目的:研究诺必擂停在大鼠和Beagle犬体内的药动学过程。方法:通过口服和静注两种给药方式,用高效液相色谱法测定血浆中诺必擂停的浓度。结果:大鼠灌胃给予诺必擂停8、16和32 mg/kg剂量后,血药浓度达峰时间tmax分别为20、30、30 min,峰浓度Cmax分别为(300±171)、(468±122)、(982±449)ng/mL,根据血药浓度AUC计算出的生物利用度F为(14.6±2.7)%。Beagle犬按4 mg/kg单剂量口服给予诺必擂停片后,tmax为(95±12)min,Cmax为(436±88)ng/mL,生物利用度F为(27.4±8.4)%。结论:灌胃给药后诺必擂停在大鼠和Beagle犬体内吸收较快但吸收程度较低,该药在两种动物的药动学参数tmax、t1/2α和t1/2β等存在明显的种属差异。
AIM: To investigate the pharmacokinetics of nobiletin in rats and Beagle dogs.METHODS: The concentration of nobiletin in plasma was measured by HPLC after intragastric administration and intravenous injection.RESULTS: In rats,the tmax values of nobiletin by intragastric administration at doses of 8,16 and 32 mg/kg were 20,30 and 30 min,respectively,and the Cmax values were(300±171),(468±122) and(982±449) ng/mL respectively and the bioavailability was(14.6±2.7)%.In Beagle dogs,the tmax value of nobiletin aft...