Abstract
In this paper, we intended to understand the mechanism of dissolution enhancement for poorly water-soluble drugs by amorphous solid dispersions containing EUDRAGIT® E PO (EPO). Equilibrium solubility enhancement for three model drugs including ibuprofen, felodipine and bifendate were tested in acidic solutions containing different concentrations of EPO. Three model drugs were prepared into amorphous solid dispersions by hot melt extrusion with EPO. Results showed that EPO can substantially solubilize model drugs in acidic solution to 20–300 fold of their thermodynamic solubilities. Linear solubilizing relationships between EPO and drugs were achieved for all three drugs. It was found that amorphous solid dispersions with drug loadings below solubilizing range showed no recrystallization in dissolution tests whereas drug concentration reduction was seen in dissolution tests when drug loadings were above the solubilizing range. By combining the results from dynamic laser scattering, critical micelle concentration (CMC) and morphology studies, it was confirmed that EPO can form micelles in acidic solution, and the CMC value was estimated as 0.99 μg/ml. In conclusion, the dissolution enhancement for poorly water-soluble drugs by amorphous solid dispersions containing EPO was combined contribution from both the physical structure of solid dispersions and the solubilizing effect of EPO.
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