Kawahara S, Tada A, Takeuchi M, Kamisaka K, Okada C, Mishima Y, Soda R, Takahashi K, Kibata M, Nagare H
Department of Internal Medicine, National Sanatorium Minami Okayama Hospital, Japan.
Kekkaku. 1994 May;69(5):351-6.
We studied the therapeutic potential of utilizing sparfloxacin (SPFX), a newly developed quinolone, to prevent various mycobacterial infections. The in vitro activity of SPFX as a preventive agent for various mycobacteria was determined using the actual count method on Ogawa egg medium. The minimal inhibitory concentrations (MICs) of SPFX were as follows: ofloxacin-sensitive M. tuberculosis, 0.16-0.32 microgram/ml; ofloxacin-resistant M. tuberculosis, 0.63-2.5 micrograms/ml; M. avium; 0.63-10 micrograms/ml (MICs were equal or less than 1.25 micrograms/ml in seven out of 11 strains); M. intracellulare, 2.5-10 micrograms/ml (MICs were equal or more than 10 micrograms/ml in 17 out of 23 strains); M. kansasii, < or = 0.08-0.16 microgram/ml; M. fortuitum, < or = 0.08 microgram/ml; M. chelonae subsp. abscessus, > 10 micrograms/ml; M. chelonae subsp. chelonae, 0.63 microgram/ml; M. scrofulaceum, < or = 0.08 microgram/ml; M. nonchromogenicum, 1.25 micrograms/ml; M. xenopi, < or = 0.08 microgram/ml; M. gordonae, < or = 0.08 microgram/ml. The average serum concentrations of SPFX during the period of multiple oral administration (200 mg once a day) were 0.35 +/- 0.16 microgram/ml before administration, 0.67 +/- 0.32 microgram/ml after one hour, 1.13 +/- 0.21 microgram/ml after two hours, 1.27 +/- 0.32 microgram/ml after four hours and 1.31 +/- 0.34 micrograms/ml after six hours. These results indicate that SPFX has a strong therapeutic potential to prevent infections due to M. tuberculosis, M. kansasii, M. fortuitum, M. chelonae subsp. chelonae, M. scrofulaceum, M. xenopi and M. gordonae. Moreover, it may be expected to be a promising agent against infections due to ofloxacin-resistant M. tuberculosis, M. avium and M. nonchromogenicum.
我们研究了新开发的喹诺酮类药物司帕沙星（SPFX）预防各种分枝杆菌感染的治疗潜力。使用小川鸡蛋培养基上的实际计数法测定了SPFX作为各种分枝杆菌预防剂的体外活性。SPFX的最低抑菌浓度（MIC）如下：对氧氟沙星敏感的结核分枝杆菌，0.16 - 0.32微克/毫升；对氧氟沙星耐药的结核分枝杆菌，0.63 - 2.5微克/毫升；鸟分枝杆菌，0.63 - 10微克/毫升（11株中有7株的MIC等于或小于1.25微克/毫升）；胞内分枝杆菌，2.5 - 10微克/毫升（23株中有17株的MIC等于或大于10微克/毫升）；堪萨斯分枝杆菌，≤0.08 - 0.16微克/毫升；偶然分枝杆菌，≤0.08微克/毫升；龟分枝杆菌脓肿亚种，＞10微克/毫升；龟分枝杆菌龟亚种，0.63微克/毫升；瘰疬分枝杆菌，≤0.08微克/毫升；非产色分枝杆菌，1.25微克/毫升；偶发分枝杆菌，≤0.08微克/毫升；戈氏分枝杆菌，≤0.08微克/毫升。多次口服给药（每日一次，200毫克）期间，SPFX的平均血清浓度在给药前为0.35±0.16微克/毫升，给药后1小时为0.67±0.32微克/毫升，2小时后为1.13±0.21微克/毫升，4小时后为1.27±0.32微克/毫升，6小时后为1.31±0.34微克/毫升。这些结果表明，SPFX具有很强的治疗潜力，可预防由结核分枝杆菌、堪萨斯分枝杆菌、偶然分枝杆菌、龟分枝杆菌龟亚种、瘰疬分枝杆菌、偶发分枝杆菌和戈氏分枝杆菌引起的感染。此外，有望成为对抗耐氧氟沙星结核分枝杆菌、鸟分枝杆菌和非产色分枝杆菌感染的有前景药物。
