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

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.
Authors	Jaleh Varshosaz, Jaber Emami, Naser Tavakoli, Mohsen Minaiyan, Nakisa Rahmani, Farid Dorkoosh, Parvin Mahzouni
Journal	Acta pharmaceutica (Zagreb, Croatia) (Acta Pharm) Vol. 62 Issue 3 Pg. 341-56 (Nov 2012) ISSN: 1846-9558 [Electronic] Poland
PMID	23470347 (Publication Type: Comparative Study, Journal Article)
Chemical References	Anti-Inflammatory Agents Excipients Tablets, Enteric-Coated Citric Acid Budesonide Cellulose Methylcellulose Lactose
Topics	Animals Anti-Inflammatory Agents (administration & dosage, chemistry, therapeutic use) Budesonide (administration & dosage, chemistry, therapeutic use) Cellulose (chemistry) Chemical Phenomena Citric Acid (chemistry) Colitis, Ulcerative (drug therapy, immunology, pathology) Colon (drug effects, immunology, pathology) Drug Compounding Drug Delivery Systems Excipients (chemistry) Hydrogen-Ion Concentration Lactose (chemistry) Male Methylcellulose (analogs & derivatives, chemistry) Particle Size Rats Rats, Wistar Solubility Tablets, Enteric-Coated

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