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A kind of metformin salt and its preparation method and application

A metformin salt and a metformin technology are applied in the field of metformin salt and its preparation, can solve the problems of unfavorable salt type sales, complex structure, high price and the like, and achieve the effects of simple and environmentally friendly preparation method, good solubility and easy preservation

Active Publication Date: 2022-08-02
GUANGZHOU UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, it also has certain hygroscopicity and is not stable enough.
Recently, a pamoate was also reported, but the structure of this acid is complex and the price is high, which is not conducive to sale as a salt

Method used

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  • A kind of metformin salt and its preparation method and application
  • A kind of metformin salt and its preparation method and application
  • A kind of metformin salt and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] Example 1: Preparation of metformin and 1-naphthalene acetate

[0069] Take 0.0430g of commercially available metformin free base, pharmaceutical excipients and 0.0621g of 1-naphthalene acetic acid, drop 1-2 drops of absolute ethanol and mix them evenly, put them in a 100mL ball mill, and add 2 zirconia balls with a diameter of 22mm. , cover the sealing cover, put it into the ball mill, set the instrument parameters to the speed of 35s -1 , run for 5 minutes, pass through a 154 μm stainless steel mesh, and obtain 0.58 g of the product metformin naphthalene acetate powder, with a yield of 98%.

[0070] The product metformin obtained in Example 1 and the yellow powder of 1-naphthalene acetate, the raw material 1-naphthaleneacetic acid, and the free base of metformin are respectively subjected to powder X-ray diffraction analysis, and the results are as follows: figure 1 shown. from figure 1 It can be seen that the characteristic diffraction peaks of the obtained yellow...

Embodiment 2

[0074] Example 2: Preparation of metformin and 2-naphthoate

[0075] Take 0.0430g of metformin free base, pharmaceutical excipients and 0.0574g of 2-naphthoic acid, drop 1-2 drops of absolute ethanol and mix them evenly. After putting the sealing cover on, put it into a ball mill, set the instrument parameters to rotate speed 35s-1, run for 5min, pass through a 154 μm stainless steel screen, and obtain the powder of metformin and 2-naphthoate.

[0076] The powders obtained from metformin and 2-naphthoic acid salt, 2-naphthoic acid and metformin free base were analyzed by powder X-ray diffraction respectively, and the results were as follows Image 6 As shown in the figure, it can be seen that the characteristic diffraction peaks of metformin and 2-naphthoate, metformin free base and 1-naphthoacetic acid are different, which means that the prepared metformin and 2-naphthoate are a new kind of the solid form.

[0077] The prepared metformin and 2-naphthoate were fully dissolve...

Embodiment 3

[0080] Example 3: Preparation of metformin and 1-hydroxy-2-naphthoate

[0081] Take 0.0430g of metformin free base, pharmaceutical excipients and 0.0627g of 1-hydroxy-2-naphthoic acid, drop 1-2 drops of absolute ethanol and mix them uniformly, put them in a 100mL ball mill, add 2 22mm diameter dioxide Zirconium ball grinding beads, cover the sealing cover, put it into the ball mill, set the instrument parameters to the speed of 35s -1 , run for 5 min, pass through a 154 μm stainless steel mesh to obtain the powder of the product metformin salt.

[0082] The powders prepared by metformin and 1-hydroxy-2-naphthoate, 1-hydroxy-2-naphthoic acid and metformin free base were analyzed by powder X-ray diffraction respectively, and the results were as follows Figure 11 As can be seen from the figure, the characteristic diffraction peaks of metformin and 1-hydroxy-2-naphthoic acid salt and metformin free base and 1-hydroxy-2-naphthoic acid are all different, indicating that the prepar...

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Abstract

The invention belongs to the field of pharmaceutical preparations and discloses a class of metformin salts and a preparation method and application thereof. The preparation method of this type of metformin salt includes the following steps: weighing the raw material drug of metformin and pharmaceutical excipient acid, uniformly mixing, and then ball-milling and passing through a 154 μm stainless steel mesh to obtain the metformin salt. Described pharmaceutical excipient acids are 1-naphthaleneacetic acid, 1-hydroxy-2-naphthoic acid, 2-hydroxy-3-naphthoic acid, 2-naphthoic acid, 1,5-dihydroxynaphthalene, 3,7-dihydroxy A kind of in 2-naphthoic acid and 2,3-dihydroxynaphthalene. Compared with the original metformin base, these new metformin salts of the present invention have weak hygroscopicity, good solubility in water, can slow down the inherent dissolution rate of metformin, are more stable, and make it easier to store, and are expected to improve the bioavailability of metformin base. . Such metformin salts will have the prospect of being applied to metformin drugs.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and particularly relates to a class of metformin salts and a preparation method and application thereof. Background technique [0002] In the research process of pharmaceutical preparations, it is necessary to go through the step of salt sieving. The solubility of drugs can be increased by 100-1000 times through salt formation. Salt formation is a method for researchers to overcome the problems of drug hygroscopicity, solubility and bioavailability through pharmaceutical methods. preferred method. [0003] Commercially available metformin is mainly sold in the form of its hydrochloride salt. Metformin free base, the raw material for metformin salt formation, has strong hygroscopicity. The commercially available metformin hydrochloride is easier to combine with crystal water, and because the inherent dissolution rate of metformin hydrochloride is too fast, it will have certain side eff...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C277/00C07C279/04C07C51/43C07C63/36A61P3/10A61P35/00A61P39/06A61P25/28A61P15/00A61P3/04
CPCC07C277/00C07C51/43A61P3/10A61P35/00A61P39/06A61P25/28A61P15/00A61P3/04C07B2200/13C07C279/04C07C63/36
Inventor 王子舟钟依灵李雅欣吴玉萍
Owner GUANGZHOU UNIVERSITY
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