中文摘要：

目的：研究α-倒捻子素大鼠灌胃给药的排泄特征。方法：采用大鼠灌胃给予α-倒捻子素的方式,在24 h内收集胆汁,48 h内收集尿液和粪便,建立并采用HPLC测定生物样品中α-倒捻子素含量。生物样品采用甲醇提取;HPLC采用C18（250 mm×4.6 mm,5μm）反相色谱柱,流动相为甲醇-水（95∶5）,流速为1.0 mL·min-1,检测波长为317 nm。结果：HPLC-UV方法测定,胆汁中α-倒捻子素浓度在0.12~120μg·mL-1,尿液中α-倒捻子素浓度在0.16~160μg·mL-1,粪便中α-倒捻子素浓度在0.26~5200μg·g-1,其峰面积与质量呈线性相关,相关系数大于0.999。α-倒捻子素灌胃给药后主要以粪排泄为主,占总药量的78.34%;其次为尿排泄,占总药量的2.32%,胆汁最低为0.10%。α-倒捻子素灌胃给药后原型药物主要通过粪便和尿途径排出体外,未发现其他代谢产物。结论：所建立的HPLC-UV测定方法符合方法学考核要求,适用于大鼠灌胃α-倒捻子素后生物样品中原型药物的测定及其排泄研究;α-倒捻子素灌胃给药后主要以粪排泄为主,以原型药物排出体外。

英文摘要：

Objective：To investigate the characteristics of α - mangostin excretion in rats after intragastric adminis- tration. Methods：Urine,feces and bile were collected after a single oral dose of 16. 4 mg · kg-l α -mangostin to rats within 48 h,48 h, and 24 h,respectively, and a high performance liquid chromatography （HPLC） with UV de- tection was developed to study the concentration of α - mangostin in the biological samples. The biological samples were treated by liquid -liquid extraction with methanol. The chromatographic separation was accomplished on a re- versed -phase C18 （250 mm × 4.6 mm,5 μm）column using methanol -water （95：5）as the mobile phase at a flow rate of 1.0 mL · min-l and the ultraviolet detection wavelength was set at 317 nm. Results：When the concentration of α- mangostin in bile was at 0. 12 -120 μg · mL-1 ,in urine at O. 16 -160 μg · mL-1 ,in fecal at 0.26 -5200 μg · mL- 1, its peak area and quality had linear correlation, and the correlation coefficients were greater than 0. 999 by the HPLC - UV method. The accumulation excretion amount of c~ - mangostin in feces and urine within 48 h were 78.34% and 2.32%, respectively, and 0. 10% in bile within 24 h. These data indicated that a - mangostin was mainly excreted in feces, followed by urine, and least in bile. By intragastric administration, the prototype drug of c~- mangostin was mainly excreted through defecation and urination, and no other metabolites were found. Conclusion ： The method is satisfactory by methodology verification and suitable for determination of α - mangostinin rat biological samples and the study of its cumulative excretion, α - Mangostin is mainly excreted in feces by the form of prototype drug in rats after intragastric administration.