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Metformin glibenclamide slow-releasing preparation

A metformin glide, sustained-release preparation technology, applied in the direction of metabolic diseases, inorganic non-active ingredients, polymer compound non-active ingredients, etc., can solve the problems of unclear hypoglycemic mechanism, enhance the sensitivity of surrounding tissues to insulin, etc., to achieve The effect of reducing the frequency of dosing, improving effectiveness or adaptability

Inactive Publication Date: 2007-10-24
刘凤鸣
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Glibenclamide exerts an acute hypoglycemic effect by stimulating the release of insulin from pancreatic islet functional cells, enhancing the sensitivity of peripheral tissues to insulin, and enhancing the uptake of glucose by peripheral tissues. The hypoglycemic mechanism of long-term administration has not yet been clarified

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1- 2

[0053] The preparation of embodiment 1-metformin glibenclamide sustained-release tablet (1)

[0054] Method: Take 250 grams of metformin, 2.5 grams of glibenclamide, 50 grams of hydroxypropyl cellulose, 15 grams of hypromellose, 10 grams of lactose, 10 grams of microcrystalline cellulose, 1 gram of carbomer, and polyethylene glycol. Glycol 4000 30 grams, mix evenly, dry granulate, add magnesium stearate to mix, compress tablet to obtain finished product, the drug content is 250 / 2.5mg / tablet. Then the dissolution rate of the metformin-glibenclamide sustained-release tablet (1) in 900 ml of water at 37° C. was measured. After release measurement, the results are shown in Table 1, which meets the requirements.

[0055] Sampling time (hours)

Embodiment 2- 2

[0056] The preparation of embodiment 2-metformin glibenclamide sustained-release tablet (2)

[0057] Method: Take 250 grams of metformin, 2.5 grams of glibenclamide, 10 grams of hydroxypropyl cellulose, 20 grams of stearyl alcohol, 15 grams of hypromellose, 1 gram of carbomer, and 10 grams of lactose, respectively, for 80 Mesh sieve, grind and mix evenly, add 95% ethanol solution of 10% polyvinylpyrrolidone as a binder and stir to make a soft material, pass through a 16-mesh sieve for granulation, dry the granules at room temperature for 2 hours, and granulate with a 16-mesh sieve , then add 4.5 grams of magnesium stearate and 2 grams of micropowder silica gel, mix well, and tablet to obtain the finished product, the drug content is 250 / 2.5mg / tablet. Then the dissolution rate of the metformin-glibenclamide sustained-release tablet (2) in 900 ml of water at 37° C. was measured. After release measurement, the results are shown in Table 2, which meets the requirements.

[0058]...

Embodiment 3- 2

[0059] The preparation of embodiment 3-metformin glibenclamide sustained-release tablet (3)

[0060] Method: Take 250 grams of metformin, 2.5 grams of glibenclamide, 35 grams of hypromellose, 5 grams of microcrystalline cellulose, and 1 g of carbomer, pass through 80-mesh sieves, mix well, and add polyethylene with a concentration of 10%. The 95% ethanol solution of pyrrolidone is used as binder and stirred to make soft material, crosses 16 mesh sieves and granulates, granules are dried at 60 DEG C for 1 hour, 16 mesh sieves are granulated, then add 2.5 grams of magnesium stearate, mix, press The tablets are finished products, and the drug content is 250 / 2.5mg / tablet. Then the dissolution rate of the metformin-glibenclamide sustained-release tablet (3) in 900 ml of water at 37° C. was measured. After release measurement, the results are shown in Table 3, meeting the requirements.

[0061] Sampling time (hours)

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PUM

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Abstract

The invention discloses a slow release agent for dimethylbiguanide glibenclamide and the preparing method. The invention takes dimethylbiguanide glibenclamide as raw material, adds main slow-release material according to a certain proportion, produces solid dispersion agent with raw material, the medicine is release slowly according to requirement to keep effective blood concentration, and acts for a long time. The product is characterized by reduced medicine taking time, increased adjustment, reduced blood concentration peak-to-valley phenomenon, improved medicine effect and safety and etc.

Description

[0001] [Technical field] The present invention relates to a sustained-release preparation of metformin-glibenclamide and a preparation method thereof. [Background technique] [0002] The research and development of sustained-release preparations has a history of more than 40 years. It releases slowly and at a non-constant rate as required in a prescribed environment. Prolonged formulation. This kind of preparation can make the human body maintain this kind of blood drug concentration for a long time, instead of dropping rapidly like ordinary preparations, so as to avoid the "peak and valley" phenomenon that occurs when common preparations are frequently administered, and ensure the safety of the drug. Sexuality, effectiveness or adaptability have been improved, thereby reducing the number of medications, which greatly facilitates patients, especially patients who have been taking medication for a long time. Commonly used oral dosage forms include matrix tablets, microporous c...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K9/48A61K47/02A61K47/12A61K47/34A61K47/38A61K47/42A61K47/44A61K31/17A61P3/10A61K47/10
Inventor 刘凤鸣
Owner 刘凤鸣
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