GEL SYSTEM OF NIMESULIDE FOR TOPICAL USE AND METHOD OF ITS PREPARING (VARIANTS) Russian patent published in 2002 - IPC

FIELD: medicine, pharmacy. SUBSTANCE: invention relates to the preparation of nimesulide as gel for topical use for treatment of patients with skin inflammations. The preparation has 0.5-7 wt.-% of nimesulide, gel-forming agent, solvent, preserving agents and, if necessary, stabilizing agent and mixture of caprylic and capric acids esters with glycerol. Gel-forming agent is taken among 0.1-5 wt.-% of carboxyvinyl polymer neutralized with triethanolamine or diisopropanolamine an aqueous solution or 0.5-10 wt. -% of polyacrylamideisoparaffin. Solvent is taken among the group including ethanol, isopropanol and diethylene glycol monoethyl ester. The concentration of ethanol and isopropanol in preparation is from 5 to 20 wt.-%, diethylene glycol monoethyl ester is from 40 to 95 wt.-%. Method of preparing the preparation involves preparing an aqueous dispersed phase containing water-soluble preserving agents and carboxyvinyl polymer, addition of alcohol solvent, dispersing nimesulide, water-insoluble preserving agents and, if necessary, additions (moistening agents and enhancers of dermal sorption), neutralization of carboxyvinyl polymer with triethanolamine or diisopropanolamine an aqueous solution. The second variant of method involves preparing an aqueous phase, preparing organic phase, dispersing organic phase in aqueous phase and neutralization of carboxyvinyl polymer by addition of triethanolamine or diisopropanolamine. An aqueous phase has water-soluble preserving agents, mixture of caprylic and capric acids esters with glycerol and homogenously dispersed carboxyvinyl polymer. Organic phase has water-insoluble preserving agents, preferably a mixture of parabens, and nimesulide in diethylene glycol monoethyl ester. Use of nonwater solvents in preparing the gel system of nimesulide provides improvement of physical-chemical indices of preparation and indices of release and absorption of nimesulide based on its ability to dissolve dermal lipid barrier. EFFECT: improved method of preparing. 7 cl, 5 ex _