LABORATORY STUDIES ON ANTITUBERCULOUS ACTIVITY OF CYCLOPENTYLRIFAMPICIN Ⅱ. A LONG-ACTING ANTITUBERCULOTIC CYCLOPENTYLRIFAMPICIN
Author(s): Pan Yu-xuan, Liu Su-mei and Li Wei-wen
Pages: 305-311+299
Year: 1985 Issue: 5
Journal: Chinese Journal of Antibiotics
Keyword: 力复霉素; 小鼠血浆; 存活时间; 抗结核分枝杆菌; 实验小鼠; 血浓度; 生物半衰期; 长效作用; 可信限; 稀释度;
Abstract: Cyclopentylrifampcin (R-77-3, DL-473)has a longer and greater activity than rifampicin and R-76-1 against tuberculosis in mice. R-77-3 has a unsually longer serum half-life (32.8 hours)and it was about 5 times and 2 times longer than rifa-mpcin (8.1 hours) and R-76-1 (17.1 hours). It has also been demonstrated that the concentrations of R-77-3 in plasma, the inhibitory and bacteriocidal activities of plasma in mice on M. tuberculosis H37Rv can be continued about 5 days and 2-3 days, respectively.The longer activity of R-77-3 against tuberculosis in vivo was confirmed by the pre-adminstration experiments. Only oral adminstration(10mg/kg) once before infection by M. tuberculosis H37Rv the period of protection can be continued for 5 days, and it was more longer than rifampicin and R-76-1.
Pages: 305-311+299
Year: 1985 Issue: 5
Journal: Chinese Journal of Antibiotics
Keyword: 力复霉素; 小鼠血浆; 存活时间; 抗结核分枝杆菌; 实验小鼠; 血浓度; 生物半衰期; 长效作用; 可信限; 稀释度;
Abstract: Cyclopentylrifampcin (R-77-3, DL-473)has a longer and greater activity than rifampicin and R-76-1 against tuberculosis in mice. R-77-3 has a unsually longer serum half-life (32.8 hours)and it was about 5 times and 2 times longer than rifa-mpcin (8.1 hours) and R-76-1 (17.1 hours). It has also been demonstrated that the concentrations of R-77-3 in plasma, the inhibitory and bacteriocidal activities of plasma in mice on M. tuberculosis H37Rv can be continued about 5 days and 2-3 days, respectively.The longer activity of R-77-3 against tuberculosis in vivo was confirmed by the pre-adminstration experiments. Only oral adminstration(10mg/kg) once before infection by M. tuberculosis H37Rv the period of protection can be continued for 5 days, and it was more longer than rifampicin and R-76-1.
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