Haruta T, Okura K, Kuroki S, Yamamoto H, Kobayashi Y
Department of Pediatrics, Kobe Central Municipal Hospital.
Jpn J Antibiot. 1989 Mar;42(3):594-7.
Concentrations of sulbactam (SBT) and ampicillin (ABPC) in the blood and cerebrospinal fluid (CSF) following an intravenous administration of SBT/ABPC at a dose of 150 mg/kg (SBT/ABPC = 1:2) were determined in 12 rabbits with staphylococcal meningitis. Drug concentrations were measured 9 times, 6 times each with intervals of 15 minutes and thereafter with intervals of 30 minutes. The results were compared with those of a group of 9 rabbits given 100 mg/kg of ABPC alone. 1. The maximum concentration of SBT in the CSF and the percentages of both the maximum concentration and the area under the concentration-time curve (AUC) of SBT in CSF vs. those in serum of the SBT/ABPC group were higher than those of ABPC and the half-life of SBT in the CSF was also longer than that of ABPC, all with significant difference. When these parameters for SBT of SBT/ABPC groups were compared with those of ABPC of the ABPC group, not much differences existed between the 2 groups except that the CSF half-life of SBT was much longer than that of ABPC. 2. The percentages of both the maximum concentration and AUC of ABPC in CSF vs. those in serum of the SBT/ABPC group were significantly lower than those of ABPC of the ABPC group. The CSF half-life of ABPC of the former group was longer than that of the latter. 3. The above results suggest that when SBT and ABPC are administered simultaneously, the penetration of ABPC into the CSF is inhibited.
对12只患有葡萄球菌性脑膜炎的兔子静脉注射剂量为150mg/kg（舒巴坦/氨苄青霉素=1:2）的舒巴坦（SBT）/氨苄青霉素（ABPC）后，测定其血液和脑脊液（CSF）中舒巴坦和氨苄青霉素的浓度。药物浓度共测量9次，前6次每隔15分钟测量一次，之后每隔30分钟测量一次。将结果与另一组单独给予100mg/kg氨苄青霉素的9只兔子的结果进行比较。1. SBT/ABPC组脑脊液中SBT的最高浓度以及脑脊液中SBT最高浓度和浓度-时间曲线下面积（AUC）相对于血清中相应值的百分比均高于ABPC组，且SBT在脑脊液中的半衰期也长于ABPC组，差异均有统计学意义。将SBT/ABPC组SBT的这些参数与ABPC组ABPC的参数进行比较时，两组之间除SBT在脑脊液中的半衰期远长于ABPC外，差异不大。2. SBT/ABPC组脑脊液中ABPC最高浓度和AUC相对于血清中相应值的百分比均显著低于ABPC组ABPC的相应值。前一组ABPC在脑脊液中的半衰期长于后一组。3. 上述结果表明，当同时给予SBT和ABPC时，ABPC向脑脊液中的渗透受到抑制。
