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Preparation and analgesic activity of Eudragit RS100 microparticles containing diflunisal.


Abstract Two different techniques, the quasi-emulsion solvent diffusion method and spray drying that provide polar and nonpolar prepn. environments, were used to prep. microspheres from Eudragit RS100 (RS) (acrylic/methacrylic copolymer) incorporating the nonsteroidal anti-inflammatory drug diflunisal. The effects of pH on the prepn. medium and drug/polymer ratio on prodn. yield and drug incorporation, as well as on the in vitro drug release at pH 1.2 and 6.8 from tabletted microparticles, were evaluated. The drug-polymer interactions and the effect of diflunisal incorporation in the polymer matrix on drug crystallinity have been evaluated by using differential scanning calorimetry, IR and UV spectroscopy, x-ray diffraction, and microscopy anal. A preliminary biol. assay confirmed that diflunisal maintains its analgesic activity after i.p. administration to rats.
Autori
PUGLISI - Giovanni
PIGNATELLO - Rosario
Altri Autori Amico Davide
Chiechio Santina
Spadaro Concetta
Giunchedi Paolo