[Development of 5-fluorouracil incorporated in microspheres for peritoneal carcinomatosis--animal experiments].
A new dosage formulation (5-FU-MS), composed of 5-fluorouracil (5-FU) incorporated in polyglactin microspheres, was studied by animal experiments, which revealed the following results. Intraperitoneal 5-FU-MS delivered greater concentrations of 5-FU for longer periods selectively to the intraperitoneal tissues, whereas it delivered a lower concentration to the blood plasma, than 5-FU solution did in rats. In mice, the 50% lethal dose value of intraperitoneal 5-FU-MS was 535 mg/kg. The toxicity of 5-FU-MS was less than 1/2 that of intraperitoneal 5-FU solution, of which the 50% lethal dose value was 242 mg/kg. Intraperitoneal 5-FU-MS at 200 mg of 5-FU/kg improved the survival curve of mice with peritoneal carcinomatosis better than the identical dose of 5-FU solution.
Hagiwara
A
A
First Dept. of Surgery, Kyoto Prefectural University of Medicine.
Takahashi
T
T
Shimotsuma
M
M
Shirasu
M
M
Tsujimoto
H
H
Ohyama
T
T
Ohgaki
M
M
Imanishi
T
T
Yamazaki
J
J
Fujita
T
T
D000818:Animals; D001202:Ascitic Fluid / Q000188:drug therapy* / Q000378:metabolism; D003692:Delayed-Action Preparations; D005472:Fluorouracil / Q000493:pharmacokinetics / Q000627:therapeutic use*; D008297:Male; D051379:Mice; D008863:Microspheres; D009374:Neoplasms, Experimental / Q000473:pathology*; D010538:Peritonitis / Q000188:drug therapy* / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar
D003692:Delayed-Action Preparations; D005472:Fluorouracil