盐酸曲马朵在健康中国志愿者体内的药动学差异  

Pharmacokinetic differences of tramadol hydrochloride in healthy Chinese volunteers

作　　者：葛萍[1] 宋敏[1] 杭太俊[1] 

机构地区：[1]中国药科大学药物分析教研室,南京210009

出　　处：《中国新药杂志》2007年第17期1415-1418,共4页Chinese Journal of New Drugs

摘　　要：目的:考察健康中国志愿者单剂量口服盐酸曲马朵片后体内药动学的差异。方法:12例健康中国志愿者单剂量口服75mg盐酸曲马朵片后,用液相色谱-荧光法测定血浆药物浓度经时过程,DAS2.0程序计算主要药动学参数。结果:血浆盐酸曲马朵测定的线性范围为2.0～500μg.L-1,定量下限为2.0μg.L-1。测得的主要药动学参数Cmax,Tmax,t1/2,AUC(0-τ),AUC(0-∞),MRT(0-τ),MRT(0-∞),CL/F和V/F分别为(336.17±69.93)μg.L-1,(2.4±0.9)h,(7.27±3.01)h,(3231.44±1319.4)h.μg.L-1,(3820.57±2118.02)h.μg.L-1,(7.80±1.31)h,(10.97±4.40)h,(24.49±10.95)L.h-1和(222.10±50.83)L。结论:盐酸曲马朵在健康中国志愿者体内存在明显的代谢类型差异,临床需加强个体用药监测。Objective： To study the pharmacokinetic differences of tramadol hydrochloride in 12 healthy Chinese volunteers after a single oral dose of 75 mg tramadol hydrochloride tablets. Methods： A sensitive and specific HPLC-FLD method was established for the determination of tramadol hydrochloride in human plasma. DAS 2.0 program was used for the pharmacokinetic analysis. Results： The linear calibration curves were obtained in the concentration range from 2.0 to 500μg·L^-1 with the lower limit of quantification being 2.0μg·L^-1. The main pharmacokinetic parameters of Cmax,Tmax,t1/2,AUC（0-τ）,AUC（0-∞）,MRT（0-τ）,MRT（0-∞） , CL/F and V/F for 12 healthy volunteers were （336.17±69.93 ）μg·L^-1,（2.4±0.9）h,（7.27±3.01）h,（3231.44±1319.40）h·μg·L^-1, （3820.57±2118.02） h·μg·L^-1, （7.80±1.31）h,（10.97±4.40）h , （24.49±10.95）L·μg·L^-1 and （222.10±50.83）L, respectively. Conclusion： There are remarkable pharmacokinetic differences of trarnadol hydrochloride between extensive and intermediate metabolize volunteers. Therefore, clinical monitoring should be conducted.

关 键 词：盐酸曲马朵 药动学差异 液相色谱-荧光法 

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