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研究重组人血管内皮抑素(rhEndostatin)静脉注射后在Beagle犬体内的药代动力学过程,为临床应用提供药代动力学数据。用酶联免疫吸附试验(ELISA)竞争法检测Beagle犬静脉注射rhEndostatin后不同时间的血药浓度,并将血药浓度-时间数据经计算机拟合,计算出相应参数。rhEndostatin静脉注射Beagle犬后,药物的分布半衰期平均为(0.34±0.04)h,消除半衰期为(16.5±1.6)h。血药浓度-时间曲线下面积(AUC)与剂量呈正相关,相关系数为0.999 9。血浆清除率(CLs)均值为(0.123±0.006)l/h,高、中、低剂量CLs基本相同。rhEndostatin在Beagle犬体内的药代动学过程基本符合线性药动学特征,血药浓度-时间曲线符合二房室模型。rhEndostatin在Beagle犬体内药代动力学过程的研究对其进一步开发具有指导价值。
To study the pharmacokinetics of recombinant human endostatin (rhEndostatin) in Beagle dogs after intravenous injection, and to provide pharmacokinetic data for clinical application. The plasma concentrations of rhEndostatin at different time after intravenous injection of rhEndostatin in Beagle dogs were detected by enzyme-linked immunosorbent assay (ELISA) competition method, and the corresponding parameters were calculated by computer. After intravenous injection of rhEndostatin into Beagle dogs, the half-life of drug distribution was (0.34 ± 0.04) h and the elimination half-life was (16.5 ± 1.6) h. The area under the plasma concentration-time curve (AUC) was positively correlated with the dose, with a correlation coefficient of 0.999 9. The plasma clearance (CLs) mean (0.123 ± 0.006) l / h, high, medium and low dose CLs basically the same. The pharmacokinetics of rhEndostatin in Beagle dogs was basically consistent with the linear pharmacokinetic characteristics, and the plasma concentration-time curve was in line with the two-compartment model. The study of pharmacokinetics of rhEndostatin in Beagle dogs has guiding value for its further development.