title: 5% amlexanox oral paste, a new treatment for recurrent minor aphthous ulcers: II. Pharmacokinetics and demonstration of clinical safety.
abstract: The safety of 5% Amlexanox paste was demonstrated in the following clinical studies: vehicle-controlled safety and efficacy studies; dermal irritation and sensitization studies; single and multiple dose pharmacokinetic studies; and a 28-day in use safety study. Minimal adverse experiences were observed with the 991 subjects that were exposed to 5% Amlexanox paste. No significant irritation or sensitization was associated with 5% Amlexanox paste. Pharmacokinetic studies indicated that systemic levels of Amlexanox are most likely due to normal gastrointestinal absorption with only limited absorption directly through the ulcer. After a 100 mg dose of 5% Amlexanox paste the average maximum concentration of Amlexanox in the serum was 120 ng/ml, occurring 2.4 hours after application. The half-life for elimination of Amlexanox was 3.5 hours, and there was no evidence of accumulation with multiple applications. Overall, the data indicate that 5% Amlexanox paste (Aphthasol) is safe for the treatment of recurrent minor aphthous ulcers.
authors.affiliation: Shaman Pharmaceuticals, Inc., South San Francisco, Calif., USA.
authors.forename: A
authors.initials: A
authors.lastname: Khandwala
authors.forename: R G
authors.initials: RG
authors.lastname: Van Inwegen
authors.forename: M R
authors.initials: MR
authors.lastname: Charney
authors.forename: M C
authors.initials: MC
authors.lastname: Alfano
mesh_terms: D000287:Administration, Topical; D000328:Adult; D000631:Aminopyridines / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D000893:Anti-Inflammatory Agents / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D019540:Area Under Curve; D004305:Dose-Response Relationship, Drug; D004341:Drug Evaluation; D005260:Female; D006801:Humans; D007408:Intestinal Absorption; D016015:Logistic Models; D008297:Male; D008657:Metabolic Clearance Rate; D010328:Patch Tests; D012449:Safety; D012867:Skin / Q000187:drug effects; D013281:Stomatitis, Aphthous / Q000188:drug therapy*
chemical_list: D000631:Aminopyridines; D000893:Anti-Inflammatory Agents; C045742:amlexanox