title: A new pharmaceutical concept for the treatment of oropharyngeal and oesophageal candidosis with fluconazole.
abstract: Administration of fluconazole in capsule form has proved effective in the prophylaxis and treatment of mucosal candidosis, particularly in immunosuppressed patients. An additional topical effect in oropharyngeal and oesophageal candidosis might be expected with a fluconazole suspension. This hypothesis was therefore tested in a crossover study in 12 healthy volunteers in whom the concentrations of the antimycotic were measured in saliva and plasma after oral administration of 100 mg fluconazole as either a capsule or a suspension. The time courses of the fluconazole concentrations were very similar with the two formulations in plasma, but significantly different in saliva. Thus, the mean Cmax for fluconazole in saliva of 551 micrograms ml-1 was reached 5 min after ingestion of the suspension, compared with a value of 3 micrograms ml-1 some 4 h after taking the capsule. The mean concentration of the antimycotic in saliva over the observation period (0-96 h) was more than 80% higher with the suspension than with the capsule.
authors.affiliation: Research and Development, Pfizer/Mack, Illertissen, Germany.
authors.forename: A
authors.initials: A
authors.lastname: Wildfeuer
authors.forename: H
authors.initials: H
authors.lastname: Laufen
authors.forename: R A
authors.initials: RA
authors.lastname: Yeates
authors.forename: T
authors.initials: T
authors.lastname: Zimmermann
mesh_terms: D000284:Administration, Oral; D000328:Adult; D000935:Antifungal Agents / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D002177:Candidiasis / Q000188:drug therapy*; D002180:Candidiasis, Oral / Q000188:drug therapy; D002214:Capsules; D018592:Cross-Over Studies; D005260:Female; D015725:Fluconazole / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D006801:Humans; D008297:Male; D008875:Middle Aged; D012463:Saliva / Q000378:metabolism; D013535:Suspensions
chemical_list: D000935:Antifungal Agents; D002214:Capsules; D013535:Suspensions; D015725:Fluconazole