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Metformin-tolbutamide new salt type and preparation method and medical application thereof

A technology of tolbutamide and metformin, which is applied in the field of medicine and chemical industry, can solve the problems of metformin instability, poor pharmaceutical properties, low solubility, etc., and achieve easy control of the crystallization process, improved hygroscopicity and stability, and improved solubility Effect

Inactive Publication Date: 2019-08-16
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, tolbutamide is a class II drug (BCS II) in the biopharmaceutical classification system, which has low solubility, so its pharmaceutical properties are not good
Metformin is unstable and easily absorbs moisture

Method used

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  • Metformin-tolbutamide new salt type and preparation method and medical application thereof
  • Metformin-tolbutamide new salt type and preparation method and medical application thereof
  • Metformin-tolbutamide new salt type and preparation method and medical application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Take 21.6mg of tolbutamide and 10.8mg of metformin in a 4mL sample bottle, add 2mL of ethyl acetate, ultrasonically dissolve and become supersaturated, react and crystallize at room temperature for 24 hours, centrifuge the suspension, discard Remove the supernatant, and dry the centrifuged solid in a blast oven at 40°C for 3 hours to obtain the metformin-tolbutamide salt form. The XRPD results are as follows: figure 1 .

Embodiment 2

[0043] Get about 3 mg of the metformin-tolbutamide salt type solid sample prepared in Example 1 and carry out dynamic moisture adsorption analysis, using VTI-SA + Determination by dynamic moisture adsorption instrument. The temperature is 25°C and the relative humidity range is 1-95%. The result shows that the water content of metformin-tolbutamide salt type changes little with the change of relative humidity, and when from 1% relative humidity to 95% relative humidity, the mass percentage of its water content does not have obvious increase, as specification attached image 3 , and the salt type remains unchanged, the XRPD pattern is as follows Figure 5 . And the known metformin prototype medicine draws wet weight gain obviously under this relative humidity condition, has been up to 86%. Figure 4 .

Embodiment 3

[0045] Take 21.6mg of tolbutamide and 10.8mg of metformin in a 4mL sample bottle, add 2mL of acetone, ultrasonically dissolve and become supersaturated, react and crystallize at room temperature for 24 hours, centrifuge the suspension, discard the upper Clear liquid, dry the centrifuged solid in a blast oven at 40°C for 3 hours to obtain the metformin-tolbutamide salt form, and the XRPD results are as follows: Figure 9 .

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Abstract

The invention discloses a metformin-tolbutamide new salt type and a preparation method and medical application thereof. The preparation method comprises the following steps: dissolving metformin and tolbutamide in an appropriate solvent, reacting, crystallizing, filtering and drying. The preparation method has simple operation, good reproducibility and easy control. The hygroscopicity and stability of the metformin-tolbutamide new salt type are greatly improved compared with that of a metformin single product, the solubility of the metformin-tolbutamide new salt type is greatly improved compared with that of a tolbutamide single product, the preparation method is simple, the crystallization process is easy to control, and the metformin-tolbutamide new salt type has good repeatability.

Description

technical field [0001] The invention belongs to the field of medicine and chemical industry, and specifically relates to a salt form of metformin-tolbutamide crystal form, a preparation method thereof, a pharmaceutical composition and application thereof. 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.S. Food and Drug Administration (FDA) approved a total of 23 new drugs, including 16 new molecular entities and 7 new biological products. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C311/58C07C303/40C07C277/08C07C279/26A61K31/18A61K31/155A61P3/10
CPCA61K31/155A61K31/18A61P3/10C07C277/08C07C279/26C07C303/40C07C311/58A61K2300/00
Inventor 龚俊波贾丽娜王梦薇尚泽仁吴送姑侯宝红尹秋响王静康
Owner TIANJIN UNIV
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