2 results about "Olmesartan" patented technology

The application discloses an olmesartan medoxomil and amlodipine besylate pharmaceutical composition and a preparation method thereof, and belongs to the technical field of medicines. The olmesartan medoxomil and amlodipine besylate pharmaceutical composition takes olmesartan medoxomil and amlodipine besylate as active ingredients, and is prepared into antihypertensive tablets by being matched with a disintegrant, a filler and a lubricant; wherein the filler is a mixture of pre-gelatinized starch and a co-processed product of microcrystalline cellulose and colloidal silicon dioxide. The preparation method adopts a direct compression process, and sequentially comprises the steps of mixing, whole-granulating, twice mixing, lubricating, tabletting and stomach-soluble film coating, and is simple in process and suitable for industrialized scale-up production. The application effectively solves the problem of low dissolution rate of the existing olmesartan medoxomil and amlodipine besylate tablets, and the prepared tablets have the advantages of high dissolution rate, similar dissolution curve to commercial preparations, high bioavailability, stable quality and good clinical application value.

This invention provides a method for synthesizing triphenylmethylolmesartan medoxomil, an intermediate of olmesartan medoxomil. The method includes hydrolyzing compound 2 in a toluene / C1-C4 lower alcohol mixed solvent under the action of an alkali to obtain a synthesis solution of an intermediate sodium salt; adding a carbonate and a phase transfer catalyst to the synthesis solution of the intermediate sodium salt to carry out a condensation reaction to obtain triphenylmethylolmesartan medoxomil. This invention effectively controls the content of impurity A in the product by using a toluene / C1-C4 lower alcohol mixed solvent system and inhibiting the high-temperature elimination reaction of hydroxyl groups by a protic alcohol solvent. This invention has a short production cycle, a simple process, and does not require changing or adding new solvents during the process, facilitating solvent recovery and reuse in industrial production and effectively reducing production costs. The synthesis method of triphenylmethylolmesartan medoxomil described in this invention has a high overall yield, high production efficiency, simple product purification, and good quality control.