Category: Formulation and Quality
Purpose: Bowel diseases such as ulcerative colitis, Crohn’s disease, amebiasis, colon cancer, etc. necessitate targeted drug delivery into the colon. EUDRAGIT® FS 100 is a novel (meth)acrylic co-polymer carrier for colonic delivery of via solid dispersions1, 2. The aim of this study was to formulate stable solid dispersions using EUDRAGIT® FS 100 as carrier polymer for both solubility enhancement and colon targeting using spray drying and melt extrusion.
Methods: Among 1:2, 1:5 and 1:9 ratios of solid dispersions of Celecoxib (Aarti Drugs) with EUDRAGIT® FS 100, 1:9 ratio was selected based on quicker dissolution for further evaluation. Anticipating highly flexible and soft nature of solid dispersions with EUDRAGIT® FS 100 alone because of its low Tg, they were co-processed with high Tg polymers like PVP K-30, Kollidon VA 64, HPMC ASMF, Sylsia 350 FCP. Silica mixture consisting of AEROPERL® 300 Pharma and Sylsia 350 FCP was added externally to the solid dispersions to reduce aggregation.
Preparation of solid dispersions via hot melt extrusion:
Celecoxib with following polymer combinations was extruded using twin screw extruder (Omicron 12, STEER Engineering) (Table 1).
Viraj Kulthe– Evonik Industries, Mumbai, Maharashtra, India
Priyanka Haksar– Mumbai, Maharashtra, India
Shraddha Joshi– Director, Formulation Development Orals, Evonik India Pvt Ltd, Mumbai, Maharashtra, India
Umesh Kapale– Mumbai, Maharashtra, India
Preeti Patil– Evonik Industries, Mumbai, Maharashtra, India
Smitha Shetty– Head of Analytical Development, Evonik Industries, Mumbai, Maharashtra, India
Firouz Asgarzadeh– Director of Technical Marketing, Evonik Corporation, Piscataway, New Jersey