Co-processed excipient for orally disintegration tablets obtained by spray drying and wet granulation.

ROSAS MD; VILLA M; CABRERA F; PIÑA J; RAMÍREZ RIGO MV.; BUCALÁ V

Rosario

Congreso; 4° Reunión Internacional de Ciencias Farmacéuticas (RICiFa 2016); 2016

Universidad de Rosario y UNC

IntroductionA co-processed excipient of mannitol and polyvinylpyrrolidone has been obtained by spray drying [1]. This product is suitable for formulation of orally disintegrating tablets-(ODTs) due to its excellent disintegration properties. In this study, the spray-drying operating conditions were modified and an alternative process was tested to obtain a product with better flow properties.Materials and MethodsMaterials: Mannitol and Polyvinylpyrrolidone-K29/32.Spray Drying. Aqueous solutions of mannitol and polyvinylpyrrolidone (9.0:1.0) were dried at inlet temperature 130°C, atomization air flowrate 500L/h, feed flowrate 2-4mL/min and aspiration 35m3/h. Wet Granulation. Mannitol was atomized with polyvinylpyrrolidone aqueous solutions (10%w/v) in a top-spray fluidized bed to obtain (9.9:0.1) mannitol: polyvinylpyrrolidone powders, by using: bed temperature 45°C, binder flowrate 100 ml/h, atomization air flowrate 10mL/min and varying the fluidization air flowrate between 0.053-0.061m3/s.Tableting. Compacts were produced using a hydraulic press.Products characterization. Size distribution was determined by laser diffraction. Powder flow properties (Carr's index-(CI) and Angle of Repose-(AR)) and the tablet disintegration time-(DT) were determined according to pharmacopoeias. The wetting time-(WT) was evaluated in distilled water. ResultsFor both processes, the yields were within 67-73% (acceptable for lab-scale). The powders had mean sizes (26.5µm and 92.04µm for spray-dried and granulated powder) significantly higher than 13.92µm obtained in [1]. The CI and AR of the granulated excipient were 36 and 34° and for the spray-dried product were 34 and 37°, indicating that both strategies improved the powder flow in comparison with 39 and 48º of the product with best yield in [1]. Compacts of spray-dried and granulated powders show DT and WT lower than 30s, being useful for ODT design. ConclusionBoth processes and the optimized operating variables allowed modifying the product quality, enhancing its functionality as excipient for direct compression.