右酮洛芬氨丁三醇注射液的人体药动学研究

目的:研究进口右酮洛芬氨丁三醇注射液在中国健康志愿者的人体药动学。方法:采用随机、开放、单剂量和多剂量口服给药的单中心试验方案。12位健康受试者单剂量和多剂量(50mg)静脉滴注右酮洛芬氨丁三醇注射液,采用液-质联用(LC-MS)法测定右酮洛芬氨的血药浓度,利用WinNonLin6.2计算药动学参数。结果:单剂量和多剂量静脉滴注右酮洛芬氨丁三醇的药动学参数为:c_(max)(6.698±1.058)、(5.088±0.525)μg·mL~(-1),t_(1/2)(2.2±0.3)、(2.4±0.7)h,t_(max)(0.5±0.1)、(0.5±0.1)h,AUC(8.043±0.907)、(6.120±0.796)μg·h·mL~(-1)。结论:右酮洛芬氨丁三醇注射液单剂量和多剂量给药的主要药动学参数的差异无统计学意义;右酮洛芬在人体内无明显蓄积。

Pharmacokinetics Study of Dexketoprofen Trometamol Injection in Healthy Volunteers

OBJECTIVE： To study the pharmacokinetics of imported Dexketoprofen trometamol injection in Chinese healthy volunteers. METHODS： In single center scheme of randomized open single and multiple oral dose, 12 Chinese healthy volunteers were randomized to administer a single and multiple dose （50 mg） of Dexketoprofen trometamol injection. The plasma concentra- tion of dexketoprofen trometamol was determined by LC-MS and its pharmacokinetic parameters were calculated by WinNonLin 6.2. RESULTS： The main pharmacokinetic parameters of dexketoprofen trometamol after a single dose and multiple dose were as follows： cmax were （6.698 ±1.058）μg·mL^-1 and （5.088 ± 0.525） μg·mL^-1,t1/2 were （2.2 ± 0.3）h and （2.4 ± 0.7）h, tmax were （0.5 ±0.1）h and （0.5 ± 0.1）h, AUC were （8.043 ±0.907）μtg·h·mL^-1 and （6.120± 0.796） μg·h·mL^-1, respectively. CONCLUSION： There is no significant difference in pharmacokinetic parameters of Dexketoprofen trometamol injection after a single and multiple administration, with no accumulation after administration.