Sulfonylurea compound and metformin salts, preparation method and application

A technology for metformin and a compound, applied in the field of chemical synthesis and crystallization, can solve the problems of poor pharmaceutical properties, low solubility, large oral dose and the like, and achieve the effects of easy control of the crystallization process, improved hygroscopic stability, and simple preparation method.
CN110804017AInactive Publication Date: 2020-02-18TIANJIN UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
TIANJIN UNIV
Publication Date
2020-02-18
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to sulfonylurea compound and metformin salts, a preparation method and application. The preparation method comprises the following steps: dissolving a sulfonylurea compound and metformin into a solvent according to a mole ratio of (1:0.9):(1:1.1) so as to obtain a mixture; performing reaction crystallization on the mixture under a condition of 25-50 DEG C for 12-48 hours; andperforming solid-liquid phase separation on the obtained product, and performing drying, so as to obtain a salt type solid product. The sulfonylurea compound is gliquidone or glibenclamide. The gliquidone-metformin salt and the glibenclamide-metformin salt provided by the invention are applied to medicines for preventing and treating diabetes. The wet absorption capacities of the salt type products provided by the invention are greatly increased when being compared with that of metformin, that is, the hygroscopy gain of the metformin is 35% when the relative humidity is 75%, and the hygroscopy gains of the salt type products are smaller than 1%; and the dissolubility of the salt type products is greatly improved when being compared with that of the sulfonylurea compound, that is, the dissolubility of the sulfonylurea compound in water is smaller than 0.03mg / ml, and the dissolubility after salt formation is 10.61mg / ml and 16.78mg / ml respectively.
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Description

technical field

[0001] The invention belongs to the technical field of chemical synthesis and crystallization, and specifically relates to the salt formation, preparation method and application of a sulfonylurea compound and metformin; the sulfonylurea compound includes glibenclamide and glibenclamide, and the formed salt is glibenclamide - metformin salts and glibenclamide-metformin salts. Background technique

[0002] According to statistics, about 70-80% of drug candidates fail to be marketed due to defects in physical and chemical properties. Therefore, improving the physical and chemical properties of drugs is of great significance for the development of new drugs. In the preclinical research and development stage of drugs, new drug R&D companies usually use the active ingredients of drugs to form salts to improve the drug's solubility, dissolution rate, hygroscopicity, stability and bioavailability and other pharmaceutical properties. In the first half of 2017, the U....

Claims

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