两种注射用盐酸尼非卡兰在Beagle犬体内的药动学比较

Comparative study on the pharmacokinetics of two Nifekalant hydrochloride injections in Beagles

目的比较两种注射用盐酸尼非卡兰在Beagle犬体内的药动学特征。方法采用随机、交叉、自身对照的试验设计,将18只Beagle犬分别先后单次静脉注射两种盐酸尼非卡兰3.125 mg·kg^(-1),用HPLC法测定其血药浓度,用Win Non Lin 6.3软件计算药动学参数并进行比较。结果分别先后单次静脉注射相同剂量的盐酸尼非卡兰供试和参比制剂3.125 mg·kg^(-1)后,犬血浆中尼非卡兰的AUC_(0→t)分别为118.01±15.74、116.39±47.66μg·m L^(-1)·min,AUC_(0→∞)分别为119.84±15.40、118.50±46.80μg·m L^(-1)·min,C_(max)分别为5.31±2.28、4.45±2.27μg·m L^(-1),T_(max)分别为1.67±1.63、1.00 min,t1/2分别为34.90±4.53、34.76±9.77 min。结论两种注射用盐酸尼非卡兰在Beagle犬体内的药动学过程无显著差异。

OBJECTIVE To compare the pharmacokinetics of two Nifekalant hydrochloride injections in Beagles. METHODS A randomized cross - over design experiment was adopt. Eighteen Beagles were received single dose of 3. 125 mg·kg^-1 of two kinds of Nifekalant hydrochloride injections by intravenous bolus successively. The plasma concentrations of Nifekalant hydrochlofide were meas- ured by an HPLC method. The pharmacokinetics parameters were calculated using software WinNonLin （ version 6.3 ）. The statistical analysis was performed using IBM SPSS statistics 10. RESULTS Following the intravenous bolus injection of Nifekalant hydrochlo- fide, the main pharmacokinetics parameters were calculated as follow： A UC0→t were 118.01±15.74 and 116.39 ±47.66 μg·m L^-1·min; A UC0-∞ were 119.84 ± 15.40 and 118.50 ± 46.80 μg·m L^-1·min; Cmax were 5.31 ± 2.28 and 4.45 ± 2.27μg·m L^-1 ; Tmax were 1.67 ± 1.63 and 1.00 min; t1/2 were 34.90 ± 4. 53 and 34. 76 ± 9.77 rain for single doses of test and reference preparation, respectively. CONCLUSION There is no significant difference of pharmacokinetics between the two kinds of Nifekalant hydrochloride injections in Beagles.