【摘要】 目的:采用HPLC-RF检测法测定氢溴酸加兰他敏的血药浓度,研究其在人体内的药动学和生物等效性。方法:24例健康男性志愿者单剂量随机交叉口服5 mg加兰他敏口服液(受试制剂)和片剂(参比制剂)。血浆样品经碱化后用乙醚提取,采用反相HPLC-RF法测定血浆中加兰他敏浓度,检测波长:激发波长290 nm,发射波长320 nm。采用3P97药动学软件计算药动学参数和相对生物利用度,并对参数进行方差分析和双单侧t检验。结果:加兰他敏口服液和片剂的主要药动学参数:Cmax分别为(31．53±5．59)和(33．44±5．72)μg·L-1;Tmax分别为(1．66±0．79)和(1．51±0．72)h;t1/2分别为(7．06±2．16)和(6．64±2．30)h;AUC0～∞分别为(340．6±77．2)和(325．5±77．7)μg·h·L-1。氢溴酸加兰他敏口服液相对生物利用度为105．6％。结论:加兰他敏口服液和片剂生物等效。更多还原

【Abstract】 Objective: To investigate the pharmacokinetics profiles and bioequivalence of galanthamine. Methods:Twenty-four healthy male volunteers were orally administered with a randomized and single crossover dose of galanthamine hydrobromide solutions (test sample) and immediate release tablets (reference sample) 5 mg. Following after the extraction of the alkalinized plasma samples of the volunteers using ether, the plasma galanthamine were quantified by reverse phase HPLC with a fluorescence-detection at Ex290 nm and Em320 nm. The pharmacokinetic parameters including variance and two-one side t test analysis and relative bioavailability were calculated using 3P97 pharmacokinetics software. Results: The main pharmacokinetic parameters of galanthamine hydrobromide solutions and tablets were as follows: Cmax(31.53±5.59) vs. (33.44±5.72)μg·L-1;Tmax(1.66±0.79)vs. (1.51±0.72)h;t1/2 (7.06±2.16)vs. (6.64±2.30)h; AUC0-∞(340.6±77.2)vs. (325.5±77.7)μg·h·L-1.The relative bioavailability of galanthamine solutions was 105. 6% . Conclusion:The two formulations were bioequivalent.更多还原