Assandri A, Ratti B, Cristina T
J Antibiot (Tokyo). 1984 Sep;37(9):1066-75. doi: 10.7164/antibiotics.37.1066.
A study on the pharmacokinetics of rifapentine, a new long-lasting rifamycin, has been carried out in the rat, the mouse and the rabbit. The investigation was made using either radioactive or unlabelled rifapentine and both the total 14C and the unchanged compound were assayed. In the rat, the overall evidence obtained was: the oral absorption of rifapentine into central compartment, due to its poor water solubility, appears to be dose-dependent with a satisfactory oral absorption (84%) after a dose of 3 mg/kg, lower (65%) after 10 mg/kg; the antibiotic undergoes rapid liver uptake while it diffuses into the tissue compartment more slowly, with particular affinity for the adrenals, pancreas and kidneys; concentrations higher than in plasma were also measured in the lungs; elimination of rifapentine from the blood and tissue compartments suggests a non linear capacity-limited kinetics where the terminal elimination phase has monoexponential course. Terminal plasma half-life ranged between 14 and 18 hours; the compound is eliminated mainly via the bile with the feces (92% of dose). In mice rifapentine shows a kinetic profile resembling that obtained in rats, whereas in rabbits is metabolized and/or eliminated much more rapidly with a half-life of only 1.8 hours.
一项关于新型长效利福霉素利福喷汀在大鼠、小鼠和兔子体内药代动力学的研究已经开展。该研究使用放射性或未标记的利福喷汀进行，同时测定了总14C和未变化的化合物。在大鼠中，获得的总体证据如下：由于利福喷汀水溶性差，其口服吸收进入中央室似乎呈剂量依赖性，3mg/kg剂量后口服吸收良好（84%），10mg/kg剂量后较低（65%）；该抗生素肝脏摄取迅速，而向组织室扩散较慢，对肾上腺、胰腺和肾脏有特别的亲和力；在肺中也测得高于血浆的浓度；利福喷汀从血液和组织室的消除表明是非线性容量限制动力学，其中终末消除相呈单指数过程。终末血浆半衰期在14至18小时之间；该化合物主要通过胆汁随粪便消除（占剂量的92%）。在小鼠中，利福喷汀的动力学特征与在大鼠中获得的相似，而在兔子中代谢和/或消除要快得多，半衰期仅为1.8小时。
