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).
引用
收藏
页码：110 / 114
页数：5
相关论文
共 50 条
  • [21] GLOBOROSEOMYCIN, A NEW ANTIFUNGAL ANTIBIOTIC
    LIU, Y
    ZHANG, Y
    ZHANG, Z
    ZHANG, M
    DAI, Z
    LIU, T
    FANG, J
    HONG, J
    CHINESE MEDICAL JOURNAL, 1979, 92 (07) : 443 - 450
  • [22] CANDICIDIN, A NEW ANTIFUNGAL ANTIBIOTIC
    LECHEVALIER, H
    ACKER, RF
    CORKE, CT
    HAENSELER, CM
    WAKSMAN, SA
    MYCOLOGIA, 1953, 45 (02) : 155 - 171
  • [23] New antifungal drugs in preclinical development
    Hector, RF
    COCCIDIOIDOMYCOSIS: CENTENNIAL CONFERENCE, 1996, : 265 - 274
  • [24] Preclinical Study of the Pharmacokinetics of a New Intravenous Dosage Form of Ubiquinol
    E. I. Kalenikova
    E. A. Gorodetskaya
    O. Y. Kulyak
    L. P. Kozaeva
    V. G. Makarov
    O. N. Pozharitskaya
    A. N. Shikov
    O. S. Medvedev
    Pharmaceutical Chemistry Journal, 2018, 51 : 949 - 953
  • [25] Preclinical Study of the Pharmacokinetics of a New Intravenous Dosage Form of Ubiquinol
    Kalenikova, E. I.
    Gorodetskaya, E. A.
    Kulyak, O. Y.
    Kozaeva, L. P.
    Makarov, V. G.
    Pozharitskaya, O. N.
    Shikov, A. N.
    Medvedev, O. S.
    PHARMACEUTICAL CHEMISTRY JOURNAL, 2018, 51 (11) : 949 - 953
  • [26] PRECLINICAL AND CLINICAL-STUDY OF QUINOCARMYCIN, A NEW ANTITUMOR ANTIBIOTIC
    OGAWA, M
    TAGUCHI, T
    INVESTIGATIONAL NEW DRUGS, 1987, 5 (01) : 110 - 110
  • [27] NEW APPROACHES IN PRECLINICAL AND CLINICAL PHARMACOKINETICS
    GRAHAM, MA
    KAYE, SB
    CANCER SURVEYS, 1993, 17 : 27 - 49
  • [28] PHARMACOKINETICS OF SULBENICILLIN, A NEW BROAD-SPECTRUM SEMISYNTHETIC PENICILLIN
    HANSEN, I
    JACOBSEN, E
    WEIS, J
    CLINICAL PHARMACOLOGY & THERAPEUTICS, 1975, 17 (03) : 339 - 347
  • [29] ACTIVITY OF VARIOTIN, A NEW ANTIFUNGAL ANTIBIOTIC
    SUZUKI, S
    SUGANUMA, A
    KISHIDA, T
    MIZUNOYA, A
    UEDA, F
    SUZUKI, Y
    KIJI, I
    KYO, T
    TAKEUCHI, M
    NAKAZAWA, S
    KISHI, N
    TSUMURA, S
    JOURNAL OF ANTIBIOTICS, 1959, 12 (05): : 244 - 248
  • [30] ANTIFUNGAL ACTIVITY OF NEW ANTIBIOTIC GRISEOFUULVIN
    STEPANISHCHEVA, Z
    ANTIBIOTIKI, 1961, 6 (09): : 41 - +
12345