The enhancers including chenopodium, menthol and Azone were able to increase the osthol percutaneous steady-state fluxes 3.09, 3.41 and 4.38 times to the control, respectively. To explain the enhancement mechanism of the promoters used, the diffusion and partitioning coefficients for osthol were calculated. It was indicated that chenopodium, menthol and Azone increased the diffusion coefficients of osthol to 1.10, 2.18 and 6.30 times respectively to the control, while decreased the SC/medium partition coefficients to 0.309, 0.341 and 0.438 times respectively. CONCLUSIONS: It was shown that the main enhancement mechanism of three skin penetration enhancers used were to destroy the barrier function of stratum comeum, reduce the resistance of drug transport through the skin and increase the diffusion coefficients of osthol.