PURPOSE: To investigate the influence of solvent properties on the phase behavior and physical stability of spray-dried solid dispersions containing naproxen and PVP K 25 prepared from binary cosolvent systems containing methanol, acetone and dichloromethane. METHODS: The viscosity, polymer globular size and evaporation rate of the spray-drying feed solutions were characterized. The solid dispersions were prepared by spray-drying drug-polymer solutions in binary solvent blends containing different proportions of each solvent. The phase behavior was investigated with mDSC, pXRD, FT-IR and TGA. Further, physical stability of solid dispersions was assessed by analyzing after storage at 75% RH. RESULTS: The solid dispersions prepared from solvent/anti-solvent mixture showed better miscibility and physical stability over those prepared from the mixtures of good solvents. Thus, solid dispersions prepared from dichloromethane-acetone exhibited the best physicochemical attributes followed by those prepared from methanol-acetone. FT-IR analysis revealed differential drug-polymer interaction in solid dispersions prepared from various solvent blends, upon the exposure to elevated humidity. CONCLUSION: Spray-drying from a cocktail of good solvent and anti-solvent with narrower volatility difference produces solid dispersions with better miscibility and physical stability resulting from the simultaneous effect on the polymer conformation and better dispersivity of drug.
PURPOSE: To investigate the influence of solvent properties on the phase behavior and physical stability of spray-dried solid dispersions containing naproxen and PVP K 25 prepared from binary cosolvent systems containing methanol, acetone and dichloromethane. METHODS: The viscosity, polymer globular size and evaporation rate of the spray-drying feed solutions were characterized. The solid dispersions were prepared by spray-drying drug-polymer solutions in binary solvent blends containing different proportions of each solvent. The phase behavior was investigated with mDSC, pXRD, FT-IR and TGA. Further, physical stability of solid dispersions was assessed by analyzing after storage at 75% RH. RESULTS: The solid dispersions prepared from solvent/anti-solvent mixture showed better miscibility and physical stability over those prepared from the mixtures of good solvents. Thus, solid dispersions prepared from dichloromethane-acetone exhibited the best physicochemical attributes followed by those prepared from methanol-acetone. FT-IR analysis revealed differential drug-polymer interaction in solid dispersions prepared from various solvent blends, upon the exposure to elevated humidity. CONCLUSION: Spray-drying from a cocktail of good solvent and anti-solvent with narrower volatility difference produces solid dispersions with better miscibility and physical stability resulting from the simultaneous effect on the polymer conformation and better dispersivity of drug.
Authors: Sandrien Janssens; Ann De Zeure; Amrit Paudel; Jan Van Humbeeck; Patrick Rombaut; Guy Van den Mooter Journal: Pharm Res Date: 2010-03-02 Impact factor: 4.200
Authors: Sandra Guns; Aswin Dereymaker; Pieterjan Kayaert; Vincent Mathot; Johan A Martens; Guy Van den Mooter Journal: Pharm Res Date: 2010-11-23 Impact factor: 4.200
Authors: Adam Bohr; Feng Wan; Jakob Kristensen; Mark Dyas; Eleanor Stride; Stefania Baldursdottír; Mohan Edirisinghe; Mingshi Yang Journal: J Mater Sci Mater Med Date: 2015-01-29 Impact factor: 3.896
Authors: Feng Wan; Adam Bohr; Morten Jonas Maltesen; Simon Bjerregaard; Camilla Foged; Jukka Rantanen; Mingshi Yang Journal: Pharm Res Date: 2012-12-11 Impact factor: 4.200
Authors: Sonal V Bhujbal; Dmitry Y Zemlyanov; Alex Cavallaro; Sharad Mangal; Lynne S Taylor; Qi Tony Zhou Journal: Mol Pharm Date: 2018-04-17 Impact factor: 4.939
Authors: Matthias E Lauer; Monira Siam; Joseph Tardio; Susanne Page; Johannes H Kindt; Olaf Grassmann Journal: Pharm Res Date: 2013-05-15 Impact factor: 4.200