Preparation of Hydrochloride Salts of Tetrazole Derivative
AssigneeKrka, Tovarna Zdravil, D.D., Novo Mesto
InventorsSilvo Zupancic, Matej Smrkolj, Renata Jaske
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Abstract
The present invention relates to sesquihydrate hydrochloride salt of irbesartan and anhydrous hydrochloride salts of irbesartan. Irbesartan used as the starting material for the preparation of the described hydrochlorides of irbesartan can be in any form, e.g. it can be used when contained in a reaction solution, in crude form, in a filtrate containing several solvents, or in anhydrous or any solvated or hydrated form, in amorphous form or any known crystal form or in a mixture thereof.
Claims29
A Sesquihydrate hydrochloride salt of irbesartan, having 2 molecules of hydrochloride and 3 molecules of water to 2 molecules of irbesartan.
A Hydrochloride salt of irbesartan containing from 0% to 7% of water.
A process for the preparation of sesquihydrate hydrochloride salt of irbesartan comprising the steps of acidifying a suspension or solution of irbesartan in water with HCl to a pH-value lower than 1.2 and stirring until sesquihydrate hydrochloride of irbesartan is precipitated.
A process for the preparation of anhydrous crystal form of hydrochloride salt of irbesartan, comprising the step of heating the sesquihydrate hydrochloride salt of irbesartan, first to a temperature of about 120° C. and then to a temperature from about 120° C. to about 160° C., wherein the entire heating period lasts more than 1 hour.
A process for the preparation of anhydrous amorphous form of hydrochloride salt of irbesartan, comprising the step of heating a sesquihydrate hydrochloride salt of irbesartan to about 160° C., wherein the entire heating lasts less than 1 hour.
A pharmaceutical composition comprising one or more hydrochloride salts of irbesartan and pharmaceutically acceptable carriers, diluents, excipients, additives, fillers, lubricants, binders, stabilisers, solvents or solvates.
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A method of treating hypertension or cardiac weakening by administering to a person in need thereof an effective amount of a hydrochloride salt of irbesartan.
Dependencies are inferred from the claim text.