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[气管内给药后脂质体包裹利福平在大鼠体内的药代动力学特征]

[Characteristics of pharmacokinetics of liposome-incorporated rifampicin in rats after intratracheal administration].

作者信息

Gurevich G L, Berezovskaia L N, Manuĭlov K K

出版信息

Antibiot Khimioter. 1992 Jul;37(7):25-8.

PMID:1456804
Abstract

Pharmacokinetics of rifampicin after its single intratracheal administration in the form of the liposome-encapsulated drug and its aqueous solution was studied on rats. It was shown that after the exposure to the liposome-incorporated rifampicin (10 mg/kg) the concentration-time curve in the blood and lungs was sigmoid with the retarded decrease in the blood drug concentration within 9 hours. The plateau segment of the curve provided at least a 4-fold longer maintenance of the rifampicin concentration in the blood and lungs at 3 to 4 micrograms/ml. The use of the liposome-incorporated antibiotic induced 2- and 1.5-fold increases in the AUC in regard to the lungs and blood, respectively.

摘要

以脂质体包裹药物及其水溶液的形式对大鼠单次气管内给予利福平后的药代动力学进行了研究。结果表明,给予脂质体包裹的利福平(10mg/kg)后,血液和肺部的浓度-时间曲线呈S形,血液药物浓度在9小时内下降缓慢。曲线的平稳段使血液和肺部利福平浓度维持在3至4μg/ml的时间至少延长了4倍。与肺部和血液相比,使用脂质体包裹的抗生素分别使AUC增加了2倍和1.5倍。

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