Preclinical Pharmacokinetics Study of Amphamide: a New Semisynthetic Antifungal Antibiotic

被引：0
|
作者：
Portnoi, Yu. A. [1 ]
Kobrin, M. B. [1 ]
Dovzhenko, S. A. [1 ]
Tevyashova, A. N. [1 ]
Treshchalin, M. I. [1 ]
Golibrodo, V. A. [1 ]
Firsov, A. A. [1 ]
机构：
[1] GF Gause Inst New Antibiot, Moscow 119021, Russia
来源：
PHARMACEUTICAL CHEMISTRY JOURNAL | 2020年 / 54卷 / 02期
关键词：
amphamide; pharmacokinetics; preclinical study; AMPHOTERICIN-B; DERIVATIVES;
D O I：
10.1007/s11094-020-02165-3
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The pharmacokinetics of amphamide, a new semisynthetic antifungal antibiotic, are studied after intravenous injection to rats and rabbits. The amphamide concentration in biological samples was determined by HPLC. Amphamide pharmacokinetics in rabbits were nonlinear. Amphamide levels in animal blood plasma decreased in a triphasic manner. The total clearance and steady-state distribution volume were greater in rats than in rabbits (0.85 vs. 0.3 - 0.5 mL center dot min(-1) center dot kg-1 and 1.5 vs. 0.6 - 0.9 L/kg, respectively). The mean residence times of amphamide in rats and rabbits were similar (30 vs. 27 - 43 h, respectively). The elimination half-lives calculated using a three-compartment model were 24 h for rats and 31 h for rabbits. The availability of rat tissue for amphamide ranged from 100% (brain) to 1700% (kidneys).
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页码：110 / 114
页数：5
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