Fenofibric acid salt of berberine and analogue thereof, crystal form, preparation method and applications thereof

Abstract

The invention discloses fenofibric acid salts of berberine and analogues thereof, a crystal form, a preparation method and applications thereof, wherein the fenofibric acid salt comprises fenofibric acid serving as an anion and berberine or a berberine analogue serving as a cation. According to the invention, the fenofibric acid salt of berberine or analogue thereof can be used for removing unnecessary cations from commercially available medicines, ie., choline cations in choline fenofibrate and / or chlorine ions in berberine hydrochloride, so that a certain side effect, including gastrointestinal irritation due to instability property of choline as an anion and high acidity of berberine hydrochloride, caused by the two pairing ions can be reduced.

Description

Technical field

[0001] The present disclosure relates to fenofibrate salts of berberine and its analogs, especially crystalline salts, which can be used in medicines or health food ingredients for the treatment or prevention of cardiovascular diseases or other diseases. The present disclosure also relates to a method for preparing a crystalline salt using berberine or its analogue as a cation, particularly a method for preparing a crystalline salt of fenofibrate salt of berberine or its analogue. Background technique

[0002] Fenofibrate, 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propionic acid-1-methylethyl ester, is a lipid regulator. It can lower the total cholesterol and triglyceride levels in the body. Fenofibrate is usually administered orally. After oral administration, fenofibrate is metabolized into fenofibrate acid in the body. In fact, fenofibrate acid is a biologically active molecule of fenofibrate. Therefore, the more soluble fenofibric acid is a new chemical enti...

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