Stavchansky S, Pearlman R S, Van Harken D R, Smyth R D, Hottendorf G H, Martin A, Newburger J, Schneider L W
J Pharm Sci. 1984 Feb;73(2):169-73. doi: 10.1002/jps.2600730208.
The relative bioavailability of sarpicillin (the methoxymethyl ester of hetacillin) from three different oral dosage forms was compared in humans employing a three-way crossover study design. Each unit dose contained 250 mg of sarpicillin in terms of anhydrous ampicillin activity. The comparative bioavailability of a tablet containing added buffer, a liquid-filled capsule, and a standard powder-filled capsule was determined. The bioavailability parameters were Cmax, tmax, and AUC of intact plasma sarpicillin levels and saliva ampicillin levels. Significant correlation was found between plasma sarpicillin levels and saliva ampicillin levels following the administration of sarpicillin. All three formulations yielded statistically similar Cmax and AUC values with respect to plasma sarpicillin and saliva ampicillin levels. However, a more rapid absorption of intact sarpicillin was observed with the buffered tablet formulation, as reflected by significantly smaller tmax for both plasma sarpicillin and saliva ampicillin levels. The faster absorption from the tablet formulation gave more precise absorption among subjects.
采用三交叉研究设计，在人体中比较了三种不同口服剂型的沙培西林（海他西林的甲氧基甲酯）的相对生物利用度。以无水氨苄西林活性计，每个单位剂量含有250mg沙培西林。测定了添加缓冲剂的片剂、液状胶囊和标准粉末填充胶囊的相对生物利用度。生物利用度参数为完整血浆沙培西林水平和唾液氨苄西林水平的Cmax、tmax和AUC。服用沙培西林后，血浆沙培西林水平与唾液氨苄西林水平之间存在显著相关性。就血浆沙培西林和唾液氨苄西林水平而言，所有三种制剂的Cmax和AUC值在统计学上相似。然而，缓冲片剂剂型观察到完整沙培西林的吸收更快，血浆沙培西林和唾液氨苄西林水平的tmax均显著更小，这反映了这一点。片剂剂型更快的吸收在受试者中产生了更精确的吸收。
