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[大鼠黄连提取物中小檗碱和药根碱的原位肠道吸收动力学]

[In situ intestinal absorption kinetics of berberine and jatrorrhizine from extractive Rhizoma Coptidis in rats].

作者信息

Tan Xiaomei, Guo Youli, Zhong Yufei

机构信息

Key Research Laboratory of New Traditional Chinese Drugs, School of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, China.

出版信息

Zhongguo Zhong Yao Za Zhi. 2010 Mar;35(6):755-8. doi: 10.4268/cjcmm20100621.

Abstract

OBJECTIVE

To investigate the in situ absorption kinetics of berberine (BER) and jatrorrhizine( JAT) at different intestine segments in rats.

METHOD

The intestinal perfusion experiment was performed on rats in vivo to observe the effects of absorption sites and drug concentration on the intestinal absorption characteristics of BER and JAT.

RESULT

The apparent absorption rate constants (Ka) of BER and JAT at duodenum, jejunum, ileum and colon were 0.1540, 0.1160, 0.9793, 0.6795 h(-1) and 0.0743, 0.0564, 0.0456, 0.0234 h(-1), respectively. The absorption of BER and JAT decreased according to the turn of duodenum, jejunum, ileum and colon. Compared to the lower segment, BER and JAT were better absorbed at the upper and middle segments of intestine in rats. The Ka of BER and JAT had no significant difference when the concentration of the extractive Rhizoma Coptidis was at 22-88 mg x L(-1). However, the absorption quantity of BER and JAT were proportional to the concentration respectively and the saturated phenomena were not observed.

CONCLUSION

Both the BER and the JAT is can be absorbed in whole intestine and the results indicated that the absorption of BER and JAT compiled with the first order kinetics through passive diffusion mechanism.

摘要

目的

研究大鼠不同肠段小檗碱(BER)和药根碱(JAT)的原位吸收动力学。

方法

对大鼠进行体内肠灌注实验,观察吸收部位和药物浓度对BER和JAT肠吸收特性的影响。

结果

BER和JAT在十二指肠、空肠、回肠和结肠的表观吸收速率常数(Ka)分别为0.1540、0.1160、0.9793、0.6795 h⁻¹和0.0743、0.0564、0.0456、0.0234 h⁻¹。BER和JAT的吸收按十二指肠、空肠、回肠和结肠的顺序降低。与下段相比,大鼠肠道上段和中段对BER和JAT的吸收更好。当黄连提取物浓度为22 - 88 mg·L⁻¹时,BER和JAT的Ka无显著差异。然而,BER和JAT的吸收量分别与浓度成正比,未观察到饱和现象。

结论

BER和JAT均可在全肠道吸收,结果表明BER和JAT的吸收符合一级动力学,通过被动扩散机制进行。

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