title: Development and optimization of metoprolol succinate gastroretentive drug delivery system.
abstract: Metoprolol succinate (MS) gastroretentive (GR) controlled release system was formulated to increase gastric residence time leading to improved drug bioavailability. Box-Behnken model was followed using novel combinations of sodium alginate (SA), sodium carboxymethylcellulose (NaCMC), magnesium alumino metasilicate (MAS) as independent variables. Floating lag time (Flag), t25, t50, t75, diffusion exponent as dependent variables revealed that the amount of SA, NaCMC and MAS have a significant effect (p < 0.05) on t25, t50, t75 and Flag. MSGR tablets were prepared and evaluated for mass, thickness, hardness, friability, drug content and floating property. Tablets were studied for dissolution for 24 h and exhibited controlled release of MS with floating for 16 h. The release profile of the optimized batch MS01 fitted first-order kinetics (R2 = 0.9868, n = 0.543), indicating non-Fickian diffusion or anomalous transport by diffusion and swelling.
authors.affiliation: Piramal Health Care Limited, Mumbai, India. sanjayboldhane@hotmail.com
authors.forename: Sanjay P
authors.initials: SP
authors.lastname: Boldhane
authors.forename: Bhanudas S
authors.initials: BS
authors.lastname: Kuchekar
mesh_terms: D000284:Administration, Oral; D000464:Alginates; D017607:Aluminum Compounds; D000538:Aluminum Silicates; D001682:Biological Availability; D002266:Carboxymethylcellulose Sodium; D003198:Computer Simulation; D004058:Diffusion; D004337:Drug Carriers; D004339:Drug Compounding; D016503:Drug Delivery Systems; D005746:Gastric Emptying; D020723:Glucuronic Acid; D006603:Hexuronic Acids; D006801:Humans; D008274:Magnesium; D017616:Magnesium Compounds; D008790:Metoprolol / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000378:metabolism / Q000493:pharmacokinetics; D017640:Silicates; D012995:Solubility; D013607:Tablets
chemical_list: D000464:Alginates; D017607:Aluminum Compounds; D000538:Aluminum Silicates; D004337:Drug Carriers; D006603:Hexuronic Acids; D017616:Magnesium Compounds; D017640:Silicates; D013607:Tablets; C033065:aluminum magnesium silicate; D020723:Glucuronic Acid; D008790:Metoprolol; D008274:Magnesium; D002266:Carboxymethylcellulose Sodium