New formulation of 5-fluorouracil in microspheres reduces toxicity in mice.
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.
Hagiwara
A
A
First Department of Surgery, Kyoto Prefectural University of Medicine, Japan.
Sakakura
C
C
Tsujimoto
H
H
Ohgaki
M
M
Imanishi
T
T
Yamazaki
J
J
Sawai
K
K
Takahashi
T
T
Yamamoto
A
A
Muranishi
S
S
Tabata
Y
Y
Ikada
Y
Y
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
D000964:Antimetabolites, Antineoplastic; D005472:Fluorouracil