title: [Affinity of T-3761 to ocular melanin and intraocular dynamics].
abstract: The affinity of T-3761 to melanin was examined with synthetic melanin comparing other quinolones. The binding rates with synthetic melanin were from 37% to 48% for tosufloxacin, sparfloxacin, ciprofloxacin and norfloxacin. Binding rate of ofloxacin at 28% was lower and T-3761 was lowest at 22%. Intraocular dynamics of T-3761 and ofloxacin were investigated in pigmented rabbits after a single oral administration at a dose of 20 mg/kg. In both drugs, the concentrations in the melanin bearing tissues were higher and the disappearances from the melanin bearing tissues were more slowly than those of the non-melanin bearing tissues. T-3761 concentrations in the melanin bearing tissues were significantly lower than ofloxacin. In vitro uptake amount to melanin bearing tissue of ofloxacin was 1.4-2.4 times larger than that of T-3761.
authors.affiliation: Research Laboratories, Toyama Chemical Co., Ltd., Japan.
authors.forename: H
authors.initials: H
authors.lastname: Hayakawa
authors.forename: K
authors.initials: K
authors.lastname: Hayashi
authors.forename: H
authors.initials: H
authors.lastname: Ishikura
authors.forename: K
authors.initials: K
authors.lastname: Nakafuku
authors.forename: Y
authors.initials: Y
authors.lastname: Takano
authors.forename: Y
authors.initials: Y
authors.lastname: Nakajima
authors.forename: M
authors.initials: M
authors.lastname: Oishi
mesh_terms: D000818:Animals; D000890:Anti-Infective Agents / Q000378:metabolism* / Q000493:pharmacokinetics; D005123:Eye / Q000378:metabolism*; D024841:Fluoroquinolones; D008543:Melanins / Q000378:metabolism*; D015242:Ofloxacin / Q000378:metabolism / Q000493:pharmacokinetics; D010078:Oxazines / Q000378:metabolism* / Q000493:pharmacokinetics; D011817:Rabbits
chemical_list: D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D008543:Melanins; D010078:Oxazines; C078052:pazufloxacin; D015242:Ofloxacin