摘要
目的:建立准确、灵敏的液相色谱-串联质谱法(LC-MS/MS)同时测定人血浆中的盐酸氟西汀和诺氟西汀,并研究健康受试者单剂量口服盐酸氟西汀胶囊试验制剂和参比制剂后的药动学和相对生物利用度。方法:20名健康男性受试者进行随机双交叉试验,分别单剂量口服20 mg盐酸氟西汀胶囊参比制剂和试验制剂,以盐酸舍曲林为内标,采用ESI正离子选择性反应测定盐酸氟西汀和诺氟西汀血浆浓度,计算药动学参数并进行生物等效性评价。结果:由两种制剂的AUC0-τ计算,受试胶囊盐酸氟西汀的相对生物利用度为(104.0±25.2)%。结论:建立的LC-MS/MS测定法准确、灵敏,结果可靠;统计分析表明盐酸氟西汀胶囊试验制剂和参比制剂生物等效。
Objective ：To establish an accurate and sensitive LC-MS/MS method for simultaneous determination of fluoxetine hydrochloride, norfluoxetine in plasma and to evaluate their pharmacokinetics and bioavailability in healthy male volunteers after a single oral dose of fluoxetine hydrochloride capsules. Methods： 20 healthy male volunteers were divided into a two-way cross-over design. A single oral dose of 20 mg capsule fluoxetine hydrochloride test and reference capsules were given to each volunteer according to an open randomized crossover study. The concentrations of fluoxetine hydrochloride and norfluoxetine in plasma were determined by LC-MS/MS with positive ion MRM detection using sertraline hydrochloride as internal standard. The pharmacokinetics and bioavailability were compared. Results： The relative bioavailability of the test compared to reference capsules was fluoxetine hydrochloride （104. 0 ±25.2）%. Conclusion： The method was proved to be accurate and sensitive. The results are reliable. The fluoxetine hydrochloride capsules were bioequivalent to equivalent doses of reference capsules.
出处
《药学与临床研究》
2008年第1期19-23,共5页
Pharmaceutical and Clinical Research
