Kalager T, Digranes A, Salveson A, Bergan T
Chemotherapy. 1985;31(6):405-9. doi: 10.1159/000238367.
Following 400 mg brodimoprim given orally to 8 volunteers, the peaks of the mean concentration curves were 3.2 +/- 1.0 mg/l in serum and 1.0 +/- 0.2 mg/l (+/- SEM) in skin blister fluid. The terminal half-lives were 25.9 +/- 2.2 h and 42.2 +/- 6.5 h in serum and blister fluid, respectively. The area under the concentration-versus-time curve for blister fluid was 73% of serum value, and the mean recovery of bioactive drug in urine during 24 h was 3.4%. Considering the minimal inhibitory concentrations of potential target organisms and the slow elimination, the results suggest that brodimoprim may be useful in the treatment of infections, and that dosage once a day may be sufficient.
8名志愿者口服400毫克溴莫普明后,血清中平均浓度曲线的峰值为3.2±1.0毫克/升,皮肤水疱液中为1.0±0.2毫克/升(±标准误)。血清和水疱液的末端半衰期分别为25.9±2.2小时和42.2±6.5小时。水疱液浓度-时间曲线下面积为血清值的73%,24小时尿液中生物活性药物的平均回收率为3.4%。考虑到潜在靶标微生物的最低抑菌浓度以及消除缓慢,结果表明溴莫普明可能对感染治疗有用,且每日一次给药可能足够。