盐酸度洛西汀肠溶片在中国健康受试者体内的药动学研究

Pharmacokinetics of enteric-coated duloxetine hydrochloride tablets in Chinese healthy volunteers

目的:建立LC-MS/MS测定人血浆中度洛西汀浓度的方法,并研究其在健康受试者体内的药动学。方法:36名受试者单剂量口服盐酸度洛西汀肠溶片60 mg后,0~72 h间隔采集血样,离心分取血浆测定血药浓度,采用DAS 2.0计算药动学参数。结果:健康受试者口服60 mg盐酸度洛西汀肠溶片后的主要药动学参数:C_(max)为(41.85±19.54)ng·m L-1,AUC_(0~72h)为(715±467)ng·h·m L^(-1),T_(max)为(6.44±2.06)h,t_(1/2)为(13.40±3.52)h。结论:该方法专属性好,灵敏、准确,能够有效的进行盐酸度洛西汀临床血样浓度的测定和药动学研究。

Objective： To establish an LC-MS /MS method for the determination of duloxetine in human plasma and study the pharmacokinetics of enteric-coated duloxetine hydrochloride tablets in Chinese healthy volunteers after a single oral dose. Methods： A single oral dose of 60 mg enteric-coated duloxetine hydrochloride tablets was given to 36 healthy volunteers. Blood samples were collected at predetermined time intervals between0 ~ 72 h. Concentrations of duloxetine in plasma were determined by LC-MS / MS and the pharmacokinetic parameters were calculated by DAS 2. 0 software. Results： The main pharmacokinetic parameters after a single dose of 60 mg enteric-coated duloxetine hydrochloride tablets were as follows： [Cmax（ 41. 85 ± 19. 54） ng·m L^-1,AUC0 ~ 72h（ 715 ± 467） ng·h·m L^-1,Tmax（ 6. 44 ± 2. 06） h,and t1 /2（ 13. 40 ± 3. 52） h],respectively. Conclusion：The method is specific,sensitive and accurate,and can be successfully applied to pharmacokinetic study of entericcoated duloxetine hydrochloride tablets after oral administration.