Brachet-Liermain A, Akbaraly J P, Quentin C, Guyot M, Coux C, Auzerie J, Bebear C
Pathol Biol (Paris). 1983 May;31(5):319-22.
Apalcillin is a new semi-synthetic penicillin of the uridino-penicillin group. The study comprises two groups of 6 subjects receiving 1 g and 2 g respectively of apalcilline by a two-hour infusion. The assays done by HPLC and microbiology show a good correlation between the two methods. The serum concentrations at the end of the infusion are: 32,2 micrograms/ml-1 (1 g) and 62,7 micrograms/ml-1 (2 g). The modelisation of the serum curves has been realized according to an open model with two compartments. A phase of rapid distribution is observed: t 1/2 alpha of 19.5 mn (1 g), 8.96 mn (2 g) followed by a phase of longer elimination: t 1/2 beta of 1.17 h (1 g), 1.15 h (2 g). The distribution volume at the steady-state is: 14.19 l (1 g), 14.76 l (2 g). This volume, much greater than the plasmatic volume, allows to suppose a good tissular diffusion of apalcilline. The urinary concentrations of the twelve first hours are: 182.64 micrograms/ml (1 g), 323 micrograms/ml (2 g). The urinary elimination during the 24 hours following the administration is: 18.58% (1 g), 16.47% (2 g).
阿帕西林是一种新型的脲基青霉素类半合成青霉素。该研究包括两组，每组6名受试者，分别通过两小时输注接受1克和2克阿帕西林。通过高效液相色谱法（HPLC）和微生物学方法进行的测定表明，这两种方法之间具有良好的相关性。输注结束时的血清浓度分别为：32.2微克/毫升-1（1克）和62.7微克/毫升-1（2克）。血清曲线的建模是根据具有两个房室的开放模型进行的。观察到一个快速分布阶段：19.5分钟（1克）、8.96分钟（2克）的t 1/2α，随后是一个较长的消除阶段：1.17小时（1克）、1.15小时（2克）的t 1/2β。稳态时的分布容积为：14.19升（1克）、14.76升（2克）。这个容积远大于血浆容积，表明阿帕西林在组织中有良好的扩散。最初12小时的尿液浓度分别为：182.64微克/毫升（1克）、323微克/毫升（2克）。给药后24小时内的尿液消除率分别为：18.58%（1克）、16.47%（2克）。
