[A study on pharmacokinetics, antimicrobial activity and clinical efficacy of sultamicillin in children]

Sultamicillin (SBTPC), a mutual prodrug for ampicillin (ABPC) and beta-lactamase inhibitor sulbactam (SBT), was evaluated for its antibacterial activity, pharmacokinetics and clinical efficacy. Pharmacokinetic studies were done in 2 subjects (a male and a female) following single oral administrations of 5 mg/kg and 10 mg/kg SBTPC fine granules after meal. Peak serum concentrations of ABPC and SBT in the 2 cases were 0.85 and 0.38 micrograms/ml and 3.74 and 3.79 micrograms/ml, respectively. Urinary excretion rates in 6 hours were 43.5-58.1% for ABPC and 33.6-53.6% for SBT. A total of 20 patients including 14 with respiratory infections, 1 with urinary tract infection and 5 with skin and soft tissue infections were treated with daily oral dose of 15.4-39.3 mg/kg SBTPC fine granules t.i.d. for 4 to 13 days. Responses were excellent in 5, good in 13 and fair in 2, hence the overall efficacy rate was 90.0%. Bacteriological responses were confirmed on 5 (62.5%) out of 8 strains which were eradicated by the treatment. SBTPC showed strong antibacterial activities against an ABPC-resistant strain of Escherichia coli. Side effects of the drug were observed in 3 patients: diarrhea in 2 and loose stool in 1. An abnormal laboratory test value, eosinophilia, was observed in only one patient.