Tanimura H, Mukaihara S, Setoyama M, Yung M, Kato H, Yotsumoto F, Nakano M
Jpn J Antibiot. 1985 Nov;38(11):3087-96.
In this study, 120 mg of micronomicin (MCR) was given to 15 cases intended for cholecystectomy intramuscularly by a single injection or 5 consecutive injections (in the evening of day -2, morning and evening of day -1, morning of day 0, and 1 hour before operation) or intravenously by 1-hour drip infusion, and levels of MCR in serum, B bile and gallbladder tissues were determined by means of HPLC and bioassay. The serum level of MCR 30 minutes after consecutive injections (8 cases) was 11.86 +/- 1.90 micrograms/ml, significantly higher than that after the single injection, 7.08 +/- 0.93 micrograms/ml. The highest bile level of MCR after consecutive injections was 10.0 micrograms/ml. The average level in 4 detectable cases, 6.33 +/- 2.06 micrograms/ml, came up to 50% of the serum level and was higher than that after the single injection, 3.53 +/- 1.39 micrograms/ml. The gallbladder tissue level of MCR after consecutive injections was 4.5 micrograms/g at the highest and 2.51 +/- 0.73 micrograms/g on the average in 5 detectable cases. This was equivalent to 20% of the serum level and higher than that after the single injection, 1.63 +/- 0.26 micrograms/g. The MIC of MCR could be determined against 8 of 10 strains detected in B bile. Against E. coli and K. pneumoniae, main causal bacteria of bile duct infections, it was as low as 0.39 to 0.78 micrograms/ml. Levels of MCR in bile and gallbladder tissues determined in this study exceeded by far the above MIC. From these results, it can be expected that clinical administration of MCR at 2 doses of 120 mg daily for 3 days or more will give rise to a sufficiently antibacterial effect against Gram-negative bacilli.
本研究中，将120mg小诺米星（MCR）给予15例拟行胆囊切除术的患者，采用单次肌内注射、连续5次注射（第-2天晚上、第-1天上午和晚上、第0天上午以及手术前1小时）或静脉滴注1小时的方式给药，并用高效液相色谱法（HPLC）和生物测定法测定血清、B胆汁和胆囊组织中MCR的水平。连续注射（8例）30分钟后血清MCR水平为11.86±1.90μg/ml，显著高于单次注射后的水平7.08±0.93μg/ml。连续注射后MCR的最高胆汁水平为10.0μg/ml。4例可检测病例的平均水平为6.33±2.06μg/ml，达到血清水平的50%，高于单次注射后的水平3.53±1.39μg/ml。连续注射后胆囊组织中MCR的最高水平为4.5μg/g，5例可检测病例的平均水平为2.51±0.73μg/g。这相当于血清水平的20%，高于单次注射后的水平1.63±0.26μg/g。在所检测的10株B胆汁菌株中，有8株可测定MCR的最低抑菌浓度（MIC）。对于胆管感染的主要致病菌大肠杆菌和肺炎克雷伯菌，其MIC低至0.39至0.78μg/ml。本研究中测定的胆汁和胆囊组织中MCR的水平远远超过上述MIC。从这些结果可以预期，临床每日2次给予120mg MCR，持续3天或更长时间，将对革兰氏阴性杆菌产生足够的抗菌作用。
