石菖蒲及其复方开心散中β-细辛醚的肠吸收特性研究

Intestinal absorption characteristics of β-asarone in Kaixinsan and Acori Tatarinowii Rhizoma

目的通过对石菖蒲及其复方开心散中β-细辛醚的肠吸收特性研究与对比,评价开心散配伍前后石菖蒲中有效成分β-细辛醚的肠吸收特性变化。方法采用大鼠翻转肠囊法,进行开心散和石菖蒲的肠吸收实验,用HPLC-DAD分析,选用Waters XbridgeTMshield C18色谱柱,流动相为乙腈-0.1%磷酸水溶液梯度洗脱,254 nm检测肠吸收液中β-细辛醚的含量,计算获得肠吸收动力学参数。结果开心散全方和石菖蒲提取物中β-细辛醚累积吸收药量均随时间线性增加,高、中、低三个剂量中β-细辛醚吸收速率常数(K_a)均无显著性差异,符合一级吸收模型。两个提取物中β-细辛醚的表观渗透系数(Paap)在三个剂量组间均无显著性差异,Paap均大于1×10^(-4)cm/min,吸收较好。综合Ka和Paap信息,开心散全方和石菖蒲提取物中β-细辛醚在大鼠小肠的吸收机制可能属被动扩散。结论对比石菖蒲提取物与开心散提取物中β-细辛醚的吸收百分率,开心散配伍前后β-细辛醚的吸收无显著性差异,说明开心散复方配伍对来自石菖蒲的类药成分β-细辛醚肠吸收无明显影响。

Objective To study the intestinal absorption characteristics ofβ-asarone in Kaixinsan and Acori Tatarinowii Rhizoma in rats.To evaluate the effects of the other drugs in Kaixinsan on intestinal absorption ofβ-asarone.Methods Everted intestinal sac model was used and the concentration ofβ-asarone was determined by HPLC-DAD.Baseline separation was achieved on an Waters Xbridge TM shield C18column with linear gradient elution of acetonitrile-0.1%polyphosphoric acid at a flow of1.0mL/min and detected at the wavelength254nm.The parameters of intestinal absorption ofβ-asarone were estimated.Results The result showed cumulated absorb dose ofβ-asarone increased linearly with the dosage both in Kaixinsan and Acori Tatarinowii Rhizoma.Absorption rate constant ofβ-asarone was no significant difference between three dosage groups andβ-asarone was first order absorption in the rat small intestine,which was consistent with Kaixinsan whole decoction and Acori Tatarinowii Rhizoma.single drug.Apparent permeability coefficients ofβ-asarone was also no significant difference between three dosage groups and were greater than1×10-4cm/min,which indicateβ-asarone is well-absorbed in the rat small intestine.In conclusion,β-asarone s absorption mechanisms can be passive diffusion.Conclusion Through study of intestinal absorption dynamics on Kaixinsan and Acori Tatarinowii Rhizoma single drugs,absorption dynamics parameter which obtained were compared with the Kaixinsan compound compatibility,the result showed that there were no significantly impacts on intestinal absorption ofβ-asarone in Acori Tatarinowii Rhizoma by compatibility.