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

被引:8
作者
Varshosaz, Jaleh [1 ,2 ]
Emami, Jaber [1 ,2 ]
Tavakoli, Naser [1 ,2 ]
Minaiyan, Mohsen [3 ,4 ]
Rahmani, Nakisa [1 ,2 ]
Dorkoosh, Farid [5 ]
Mahzouni, Parvin [6 ]
机构
[1] Isfahan Univ Med Sci, Dept Pharmaceut, Fac Pharm, Esfahan, Iran
[2] Isfahan Univ Med Sci, Novel Drug Delivery Syst Res Ctr, Esfahan, Iran
[3] Isfahan Univ Med Sci, Dept Pharmacol, Fac Pharm, Esfahan, Iran
[4] Isfahan Univ Med Sci, Isfahan Pharmaceut Sci Res Ctr, Esfahan, Iran
[5] Univ Tehran Med Sci, Fac Pharm, Dept Pharmaceut, Tehran, Iran
[6] Isfahan Univ Med Sci, Dept Clin Pathol, Fac Med, Esfahan, Iran
关键词
colon delivery; three layered pellets; Eudragit E; budesonide; HPMC AS; HPMC; RELEASE;
D O I
10.2478/v10007-012-0025-y
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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.
引用
收藏
页码:341 / 356
页数:16
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