Yan Bin, Xing Dongming, Ding Yi, Tao Jialin, Du Li-Jun
Institute of Medicinal Plant, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100094, China.
J Pharm Biomed Anal. 2005 Feb 23;37(2):297-301. doi: 10.1016/j.jpba.2004.10.046.
A new HPLC method for the determination of puerarin in cerebral ischemia reperfusion rat plasma is introduced. Puerarin, the principal bioactive component of puerariae radix isoflavone, was extracted from plasma by methanol. The HPLC separation was then performed on a reversed-phase C18 column using water-acetonitrile (89:11, v/v) as eluting solvent system, and UV detection at 252 nm to measure the analyte with a limit of quantitation about 9.44 ng ml(-1). The calibration curve for puerarin was linear (r=0.9998) in the concentration range of 9.44-1208.00 ng ml(-1), both intra- and inter-day precision of the puerarin were determined and their coefficient of variation did not exceed 10%. The validated method has been successfully applied for pharmacokinetic studies of puerarin from rat plasma after intravenous administration of puerariae radix isoflavone. Another novel finding of this study was that the elimination rate of puerarin was significantly slower in the cerebral ischemia reperfusion rat than in the normal rat, judging by the pharmacokinetic parameters obtained. Since puerariae radix isoflavone was mainly administrated to the patients suffering from cerebralvascular diseases, the pharmacokinetic studies performed on the pathological animal models were suitable references for clinical application.
介绍了一种测定脑缺血再灌注大鼠血浆中葛根素的高效液相色谱新方法。葛根素是葛根异黄酮的主要生物活性成分，采用甲醇从血浆中提取。然后在反相C18柱上进行高效液相色谱分离，以水 - 乙腈（89:11，v/v）作为洗脱溶剂系统，并在252 nm处进行紫外检测以测定分析物，定量限约为9.44 ng ml(-1)。葛根素的校准曲线在9.44 - 1208.00 ng ml(-1)浓度范围内呈线性（r = 0.9998），测定了葛根素的日内和日间精密度，其变异系数均不超过10%。该验证方法已成功应用于静脉注射葛根异黄酮后大鼠血浆中葛根素的药代动力学研究。本研究的另一个新发现是，根据获得的药代动力学参数判断，脑缺血再灌注大鼠中葛根素的消除速率明显慢于正常大鼠。由于葛根异黄酮主要用于治疗脑血管疾病患者，因此在病理动物模型上进行的药代动力学研究可为临床应用提供合适的参考。
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