Method for preparing ezetimibe tablets

Abstract

The invention relates to the field of drug synthesis and in particular relates to a method for preparing ezetimibe tablets. The method comprises the following steps: S1, dissolving fluorobenzoylbut anoic acid and ezetimibe into ethanol, and dissolving the ethanol in an aqueous solution; S2, mixing gases of carbon dioxide and oxygen under the conditions of pressure of 30-40Mpa and temperature of 65-70 DEG C, and introducing the mixture into the aqueous solution so as to obtain ultrafine particle mixed powder containing ezetimibe, fluorobenzoylbut anoic acid and ethanol; S3, enabling the ultrafine particle mixed powder containing ezetimibe, fluorobenzoylbut anoic acid and ethanol to be coated with pectin; and S4, mixing the ultrafine particle mixed powder coated with pectin on auxiliary materials, coating a layer of pectin, and tabletting. According to the method for preparing ezetimibe tablets disclosed by the invention, the produced ezetimibe tablets can be dissolved in a human body ina staged manner, the safety of the ezetimibe tablets in the medication process is improved, and the absorption rate of the ezetimibe tablets absorbed in the human body is increased.

Description

technical field [0001] The invention relates to the field of drug synthesis, in particular to a preparation method of ezetimibe tablets. Background technique [0002] Ezetimibe, the English name is Ezetimibe, the chemical name is 1-(4-fluorophenyl)-(3R)-[3-(4-fluorophenyl)-(3S)-hydroxypropyl]-(4S) -(4-Hydroxyphenyl)-2-propionolactam, ezetimibe has many synthetic routes, but the routes seen before have either long synthetic steps and low yields, or expensive starting materials and high cost, or many by-products , Exhaust gas waste water and waste materials will put pressure on the environment. In addition, the current production of ezetimibe tablets, when patients take them, is often due to the rapid release of ezetimibe, and the gastric juice and intestinal tract have no time to absorb and process, which is easy to damage the stomach. and intestinal adverse effects. [0003] Therefore, it is necessary to propose a method for preparing ezetimibe tablets that solves the abov...

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Problems solved by technology

[0002] Ezetimibe, the English name is Ezetimibe, the chemical name is 1-(4-fluorophenyl)-(3R)-[3-(4-fluorophenyl)-(3S)-hydroxypropyl]-(4S) -(4-Hydroxyphenyl)-2-propionolactam, ezetimibe has many synthetic routes, but the routes seen before have either long synthetic steps and low yields, or expensive starting materials and high cost, or many by-products , Exhaust gas waste water and waste materials will put pressure on the environment. In addition, the current production of ezetimibe tablets, when patients take them, is often due to the rapid release of ezetimibe, and the gastric juice and intestinal tract have no time to absorb and process, which is easy to damage the stomach. adverse effects on the gut

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