阿托伐他汀钙与阿昔莫司联用在中国健康人体的药代动力学

Pharmacokinetic study of atorvastatin coadministrated with acipimox in healthy volunteers

目的评价阿托伐他汀钙与阿昔莫司联用后在中国健康人体内的药代动力学特征。方法 18名健康受试者单次空腹同时口服阿托伐他汀钙10 mg与阿昔莫司250 mg后,分别用LC-MS/MS,HPLC测定不同时间点血浆中阿托伐他汀与阿昔莫司的浓度,DAS 2.1软件计算相应的药代动力学参数。结果药代动力学参数如下,阿托伐他汀:t1/2为(11.75±2.48)h,tmax为(0.33±0.12)h,Cmax为(11.33±4.36)ng·mL-1,AUC0-t为(57.57±25.91)ng·mL-1·h;阿昔莫司:t1/2为(1.55±0.18)h,tmax为(1.32±0.62)h,Cmax为(3.65±1.08)μg·mL-1,AUC0-t为(12.84±2.73)μg·mL-1·h。与单独给药药代动力学参数基本接近。结论阿托伐他汀与阿昔莫司联用后彼此药代动力学行为未发生明显改变,联用可能不存在药代动力学方面的相互作用。

Objective To study the pharmacokinetic characteristics of atorvastatin coadministrated with acipimox in Chinese healthy volunteers. Methods Eighteen volunteers were given atorvastatin 10 mg together with acipimox 250 mg. The concentrations of atorvastatin and acipimox in plasma were analyzed by LC -MS/MS and HPLC, respectively. The phar- macokinetic parameters were calculated with DAS 2.1 sofwtare. Results The main pharmacokinetic parameters for atorvastatin were as follow： t1/2 were （11.75 ±2.48） h, tmax were （0.33 ±0. 12）h, Cmax were （11.33 ± 4.36） ng . mL-1, AUC0-t, were （57.57 ±25.91） ng . mL-1. h, respec- tively. The main pharmacokinetic parameters for acipimox were as follow： t1/2 were （1.55 ±0. 18）h, tmax were （1.32 ±0. 62）h, Cmax were （3.65 ± 1.08） μg .mL-1, AUC0-t, were （12.84 ± 2.73） μg . mL-1. h. The results are concordant with those after administration of atorvastatin and acipimox alone. Conclusion The pharmacokinetic charateristics of atorv- astatin and acipimox may not be changed with each other after atorvastatin coadministrated with acipimox in Chinese healthy volunteers.