Dissolution Enhancement Using Different Formulation Approaches. Dissolution Enhancement of a Poorly Soluble Model Drugs Using Different Formulation Approaches for Immediate Release

      Аннотация: The objective of this study was to design Bilayered tablets (SNFML) and to enhance the in vitro release rates. Several techniques were compared for improving the dissolution of model drugs SNFML, poorly soluble drugs. Particle size reduction was realized by jet milling (Micronization of SNML), use of solubility enhancers in the formulation like Klucel-Lf and sodium lauryl sulphate with reduction of surface energy by co-sifting, SNML with lactose showed the immediate release profile when compared with the unmicronized drug. Micronization of SNML enhanced its dissolution rate in Discriminative media (8.2% in 30 min) compared to unmicronized drug (1.3% in 30 min). SNML drug products commercially available on the German, French and Indian markets dissolved similarly to unmicronized SNML, but significantly slower than the micronized drug. The results suggest that Micronization, use of solubility enhancers and reduction of surface energy by co-sifting are powerful ways for the preparation of immediate release formulations of SNFML, and could potentially lead to improvements in the bioavailability of oral SNFML products.

Ключевые слова: dissolution enhancement, Poorly water-soluble drugs, Hydrophilic polymers, Micronization, SNFML