盐酸莫西沙星片在健康志愿者体内两种条件下的药动学研究

Pharmacokinetics of Moxifloxacin hydrochloride tablets in the healthy volunteers under two conditions

目的研究盐酸莫西沙星片在健康志愿者体内两种条件下的药动学。方法采用随机交叉自身对照试验设计,24名健康男性志愿者随机交叉单剂量空腹(或餐后)口服400 mg盐酸莫西沙星片。采用HPLC-UV法测定受试者血浆中莫西沙星的浓度,计算药动学参数,评价制剂在两种条件下的药动学行为。结果空腹条件下,盐酸莫西沙星片的主要药动学参数为:Tmax=1.55±0.96 h,Cmax=3.45±0.88μg·m L-1,AUC0-t=58.77±13.02μg·m L-1·h,AUC0-∞=60.50±13.71μg·m L-1·h;餐后条件下,盐酸莫西沙星片的主要药动学参数为:Tmax=2.66±1.48 h,Cmax=3.16±0.70μg·m L-1,AUC0-t=57.01±9.95μg·m L-1·h,AUC0-∞=59.00±10.60μg·m L-1·h。结论餐后与空腹条件相比,除了Tmax有所延迟外,其余药动学参数均无太大差别,表明食物可能会减缓盐酸莫西沙星的吸收。

OBJECTIVE To investigate the pharmacokinetics of Moxifloxacin hydrochloride tablet（ MH） in healthy volunteers under two conditions. METHODS A single oral dose of 400 mg of MH was given respectively to 24 healthy male volunteers according to an open randomized crossover design under fasting or postprandial condition. The plasma concentration of MH was determined by HPLC-UV method,and the pharmacokinetic parameters were calculated. The pharmacokinetic behaviors under two conditions were estimated.RESULTS The main pharmacokinetic parameters of MH under fasting condition were as followings： Tmaxwas 1. 55 ± 0. 96 h,Cmaxwas3. 45 ± 0. 88 μg·mL^-1,AUC0- twas 58. 77 ± 13. 02 μg·mL^-1·h,AUC0- ∞was 60. 50 ± 13. 71 μg·mL^-1·h. The main pharmacokinetic parameters of MH under postprandial condition were as followings： Tmaxwas 2. 66 ± 1. 48 h,Cmaxwas 3. 16 ± 0. 70 μg·mL^-1,AUC0- t was 57. 01 ± 9. 95 μg·mL^-1·h,AUC0- ∞was 59. 00 ± 10. 60 μg·mL^-1·h. CONCLUSION Compared to the fasting condition,except that the Tmaxof postprandial condition was delayed,other pharmacokinetic parameters barely have difference between each other. The results show that food may delayed the absorption of MH.