摘要
目的 :研究水杨酸甲酯 (MS)在小猪皮肤中同时渗透和代谢特性及在皮肤匀浆中的代谢作用。方法 :用Valin Chien双室扩散池和HPLC法测定接受液中水杨酸甲酯和代谢物水杨酸 (SA)的浓度 ;用猪皮肤于磷酸缓冲液中匀浆 ,将匀浆液于3 7℃保温 ,定时取样 ,用HPLC测定水杨酸甲酯及代谢物的浓度。结果 :不同浓度的水杨酸甲酯在皮肤渗透时均有一定程度的代谢 ,速率 (flux)随着供给池浓度增加而增加 ,在高浓度时达到一平台 ;水杨酸甲酯的浓度在加入皮肤匀浆后逐渐降低 ,说明是由皮肤中酶水解所致。结论 :水杨酸甲酯在皮肤渗透及皮肤匀浆中 ,具有一定的代谢。
OBJECTIVE Studies of methyl salicylate (MS) with and without skin homogenate were also conducted at 37℃. In vitro simultaneous transport and metabolism of methyl salicylate were studied using skin from pig. METHODS In vitro simultaneous skin permeation and metabolism experiment of MS was done in Valin Chien diffusion cells at 37℃.A metabolism experiment was carried out using skin homogenate. Both MS and metabolite, salicylic acid(SA), were detected in all receiver solutions.RESULTS No chemical hydrolysis of MS was found,indicating that the MS was hydrolyzed during the skin permeation process.The flux from MS solution increased with the donor concentration, and reached a plateau at the high concentration range.The concentration of MS decreased by skin homogenate, indicating that the hydrolysis of MS is caused by skin enzymes. CONCLUSIONS skin enzymes can metebolize the MS during the permeation process, and in skin homogenate.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2001年第8期451-453,共3页
Chinese Journal of Hospital Pharmacy
基金
国家自然科学基金资助项目 ( 39970 880 )