Bioassay study of absorption, distribution and excretion of ny-198 compared with norfloxacin and ofloxacin

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

Research output: Contribution to journalArticlepeer-review

8 Citations (Scopus)

Abstract

NY-198, a new pyridonecarboxylic acid dervative, is similar to norfloxacin (NFLX) and ofloxacin (OFLX) in its in vitro antibacterial properties but superior to them in vivo, one probable reason being that NY-198 is more easily absorbed and distributed in tissues than NFLX and OFLX after a single oral administration. We therefore studied absorption, distribution and urinary excretion of NY-198 in mice, rats and dogs and compared them with NFLX and OFLX. In mice, serum concentration of NY-198 reached a peak (Cmax) quickly and was higher than that of OFLX at the respective times after administration. The area under the curve (AUC) of NY-198 was about 1.8 times that of OFLX. NFLX was much lower than NY-198 and OFLX in both parameters. In rats, NY-198 was similar to OFLX in Cmax but its AUC was about 1.7 times that of OFLX. The urinary excretion rate of NY-198 was 69.9% within 24 h after administration, those of OFLX and NFLX were 43.5 and 12.7%. Further, the distribution in each tissue was best in NY-198. In dogs, NY-198 was similar to OFLX in Cmax and AUC but its T1/2 was longer than that of OFLX, being 6.47 and 5.45 h respectively. The urinary excretion rate of NY-198 was 53.8% and that of OFLX 39.7% within 72 h after administration. Our results indicate that NY-198 is superior to NFLX and OFLX in absorption, distribution and excretion in mice, rats and dogs.

Original languageEnglish
Pages (from-to)188-194
Number of pages7
JournalChemotherapy
Volume36
DOIs
Publication statusPublished - 1988

ASJC Scopus subject areas

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

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