PROCESS FOR THE PREPARATION OF A COMPOSITION BASED ON PRIME-RELEASED LIBERALIZATION TRIMEBUTIN

摘要

PURPOSE: To obtain a sustained release composition which comprises trimebutine as a base, has an action to control the digestive function, particularly is useful for treatment of gastroesophageal regurgitation. CONSTITUTION: 2-Dimethylamino-2-phenyl-1-butyl 3,4,5-trimethoxybenzoate (trimebutine) or its salt is used as an active substance and dispersed in a hydrophilic porous matrix of hydroxypropyl methyl cellulose. In addition, a water-soluble diluent (for example, lactose) and tartaric acid are formulated and made into tablets thereby giving the objective sustained release tablets. This composition comprises 35-45wt.% of trimebutine of the formula, 15-20wt.% of hydroxypropyl methyl cellulose, 20-25wt.% of a water-soluble diluent and 10-20wt.% of tartaric acid. Each of the tablets suitably contains the active substance in an amount of 175-325mg.