Glipizide compound as well as pharmaceutical composition containing glipizide compound and preparation method of glipizide compound

A technology of glipizide and compounds, applied in the field of glipizide compounds and pharmaceutical compositions containing the compounds and their preparation, can solve the problems of poor compliance, low solubility of glipizide, difficulty in swallowing, etc., and achieve dissolution Consistent speed, excellent dissolution in vitro, and improved water solubility

Active Publication Date: 2014-10-08
HUNAN WARRANT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the low solubility of glipizide, it must be sieved with a specific sieve mesh number of 80-120 mesh, which is not only complicated in process, but also wastes a lot
In addition, in order to make the dissolution rate of glipizide meet the requirement, the invention of this patent adds a large amount of disintegrant or other auxiliary materials, and the tablet weight is as high as 450-880 mg, which makes it very difficult for patients to swallow and has poor compliance.

Method used

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  • Glipizide compound as well as pharmaceutical composition containing glipizide compound and preparation method of glipizide compound
  • Glipizide compound as well as pharmaceutical composition containing glipizide compound and preparation method of glipizide compound
  • Glipizide compound as well as pharmaceutical composition containing glipizide compound and preparation method of glipizide compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] [embodiment 1] preparation of glipizide compound

[0044]Get glipizide crude drug 500g, add the mixed solution of DMF / isopropanol, wherein the volume ratio of DMF and isopropanol is 2:1, the consumption ratio of glipizide crude drug and mixed solution is 1g: 10ml, Heat to 40°C, after the glipizide raw material is dissolved, add activated carbon for decolorization, the amount of added activated carbon is 0.2% g / ml of the total volume of the liquid, stir and adsorb for 25 minutes, filter for decarbonization and sterilization; the filtrate is transferred to the reaction In the kettle, slowly add acetone at a stirring rate of 25r / min, the volume ratio of acetone to the mixed solution is 3:1, after the addition is complete, cool down to 0°C, filter, wash with acetone for 3 times, and dry under reduced pressure for 5h. A white crystalline powder was obtained.

[0045] Gained white crystalline powder uses Cu-Kα ray to measure the X-ray powder diffraction pattern that obtains ...

Embodiment 2

[0046] [embodiment 2] preparation of glipizide compound

[0047] Get glipizide bulk drug 500g, add the mixed solution of DMF / isopropanol, wherein the volume ratio of DMF and isopropanol is 4:1, the consumption ratio of glipizide bulk drug and mixed solution is 1g: 15ml, Heat to 45°C, after the glipizide raw material is dissolved, add activated carbon for decolorization, the amount of added activated carbon is 0.2% g / ml of the total volume of the liquid, stir and adsorb for 25 minutes, filter for decarbonization and sterilization; the filtrate is transferred to the reaction In the kettle, slowly add acetone under the condition of a stirring rate of 30r / min, the volume ratio of acetone to the mixed solution is 6:1, after the addition is completed, cool down to 5°C, filter, wash with acetone for 3 times, and dry under reduced pressure for 5h. A white crystalline powder was obtained.

[0048] Gained white crystalline powder uses Cu-Kα ray to measure the X-ray powder diffraction p...

Embodiment 3

[0049] [embodiment 3] preparation of glipizide compound

[0050] Get glipizide bulk drug 500g, add the mixed solution of DMF / isopropanol, wherein the volume ratio of DMF and isopropanol is 3:1, the consumption ratio of glipizide bulk drug and mixed solution is 1g: 12ml, Heat to 42°C, after the glipizide raw material is dissolved, add activated carbon for decolorization, the amount of added activated carbon is 0.2% g / ml of the total volume of the liquid, stir and adsorb for 25 minutes, filter for decarbonization and sterilization; the filtrate is transferred to the reaction In the kettle, slowly add acetone at a stirring rate of 28r / min, the volume ratio of acetone to the mixed solution is 5:1, after the addition is complete, cool down to 3°C, filter, wash with acetone for 3 times, and dry under reduced pressure for 5h. A white crystalline powder was obtained.

[0051] Gained white crystalline powder uses Cu-Kα ray to measure the X-ray powder diffraction pattern that obtains a...

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PUM

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Abstract

The invention belongs to the technical field of medicines and particularly relates to a glipizide compound as well as a pharmaceutical composition containing the glipizide compound and a preparation method of the glipizide compound. The glipizide compound has a structural formula shown in the specification, and the X-ray powder diffraction pattern, measured by virtue of Cu-Kalpha ray of the glipizide compound is shown in Figure 1. The glipizide compound provided by the invention is a novel crystalline form compound of glipizide, thus the water solubility of the compound can be significantly increased; and the purpose of synchronization release of a pharmaceutical composition comprising the compound and metformin hydrochloride can be achieved, in-vitro dissolution is excellent, the clinical curative effect of the pharmaceutical composition is equivalent to that of the commercially available bulk drug and the pharmaceutical composition has better security.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a glipizide compound, a pharmaceutical composition containing the compound and a preparation method thereof. Background technique [0002] Statistics from the World Health Organization show that WHO estimates that more than 350 million people worldwide suffer from diabetes. The situation in China is even less optimistic. There are currently about 100 million people with diabetes in China, and nearly 500 million people are facing a high risk of developing diabetes in the future. The onset of diabetes is showing a younger trend. [0003] Metformin Glipizide Tablets is a compound preparation of glipizide and metformin hydrochloride. The two drugs improve blood sugar control in patients with type 2 diabetes through complementary mechanisms of action. While reducing blood sugar levels, it also reduces the levels of free fatty acids and triglycerides, thereby inhibiting t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D241/24A61K31/64A61K9/20A61P3/10A61K31/155
CPCC07D241/24
Inventor 徐小强
Owner HUNAN WARRANT PHARMA
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