Oliveira C H, Abib E, Vannuchi Y B, Sucupira M, Ilha J, De Nucci G
Department of Pharmacology, São Paulo, Brazil.
Int J Clin Pharmacol Ther. 2001 Apr;39(4):167-72. doi: 10.5414/cpp39167.
To compare the bioavailability of two amoxicillin oral suspension (250 mg/5 ml) formulations and two amoxicillin capsule (500 mg) formulations (Amoxicilina from Medley S/A Indústria Farmaceûtica, Brazil, as test formulations and Amoxil from SmithKline Beecham Laboratórios Ltda., Brazil, as reference formulations) in 48 volunteers of both sexes.
The study was conducted open with a randomized two-period crossover design and a one-week washout period. Plasma samples were obtained over a 12-hour interval. Amoxicillin concentrations were analyzed by combined reversed phase liquid chromatography and tandem mass spectrometry (LC-MS-MS) with positive ion electrospray ionization using the selected ion monitoring method. From the amoxicillin plasma concentration vs. time curves the following pharmacokinetic parameters were obtained: AUC(last), AUC(0-infinity) and Cmax.
Geometric mean of Amoxicilina/Amoxil 250 mg/5 ml individual percent ratio was 103.70% for AUC(last), 103.15% for AUC(0-infinity) and 106.79% for Cmax. The 90% confidence intervals were 97.82-109.94%, 97.40 to 109.24%, and 96.38-118.33%, respectively. Geometric mean of Amoxicilina/Amoxil 500 mg capsule individual percent ratio was 93.26% for AUC(last), 93.27% for AUC(0-infinity) and 90.74% for Cmax. The 90% confidence intervals were 85.0-102.33%, 85.12-102.31%, and 80.14-102.73%, respectively.
Since the 90% CI for both Cmax, AUC(last) and AUC(0-inifnity) were within the 80-125% interval proposed by the Food and Drug Administration, it was concluded that Amoxicilina 250 mg/5 ml oral suspension and Amoxicilina 500 mg capsule were bioequivalent to Amoxil 250 mg/5 ml oral suspension and to Amoxil capsule 500 mg, respectively, with regard to both the rate and extent of absorption.
比较两种阿莫西林口服混悬液（250mg/5ml）制剂和两种阿莫西林胶囊（500mg）制剂（巴西Medley S/A Indústria Farmaceûtica公司生产的Amoxicilina作为受试制剂，巴西SmithKline Beecham Laboratórios Ltda.公司生产的Amoxil作为参比制剂）在48名男女志愿者中的生物利用度。
本研究采用开放、随机双周期交叉设计，洗脱期为1周。在12小时间隔内采集血浆样本。采用反相液相色谱和串联质谱联用（LC-MS-MS），通过正离子电喷雾电离和选择离子监测法分析阿莫西林浓度。从阿莫西林血浆浓度-时间曲线中获得以下药代动力学参数：AUC（末次）、AUC（0至无穷大）和Cmax。
Amoxicilina/Amoxil 250mg/5ml的个体百分率比值的几何均值，AUC（末次）为103.70%，AUC（0至无穷大）为103.15%，Cmax为106.79%。90%置信区间分别为97.82 - 109.94%、97.40至109.24%和96.38 - 118.33%。Amoxicilina/Amoxil 500mg胶囊的个体百分率比值的几何均值，AUC（末次）为93.26%，AUC（0至无穷大）为93.27%，Cmax为90.74%。90%置信区间分别为85.0 - 102.33%、85.12 - 102.31%和80.14 - 102.73%。
由于Cmax、AUC（末次）和AUC（0至无穷大）的90%置信区间均在食品药品监督管理局提出的80 - 125%区间内，得出结论：就吸收速率和程度而言，Amoxicilina 250mg/5ml口服混悬液和Amoxicilina 500mg胶囊分别与Amoxil 250mg/5ml口服混悬液和Amoxil 500mg胶囊生物等效。
