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A kind of metformin crystal and its pharmaceutical composition with saxagliptin and preparation method

A technology of metformin and its composition, which is applied in the field of medicine, can solve the problems of being unsuitable for industrial production, affecting the stability of drugs, and increasing the cost of preparation, so as to achieve the effects of saving preparation cost and process, reducing the amount and type of auxiliary materials, and improving curative effect

Active Publication Date: 2011-12-07
HAINAN JINRUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

On the one hand, the above-mentioned sustained-release preparations have high requirements on the process, which increases the preparation cost, and are not suitable for industrial production; affecting the stability of the drug

Method used

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  • A kind of metformin crystal and its pharmaceutical composition with saxagliptin and preparation method
  • A kind of metformin crystal and its pharmaceutical composition with saxagliptin and preparation method
  • A kind of metformin crystal and its pharmaceutical composition with saxagliptin and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] [Example 1] Preparation of metformin crystals

[0052] 1) dissolving metformin powder in a water / ethanol mixed solution to form a metformin solution;

[0053] 2) Under stirring, add chloroform dropwise to the metformin solution prepared in step 1) until it becomes turbid;

[0054] 3) heating the turbid solution obtained in step 2) under an ultrasonic field until the solution becomes clear, and filtering;

[0055] 4) Leave the filtrate obtained in step 3) until the product precipitates, filter, wash the filter cake with anhydrous chloroform, and dry in vacuum to obtain metformin crystals.

[0056] The particle diameter of the metformin crystals obtained is 80 μm, and the X-ray powder diffraction pattern (see figure 1 ) in the characteristic peaks are displayed at 2θ of 11.2, 12.8, 14.9, 15.2, 15.3, 18.8, 22.8, 23.5, 26.6.

Embodiment 2

[0057] [Example 2] Preparation of metformin crystals

[0058] 1) Dissolve metformin powder in a water / ethanol mixed solution with a volume ratio of 1:8 to make a concentration of 10mol L -1 metformin solution;

[0059] 2) Under stirring, at 25°C, add chloroform dropwise to the metformin solution prepared in step 1) at a rate of 1ml / min until it becomes turbid;

[0060] 3) Heat the turbid solution obtained in step 2) to 40° C. under an ultrasonic field until the solution becomes clear, and filter;

[0061] 4) Stand the filtrate obtained in step 3) at 20° C. for 2 days until the product precipitates, filter, wash the filter cake with anhydrous chloroform, and dry in vacuum to obtain metformin crystals.

[0062] The obtained metformin crystals have a particle size of 60 μm, and the X-ray powder diffraction pattern measured by Cu-Kα rays is consistent with that of Example 1.

Embodiment 3

[0063] [Example 3] Preparation of metformin crystals

[0064] 1) Dissolve metformin powder in a water / ethanol mixed solution with a volume ratio of 1:3 to make a concentration of 25mol L -1 metformin solution;

[0065] 2) Under stirring, at 15°C, add chloroform dropwise to the metformin solution prepared in step 1) at a rate of 3ml / min until it becomes turbid;

[0066] 3) Heating the turbid solution obtained in step 2) to 50° C. under an ultrasonic field until the solution becomes clear, and filtering;

[0067] 4) Stand the filtrate obtained in step 3) at 25° C. for 2 days until the product precipitates, filter, wash the filter cake with anhydrous chloroform, and dry in vacuum to obtain metformin crystals.

[0068] The obtained metformin crystals have a particle size of 100 μm, and the X-ray powder diffraction pattern measured by Cu-Kα rays is consistent with that of Example 1.

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Abstract

The invention discloses a melbine crystal and a medicinal composition of melbine and saxagliptin and a preparation method thereof. The medicinal composition consists of active ingredients of medicines and a pharmaceutic adjuvant, wherein the active ingredients of the medicines comprise the following components in part by weight: 5 to 30 parts of saxagliptin and 200 to 800 parts of melbine, and the melbine is the melbine crystal; and the pharmaceutic adjuvant comprises a filling agent, a disintegrating agent, an adhesive and a lubricating agent. The melbine crystal used in the medicinal composition has the characteristic of low solubility, so the sustained-release effect of the melbine is realized by using ordinary matrix materials in the medicinal composition prepared from the melbine andthe saxagliptin, the administration safety is improved; and the synergistic effect of the melbine and the saxagliptin is good, so the curative effect is improved. In addition, due to the adoption of few matrix materials, the stability of the medicines is improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a metformin crystal, a pharmaceutical composition thereof and saxagliptin and a preparation method thereof. Background technique [0002] Saxagliptin, its molecular formula is: C 18 h 25 N 3 o 2 , the structural formula is as follows: [0003] [0004] Saxagliptin is an incretin hypoglycemic drug. Unlike other drugs that simply promote insulin secretion, incretin hypoglycemic drugs are glucose-dependent because of their effects, that is, only when blood sugar rises Only then "command" the production of insulin, so it has a protective effect on the function of pancreatic beta cells. A number of international studies have shown that incretins can not only promote the secretion of insulin by pancreatic β cells, lower blood sugar, but also reduce the apoptosis of β cells, thereby delaying the disease process and hopefully fundamentally curbing the process of type...

Claims

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Application Information

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IPC IPC(8): A61K31/403A61K31/155A61K9/28A61P3/10
Inventor 马鹰军王小树钟正明罗韬
Owner HAINAN JINRUI PHARMA
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