白花蛇舌草注射液中对香豆酸的药代动力学研究  

Study on Pharmacokinetics of p - Coumaric Acid in Baihuasheshecao Injection

作　　者：冉桂梅[1] 何彬[1] 姚国灿[1] 宝炉丹[1] 郭兴杰[1] 

机构地区：[1]沈阳药科大学,沈阳110016

出　　处：《药物分析杂志》2005年第7期759-761,共3页Chinese Journal of Pharmaceutical Analysis

摘　　要：目的:建立反相高效液相色谱法对白花蛇舌草中对香豆酸进行药代动力学研究。方法:血浆样品用甲醇沉淀蛋白,采用Diamonsil C18色谱柱(200 mm×4.6 mm,5μm),流动相为乙腈-1%醋酸(21:79,v/v),流速1.0 mL·min-1,检测波长为 322 nm,进样量为20 μL,内标为橙皮苷。结果:对香豆酸浓度在0.085-10.6μg·mL-1(r=0.9990)时与对香豆酸和橙皮苷峰面积比呈良好的线性关系,提取回收率和方法回收率分别为97.6%-110.0%和96.1%-100.5%,日内和日间的RSD均小于10%,大鼠腹腔注射白花蛇舌草注射液后,对香豆酸的药动学行为符合二室模型,Ka为(0.260±0.050)min-1,T1/2(Ka)为 (6.77±3.34)min,T1/2α为(33.83±8.52)min,T1/2β为(2.78±0.58)min,k21为(0.0676±0.0538)min-1,k10为(0.0489± 0.0154)min-1,k12为(0.0463±0.0354)min-1,AUC为(124.3±62.8)μg·min·mL-1,Tmax和Cmax实测值分别为(6.19± 0.99)min和(3.27±1.46)μg·mL-1。结论:该方法灵敏、准确,适合于对香豆酸的药代动力学研究。Objective:To develop a sensitive and specific HPLC method for study the pharmacokinetics of p-coumaric acid in rat. Methods: After ip of Baihuasheshecao injection in rat, the plasma samples were purified after precipitation of protein with methanol. The internal standard was hesperidin. The operation was carried out on the Diamonsil C18 column with the mobile phase consisting of a mixture of acetonitrile - 1% acetic acid (21:79 ,v/v) at a flow rate of 1.0 mL·min -1. The detection wavelength was 322 nm. The injection volume was 20μL. Results: The calibration curve was linear in the range of 0.085-10.6μg·mL-1 (r=0.9990)for p - coumaric acid. The concentration - time curve of p - coumaric acid in rat after ip administration was shown to fit two - compartment open model. The pharmacokinetic parameters of p-coumaric acid were as follows:Ka = (0.260±0. 050) min-1 ; T1/2(Ka) = (6.77±3.34) min;T1/2a=(33.83±8.52) min; T1/2β= (2.78±0.58) min; k21=(0.0676±0.0538) min-1; k10=(0.0489±0.0154) min-1; A12 = (0.0463±0.0354) min-1; AUC=(124.3±62.8) μg·min·mL-1; Tmax= (6.19±0.99) min;Cmax = (3.27±1.46) μg·mL-1. Conclusion:The method is sensitive,accurate with a good reproductivity.

关 键 词：白花蛇舌草注射液 药代动力学研究 对香豆酸 反相高效液相色谱法 C18色谱柱 提取回收率 沉淀蛋白 血浆样品 检测波长 线性关系 腹腔注射 二室模型 橙皮苷 流动相 峰面积 酸浓度 RSD k12 min AUC 

分 类 号：R818.82[医药卫生—放射医学] R285.6[医药卫生—临床医学]