渗透促进剂对蛇床子素透皮吸收的影响

 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3.09，3.41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0.309，0.341及0.438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。

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

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 fluxes3.09,3.41 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 corneum,reduce the resistance of drug transport through the skin and increase the diffusion coefficients of osthol.