Development of the Composition and Technology for Production a Solid Dispersion System by Hot Melt Extrusion to Increase the Bioavailability of the Active Substance

Introduction. The solubility of an active pharmaceutical ingredient plays a major role in drug absorption. Hot melt extrusion is batch or continuous process that allows creating solid dispersion systems based on various carriers order to increase and bioavailability substances. Development effective safe analgesics one the most vital tasks organic medicinal chemistry. An innovative non-opioid analgesic with very low toxicity dosage, but practically insoluble water, was used this work. It suggested obtain by hot bioavailability. Aim. technology for production system PAV-0056 as substance Plasdone™ S-630 polymeric carrier solubility. Materials methods. (methyl-2-(7-nitro-2-oxo-5-phenyl-3-propoxy-2,3-dihydro-1H-benzo[e][1,4]diazepin-1-yl)acetate) (JSC "Organica", Russia) Figure 1; (Boai NKY Pharmaceuticals Ltd., China); PEG-1500 (Clariant, Switzerland); acetonitrile chromatography (Thermo Fisher Scientific, Germany). Extrudates were obtained using HAAKE™ MiniCTW co-rotating twin-screw laboratory extruder examined optical microscopy differential scanning calorimetry, time water solution stability determined. quantitative content related impurities 2.5 % determined HPLC-UV. Results discussion. conditions established mixture S-630. Stability extrudate studied, extrudates Based binary mixture, composition containing 10 developed. optimal chosen obtaining meets requirements regulatory documentation impurities. Conclusion. proved be unsuccessful creation SDS due significant accumulation during process. By adding composition, it possible considerably lower operating temperature process, reduce impurity extrudate, maintain satisfactory water.