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Metformin acidic double salt compound and preparation method

A technology of metformin acid and metformin, which is applied in the field of metformin acid double salt compound and its preparation, and can solve problems such as the inability to prevent cancer recurrence and metastasis

Active Publication Date: 2010-04-07
HANGZHOU ADAMERCK PHARMLABS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It shows that the combined drug can also quickly reduce the tumor mass and prevent the deterioration for a long time, but the use of doxorubicin alone cannot prevent the recurrence and metastasis of cancer

Method used

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  • Metformin acidic double salt compound and preparation method
  • Metformin acidic double salt compound and preparation method
  • Metformin acidic double salt compound and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043]

[0044] In a 100ml reaction flask, add 129.16mg of metformin, dissolve it with 50ml of absolute ethanol, stir, add 98mg of sulfuric acid, after the reaction is complete, recover and concentrate to obtain 223mg of metformin sulfate, and then mix the metformin acid salt with acetone and add 54mg of sodium methoxide Reacted for 2 hours, concentrated under reduced pressure, added appropriate amount of ether, precipitated solid, filtered, washed with ether, and dried to obtain 240 mg of white solid metformin sodium bisulfate double salt.

Embodiment 2

[0046]

[0047] In a 100ml reaction flask, add 129.16mg of metformin, dissolve it with 50ml of anhydrous methanol, stir, add 98mg of sulfuric acid, after the reaction is complete, recover and concentrate to obtain 220mg of metformin sulfate, and then mix the metformin acid salt with acetone and add 70mg of potassium methoxide Reacted for 2 hours, concentrated under reduced pressure, added appropriate amount of petroleum ether, precipitated solid, filtered, washed with petroleum ether, and dried to obtain 253 mg of white solid metformin potassium hydrogen sulfate double salt.

Embodiment 3

[0049]

[0050] Add 129.16mg of metformin to a 100ml reaction flask, dissolve it with 50ml of anhydrous acetone, stir, add 98mg of sulfuric acid, after the reaction is complete, recover and concentrate to obtain 218mg of metformin sulfate, and then mix the metformin acid salt with acetone and add 164mg of cesium methoxide Reacted for 2 hours, concentrated under reduced pressure, added appropriate amount of n-hexane, precipitated solid, filtered, washed with n-hexane, and dried to obtain 344 mg of white solid metformin cesium hydrogen sulfate double salt.

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Abstract

The invention provides a metformin acidic double salt, which is prepared by the following steps: mixing metformin and H2Y or MHR for reaction; concentrating; adding a weak polar solvent for crystallization; and filtering and drying. The metformin acidic double salt has the characteristics of good stability and improvement on bioavailability, and is converted into metformin in vivo so as to achieve the aim of killing cancer stem cells. The metformin acidic double salt can be used with other anti-tumor chemotherapy medicines to achieve better treatment effect. The structural general formula of the metformin acidic double salt is shown as follows.

Description

Technical field [0001] The invention belongs to the technical field of chemical pharmacy, and relates to a metformin acid double salt compound and a preparation method thereof. The metformin acid double salt of the present invention has the characteristics of good stability and improved bioavailability, and is transformed into metformin in the body, thereby achieving the purpose of killing cancer stem cells. It is used in combination with other chemotherapeutics for cancer treatment. Treatment, recurrence and metastasis. technical background [0002] The structural formula of Guanfacine is as follows: [0003] [0004] The clinical application is Metformin Hydrochloride (Metformin Hydrochloride), whose chemical name is 1,1-dimethyl biguanide hydrochloride. The pharmacological action is that metformin hydrochloride is a hypoglycemic agent, which can improve the blood glucose tolerance of patients with type 2 diabetes and reduce the basic and postprandial blood glucose. The mechan...

Claims

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Application Information

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IPC IPC(8): C07C279/26A61K31/155A61P35/00
Inventor 漆又毛揭清张冯敏顾颖
Owner HANGZHOU ADAMERCK PHARMLABS INC
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