Flumizole, a new nonsteroidal anti-inflammatory agent.
Flumizole is a potent anti-inflammatory agent in animal models with an inhibitory activity severalfold that of indomethacin in rat foot edema and prostaglandin synthetase tests. The drug was well absorbed from the GI tract when administered in the solution used in pharmacological assays. However, markedly poorer absorption of the solid form of this poorly water-soluble agent led to the development of a flumizole dispersion with polyethylene glycol 6000. The solid dispersion exhibited an increased dissolution rate in simulated gastric fluid and improved absorption properties in dogs relative to unformulated flumizole. Studies with a capsule formulation of the solid dispersion in human volunteers were indicative of good drug absorption. Plasma levels of flumizole were rapidly achieved and declined with a short half-life (2-7 hr) in rats, dogs, and humans.
D000284:Administration, Oral; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000378:metabolism / Q000494:pharmacology* / Q000627:therapeutic use; D001682:Biological Availability; D016861:Cyclooxygenase Inhibitors; D004285:Dogs; D004487:Edema / Q000188:drug therapy; D004890:Erythema / Q000188:drug therapy; D005243:Feces / Q000032:analysis; D005260:Female; D006099:Granuloma / Q000188:drug therapy; D006168:Guinea Pigs; D007093:Imidazoles / Q000378:metabolism / Q000494:pharmacology* / Q000627:therapeutic use; D007213:Indomethacin / Q000494:pharmacology; D007263:Infusions, Parenteral; D007274:Injections, Intraperitoneal; D008297:Male; D010653:Phenylbutazone / Q000494:pharmacology; D051381:Rats
D000893:Anti-Inflammatory Agents; D016861:Cyclooxygenase Inhibitors; D007093:Imidazoles; D010653:Phenylbutazone; D007213:Indomethacin; C011252:flumizole