Sourgens H, Bertola M A, Verschoor J S C, Kuipers M, Rayer B
University of Münster, Germany.
Int J Clin Pharmacol Ther. 2004 Mar;42(3):165-73. doi: 10.5414/cpp42165.
A new amoxicillin/clavulanic acid tablet formulation (Solutab tablet, Forcid Solutab) containing amoxicillin/clavulanic acid (875/125) has been developed. The aim of the present study was to demonstrate bioequivalence between the new tablet formulation (test), taken as an intact tablet and after prior dispersal, versus the originator product viz. Augmentan film-coated tablet (875/125) used as reference. The study was performed in 48 healthy volunteers according to an open, single-dose, crossover design. Bioequivalence was demonstrated using Cmax and AUC(0-infinity) as primary parameters of evaluation for both amoxicillin and clavulanic acid with 90% confidence intervals of the ratios Solutab tablet/Augmentan within the range of 0.8-1.25. The duration of the plasma concentration exceeding the amoxicillin minimal inhibitory concentration (MICs) was calculated using individual plasma concentration-time curves and compartmental analysis. The data showed that the bioavailability characteristics of the test tablet, taken intact or in dispersed form, and the reference tablets were very similar. The analysis, moreover, also confirmed the appropriateness of using a b.i.d. dosage regimen for both formulations, taking into account the pharmacodynamic breakpoint values for some major pathogens.
已研发出一种含有阿莫西林/克拉维酸（875/125）的新型阿莫西林/克拉维酸片剂制剂（Solutab片剂，Forcid Solutab）。本研究的目的是证明新型片剂制剂（试验品）在完整服用和预先分散后与原研产品即用作参比的奥格门汀薄膜包衣片（875/125）之间的生物等效性。该研究按照开放、单剂量、交叉设计在48名健康志愿者中进行。以阿莫西林和克拉维酸的Cmax和AUC(0-无穷大)作为主要评价参数，证明了生物等效性，Solutab片剂/奥格门汀的比值的90%置信区间在0.8 - 1.25范围内。使用个体血浆浓度-时间曲线和房室分析计算血浆浓度超过阿莫西林最低抑菌浓度（MICs）的持续时间。数据表明，完整服用或分散服用的试验片剂与参比片剂的生物利用度特征非常相似。此外，考虑到一些主要病原体的药效学折点值，分析还证实了两种制剂采用每日两次给药方案的合理性。
