马钱子总碱囊泡凝胶经皮给药后在大鼠组织中的分布研究

Tissue distribution of total alkaloids in Strychni Semen vesicle gel in rats after transdermal administration

目的研究马钱子总碱囊泡凝胶经皮给药后在大鼠组织中的分布。方法 18只SD大鼠经皮给予马钱子总碱囊泡凝胶后0.5、2、6 h,采集大鼠皮肤、骨骼肌、脑、心、肺、肝、脾、肾、胃、小肠、脂肪、睾丸、子宫、关节等组织,以溶剂萃取法对样品进行提取,应用LC-MS/MS联用技术对各组织中的马钱子碱和士的宁进行测定。结果经皮给药后,马钱子碱和士的宁在大鼠体内分布较广,主要分布在肺、肝、肾、小肠,其次为心脏、关节、皮肤等,而在脑、肌肉、脂肪中的分布量较低。结论马钱子总碱囊泡凝胶能减少马钱子碱和士的宁在脑、心脏的分布,有利于降低中枢毒性和心脏毒性。

Objective To study the tissue distribution of total alkaloids in Strychni Semen vesicle gel after transdermal administration in rats. Methods Total alkaloids in Strychni Semen vesicle gel was applied to 18 SD rats of SPF grade. Tissues of skin, skeletal muscle, brain, heart, lung, liver, spleen, kidney, stomach, intestine, fat, testicle, uterus, and joint were collected at 0.5, 2, and 6 h after transdermal administration. Samples were extracted by ethyl acetate-n-butanol （7 ： 3） and brucine and strychnine in each tissue were determined by LC-MS/MS method. Results The two ingredients were mainly distributed in lung, liver, kidney, and intestine, followed with heart, joint, and skin, while low in brain, tousle, and fat. Conclusion Total alkaloids in Strychni Semen vesicle gel could reduce the distribution of brucine and strychnine in brain and heart, which is benefit to lower the toxicity of the two ingredients in central nervous system and cardiovascular system.