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目的:考察马钱子总生物碱中马钱子碱透皮吸收性质。方法:测定总生物碱中马钱子碱的油水分配系数;用改良的Franz扩散池法,选择离体大鼠腹部皮肤为渗透屏障,高效液相色谱(HPLC)法测定其中马钱子碱的浓度。结果:与马钱子碱对照品相比,总生物碱中马钱子碱在pH 5,7.4,9的磷酸盐缓冲液(PBS)中的油水分配系数均无显著性差异;在pH 7.4和9的PBS中,透皮吸收速率分别提高1.40和1.26倍(P<0.05),累积透过率也有显著提高(P<0.05),而在pH 5的PBS中透皮吸收性质无显著性差异。结论:总生物碱中其他生物碱在游离型状态时对马钱子碱的透皮吸收有一定的促进作用。
Objective: To investigate the transdermal absorption of brucine in total alkaloids of Strychnos nux-vomica. Methods: The oil-water partition coefficients of strychnine in total alkaloids were determined. The skin of abdomen of isolated rats was selected as the osmotic barrier by modified Franz diffusion cell method. The content of brucine in brucine was determined by high performance liquid chromatography concentration. Results: Compared with brucine reference substance, there was no significant difference in the oil-water partition coefficients of brucine in total alkaloids in phosphate buffer (PBS) at pH 5, 7.4, 9; Transdermal absorption rate increased by 1.40 and 1.26 times (P <0.05), and the cumulative transmission rate also increased significantly (P <0.05), while there was no significant difference in transdermal absorption property in pH 5 PBS. CONCLUSION: The other alkaloids in total alkaloids may promote the transdermal absorption of brucine in free-form state.