盐酸美普他酚注射液在健康人体的药代动力学  

Pharmacokinetics of meptazinol hydrochloride injection in healthy volunteers

作　　者：黄露[1] 葛苗苗[1] 舒成仁[1] 卫乐乐[1] 黎维勇[1] 

机构地区：[1]华中科技大学同济医学院附属协和医院临床药学室,武汉430022

出　　处：《中国临床药理学杂志》2011年第1期29-32,共4页The Chinese Journal of Clinical Pharmacology

摘　　要：目的在中国健康志愿者中进行盐酸美普他酚注射剂(麻醉镇痛药)的药代动力学研究。方法 36名健康志愿者分为3个剂量组(静注25和50 mg);肌肉注射给药(推注75 mg)。用HPLC-MS/MS法测定血浆中美普他酚浓度变化,以DAS2.0软件进行数据处理,求算药代动力学参数。结果盐酸美普他酚注射剂3个剂量组的AUC0-t分别为(241.50±50.25),(621.72±208.10)和(898.16±194.29)ng.h.mL-1;AUC0-∞分别为(247.79±51.98),(636.10±213.05)和(921.14±214.86)ng.h.mL-1;Cmax分别为(203.58±38.61),(393.98±66.92)和(347.64±72.94)ng.mL-1;tmax分别为(0.05±0.02),(0.05±0.02)和(0.56±0.33)h;t1/2分别为(2.24±0.85),(2.19±0.66)和(2.18±0.42)h;静脉给药2个剂量组间药代动力学参数(AUC0-∞,Cmax,t1/2z,CLz,Vz)差异无统计学意义。单次肌肉推注75 mg组相对单次静脉推注50 mg组,计算平均相对生物利用度为96.54%。结论静脉注射给药25～50 mg时,盐酸美普他酚在中国健康人体内AUC,AUC,C随着剂量的增加而增加。Objective To evaluate the pharmacokinetics of meptazinol hydrochloride injection in Chinese healthy volunteers. Methods Thirty -six healthy volunteers were devided into three groups. Two groups received a single dose of 25 mg and 50 mg meptazinol hydrochloride intravenously, the other group received a single dose of 75 mg meptazinol hydrochloride intramuscularly. Concentrations of meptazinol in plasma were determined by HPLC - MS/MS. The pharmacokinetic parameters were calculated by DAS 2.0 software. Results The main pharmacokinetie parameters of three groups were as follows： AUC0-1, were （241.50 ±50. 25）, （621.72 ±208.10） and （898.16 ± 194.29） ng · h · mL^-1 ; AUC0-∞ were （247.79 ±51.98）, （636. 10 ±213.05） and （921.14 ± 214. 86） ng · h · mL^-1; Cmax were （203.58 ± 38.61）, （393.98 ± 66.92） and （347.64±72.94） ng · mL-1;tmax were （0.05 ±0.02）, （0.05 ±0. 02） and （0. 56 ±0. 33） h;t1/2 were （2.24 ±0. 85） ,（2. 19 ± 0.66） and （2. 18 ± 0. 42 ） h, respectively. There were no significant difference of AUC0-∞ , C t1/2z, CLz, Vz in two groups （ intravenous groups） by analysis of variance. The relative bioavailability of 75 mg intramuscularly to 50mg intravenously was 96.54%. Conclusion The pharmacokinetic parameters such as AUC0-t, AUC0-∞, C directly propotion to doses of 25 -50 mg intravenously in human body.

关 键 词：盐酸美普他酚注射剂 药代动力学 高效液相色谱-串联质谱 

分 类 号：R969.1[医药卫生—药理学] R971.2[医药卫生—药学]