Acta Pharm. 62 (2012) 341-356
Original research paper
Colon
specific delivery of budesonide based on triple coated pellets: In vitro/in vivo evaluation
JALEH
VARSHOSAZ, JABER EMAMI, NASER
TAVAKOLI, MOHSEN MINAIYAN, NAKISA RAHMANI,
FARID DORKOOSH and PARVIN MAHZOUNI
1 Department
of Pharmaceutics, Faculty of Pharmacy and Novel Drug Delivery Systems Research
Center, Isfahan University of Medical Sciences, Isfahan, Iran
2 Department of Pharmacology, Faculty of Pharmacy
and Isfahan Pharmaceutical Sciences Research Center, Isfahan University of
Medical Sciences, Isfahan, Iran
3 Department
of Pharmaceutics, Faculty of Pharmacy, Tehran University of Medical Sciences,
Tehran, Iran
4 Department
of Clinical Pathology, Faculty of Medicine, Isfahan University of Medical
Sciences, Isfahan, Iran
Accepted June 11, 2012
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 citric acid 20 % (m/m) 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.
Keywords: colon delivery, three layered pellets, Eudragit E,
budesonide, HPMC AS, HPMC