Preparation and in vitro evaluation of mebeverine HCl colon-targeted drug delivery system.
Mebeverine HCl is a water soluble drug commonly used to treat irritable bowel syndrome by acting directly on the smooth muscles of the colon. This work was aimed at the formulation and in vitro evaluation of a colon-targeted drug delivery system containing mebeverine HCl. Matrix tablets were prepared using ethyl cellulose (EC), Eudragit RL 100 either solely or in combination by wet granulation technique. Dissolution was carried out in 0.1 N HCl for 2?h followed by pH 6.8 phosphate buffer for eight hours. Uncoated forms released more than 5% drug in 0.1 N HCl therefore, Eudragit L100 was used as a coat. The results indicated very slow release profile. As a result, single retardant was used to prepare the matrix and coated by Eudragit L 100. The matrix containing 7% Eudragit RL 100 and 6% of binder was subjected to further studies to assess the effect of different coats (Eudragit L 100-55 and cellulose acetate phthalate) and different binders (pectin and sodium alginate) on the release profile. Eudragit L 100 and pectin were the best coating agent and binder, respectively. The final formula was stable and it can be concluded that the prepared system has the potential to deliver mebeverine HCl in vivo to the colon.
Abdullah
Ghassan Z
GZ
School of Pharmaceutical Sciences, Universiti Sains Malaysia, Minden 11800, Penang, Malaysia. ghassanalyasiri@yahoo.com
Abdulkarim
Muthanna F
MF
Chitneni
Mallikarjun
M
Mutee
Ahmed F
AF
Ameer
Omar Z
OZ
Salman
Ibrahim M
IM
Noor
Azmin M
AM
D000464:Alginates / Q000737:chemistry; D002482:Cellulose / Q000031:analogs & derivatives / Q000737:chemistry; D003106:Colon / Q000378:metabolism; D016503:Drug Delivery Systems / Q000379:methods*; D005079:Excipients / Q000737:chemistry*; D020723:Glucuronic Acid / Q000737:chemistry; D006603:Hexuronic Acids / Q000737:chemistry; D006801:Humans; D006863:Hydrogen-Ion Concentration; D010276:Parasympatholytics / Q000008:administration & dosage*; D010368:Pectins / Q000737:chemistry; D010627:Phenethylamines / Q000008:administration & dosage* / Q000493:pharmacokinetics; D011109:Polymethacrylic Acids / Q000737:chemistry; D012995:Solubility; D013608:Tablets, Enteric-Coated / Q000737:chemistry* / Q000493:pharmacokinetics
D000464:Alginates; D005079:Excipients; D006603:Hexuronic Acids; D010276:Parasympatholytics; D010627:Phenethylamines; D011109:Polymethacrylic Acids; D013608:Tablets, Enteric-Coated; C038300:methylmethacrylate-methacrylic acid copolymer; C005096:mebeverine; C013517:ethyl cellulose; D010368:Pectins; D020723:Glucuronic Acid; D002482:Cellulose; C011708:cellulose acetate phthalate