Disposition and metabolism of NY-198 I. Bioassay study of absorption, distribution and excretion in various animals

Eiichi Okezaki, Kohichi Ohmichi, Shoji Kojice, Yoshie Takahashi, Eiichi Makino, Tetsuya Terasaki, Akira Tsuji

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10 Citations (Scopus)

Abstract

Absorption, distribution and excretion of NY-198, a new pyridonecarboxylic acid derivative, were examined by bioassay in mice, rats and dogs after a single oral and intravenous administration. 1. The peak serum concentration (Cmax) of NY-198 after oral administration to mice, rats and dogs at a dose of 20mg/kg were 5.30, 9.73 and 9.64 μg/ml, namely, Cmax in mice was lower than in rats and dogs. Ratios of area under the curve (AUC) of oral to intravenous administration (p.o./i.v.) to rats (20 mg/kg) and dogs (5 mg/kg) were 0.85 and 0.92. NY-198 showed excellent oral absorbability in rats and dogs. 2. Cmax of NY-198 after oral administration to rats at a dose of 10, 20 and 40 mg/kg was 5.90, 9.73 and 22.46 μg/ml. Their AUC's were 11.4, 22.6 and 55.1 μg/ml, respectively. Cmax and AUC increased dose-dependently. 3. The urinary excretion rate of NY-198 after oral administration of 20 mg/kg was 69.9% within 24 h in rats and 53.8% within 72 h in dogs. Urinary recovery of NY-198 was excellent. 4. After oral administration to rats, NY-198 was distributed in kidney, liver, prostate and skeletal muscle at higher than serum levels, but in lung it was slightly lower. 5. Antibacterial metabolites in urine of rat, dog and monkey after oral administration were examined by TLC-bioautography and no active metabolites were detected. These results indicate that NY-198 is excellently absorbed after oral administration, distributed in most tissues of the body at high concentrations and that it is not metabolized, but excreted unchanged mainly into urine.

Original languageEnglish
Pages (from-to)132-137
Number of pages6
JournalChemotherapy
Volume36
DOIs
Publication statusPublished - 1988 Jan 1
Externally publishedYes

ASJC Scopus subject areas

  • Pharmacology (medical)
  • Infectious Diseases
  • Pharmacology
  • Drug Discovery
  • Oncology

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