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Micronization of Solid Dispersion Pellets: Physical Characterization and Improved Dissolution

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Abstract:

Fluid-bed coating technology has been employed to prepare solid dispersion of poorly water-soluble drugs, which however has several disadvantages such as limited dissolution surface and insufficient dissolution rate. The objective of this study was to micronize solid dispersion pellets into fine powders to improve drug dissolution. Particularly, the solid dispersion pellets of ursodeoxycholic acid of different coating weight gain have been prepared using fluid-bed coating technique, and micronized to obtain fine powders that were subsequently blended with microcrystalline cellulose, crospovidone and Aerosil in weight ratios of 5:3:2:0.2 for tableting. Compared with pure solid dispersion powders, the blends exhibited improved compression index and angle of repose as well as acceptable flowability. In addition, the tablet tensile strength increased linearly with compression pressures, indicating good compactability of the blends. Furthermore, the drug dissolution improved significantly after micronization, which can be over 90% after 10 min. In contrast, their pellet counterparts dissolved less than 25% after 10 min, and the dissolution degree decreased as coating weight gain increased. It can be concluded that micronization of solid dispersion pellets provided a good alternative to produce solid dispersion powders with desirable properties as well as improved overall dissolution rate.

Keywords: DISSOLUTION; FLUID-BED; MICRONIZATION; PELLETS; SOLID DISPERSION; URSODEOXYCHOLIC ACID

Document Type: Research Article

DOI: https://doi.org/10.1166/asl.2012.2013

Publication date: 2012-03-01

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