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目的:研究炒白芍提取物中芍药苷(Pae)在大鼠不同肠段的肠外翻囊模型中的吸收动力学特征及其与P-gp的相互作用。方法:采用大鼠肠外翻囊模型,以Pae为炒白芍提取物中代表成分,用HPLC对其进行检测,计算Pae的肠吸收动力学参数,分析Pae的肠吸收特征。结果:炒白芍提取物不同浓度时Pae在不同肠段的吸收均为线性吸收,其回归相关系数的平方(R2)均>0.9以上,符合零级吸收;其Ka随给药剂量的增加而增加,说明其为被动吸收。Pae在不同肠段吸收总趋势为空肠>回肠>结肠。炒白芍提取物与维拉帕米(Ver)合用时,Pae在回肠中吸收显著增加(P<0.05);口服炒白芍提取物后,在回肠段对Rho 123的外排量增加(P<0.01)。结论:Pae在肠道中吸收为零级吸收,吸收机制为被动吸收。Pae可能为P-gp底物,炒白芍提取物能诱导肠道中P-gp的表达。
OBJECTIVE: To study the absorption kinetics of paeoniflorin (Pae) in rat intestinal rotator capsules of different intestinal segments and its interaction with P-gp. METHODS: The rat intestine pellicle model was used. Pae was selected as the representative component in the extract of Radix Paeoniae Rubra. HPLC was used to determine the Pae’s intestinal absorption kinetic parameters and the intestinal absorption characteristics of Pae were analyzed. RESULTS: The absorption of Pae in different intestinal segments was linearly absorbed when the extracts were used at different concentrations. The squared regression coefficients (R2) were all above 0.9, which was in accordance with the zero-order absorption. The Ka was increased with the increase of the dose. Increase, indicating that it is passively absorbed. The total absorption of Pae in different intestinal segments was jejunum> ileum> colon. The absorption of Pae in the ileum was significantly increased when the fried white peony root extract was combined with verapamil (Ver) (P<0.05); after oral administration of the extract, the efflux of Rho 123 in the ileum segment increased (P<0.05). <0.01). Conclusion: Pae absorbs zero-level absorption in the intestine, and the absorption mechanism is passive absorption. Pae may be a P-gp substrate, and the extract of fried peony can induce the expression of P-gp in the intestine.