制何首乌3种成分在动脉粥样硬化大鼠血浆中的测定

Determination of three constituents in Polygoni multiflori Radix Praeparata in plasma of atherosclerosis rats

目的测定制何首乌Polygoni multiflori Radix Praeparata 3种成分在动脉粥样硬化大鼠血浆中的含有量。方法大鼠灌胃制何首乌CMC-Na溶液后,采集血浆。HPLC分析采用Hypersil C18色谱柱(250 mm×4.6 mm,5μm);流动相乙腈-0.03%磷酸,梯度洗脱;体积流量0.9 m L/min;检测波长280 nm,柱温30℃。DAS2.0软件绘制血药浓度-时间曲线,计算药动学参数。结果二苯乙烯苷、大黄素、大黄素甲醚分别在61.25~6 125μg/L(r=0.999 8)、12.6~3 150μg/L(r=0.999 3)、24.1~6 030μg/L(r=0.999 5)范围内线性关系良好,方法回收率99.5%~105.8%,RSD 1.3%~3.3%;提取回收率87.2%~96.3%,RSD 3.2%~5.9%。3种成分的药动学行为均符合二室模型,但其在血浆中的含有量远低于在药材中。结论二苯乙烯苷、大黄素和大黄素甲醚在动脉粥样硬化大鼠血浆中生物利用率较低,可能与灌胃制何首乌后成分的肠道吸收有关。

AIM To establish an HPLC method for determining the contents of three constituents in Polygoni multiflori Radix Praeparata in plasma of atherosclerosis rats. METHODS After the rats were intragastrically administrated with Polygoni multiflori Radix Praeparata CMC-Na solution,the plasma was collected. The HPLC analysis was carried out on a 30 ℃ thermostatic Hypersil C18column（ 250 mm × 4. 6 mm,5 μm）,with the mobile phase comprising of acetonitrile-0. 03% phosphoric acid flowing at 0. 9 m L / min in a gradient elution manner,and the detection wavelength was set at 280 nm. DAS2. 0 software was applied to drawing concentration-time curves and calculating pharmacokinetic parameters. RESULTS Stilbene glucoside,emodin and physcion showed good linear relationships within the ranges of 61. 25-6 125 μg / L（ r = 0. 999 8）,12. 6-3 150 μg / L（ r = 0. 999 3） and24. 1-6 030 μg / L（ r = 0. 999 5）,respectively. The method recoveries were 99. 5%-105. 8% with the RSDs of1. 3%-3. 3%,while the extraction recoveries were 87. 2%-96. 3% with the RSDs of 3. 2%-5. 9%. The pharmacokinetic behaviors of three constituents all accorded with two-compartment model,but their contents in plasma were much lower than those in medicinal material. CONCLUSION The bioavailabilities of stilbene glucoside,emodin and physcion are relatively low in plasma of atherosclerosis rats,which may be related to constituents＇ intestinal absorption after intragastric administration with Polygoni multiflori Radix Praeparata.