Nobori T, Katoh Y, Ochiai H, Ochiai H, Kawai K, Kamiya H, Sakurai M
Jpn J Antibiot. 1985 Jul;38(7):1882-8.
Fundamental and clinical studies were performed with aspoxicillin (ASPC), a new developed injectable broad penicillin, in pediatric infectious diseases, and the following results were obtained. Pharmacokinetics ASPC was administered to 2 cases at a dose of 20 mg/kg by one shot intravenous injection. The mean half-life (T 1/2) was 1.17 hours. The mean urinary excretion rate was 58.4% during 6 hours after ASPC treatment. In 3 cases of intravenous drip infusion with a period of 1 hour at a dose of 10 mg/kg (2 cases) and 20 mg/kg (1 case), the half-lives (T 1/2) were 1.7 hours, 3.5 hours and 1.0 hour, respectively. The urinary recovery rate during 6 hours after administration was 57.7%, 32.6% and 42.7%, respectively. At only one case treated with 10 mg/kg intravenous drip infusion, the half-life was prolonged and urinary excretion rate was lower than other 2 cases. Clinical study ASPC was administered 50-80 mg/kg/day for 4-8 days to 22 children comprising 6 tonsillitis, 2 bronchitis, 6 pneumonia and 8 urinary tract infections. Clinical efficacy was excellent in 13 cases, good in 8 cases and fair in 1 case, the total cure rate was 95%. As for the clinical response classified by diagnosis, the each efficacy rate of tonsillitis, bronchitis and pneumonia was 100%, and that of urinary tract infection was 87.5%. Clinical side effect and abnormal laboratory findings were not observed in any cases. From the above results, it was concluded that ASPC was one of the useful secure drug for treatment of infections in pediatric field.
对新开发的注射用广谱青霉素阿扑西林（ASPC）进行了儿科传染病的基础和临床研究，获得了以下结果。药代动力学：对2例患儿单次静脉注射阿扑西林，剂量为20mg/kg。平均半衰期（T1/2）为1.17小时。阿扑西林治疗后6小时内平均尿排泄率为58.4%。3例患儿分别以10mg/kg（2例）和20mg/kg（1例）的剂量静脉滴注1小时，其半衰期（T1/2）分别为1.7小时、3.5小时和1.0小时。给药后6小时内的尿回收率分别为57.7%、32.6%和42.7%。仅1例以10mg/kg静脉滴注治疗的患儿半衰期延长，尿排泄率低于其他2例。临床研究：对22名儿童（包括6例扁桃体炎、2例支气管炎、6例肺炎和8例尿路感染）给予阿扑西林50 - 80mg/kg/天，治疗4 - 8天。临床疗效：优13例，良8例，中1例，总治愈率为95%。按诊断分类的临床反应中，扁桃体炎、支气管炎和肺炎的有效率均为100%，尿路感染的有效率为87.5%。所有病例均未观察到临床副作用和实验室检查异常。从上述结果得出结论，阿扑西林是儿科领域治疗感染的有效安全药物之一。
