盐酸美普他酚注射液在健康人体的药动学研究

Pharmacokinetics of meptazinol hydrochloride injection in healthy volunteers

摘要：目的研究盐酸关普他酚注射液在健康志愿者体内的药动学。方法采用随机开放、二重3X3拉丁方试验设计，12名健康志愿者（男女各半），分别单剂量肌内注射50、100或150mg三种剂量的盐酸美普他酚注射液后，采用HPLC—MS／MS法测定血浆中美普他酚浓度，计算药动学参数。结果盐酸美普他酚注射剂5（1、100或150mg三个剂量组的AUC0-t分别为（416．1±76．43），（934．9±180．8）和（1515±343．37）μg／（h·L）；AuC0-∞分别为（431±79．76），（960．1±192．8）和（1552±351．1）μg／（h·L）；Cmax分别为（163．3±53．96），353．9±83．28）和（519．4±117．4）LLg／L；tmax分别为（0．59±058），（0.36±0．12）和（0．56±0．39）h；t1／2分别为（2．41±0．54），（2．17±0.35）和（2．12±0．24）h。结论单次肌内注射50-150mg剂量范围内的盐酸美普他酚注射液后，关普他酚的体内过程符合1级速率线性动力学过程。，

[ Objective ] To evaluate the pharmacokinetics of meptazinol hydrochloride injection in Chinese healthy volunteers. [Methods] 12 healthy volunteers were received a single dose of 50, 100 or 150 mg meptazinol hy- drochloride intramuscularly. Concentrations of meptazinol in plasma were determined by HPLC-MS/MS. [ Results ] The main pharmacokinetic parameters of three groups were as follows： AUC0-t were （416.1_±76.43）, （934.9±180.8） and （1 515±343.37） μg/（h＇L）; AUCO-∞ were （431±79.76）, （960.1±192.8） and （1 552±351.1）pog/（h＇L）; Cmax were （163.3±53.96）, （353.9±83.28） and （519.4±117.4）μg/L; tmax were （0.59±0.58）, （0.36±0.12） and （0.56±0.39）h; tl/2 were （2.41±0.54）, （2.17±0.35） and （2.12±0.24）h, respectively. [Conclusion] The plasma concentrations of meptazi- nol in Chinese healthy volunteers were proceeded in an apparently mono-exponential fashion after a single dose of 50, 100 or 150 mg meptazinol hydrochloride intramuscularly.