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

• Main Authors: ZHAO ZONGMIN, XIE YONGJU, TANG YUTAO, WU DEDONG, ZHUO CHEN
• Format: Patent
• Language: Chinese; English
• Published: 12.05.2020
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

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. 本发明公开了一种黄连素及其类似物的非诺贝特酸盐、晶型，制备方法及应用，其包括作为阴离子的非诺贝特酸和作为阳离子的黄连素或黄连素类似物。本发明公开的黄连素或其类似物的非诺贝特酸盐从市售药物中除去不需要的阳离子，如除去非诺贝特酸胆碱盐中的胆碱阳离子和/或用于黄连素盐酸盐中的氯离子，从而减少由这两种配对离子引起的一些副作用，包括避免胆碱作为阴离子不稳定性质和因黄连素盐酸盐的高酸度引起的胃肠道刺激作用。