Sirot J, Prive L, Lopitaux R, Glanddier Y
Pathol Biol (Paris). 1983 May;31(5):438-41.
Sixty eight patients received either an oral single dose of 300 mg (or 300 mg/12 h), or an oral single dose of 600 mg (or 600 mg/24 h) of rifampicin. In every case samples of serum and bone were collected 3 h, 12 h, and 24 h after the last oral dose. Rifampicin levels measured at 3 h and 12 h in cortical bone samples increased significantly with the dose of the drug. The only dose which determines activity in cortical bone at the 3rd hour was the dose of 600 mg. When the dose was increased from 300 mg/12 h to 600 mg/24 h the ratio spongious bone/serum increased from 0.19 to 0.41 at 3d h and from 0.24 to 0.29 at the 12th hour; the ratio cortical bone serum was 0.20 at the 3rd hour after a dose of 600 mg. In any case tissue levels varied in a parallel direction to serum levels and were superior in spongious bone to the MIC of S. aureus sensitive strains until 12 h after the 600 mg dose. According to these results, it appears that the best dose for treating S. aureus bone infection seems to be 600 mg/12 h.
68名患者接受了口服单剂量300毫克(或300毫克/12小时)或口服单剂量600毫克(或600毫克/24小时)的利福平。在每种情况下,在最后一次口服剂量后的3小时、12小时和24小时采集血清和骨样本。皮质骨样本在3小时和12小时测得的利福平水平随药物剂量显著增加。在第3小时决定皮质骨活性的唯一剂量是600毫克。当剂量从300毫克/12小时增加到600毫克/24小时时,松质骨/血清比值在第3小时从0.19增加到0.41,在第12小时从0.24增加到0.29;在600毫克剂量后的第3小时,皮质骨血清比值为0.20。在任何情况下,组织水平与血清水平呈平行变化,在600毫克剂量后12小时内,松质骨中的组织水平高于金黄色葡萄球菌敏感菌株的最低抑菌浓度。根据这些结果,似乎治疗金黄色葡萄球菌骨感染的最佳剂量似乎是600毫克/12小时。