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Preclinical Pharmacokinetics Study of Amphamide: a New Semisynthetic Antifungal Antibiotic

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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 ∙ min–1 ∙ 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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Authors and Affiliations

  1. G. F. Gause Institute of New Antibiotics, Moscow, 119021, Russia

    Yu. A. Portnoi, M. B. Kobrin, S. A. Dovzhenko, A. N. Tevyashova, M. I. Treshchalin, V. A. Golibrodo & A. A. Firsov

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  1. Yu. A. Portnoi
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  2. M. B. Kobrin
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  3. S. A. Dovzhenko
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  4. A. N. Tevyashova
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  5. M. I. Treshchalin
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  6. V. A. Golibrodo
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  7. A. A. Firsov
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Correspondence to Yu. A. Portnoi.

Additional information

Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 54, No. 2, pp. 8 – 12, February, 2020.

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Portnoi, Y.A., Kobrin, M.B., Dovzhenko, S.A. et al. Preclinical Pharmacokinetics Study of Amphamide: a New Semisynthetic Antifungal Antibiotic. Pharm Chem J 54, 110–114 (2020). https://doi.org/10.1007/s11094-020-02165-3

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  • DOI: https://doi.org/10.1007/s11094-020-02165-3

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