<abstract xmlns="http://www.w3.org/1999/xhtml"><p>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 % (<italic>m</italic>/<italic>m</italic>) citric acid in the cores coated with HPMC at a coating level of 6 % (<italic>m</italic>/<italic>m</italic>), Eudragit E containing Avicel RC 581 (30 %) as pore former at a coating level of 30 % (<italic>m</italic>/<italic>m</italic>) and HPMC AS at a coating level of 15 % (<italic>m</italic>/<italic>m</italic>) 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.</p></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.

Colon specific delivery of budesonide based on triple coated pellets: in vitro/in vivo evaluation

Department of Pharmaceutics, Faculty of Pharmacy and Novel Drug Delivery Systems Research Center, Isfahan University of Medical Sciences Isfahan, Iran

Department of Pharmacology, Faculty of Pharmacy and Isfahan Pharmaceutical Sciences Research Center, Isfahan University of Medical Sciences Isfahan, Iran

Department of Pharmaceutics, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran

Department of Clinical Pathology, Faculty of Medicine, Isfahan University of Medical Sciences, Isfahan, Iran

Acta Pharmaceutica

Three layered pellets of budesonide were prepared for colon delivery by the extrusion-spheronization method. The coatings consisted of hydroxypropylmethyl...

Colon specific delivery of budesonide based on triple coated pellets: in vitro/in vivo evaluation

Data publikacji: 06 lis 2012

Zakres stron: 341 - 356

DOI: https://doi.org/10.2478/v10007-012-0025-y

Słowa kluczowe
colon delivery, three layered pellets, Eudragit E, budesonide, HPMC AS, HPMC

This content is open access.

Colon specific delivery of budesonide based on triple coated pellets: in vitro/in vivo evaluation

Data publikacji: 06 lis 2012

Zakres stron: 341 - 356

DOI: https://doi.org/10.2478/v10007-012-0025-y

Słowa kluczowecolon delivery, three layered pellets, Eudragit E, budesonide, HPMC AS, HPMC

This content is open access.

Słowa kluczowe
colon delivery, three layered pellets, Eudragit E, budesonide, HPMC AS, HPMC