| 摘要: |
| 目的建立HPLCMS法测定人血浆中茴拉西坦的活性代谢物对甲氧基苯甲酰氨基丁酸(ABA)的浓度,比较2种茴拉西坦胶囊的人体生物等效性。方法24名健康男性志愿者单剂量交叉口服受试制剂或参比制剂200 mg,采用HPLCMS法测定血浆中不同时间点茴拉西坦代谢物ABA的血药浓度,计算主要药代动力学参数及相对生物利用度,评价2种制剂的生物等效性。结果受试制剂和参比制剂的主要药动学参数: Cmax分别为(9.30±5.13)和(8.70±3.17) μg/ml; tmax分别为(38.41±17.89)和(39.09±19.92) min; t 1/2分别为(37.21±10.51)和(38.45±9.24 ) min; AUC0t分别为(555.21±157.10)和(545.39±97.22) μg/(ml·min); AUC0∞分别为(566.24±158.01)和(554.71±100.32) μg/(ml·min)。以AUC0t 和AUC0∞计算,受试制剂的相对生物利用度F0t和F0∞分别为(101.22±17.17)%和(101.52±16.63)%。2种制剂的主要药代动力学参数差异无统计学意义。结论2种茴拉西坦胶囊具有生物等效性。 |
| 关键词: 茴拉西坦 对甲氧基苯甲酰氨基丁酸 生物等效性 高压液相色谱-质谱法 |
| DOI：10.3724/SP.J.1008.2011.053 |
| 投稿时间：2010-11-05修订日期：2010-12-11 |
| 基金项目: |
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| HPLC-MS in evaluating bioequivalence of two kinds of aniracetam capsules in healthy volunteers |
| L Lei,ZHAO Liang,ZHOU Gui-chen,CHEN Jun,ZHANG Guo-qing* |
| (Department of Pharmacy, Eastern Hepatobiliary Surgery Hospital, Second Military Medical University, Shanghai 200438, China) |
| Abstract: |
| ObjectiveTo establish a HPLCMS method for determinating the concentration of 4panisamidobutyric acid(ABA),the main active metabolite of aniracetam capsules in the plasma, and to compare the bioequivalence of two aniracetam capsules in healthy volunteers.Methods Twentyfour healthy male volunteers were randomly given an oral single dose of 200 mg test or reference aniracetam capsules in a crossover manner. The concentrations of ABA were assayed by HPLCMS at different time points. The main pharmacokinetic parameters and the relative bioavailability of two preparations were calculated, and their bioequivalence was evaluated．ResultsThe pharmacokinetic parameters of test and reference preparations were as fol1ows: Cmax being (9.30±5.13) and (8.70±3.17) μg/ml; t max being (38.41±17.89) and (39.09±19.92) min; t 1/2 being (37.21±10.51) and (38.45±9.24 ) min; AUC0t being (555.21±157.10) and (545.39±97.22) μg/(ml·min), and AUC0∞ being (566.24±158.01) and (554.71±100.32) μg/(ml·min), respectively. Relative bioavailability F0t and F0∞ values of the test preparation were (101.22±17.17)% and (101.52±16.63)%, respectively. No significant differences were found in the main pharmacokinetic parameters between the two preparations. ConclusionThe two aniracetam preparations tested in the present study are |
| Key words: aniracetam 4-p-anisamidobutyric acid bioequivalence high pressure liquid chromatography-mass spectrometry |
