5% amlexanox oral paste, a new treatment for recurrent minor aphthous ulcers: II. Pharmacokinetics and demonstration of clinical safety

Oral Surg Oral Med Oral Pathol Oral Radiol Endod. 1997 Feb;83(2):231-8. doi: 10.1016/s1079-2104(97)90010-x.

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.

Publication types

  • Clinical Trial
  • Multicenter Study
  • Randomized Controlled Trial

MeSH terms

  • Administration, Topical
  • Adult
  • Aminopyridines / adverse effects
  • Aminopyridines / blood
  • Aminopyridines / pharmacokinetics*
  • Aminopyridines / therapeutic use*
  • Anti-Inflammatory Agents / adverse effects
  • Anti-Inflammatory Agents / blood
  • Anti-Inflammatory Agents / pharmacokinetics*
  • Anti-Inflammatory Agents / therapeutic use*
  • Area Under Curve
  • Dose-Response Relationship, Drug
  • Drug Evaluation
  • Female
  • Humans
  • Intestinal Absorption
  • Logistic Models
  • Male
  • Metabolic Clearance Rate
  • Patch Tests
  • Safety
  • Skin / drug effects
  • Stomatitis, Aphthous / drug therapy*

Substances

  • Aminopyridines
  • Anti-Inflammatory Agents
  • amlexanox