PELLET FORMULATIONS OF ACID-LABILE ANTIULCER BENZIMIDAZOLE COMPOUNDS

摘要

They comprise inert granules of sugar/starch which are: initially coated with a non-alkaline active layer having the benzimidazole compound (omeprazole, lansoprazole, pantoprazole, rabeprazole, etc.), sodium and/potassium salts of acids of formula R-O-SO3H wherein R is an alkyl radical of a (C6-C20)-fatty acid (preferably sodium lauryl sulfate), (C6-C20)-fatty acids (preferably oleic acid), sodium and/or potassium salts Of (C6-C20)-fatty acids (preferably potassium oleate), sodium carboxymethyl starch and polyvinylpyrrolidone; secondly coated with a non-alkaline barrier layer having hydroxypropylmethylcellulose; and finally coated with an enteric layer. The preferred molar ratio (sodium lauryl sulfate):(oleic acid + potassium oleate) is between 4:1 and 6:1. All coatings are done with aqueous solutions, suspensions or dispersions at a relatively high temperature, and all dryings are done at a relatively low temperature and for a relatively short time. They are stable over time and useful for oral administration.