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目的阐明毛兰素注射液在SD大鼠体内药动学规律。方法 SD大鼠分别单次和隔天、每隔一个半衰期一次多剂量静脉注射毛兰素注射液。采用高效液相色谱-质谱联用(HPLC-MS)测定大鼠静脉注射后不同时间大鼠血浆中毛兰素的血药浓度。结果大鼠单次静脉注射25,50,100mg·kg-1毛兰素注射液的主要药动学参数为:T1/2β分别为3.66,3.75,3.89h;AUC0-12分别为1453.0,3041.6,6731.6ng·mL-1·h;AUC0-∞分别为1462.0,3077.3,6788.7ng·mL-1·h;Vd分别为11.67,10.37,3.38L·kg-1;CL分别为0.049,0.089,0.024L·kg-1·h-1;MRT分别为0.18,0.28,0.21h;50mg·kg-1剂量的毛兰素注射液隔日给药5次其药动学参数与单次给药相近;而50mg·kg-1剂量的毛兰素注射液每隔一个半衰期一次给药5次的T1/2β为5.43h,AUC(S0)(0-t)为9800.8ng·mL-1·h。结论毛兰素注射液在大鼠体内的动力学过程与剂量相关,毛兰素注射液单剂量给药的体内药动学符合开放型二房室模型,T1/2β与给药剂量与关,表明毛兰素在大鼠体内的消除过程符合一级动力学规律。隔日多剂量给药的消除过程亦符合一级动力学规律;而每隔一个半衰期一次多剂量给予50mg·kg-1剂量的毛兰素其在大鼠体内则呈非线性消除。
Objective To elucidate the pharmacokinetics of erigeron injection in SD rats. Methods Sprague - Dawley rats were injected with multiple doses of intravenous injection of Erianthus injection once or twice a day for every one half - life. Plasma concentrations of Erianin in rats plasma were determined by HPLC-MS after intravenous injection. Results The main pharmacokinetic parameters of single injection of 25, 50 and 100 mg · kg-1 eugenol into rats were: T1 / 2β were 3.66,3.75,3.89h; AUC0-12 were 1453.0,3041.6,6731.6 ng · mL-1 · h; AUC0-∞ were 1462.0,3077.3,6788.7ng · mL-1 · h, Vd were 11.67,10.37,3.38L · kg-1, respectively; CL were 0.049,0.089,0.024L · kg-1 · h-1; MRT were 0.18,0.28,0.21h; 50mg · kg-1 doses of Eriyon injection medication every other day 5 times its pharmacokinetic parameters similar to a single administration; and 50mg · kg- The T1 / 2β was 5.43h and the AUC (S0) (0-t) was 9800.8ng · mL-1 · h for five doses of once-daily half-life of the Erianthus injection. Conclusion The kinetics of injection of erigeron in rats is dose-dependent. The pharmacokinetics of single dose injection of erigeron injections in vivo is consistent with the open two-compartment model. The dose and dose of T1 / 2β and the dose Elan in rats in the elimination process in line with the laws of first-order kinetics. The elimination of multiple dose administration on the next day was also in accordance with the first order kinetics, while once every other half-dose of multiple doses of 50 mg · kg-1 doses of erianin was non-linearly eliminated in rats.