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Colon Specific Delivery of Budesonide Based on Triple Coated Pellets: In Vitro/In Vivo Evaluation Publisher Pubmed



Varshosaz J1 ; Emami J1 ; Tavakoli N1 ; Minaiyan M2 ; Rahmani N1 ; Dorkoosh F3 ; Mahzouni P4
Authors

Source: Acta Pharmaceutica Published:2012


Abstract

Three layered pellets of budesonide were prepared for colon delivery by the extrusion-spheronization method. The coatings consisted of hydroxypropylmethyl cellulose (HPMC) (as barrier layer), Eudragit E (as rate controlling layer) and hydroxypropylmethyl cellulose acetate succinate (HPMC AS) (as enteric layer). The rate controlling layer was further modified using various pore formers. Dissolution studies were carried out at pH 1.2, 7.4 and 6.8. Pellet core composition and type and level of pore former affected the drug release from pellets. Pellets containing 20 % (m/m) citric acid in the cores coated with HPMC at a coating level of 6 % (m/m), Eudragit E containing Avicel RC 581 (30 %) as pore former at a coating level of 30 % (m/m) and HPMC AS at a coating level of 15 % (m/m) had the best release profiles. These pellets showed promising results in alleviating the conditions of an experimental model of colitis induced by trinitrobenzenesulfonic acid in rats.
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