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洋川芎内酯I大鼠在体肠吸收动力学研究
引用本文:于泽,魏海,熊耀坤,林晓,梁爽,冯怡.洋川芎内酯I大鼠在体肠吸收动力学研究[J].中国药学杂志,2013,48(8):628-632.
作者姓名:于泽  魏海  熊耀坤  林晓  梁爽  冯怡
作者单位:1.上海中医药大学,中药现代制剂技术教育部工程研究中心,上海 201203; 2.上海中医药大学,中医方证与系统生物学研究中心,上海 201203; 3.上海中医药大学中药学院,上海 201203)
基金项目:国家教育部科学技术研究重点项目(211060);上海市科委上海市自然科学基金项目(11ZR1434500);上海市教委重点学科项目(J50302);上海市教育委员会科研创新项目重点项目(11zz112,12ZZ124)
摘    要: 目的 研究洋川芎内酯I大鼠在体肠吸收特性。方法 运用大鼠在体单向灌流技术考察洋川芎内酯I在大鼠4个肠段的吸收动力学特征;采用高效液相色谱法(HPLC)测定灌流液中洋川芎内酯I的含量;从药物质量浓度、吸收部位、灌流介质3个方面对洋川芎内酯I的各肠段吸收特性进行考察;利用重量法计算动力学参数。结果 不同质量浓度(514、257和128.5 μg·mL-1)洋川芎内酯I在相同肠段的吸收速率常数ka和表观吸收系数Papp均无显著性差异(P>0.05);十二指肠段的表观吸收系数Papp与空肠、回肠和结肠均有极显著性差异(P<0.001),而空肠、回肠、结肠间均无显著性差异。结论 洋川芎内酯I在大鼠肠道的吸收在所选剂量范围内呈线性动力学过程,提示其吸收可能以被动转运为主;在大鼠各肠段均有较好吸收,其中十二指肠为其最佳吸收部位。

关 键 词:洋川芎内酯I  肠吸收  重量法  药剂学
收稿时间:2012-10-30;

In situ Intestinal Absorption Kinetics of Senkyunolide I in Rats
YU Ze,WEI Hai,XIONG Yao-kun,LIN Xiao,LIANG Shuang,FENG Yi.In situ Intestinal Absorption Kinetics of Senkyunolide I in Rats[J].Chinese Pharmaceutical Journal,2013,48(8):628-632.
Authors:YU Ze  WEI Hai  XIONG Yao-kun  LIN Xiao  LIANG Shuang  FENG Yi
Institution:1.Engineering Research Center of Modern Preparation Technology of TCM of Ministry of Education, Shanghai University of TCM, Shanghai 201203, China; 2.Center for TCM and Systems Biology, Shanghai University of TCM, Shanghai 201203, China; 3.School of Pharmacy, Shanghai University of TCM, Shanghai 201203, China
Abstract:OBJECTIVE To study the in situ intestinal absorption kinetics of senkyunolide I in rats. METHODS The absorption of senkyunolide I in four segments of rat intestine was investigated using the in situ single-pass perfusion method, and the drug content was measured by HPLC. The absorption kinetics of senkyunolide I at different segments of intestine, drug concentration, and perfusion medium were studied. RESULTS Drug concentration had no significant influence on the ka and the Papp values of senkyunolide I (P>0.05) in the range of 128.5-514 μg·mL-1. Papp values of senkyunolide I at duodenum were significantly higher than those at the other three regions of intestine (P<0.001). But no significant differences in the Papp value (P>0.05) were found among jejunum, ileum, and colon. CONCLUSION The absorption of senkyunolide I complied with linear kinetics in the dose range studied, indicating that its absorption may be mediated mainly by passive transport. Senkyunolide I could be absorbed at all the studied intestinal segments while duodenum seemed to be the best absorption segment for it.
Keywords:senkyunolide I  intestinal absorption  gravimetric method  pharmaceutics
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