Patent Evaluation: Prostaglandin Synthesis Inhibitors in Foam Formulations

Summary

Novelty: A topical anti-inflammatory pharmaceutical composition in the form of foam is disclosed. The composition contains as active principle ketoprofen lysine salt. The salt is said to inhibit the biosynthesis of prostaglandins, prostacyclines and thromboxane. The composition is useful for the local treatment of painful and phlogistic conditions of rheumatic or traumatic nature, of the articulations of the muscles, tendons and ligaments.

Biology: Data are provided on the absorption of the hydrophile solution of ketoprofen lysine salt on female rabbits after topical administration of the composition in the form of foam. Ketoprofen acid levels in plasma and urine samples were determined. The results support the utility of the composition.

Chemistry: The foam composition contains as active principle ketoprofen lysine salt in a concentration from 10-20% p/volume of solution, a suitable ionic or non-ionic emulsifier in a concentration of from 2-8% p/volume of solution, a suitable emollient in concentration of from 3-4% p/volume of solution, a suitable thickener in concentration of from 0.2-3% p/volume of solution, an optional suitable scent in concentration of from 0.5-0.02 p/volume of solution and a suitable bacteriostatic compound in concentration from 0.1-0.5% p/volume of solution and that the propellant gas which is used consists of the mixture butane:propane:isobutane in a concentration of from 3-7% p/p.