天天胶囊及其原料芦荟在大鼠体内的存在形式研究

Existence forms of Tiantian Capsules and its raw material Aloe in rats

为了阐明组方药材芦荟对天天胶囊体内存在形式(原形成分和代谢产物)的贡献,首次对芦荟、天天胶囊及去芦荟天天胶囊在大鼠体内的存在形式进行了研究。大鼠灌胃给药,每天1次,连续灌胃7 d。收集给药7 d的全部尿液和粪便,最后一次灌胃给药后分别于0.5、1、1.5 h收集血液。采用UHPLC⁃Q⁃TOF⁃MS检测和鉴定生物样品中的存在形式,分别鉴定了芦荟给药组、天天胶囊给药组、去芦荟天天胶囊给药组生物样品中的原形成分34、28、2个及代谢产物64、94、0个。代谢反应类型主要为甲基化、氢化、羟基化、脱羟基、葡萄糖醛酸结合、硫酸结合等。该研究首次阐明了芦荟、天天胶囊、去芦荟天天胶囊在大鼠体内的存在形式和部分代谢途径,为进一步揭示其显效形式奠定基础,并对中药芦荟和天天胶囊的作用机制及质量控制研究具有重要意义。

This study explored the existence forms(original constituents and metabolites)of Tiantian Capsules,Aloe,and Tiantian Capsules without Aloe in rats for the first time,aiming to clarify the contribution of Aloe to the existence form of Tiantian Capsules.Rats were administrated with corresponding drugs by gavage once a day for seven consecutive days.All urine and feces samples were collected during the seven days of administration,and blood samples were collected 0.5,1,and 1.5 h after the last administration.UHPLC⁃Q⁃TOF⁃MS was employed to detect and identify the original constituents and metabolites in the samples.A total of 34,28,and 2 original constituents and 64,94,and 0 metabolites were identified in the samples of rats administrated with Aloe,Tiantian Capsules,and Tiantian Capsules without Aloe,respectively.The main metabolic reactions were methylation,hydrogenation,hydroxylation,dehydroxylation,glucuronidation,and sulfation.This study clarified for the first time the existence forms and partial metabolic pathways of Aloe,Tiantian Capsules,and Tiantian Capsules without Aloe in rats,laying a foundation for revealing their effective forms.The findings are of great significance to the research on the functioning mechanism and quality control of Aloe and Tiantian Capsules.