Moraes M E, Lerner F E, Perozin M, Moraes M O, Frota Bezerra F A, Sucupira M, Corso G, De Nucci G
Pharmacology Department, Ceará Federal University, Brasil.
Int J Clin Pharmacol Ther. 1998 Dec;36(12):661-5.
To compare the bioavailability of 2 sertraline tablets formulations (Tolrest from Laboratórios Biosintética, and Zoloft from Laboratórios Pfizer, Brazil) in 24 healthy volunteers of both sexes (12 male and 12 female) who received a single 50 mg dose of each sertraline formulation.
The study was conducted open with randomized two-period crossover design and a 14-day washout period. Plasma samples were obtained over a 96-hour interval and sertraline concentrations were analyzed by combined reversed phase liquid chromatography and tandem mass spectrometry (LC-MS-MS) with positive ion electrospray ionization using selected ion monitoring method. From the plasma sertraline concentration vs. time curves the following pharmacokinetic parameters were obtained: AUC(0-96h), AUC(0-infinity), Cmax, Cmax/AUC(0-96h), Tmax, ke, and t(1/2).
Pharmacokinetic parameters presented normal distribution according to Probit' s plot and Kolmogorov Smirnov's test, and the variance of AUC(0-96h), AUC(0-infinity) or Cmax were homoscedastic. Geometric mean Tolrest/Zoloft individual percent ratio was 95.22% for AUC(0-96h), 99.87% for Cmax, 100.4% for AUC(0-infinity), 103.6% for Ke, 96.0% for t(1/2) and 93.7% for Tmax.
Since the 90% CI for both Cmax and AUC(0-96h) mean ratio were within the 80-125% interval proposed by the Food and Drug Administration, it was concluded that Tolrest was bioequivalent to Zolof for both extent and rate of absorption in a single dose administration.
比较两种舍曲林片剂制剂（来自Laboratórios Biosintética的Tolrest和来自巴西Laboratórios Pfizer的Zoloft）在24名健康男女志愿者（12名男性和12名女性）中的生物利用度，这些志愿者每人接受单次50mg剂量的每种舍曲林制剂。
本研究采用开放的随机两周期交叉设计，洗脱期为14天。在96小时内采集血浆样本，采用反相液相色谱-串联质谱联用（LC-MS-MS）结合正离子电喷雾电离和选择离子监测法分析舍曲林浓度。从血浆舍曲林浓度-时间曲线中获得以下药代动力学参数：AUC(0-96h)、AUC(0-∞)、Cmax、Cmax/AUC(0-96h)、Tmax、ke和t(1/2)。
根据概率图和柯尔莫哥洛夫-斯米尔诺夫检验，药代动力学参数呈正态分布，AUC(0-96h)、AUC(0-∞)或Cmax的方差具有齐性。Tolrest/Zoloft个体几何平均百分比比值，AUC(0-96h)为95.22%，Cmax为99.87%，AUC(0-∞)为100.4%，Ke为103.6%，t(1/2)为96.0%，Tmax为93.7%。
由于Cmax和AUC(0-96h)平均比值的90%置信区间在食品药品监督管理局提出的80%-125%区间内，因此得出结论：在单剂量给药中，Tolrest在吸收程度和吸收速率方面与Zolof生物等效。
