DESIGN OF THE COMPOSITION AND TECHNOLOGY OF LONG-ACTING ORAL NIMESULIDE GEL
Introduction. Oral gels combine the benefits of oral liquid and solid formulations. They are characterized by the high bioavailability of dispersed and dissolved drug substances. Nimesulide is one of the most popular analgesics on the Russian pharmaceutical market. Objective: to design a novel nimesulide formulation with optimal biopharmaceutical parameters. Material and methods. The object of the investigation is micronized nimesulide substance (India). The complex polymer carrier (CPC) Kollicoat®MAE 100P (BASF), Carbopol 974 P (Lubrizol) were used as polymer matrix formers; the viscosity modifiers were various cellulose derivatives, such as methylcellulose, sodium carboxymethylcellulose, hydroethylcellulose, and hydroxypropylcellulose. The content of nimesulide was determined spectrophotometrically. Results. The release of nimesulide from the obtained experimental samples of long-acting gel was assessed. Whether the matrix formers and gel formers of cellulose derivatives might be used simultaneously to obtain long-acting oral nimesulide gel was studied. The samples of gels based on CPC and Kollicoat®MAE 100 P showed an extended release. Conclusion. The biopharmaceutical studies conducted to design the composition and technology of long-acting oral nimesulide gels based on the derivatives of acrylic acid and polymethacrylic acid have revealed 3 compositions that are most promising for further investigations: CPC 2.0% with the addition of Benecel™ 2.0% and Kollicoat®MAE 100P 10.0%; or Benecel™ 2.0% and Kollicoat®MAE 100P 10.0%; or Blanose™ 2.0%. The composition of the gels will be finally chosen on the basis of results of studying the stability of the obtained samples during storage.