Physical properties and solubility studies of Nifedipine-PEG 1450/HPMCAS-HF solid dispersions

AbstractLow-order high-energy nifedipine (NIF) solid dispersions (SDs) were generated by melt solvent amorphization with PEG 1450 and HPMCAS-HF to increase NIF solubility while achieving acceptable physical stability. HPMCAS-HF was used as a crystallization inhibitor. Individual formulation components, their physical mixtures (PMs), and SDs were characterized by DSC, PXRD, and FTIR. NIF solubility and percent crystallinity (PC) were determined at initial time and after 5 days stored at 25°C and 60% RH. FTIR indicated that hydrogen bonding was involved with the amorphization process. FTIR showed that NIF:HPMCAS-HF intermolecular interactions were weaker than NIF:PEG 1450 interactions. NIF:PEG 1450 SD solubilities were significantly higher than their PM counterparts (p<0.0001). The solubilities of NIF:PEG 1450:HPMCAS-HF SDs were significantly higher than their corresponding NIF:PEG 1450 SDs (p<0.0001-0.043). All the SD solubilities showed a statistically significant decrease (p<0.0001) after storage for fiv...