美洛昔康注射液人体的药动学研究

Pharmacokinetics of Meloxicam Injection in Chinese Healthy Volunteers

目的研究单剂量和多剂量肌注美洛昔康后的药代动力学。方法30名健康志愿者单剂量肌注3.75、7.5、15mg和11名健康志愿者7次肌注7.5mg后,采用LC/MS/MS法测定血浆中美洛昔康的浓度,DAS软件对各组药-时曲线进行拟合,并计算药代动力学参数。结果其药-时曲线符合开放性二室模型,呈一级消除动力学;分别得到3个单剂量组及多剂量组美洛昔康的Cmax、Tmax、AUC0-96h、t1/2β、MRT0-∞、Vd/F、CL/F各值;单剂量组28名强代谢型的Cmax、AUC0-96h与给药剂量呈线性正相关。结论各组受试者注射后耐受性好,其在受试者体内的药动学存在明显个体差异。可为美洛昔康注射液在临床用药的安全性和有效性提供依据。

Aim To study the pharmacokinetics of meloxicam after a single and multiple muscular injection in healthy volunteers. Methods After a single dose of 3.75mg,7.5 mg and 15 mg in 30 volunteers, and daily dose of 7.5mg for 7days in 11 volunteers, a HPLC/MS/MS method was used to determine the plasma concentration of meloxicam. The plasma concentration-time curves were simulated by Drug And Statistic software and the pharmacokinetic parameters were calculated. Results The plasma concentration-time curves of meloxicam were consistent with the two-compartment model with first order rate elimination,The pharmacokinetic parameters of the three single-doses and multiple-dose were as follows：Cmax、Tmax、AUC0-96h、t1/2β、MRT0-∞、Vd/Fand CL/F respectively. The Cmax and AUC0-96h were in highly linear positive correlation with the doses in the single-dose group. Conclusion The tolerance of meloxicam injection was good for all volunteers, and there were significant individual differences in the pharmacokinetics of meloxicam in volunteers. The results may provide evidence of safety and effectiveness for clinical use of meloxicam injection.