复方广痛消水提物中3个成分的离体直肠吸收动力学研究

目的考察复方广痛消水提物中有效成分延胡索乙素(THP)、盐酸小檗碱(Ber)和芍药苷(Pae)在大鼠直肠段的吸收特性。方法采用大鼠离体非翻转肠囊模型,以LC-MS/MS对不同浓度的复方广痛消水提物中的THP、Ber和Pae进行检测,计算各成分的吸收速率常数(Ka),分析它们在直肠部位的吸收特征。结果不同浓度复方广痛消水提物中的THP、Ber和Pae在直肠段均为线性吸收,r2均>0.95。随着THP浓度的增高其Ka无显著变化(P>0.05);Ber和Pae的Ka随着浓度的增加而增大(P<0.01)。结论 THP在直肠的吸收呈现一级动力学特征,其吸收形式可能为被动扩散;而Ber和Pae的吸收形式并非简单的被动扩散,可能有转运载体的介导。

In vitro rat rectal absorption kinetics of 3 components in extract of compound Guangtongxiao

Objective To investigate the in vitro absorption kinetics of tetrahydropalmatine（THP）, berberine hydrochloride（Ber） and paeonifl orin（Pae） of compound Guangtongxiao extracts in rat rectal segment. Methods The noneverted rectal sac model was adopted. Rectal sac fl uid samples at different time points after administration of 3 concentrations of compound Guangtongxiao extract were collected and detected by LC-MS/MS, and the absorption rate constants（Ka） to describe the character of absorption was calculated. Results The absorption of THP, Ber and Pae was linear at different concentrations, and the square of coefficient correlation exceeded 0.95. The Ka of THP remained the same when the extract was at different concentrations（P 0.05）, which was consistent with first order process. The Ka of Ber and Pae increased along with the raised dosage of compound Guangtongxiao extract（P 0. 01）, which conformed to the zero order process. Conclusion The absorption of THP in rat rectal is a first-order process with passive diffusion mechanism. The absorption of Ber and Pae in rat rectal is not simply passive diffusion, and transporter carrier may involve in the mediation.