Selection of the suitable polymer for supercritical fluid assisted preparation of carvedilol solid dispersions.

作者: Jelena Djuris , Stoja Milovanovic , Djordje Medarevic , Vladimir Dobricic , Aleksandra Dapčević

DOI: 10.1016/J.IJPHARM.2018.11.015

关键词:

摘要: Abstract Solid dispersions production is one of the substantial approaches for improvement poor drug solubility. Additionally, supercritical fluid assisted method preparation solid can offer many advantages in comparison to conventional melting or solvent-evaporation methods. Miscibility analysis provides valuable guidance selection most appropriate polymeric carrier dispersion interest. In addition increased release rate, should have proper mechanical attributes order be successfully formulated final dosage form such as tablet. Therefore, several pharmaceutical grade polymers been selected development BCS Class II carvedilol (CARV) dispersions. They were compared based on behavior CO2 and affinity towards CARV calculated from miscibility analysis. By utilization method, with (co)polymers (polyvinylpyrrolidone (PVP), hydroxypropyl methylcellulose (HPMC), Soluplus® Eudragit®) obtained. Properties prepared CARV-polymer observed by polarizing scanning electron microscopy analyzed differential calorimetry Fourier transform infrared spectroscopy. was additionally characterized X-ray powder diffraction. Furthermore, vitro dissolution studies dynamic compaction performed samples Among studied polymers, PVP HPMC identified highest CARV, δp values. This has also confirmed efficiency CARV-PVP CARV-HPMC state characterization indicated that dispersed either molecularly, amorphous form, depending interactions each polymer. Determination properties revealed superior compactibility tabletability. highlighted further tablets form. Presented study an example efficient approach poorly soluble satisfactory tableting properties.

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