Development of Prednisone:Polyethylene Glycol 6000 Fast-Release Tablets From Solid Dispersions: Solid-State Characterization, Dissolution Behavior, and Formulation Parameters

LEONARDI D.; BARRERA, M.G.; LAMAS, M.C.; SALOMON, C.J.

AAPS PHARMSCI

American Association of Pharmaceutical Scientists

Año: 2007 vol. 8 p. 1 - 8

1522-1059

ABSTRACT   The aim of the current study was to design oral fast release polymeric tablets of prednisone and to optimize the drug dissolution profile by modifying the carrier concentration. Solid dispersions were prepared by the solvent evaporation method at different drug:polymer ratios (w/w). The physical state and drug:carrier interactions were analysed by X-ray diffraction, infrared spectra, and scanning electron microscopy. Dissolution rate of prednisone from solid dispersions was markedly enhanced by increasing the polymer concentration. The tablets were prepared from solid dispersion systems using polyethylene glycol (PEG) 6000 as a carrier at low and high concentration. The results showed that PEG 6000-based tablets exhibited a significantly higher prednisone dissolution (80% within 30 min), than the conventional tablet prepared without PEG 6000 (<25% within 30 min). In addition, the good disintegration and very good dissolution performance of the developed tablets without adding any superdisintegrant highlighted the suitability of these formulated dosage forms. The stability studies carried out in normal and accelerated conditions during twelve months showed that prednisone exhibited high stability in both PEG 6000 solid dispersion powders and tablets. The X-ray diffractometry showed that the degree of crystallinity of prednisone in solid dispersions decreased when the ratio of the polymer increased, suggesting that the drug is present inside the samples in different physical states. The FT-IR spectroscopic studies showed the stability of prednisone and the absence of well-defined drug:polymer interactions. SEM pictures showed a novel morphology of the dispersed systems in comparison with the pure components.