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Abstract
Objective: The aim of this study was to evaluate the applicability of POVACOATTM, a hydrophilic PVA copolymer, as a solid dispersion (SD) carrier for hot-melt extrusion (HME).
Methods: Bifendate (DDB), a water-insoluble drug, was chosen as the model drug. DDB was hot-melt extruded by a co-rotating twin screw extruder with POVACOATTM. The SD formability of POVACOATTM was investigated by varying the composition ratios. Solid state characterization was evaluated by differential scanning calorimetry, powder X-ray diffraction, scanning electron microscopy and Fourier transformation infrared spectroscopy. In order to have a better knowledge of the mechanism of dissolution enhancement, dissolution study, phase solubility study and crystallization study of DDB from supersaturated solutions were performed. In addition, the storage stability of the extrudate containing 10% DDB was investigated.
Results: Physical characterizations showed that DDB was amorphous up to 15% drug loading. The phase solubility study revealed an AL-type curve. Moreover, POVACOATTM was found to have an inhibitory effect on crystallization from supersaturated solutions. Compared with the pure DDB and physical mixture, the dissolution rate and solubility of extrudates were significantly enhanced and the drug loading markedly affected the dissolution of SDs. Furthermore, the stability test indicated that 10% DDB-SD was stable during storage (40 °C/75% RH).
Conclusion: The results of this study demonstrate that POVACOATTM is a valuable excipient for the formulation of solid dispersions prepared by HME to improve dissolution of poorly water-soluble drugs.