Armengaud M, Massip P, Tran Van Tho A, Chan Lai Wane L
Nouv Presse Med. 1982 Feb 4;11(5 Pt 2):368-72.
The passage of mezlocillin into the CSF was investigated in normal dogs and in dogs with experimentally induced Staphylococcus aureus meningitis. The areas under the curves (AUC) of mezlocillin concentrations in blood and CSF were compared. The antibiotic was administered by slow (1 hour) intravenous infusion in doses of 100, 200 and 400 mg/kg bodyweight. Samples of blood and CSF were collected simultaneously 30, 40, 60, 75, 90, 105, 120, 180 and 240 minutes after the infusion. The penetration of mezlocillin into the CSF of dogs with non-inflamed meninges was poor (peak less than or equal to 2 micrograms/ml, CSF/serum AUC ratio : 0.9 %), but it was very substantial in dogs with meningitis. After the 200 mg/kg dose, the mean CSF peak was 43 micrograms/ml (range : 33-60 micrograms/ml) and the CSF/serum AUC ratio was 26.6 %. Similar experiments were performed with other beta-lactam antibiotics. In dogs with healthy meninges the CSF/serum AUC ratios were 0.52 % with amoxycillin, 0.75 % with cefuroxime, 1.05 % with cefamandole, 1.18 % with cefoxitin and 3.6 % with cefotaxime. In dogs with meningitis, the corresponding ratios were 16.3 % with cefotaxime, 17.4 % with cefamandole, 18.5 % with cefoxitin, 18.6 % with amoxycillin and 18.7 % with cefuroxime. These results suggest that cefotaxime penetrates best across normal meninges and mezlocillin across inflamed meninges.
在正常犬以及实验性诱导产生金黄色葡萄球菌脑膜炎的犬中研究了美洛西林进入脑脊液的情况。比较了血液和美洛西林脑脊液浓度曲线下面积（AUC）。通过缓慢（1小时）静脉输注给予抗生素，剂量分别为100、200和400mg/kg体重。输注后30、40、60、75、90、105、120、180和240分钟同时采集血液和脑脊液样本。美洛西林进入未发炎脑膜的犬脑脊液的情况较差（峰值小于或等于2微克/毫升，脑脊液/血清AUC比值：0.9%），但在患脑膜炎的犬中则非常显著。给予200mg/kg剂量后，脑脊液平均峰值为43微克/毫升（范围：33 - 60微克/毫升），脑脊液/血清AUC比值为26.6%。用其他β-内酰胺类抗生素进行了类似实验。在脑膜健康的犬中，阿莫西林的脑脊液/血清AUC比值为0.52%，头孢呋辛为0.75%，头孢孟多为1.05%，头孢西丁为1.18%，头孢噻肟为3.6%。在患脑膜炎的犬中，相应比值分别为：头孢噻肟16.3%，头孢孟多17.4%，头孢西丁18.5%，阿莫西林18.6%，头孢呋辛18.7%。这些结果表明，头孢噻肟穿过正常脑膜的渗透性最佳，而美洛西林穿过发炎脑膜的渗透性最佳。
