[Clinical and pharmacokinetic studies on sultamicillin fine granules in pediatrics]

Sultamicillin (SBTPC) is a mutual prodrug of sulbactam (SBT) and ampicillin (ABPC). A study has been performed to evaluate pharmacokinetic properties and clinical usefulness of SBTPC fine granules in the treatment of pediatric infections. After an oral dose of 5-15 mg/kg of SBTPC fine granules, peak serum concentrations of ABPC and SBT were 1.18-3.26 micrograms/ml and 0.97-3.05 micrograms/ml, respectively at 1 hour. Serum half-lives for elimination (T 1/2 (beta] of ABPC and SBT were 0.83-1.83 hours and 0.94-1.71 hours, respectively. Serum concentrations of ABPC at 1-6 hours after an oral administration of SBTPC fine granules were similar to those of SBT. Serum concentrations of ABPC and SBT were proportional to dose levels of SBTPC fine granules. Following oral administrations of 5-15 mg/kg, 33.9-64.8% of ABPC and 38.1-76.6% of SBT were recovered in urine in 6 hours. SBTPC fine granules were administered in a daily dose of approximately 30 mg/kg divided into 3 doses to 14 pediatric patients with bacterial infections. All 14 were cured with 11 excellent and 3 good clinical response to this drug. Microbiological eradication was obtained in 85.7%. beta-Lactamase-producing ABPC-resistant strains were eradicated. Adverse effects including laboratory test values that may be attributed to the administration of SBTPC fine granules were not observed except a treatment episode of diarrhea in 1 patient.