IMPROVED CHEMICAL PROCESS AND PHARMACEUTICAL FORMULATION

摘要

Process for the manufacturing of slightly soluble or less soluble alkaline salts of substituted sulphinyl heterocycles containing an imidazole moiety with formula (I), preferably alkaline salts of a proton pump inhibitor compound, wherein the process comprises the step of reacting the substituted sulphinyl heterocycle of formula (I) with a source of the cation in the presence of a base, characterized by a washing step in which the prepared alkaline salt of the substituted sulphinyl compound is washed with a basic aqueous solvent mixture. The obtained bulk drug substance resulting in a bulk product that in an aqueous suspension of the substituted sulphinyl heterocycle having a pH not significantly lower than that of a saturated water solution of the pure compound prepared. Alternatively, the process for manufacturing a pharmaceutical dosage form comprising the active substance could be adjusted. For instance the pH of an aqueous suspension of the active substance is adjusted to a pH not significantly lower than that of a saturated water solution of the pure compound. The processes are preferably useful in the manufacturing of omeprazole magnesium salt or magnesium salt of one of its single enantiomers used in pharmaceutical dosage forms.