重组人内抑素在猕猴体内的药物代谢动力学  

The pharmacokinetic study of recombinant human endostatin in monkeys

作　　者：张锋[1] 陈飞虎[1] 

机构地区：[1]安徽医科大学药学院,合肥230032

出　　处：《安徽医科大学学报》2011年第8期762-764,共3页Acta Universitatis Medicinalis Anhui

摘　　要：目的通过静脉及皮下给药,研究重组人内抑素(rhEndostatin)在猕猴体内的药物代谢动力学过程,为临床合理用药提供依据和参考。方法通过高效液相色谱法和放射性检测法分别测定静脉及皮下给药后猕猴血液中重组人内抑素的放射性活性以及其浓度,进而求出其药物代谢动力学参数。结果静脉及皮下给药后,其主要药物代谢动力学参数分别为:t1/2α254 min,t1/2β764 min,平均滞留时间(MRT)969 min,曲线下面积(AUC)2 893 mg/L.min-1;Cmax4.01 mg/L,Tmax30 min,MRT1 982 min,AUC 2 502 mg/L.min-1。结论皮下给药不仅吸收速度较快,且吸收程度也很高,绝对生物利用度达到86.5%,提示皮下给药是合理的给药方式。Objective To study the pharmacokinetics process about recombinant human endostatin（rhEndostatin） in monkeys by intravenous and subcutaneous administration.To provide the reference of the clinical rational drug using.Methods The concentration and radioactivity of rhEndostatin in blood were calculated by high performance liquid chromatography and radioactive detection to calculate pharmacokinetic parameters.Results The main pharmacokinetic parameters of intravenous and subcutaneous administration were t1/2α 254 min,t1/2β764 min,MRT 969 min,AUC 2 893 mg/L·min-1;Cmax 4.01 mg/L,Tmax 30 min,MRT 1 982 min,AUC 2 502 mg/L·min-1 respectively.Conclusion Subcutaneous administration has a faster and higher process of absorption and the absolute bioavailability is 86.5%,which is a reasonable way.

关 键 词：内皮抑素类/药代动力学 色谱法 高压液相 

分 类 号：R977.6[医药卫生—药品]