盐酸度洛西汀肠溶片在健康人体内的药动学  

Pharmacokinetics of duloxetine hydrochloride enteric-coated tablets in healthy volunteers

作　　者：刘家稳[1] 赵瑞柯[1] 程刚[1] 唐靖[1] 宋娟[1] 彭文兴[1] 

机构地区：[1]中南大学湘雅二医院临床药学教研室,湖南长沙410011

出　　处：《中国医院药学杂志》2009年第17期1451-1454,共4页Chinese Journal of Hospital Pharmacy

摘　　要：目的:研究盐酸度洛西汀肠溶片在健康人体内的药动学。方法:采用液相色谱-串联质谱法(LC-MS/MS)测定健康志愿者单剂量和多剂量口服盐酸度洛西汀肠溶片后的血药浓度,计算药动学参数。结果:健康志愿者单剂量口服30,60,90mg盐酸度洛西汀肠溶片,Cmax为(22.5±15.2),(44.4±17.2),(60.8±27.8)μg·L-1,AUC0-60为(328.6±203.6),(696.0±337.8),(1219.3±598.3)μg.h.L-1,AUC0-∞为(359.7±201.0),(733.8±343.4),(1280.5±644.81)μg.h.L-1,tmax为(6.8±2.0),(6.1±1.3),(6.6±1.6)h,t1/2为(13.0±3.6),(12.8±2.3),(11.7±2.1)h。Cmax、AUC0-60、AUC0-∞在30～90mg内与给药剂量呈线性关系。统计分析结果表明tmax、t1/2在上述不同剂量组之间差异无显著性(P>0.05)。受试者连续给药3d后血药浓度达稳态,达到稳态后的Csmsax为(47.3±17.0)μg·L-1,Csmsin为(27.9±9.5)μg·L-1,AUC(ss0-12)为(407.25.6±125.9)μg.h.L-1。结论:盐酸度洛西汀肠溶片体内吸收程度(Cmax、AUC0-60)在30～90mg给药剂量内具有线性动力学特征。OBJECTIVE To study the pharmacokinetics of duloxetine hydrochloride enteric-coated tablets in healthy volun teers, METHODS Determine the concentration of duloxetine in plasma after the volunteers＇ administration of a single dose or multiple doses of duloxetine by liquid chromatographytandem mass spectrometry （LC MS/MS）. RESULTS After the healthy volunteers received a single dose of 30,60,90 rng duloxetine, the main pharmacokinetics parameters were as follows：Cmax were （22.5±15.2）,（44.4±17.2）,（60.8±27.8）μg·L^-1,AUC0-60were（328.6±203.6）,（696.0±337.8）,（1219.3±598.3）μg·h·L^-1,AUC0-∞were（359.7±201.0）,（733.8±343.4）,（1280.5±644.81）μg·h·L^-1,tmax were（6.8±2.0）,（6.1±1.3）,（6.6±1.6）h,t1/2were（13.0±3.6）,（12.8±2.3）,（11.7±2.1）h.Cmax、AUG0-∞. In the dose of 30 - 90 rag there was a significantly dependability between Cmax, AUC0- 60 ,AUC0-∞ and dosage. The statistical result showed that tmax ,t1/2 had no significant difference（P〉0. 05） in three groups. Steady state was achieved after 3 day consecutive administration. Cmax was （47.3±17.0）μg·L^-1,Gmaxs were（27.9±9.5）μg·L^-1,AUC（0-12）were（407.25.6±125.9）μg·h·L^-1. CONCLUSION The dynamics of duloxetine hydrochloride enteric-coated tablets in vivo are linear in the dosage of 30-90 mg. KEY WORDS： duloxetine hydrochloride; pharmacokinetics; LC-MS/MS

关 键 词：盐酸度洛西汀 药动学 液相色谱一串联质谱 

分 类 号：R978.15[医药卫生—药品] R969.1[医药卫生—药学]