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Epalrestat-metformin salt as well as preparation method and application thereof

A metformin and epalrestat technology, applied in the field of medicine and chemical industry, can solve the problems of poor physical and chemical properties, metformin instability, low solubility, etc., and achieve the effects of easy control of the crystallization process, reduced hygroscopicity, and reduced hygroscopicity

Active Publication Date: 2021-09-03
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Epalrestat is a Class II drug (BCS II) in the Biopharmaceutical Classification System, which has low solubility, which greatly limits its efficacy
Metformin is unstable and easily absorbs moisture
Traditional drug combinations cannot improve their poor physicochemical properties

Method used

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  • Epalrestat-metformin salt as well as preparation method and application thereof
  • Epalrestat-metformin salt as well as preparation method and application thereof
  • Epalrestat-metformin salt as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Take 32.0mg of epalrestat and 12.9mg of metformin (molar ratio is 1:1) into a 4mL sample bottle, add 2mL of ethanol, sonicate, dissolve and become supersaturated, react and crystallize at 15°C for 24 hours, The suspension is centrifuged, the supernatant is discarded, and the centrifuged solid is dried in a blast drying oven at 105° C. for 3 hours to obtain the epalrestat-metformin salt.

[0047] figure 1 Prepare the XRD figure of product for embodiment 1, from figure 1 It can be seen that the diffraction angle is 2θ, which means that there are features at 10.87, 11.34, 12.70, 12.90, 15.00, 16.29, 16.37, 16.67, 17.48, 19.27, 19.64, 20.28, 20.99, 21.81, 22.92, 24.00, 24.50, 25.05, 266.88, 2 peak.

[0048] figure 2 Prepare the DSC figure that obtains product for embodiment 1, from figure 2 It can be seen that the differential scanning calorimetry spectrum of the epalrestat-metformin salt prepared in this example has a sharp endothermic peak at 215.7° C., which is the...

Embodiment 2

[0056] Take 32.0mg of epalrestat and 11.9mg of metformin (molar ratio is 1:0.92) into a 4mL sample bottle, add 2mL of isopropyl acetate, sonicate to make it dissolve and become supersaturated, react and crystallize at 60°C After 12 hours, the suspension was centrifuged, the supernatant was discarded, and the centrifuged solid was dried in a blast oven at 60° C. for 1 hour to obtain epalrestat-metformin salt.

[0057] Carry out XRD test to the product that embodiment 2 obtains, be 0.87,11.34,12.70,12.90,15.00,16.29,16.37,16.67,17.51,19.27,19.64,20.28,20.99,21.81,22.92,24.00,24.50, There are characteristic peaks at 25.10, 26.10, and 26.88. , so the product is the epalrestat-metformin salt.

[0058] The product obtained in Example 2 was tested by DSC. As can be seen from the test results, there is a sharp endothermic peak at 216.4° C., which is the melting point of epalrestat-metformin salt.

[0059] Embodiment 2 adopts the same method as Example 1 to carry out hygroscopicity t...

Embodiment 3

[0061] Take 32.0mg of epalrestat and 15.4mg of metformin (the molar ratio is 1:1.19) into a 4mL sample bottle, add 2mL of acetonitrile and ethyl acetate, and ultrasonically dissolve it and make it supersaturated. After 48 hours of crystallization, the suspension was centrifuged, the supernatant was discarded, and the centrifuged solid was dried at a room temperature of 25° C. for 12 hours to obtain the epalrestat-metformin salt.

[0062] Carry out XRD test to the product that embodiment 3 obtains, test product is 0.87,11.34,12.78,12.90,15.00,16.29,16.37,16.67,17.48,19.27,19.64,20.28,20.99,21.81,22.87,24.00, There are characteristic peaks at 24.50, 25.05, 26.10, and 26.88. , so the product is the epalrestat-metformin salt.

[0063] The product obtained in Example 3 was tested by DSC. From the test results, there is a sharp endothermic peak at 215.9° C., which is the melting point of epalrestat-metformin salt.

[0064] Embodiment 3 adopts the same method as Example 1 to carry ...

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Abstract

The invention discloses epalrestat-metformin salt as well as a preparation method and application thereof. The molecular formula of the epalrestat-metformin salt is C19H24N6O3S2, and the molecular weight of the epalrestat-metformin salt is 448.6; the epalrestat-metformin salt is in a crystalline state. The preparation method of the epalrestat-metformin salt comprises the following steps: dissolving epalrestat and metformin in a solvent according to a molar ratio of 1: 0.8-1: 1.2 to obtain a mixture; reacting and crystallizing the mixture for 12-48 hours under the condition of 15-60 DEG C; and carrying out solid-liquid phase separation on the obtained product, and drying to obtain the epalrestat-metformin salt. Compared with a metformin single product, the epalrestat-metformin salt form provided by the invention has the advantages that the strong hygroscopicity is greatly improved, the solubility is greatly improved compared with an epalrestat single product, meanwhile, the preparation method is simple to operate, the crystallization process is easy to control, and the reproducibility of the salt form is good.

Description

technical field [0001] The invention belongs to the field of medicine and chemical industry, and in particular relates to an epalrestat-metformin salt and a preparation method and application thereof. Background technique [0002] Complex diseases such as infectious diseases, AIDS, cancer, diabetes, and cardiovascular diseases have become important factors restricting the increase in the average life expectancy of human beings. Since monotherapy (that is, targeting specific receptors) has no significant effect in the treatment of many complex diseases, combination drugs have become It has become a generally recognized drug development strategy, and combination drugs are generally realized through compound preparations or taking multiple drugs at the same time. Compound preparation refers to the combination of two or more pharmaceutically active molecules (APIs) in a single dose, which not only has a more effective therapeutic effect than single administration, but also has t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D277/36C07C279/26C07C277/08A61P3/10
CPCC07D277/36C07C279/26A61P3/10C07B2200/13
Inventor 龚俊波孙晶晶贾丽娜吴送姑韩丹丹刘裕
Owner TIANJIN UNIV
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