Haruta T, Kuroki S, Okura K, Nikami H, Nishio T, Kobayashi Y
Department of Pediatrics, Kobe City General Hospital.
Jpn J Antibiot. 1994 Jul;47(7):869-72.
The transferability of biapenem (L-627) to cerebrospinal fluid (CSF) was studied employing rabbits with experimental meningitis caused by Staphylococcus aureus. The mean plasma concentration was 192 +/- 12.8 micrograms/ml at 15 minutes after intravenous administration of the drug at a dose level of 100 mg/kg. The mean concentration in CSF was maximum at 45 minutes after administration at 11.4 +/- 2.19 micrograms/ml. Pharmacokinetic parameters calculated from these values were as follows, Cmax (CSF/plasma): 5.96%; AUC (CSF/plasma): 8.15% between 15 and 60 minutes, 12.1% between 15 and 120 minutes and 15.0% between 15 and 180 minutes; T1/2 for L-627 in CSF: 152 minutes; T1/2 (CSF/plasma): 3.34. In comparison with those of other beta-lactam antibiotics that were obtained in the same way, the transferability of L-627 was intermediate, and in consideration of the antimicrobial potency against the main pathogens of meningitis, it appears worthwhile of running clinical trials for this drug.
采用由金黄色葡萄球菌引起实验性脑膜炎的家兔,研究了比阿培南(L - 627)向脑脊液(CSF)中的转移情况。以100mg/kg的剂量静脉给药后15分钟,血浆平均浓度为192±12.8微克/毫升。给药后45分钟时脑脊液中的平均浓度最高,为11.4±2.19微克/毫升。根据这些值计算的药代动力学参数如下,Cmax(脑脊液/血浆):5.96%;AUC(脑脊液/血浆):15至60分钟之间为8.15%,15至120分钟之间为12.1%,15至180分钟之间为15.0%;L - 627在脑脊液中的T1/2:152分钟;T1/2(脑脊液/血浆):3.34。与以相同方式获得的其他β-内酰胺抗生素相比,L - 627的转移能力处于中等水平,并且考虑到其对脑膜炎主要病原体的抗菌效力,对该药物进行临床试验似乎是值得的。