Guibert J, Kitzis M D, Yamabe S, Acar J F
Chemioterapia. 1985 Aug;4(4):293-8.
Lenampicillin (LAPC) is a novel prodrug of ampicillin (ABPC) which is under development by KANEBO Ltd. and TORII Pharmaceutical Co. The single- and multiple-dose pharmacokinetic studies were performed on six healthy male volunteers. Amoxicillin (AMPC) was used as control drug. The oral single-dose studies of LAPC (equivalent to 250 mg ANPC) and of AMPC (500 mg) demonstrated that the mean peak serum concentrations of ABPC and AMPC were 11.4 +/- 0.8 micrograms/ml at 40 min and 8.5 +/- 0.7 micrograms/ml at 50-90 min, respectively. The half-lives and the areas under the concentration-time curves were the same for both antibiotics on an equimolar basis. The oral multiple-dose studies of LAPC and AMPC (twice a day for 8 days with the same single dose as above) showed that no measurable accumulation and no remarkable variations between the single- and multiple-dose pharmacokinetics were observed. No adverse effects were recorded for any subject. LAPC proved to have unique pharmacokinetic properties as compared with AMPC and high safety, and its further development to clinical trials appears warranted.
仑氨西林（LAPC）是一种新型氨苄西林（ABPC）前体药物，由佳丽宝有限公司和鸟居制药公司正在开发。对6名健康男性志愿者进行了单剂量和多剂量药代动力学研究。阿莫西林（AMPC）用作对照药物。LAPC（相当于250mg ANPC）和AMPC（500mg）的口服单剂量研究表明，ABPC和AMPC的平均血清峰值浓度分别在40分钟时为11.4±0.8微克/毫升和在50 - 90分钟时为8.5±0.7微克/毫升。在等摩尔基础上，两种抗生素的半衰期和浓度 - 时间曲线下面积相同。LAPC和AMPC的口服多剂量研究（每天两次，共8天，单剂量与上述相同）表明，未观察到可测量的蓄积，且单剂量和多剂量药代动力学之间无明显差异。未记录到任何受试者有不良反应。与AMPC相比，LAPC具有独特的药代动力学特性和高安全性，因此有必要进一步开展临床试验。
