title: 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.affiliation: Department of Pharmaceutics, Faculty of Pharmacy and Novel Drug Delivery Systems Research Center, Isfahan University of Medical Sciences, Isfahan, Iran. varshosaz@pharm.mui.ac.ir
authors.forename: Jaleh
authors.initials: J
authors.lastname: Varshosaz
authors.forename: Jaber
authors.initials: J
authors.lastname: Emami
authors.forename: Naser
authors.initials: N
authors.lastname: Tavakoli
authors.forename: Mohsen
authors.initials: M
authors.lastname: Minaiyan
authors.forename: Nakisa
authors.initials: N
authors.lastname: Rahmani
authors.forename: Farid
authors.initials: F
authors.lastname: Dorkoosh
authors.forename: Parvin
authors.initials: P
authors.lastname: Mahzouni
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000627:therapeutic use; D019819:Budesonide / Q000008:administration & dosage* / Q000737:chemistry / Q000627:therapeutic use; D002482:Cellulose / Q000737:chemistry; D055598:Chemical Phenomena; D019343:Citric Acid / Q000737:chemistry; D003093:Colitis, Ulcerative / Q000188:drug therapy / Q000276:immunology / Q000473:pathology; D003106:Colon / Q000187:drug effects / Q000276:immunology / Q000473:pathology; D004339:Drug Compounding; D016503:Drug Delivery Systems; D005079:Excipients / Q000737:chemistry*; D006863:Hydrogen-Ion Concentration; D007785:Lactose / Q000737:chemistry; D008297:Male; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D013608:Tablets, Enteric-Coated
chemical_list: D000893:Anti-Inflammatory Agents; D005079:Excipients; D013608:Tablets, Enteric-Coated; D019343:Citric Acid; D019819:Budesonide; D002482:Cellulose; D008747:Methylcellulose; D007785:Lactose