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采用RP-HPLC法,分别于SD大鼠灌胃给予鸡肝散提取物后0.17、0.5、1、2、4和6h,测定大鼠胃肠道组织中游离以及总的木犀草素的含量,以及血浆、心、肝、肺、肾中总的木犀草素的含量。结果表明,鸡肝散提取物中主要成分木犀草素苷在肠道中迅速水解成木犀草素而被吸收,在胃肠道组织中主要以苷元木犀草素形式存在。木犀草素经吸收后快速分布至各组织,其中代谢比较旺盛的肝、肾组织中木犀草素的含量高于心、肺组织中;肾、心、肺组织中的木犀草素含量均为1h时达最大,这与血药浓度达峰时间相似;而在肝组织中,药物分布迅速,0.17h已达高峰;在其他组织中因检测灵敏度问题而未被检出。建立的大鼠生物样本中木犀草素的含量测定方法具有灵敏、准确、专属性强等特点,可用于鸡肝散药效成分木犀草素的体内药动学研究。
RP-HPLC was used to determine free and total luteolin in the gastrointestinal tissues of SD rats after intragastric administration of chicken liver extract to SD rats for 0.17, 0.5, 1, 2, 4 and 6 h. As well as total luteolin levels in plasma, heart, liver, lungs, and kidneys. The results showed that luteolin glucoside, the main component of the extract from Jigansan, was rapidly hydrolyzed into luteolin in the intestine and absorbed. In the gastrointestinal tract, luteolin was mainly present in the form of aglycone luteolin. Luteolin was rapidly distributed to various tissues after absorption. The content of luteolin in liver and kidney tissues where metabolism was relatively high was higher than that in heart and lung tissues; the content of luteolin in kidney, heart and lung tissues was 1h. The maximum time was reached, which was similar to the peak time of blood drug concentration. In liver tissue, the drug distribution was rapid and reached the peak at 0.17 h. In other tissues, it was not detected due to the sensitivity problem. The determination method of luteolin in rat biological samples has the characteristics of sensitivity, accuracy, specificity, etc., and can be used for the in vivo pharmacokinetic study of luteolin, a medicinal ingredient of Jigan Powder.