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利福美坦(rifametane)是一种新的半合成利福霉素衍生物,即3-[(1-二乙氨亚乙基)连氮甲基]利福霉素SV.Potkar等在8名健康男性志愿者中,以单剂口服300mg利福平为对照,对单剂口服300mg利福美坦的药物动力学方式和安全性进行了一项随机开放式交叉研究.利福美坦的药物动力学性质显著优于利福平,血药峰浓度分别为7.82±0.40和4.04±0.50mg/L(P<0.001);清除半衰期分别为10.58±0.19和1.89±0.16h(P<0.001);药一时曲线下面积分别为142.32±9.31和19.91±2.70mg·h/L(P<0.001);平均保留时间分别为18.05±0.72和3.93±0.17h(P<0.001).服用利福美坦至72h时,尿中药物清除总量仅为6.00±0.73mg,而服用利福平至24h时,尿中药物清除总量就达24.61±3.89mg,超过前者的4倍.服药60h后,利福美坦的血药水平仍保持在对结核分枝杆菌的最低抑菌浓度(≈0.2mg/l)之上.经计算,每60h服用300mg利福美坦,足以将血药浓度保持在最
Rifametane is a novel semi-synthetic rifamycin derivative, namely, 3 - [(1-diethylaminoethylidene) azinomethyl] rifamycin SV.Potkar et al in 8 In a healthy male volunteer, a randomized open-label crossover study was conducted on the pharmacokinetics and safety of a single oral dose of 300 mg of rifampicin with a single oral dose of 300 mg of rifampicin.Furthermore, pharmacokinetics (P <0.001). The half-life of elimination was 10.58 ± 0.19 and 1.89 ± 0.16 h (P <0.001), respectively. The area under the curve was 142.32 ± 9.31 and 19.91 ± 2.70 mg · h / L, respectively (P <0.001), and the average retention time was 18.05 ± 0.72 and 3.93 ± 0.17 h (P <0.001) The total amount of urinary drug clearance was only 6.00 ± 0.73mg, while taking rifampicin to 24h, the total amount of urinary drug clearance reached 24.61 ± 3.89mg, more than 4 times the former after taking 60h, rifampicin blood The drug level remained above the minimum inhibitory concentration against Mycobacterium tuberculosis (≈0.2 mg / l) calculated to take 300 mg of rifammethane every 60 h, enough to keep the plasma concentration at its peak