用HPLC研究α-倒捻子素大鼠灌胃给药的排泄  

Study on α-mangostin excretion in rats after intragastric administration by HPLC-UV method

作　　者：赵岩[1] 唐国胜[1] 侯莹莹[1] 蔡恩博[1] 刘双利[1] 杨鹤[1] 张连学[1] 王士杰[2] 

机构地区：[1]吉林农业大学中药材学院,长春130118 [2]吉林农业科技学院中药学院,吉林132101

出　　处：《药物分析杂志》2014年第10期1782-1786,共5页Chinese Journal of Pharmaceutical Analysis

基　　金：国家科技支撑计划项目(2011BAI03B01;2009GJB10031);国家公益性行业科研专项(201303111);吉林省科技发展计划项(20126046;20140204013YY;20130303094;YYZX201258;20140311050YY);吉林省中医药产业发展专项(YYZX201258);国家自然科学基金(31000154)

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。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.

关 键 词：山竹 氧杂蒽酮 α-倒捻子素 灌胃给药代谢分析 药物排泄分析 生物样品药物测定 高效液相色谱法 

分 类 号：R917[医药卫生—药物分析学]