洋川芎内酯I大鼠在体肠吸收动力学研究

于泽，魏海*，熊耀坤，林晓*，梁爽，冯怡*

中国药学杂志 ›› 2013, Vol. 48 ›› Issue (8) : 628-632.

PDF(823 KB)
中国药学杂志
PDF(823 KB)
中国药学杂志 ›› 2013, Vol. 48 ›› Issue (8) : 628-632. DOI: 10.11669/cpj.2013.08.012
论著

洋川芎内酯I大鼠在体肠吸收动力学研究

  • 于泽1，魏海*，熊耀坤1，林晓*，梁爽1，冯怡1*
作者信息 +

In situ Intestinal Absorption Kinetics of Senkyunolide I in Rats

  • YU Ze1,WEI Hai2*,XIONG Yao-kun1,LIN Xiao3,LIANG Shuang1,FENG Yi1*
Author information +
文章历史 +

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。

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.

关键词

洋川芎内酯I / 肠吸收 / 重量法 / 药剂学

Key words

senkyunolide I / intestinal absorption / gravimetric method / pharmaceutics

引用本文

EndNote

Ris (Procite)

Bibtex

导出引用
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 https://doi.org/10.11669/cpj.2013.08.012
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 https://doi.org/10.11669/cpj.2013.08.012
中图分类号： R969.1   

参考文献

Ch. P (2010) VolⅠ(中国药典2010年版．一部) . 2010：38.
YUAN Y， LIN X， FENG Y， et al. In vivo transmigration of anti-migrainous compounds from Ligusticum chuanxiong Hort. Chin Pharm J(中国药学杂志)，2010， 45(9)：694-697.
HE C Y， WANG S， FENG Y， et al. Pharmacokinetics， tissue distribution and metabolism of senkyunolide I， a major bioactive component in Ligusticum chuanxiong Hort. J Ethnopharmacol， 2012， 142(3)：706-713.
ZHAO Y H， JIA X B， CHEN Y， et al. Studies on rat intestinal absorption of the total flavones of epimedium in situ. Chin Pharm J(中国药学杂志)，2008， 43(3)188-191.
WEI H， LBENBERG R. Biorelevant dissolution media as a predictive tool for glyburide a class II drug. Eur J Pharm Sci， 2006， 29(1)45-52.
LI S C， LIU J P， ZENG Z Z， et al. Study on the solubility and permeability of TanshinoneⅡA and on the excipients increasing the solubility and permeability . Lishizhen Med Mater Med Res(时珍国医国药)，2008， 19(7)：1724-1726.
HONG L J， PAN W S， PAN Y S， et al. Intestinal absorption kinetics of nimesulide in rats in vivo. Chin J New Drugs Clin Rem(中国新药与临床杂志)，2009， 28(2)：130-133.
NAGARE N， DAMRE A， SINGH K S， et al. Determination of site of absorption of propranolol in rat gut using in situ single-pass intestinal perfusion. Indian J Pharm Sci， 2010， 72(5)：625-629.
FAGERHOLM U， JOHANSSON M， LENNERNS H. Comparision between permeability coefficients in rat and human jejunum. Pharm Res， 1996， 13(9)：1336-1342.

基金

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)
PDF(823 KB)

Accesses

Citation

Detail
段落导航
相关文章

/

〈 〉