title: Reduction of gastric ulcerogenicity during multiple administration of diclofenac sodium by a novel solid-in-oil suspension.
abstract: This article reports a significant reduction of gastric ulcerogenicity by complex formation of a nonsteroidal anti-inflammatory drug with surfactants. Diclofenac sodium (DFNa) was suspended in medium chain triglyceride (MCT) by forming a complex with an edible lipophilic surfactant. Two types of suspensions, prepared through a membrane emulsification with different pore sizes, were evaluated according to the degree of gastric damage following multiple oral administration in rats. It was shown that gastric ulcerogenicity of DFNa was reduced by the surfactant-drug complexes, at doses up to 12 mg/kg, whereas severe gastric damage was observed upon oral administration of the aqueous solution at doses of 6 mg/kg. Comparable blood levels of DFNa were observed after administration of solution and suspension formulations.
authors.affiliation: Department of Applied Chemistry, Graduate School of Engineering, Kyushu University, Fukuoka, Japan.
authors.forename: Hongyu
authors.initials: H
authors.lastname: Piao
authors.forename: Akihiko
authors.initials: A
authors.lastname: Hirata
authors.forename: Hideakira
authors.initials: H
authors.lastname: Yokoyama
authors.forename: Takeru
authors.initials: T
authors.lastname: Fujii
authors.forename: Ichiro
authors.initials: I
authors.lastname: Shimizu
authors.forename: Susumu
authors.initials: S
authors.lastname: Ito
authors.forename: Noriho
authors.initials: N
authors.lastname: Kamiya
authors.forename: Masahiro
authors.initials: M
authors.lastname: Goto
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000627:therapeutic use*; D004008:Diclofenac / Q000008:administration & dosage* / Q000627:therapeutic use*; D009821:Oils / Q000008:administration & dosage*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013270:Stomach / Q000473:pathology; D013276:Stomach Ulcer / Q000188:drug therapy*; D013535:Suspensions
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D009821:Oils; D013535:Suspensions; D004008:Diclofenac