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Influence of water uptake, gel network, and disintegration time on prednisone release from encapsulated solid
Darío Leonardi1, Claudio J Salomon
1Area Tecnología Farmacéutica, Departamento Farmacia, Facultad de Cs. Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, IQUIR (CONICET), 2000, Rosario, Argentina.
Abstract:
Prednisone is considered the glucocorticoid of choice for anti-inflammatory and immunosuppressant effects. However, its very low aqueous solubility can compromise oral bioavailability. Changes in the dissolution of a prednisone-PEG 6000 solid dispersion into capsule were investigated by addition of pregelatinized starch. Physical state of prednisone:PEG 6000 was analyzed by X-ray diffractometry, and scanning electron microscopy. Capsule formulations containing prednisone-PEG 6000 and pregelatinized starch showed superior dissolution properties (> 95% in 60 min) when compared with reference capsules without disintegrant (< 45% in 60 min). Water uptake and disintegration time were directly correlated with pregelatinized starch amount. The morphology of prednisone-PEG 6000 particles with disintegrant was analyzed by SEM, showing a novel surface structure. Thus, solid dispersions of a poorly water soluble drug combined with a disintegrant were confirmed as a valid approach to the improvement of drug dissolution.
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