title: New formulation of 5-fluorouracil in microspheres reduces toxicity in mice.
abstract: A new dosage formulation of 5-fluorouracil incorporated in microspheres (5-FU-MS) was developed for the treatment of peritoneal carcinomatosis. We studied the acute toxicity and side effects of i.p. 5-FU-MS in mice. The 50% lethal dose value for 5-FU-MS was 535.4 mg/kg of 5-FU, which was 2.22 times that of the aqueous 5-FU solution. Deaths occurred 12-17 days after the administration of 5-FU-MS, but within 11 days after the administration of aqueous 5-FU. Thus, lethal toxicity appeared later with 5-FU-MS than with aqueous 5-FU. There were no differences in pathologic findings on autopsy between mice given the two dosage formulations.
authors.affiliation: First Department of Surgery, Kyoto Prefectural University of Medicine, Japan.
authors.forename: A
authors.initials: A
authors.lastname: Hagiwara
authors.forename: C
authors.initials: C
authors.lastname: Sakakura
authors.forename: H
authors.initials: H
authors.lastname: Tsujimoto
authors.forename: M
authors.initials: M
authors.lastname: Ohgaki
authors.forename: T
authors.initials: T
authors.lastname: Imanishi
authors.forename: J
authors.initials: J
authors.lastname: Yamazaki
authors.forename: K
authors.initials: K
authors.lastname: Sawai
authors.forename: T
authors.initials: T
authors.lastname: Takahashi
authors.forename: A
authors.initials: A
authors.lastname: Yamamoto
authors.forename: S
authors.initials: S
authors.lastname: Muranishi
authors.forename: Y
authors.initials: Y
authors.lastname: Tabata
authors.forename: Y
authors.initials: Y
authors.lastname: Ikada
mesh_terms: D000818:Animals; D000964:Antimetabolites, Antineoplastic / Q000737:chemistry / Q000493:pharmacokinetics / Q000506:poisoning / Q000633:toxicity*; D001835:Body Weight / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D004354:Drug Screening Assays, Antitumor; D005472:Fluorouracil / Q000737:chemistry / Q000493:pharmacokinetics / Q000506:poisoning / Q000633:toxicity*; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D008863:Microspheres; D014018:Tissue Distribution
chemical_list: D000964:Antimetabolites, Antineoplastic; D005472:Fluorouracil