Sustained-release preparation of compound metformin hydrochloride rosiglitazone and preparation method thereof

A technology for compound metformin hydrochloride and metformin hydrochloride, which can be applied to medical preparations containing active ingredients, pharmaceutical formulations, metabolic diseases, etc., and can solve problems such as large dosage, adverse reactions, hypoglycemia, etc.

Inactive Publication Date: 2010-03-31
北京利乐生制药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, this compound preparation is already on the market, but it is only a common release preparation
Moreover, the compound preparation is frequently taken and taken in large doses, and a series of adverse reactions are prone to occur, such as hypoglycemia, severe gastrointestinal reactions, etc.

Method used

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  • Sustained-release preparation of compound metformin hydrochloride rosiglitazone and preparation method thereof
  • Sustained-release preparation of compound metformin hydrochloride rosiglitazone and preparation method thereof
  • Sustained-release preparation of compound metformin hydrochloride rosiglitazone and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Embodiment 1: metformin hydrochloride rosiglitazone double-layer sustained-release tablet

[0016] prescription:

[0017]

[0018] Preparation:

[0019] Metformin hydrochloride is passed through a 100-mesh sieve, HPMC-15M, HPMC-4M, and microcrystalline cellulose are passed through a 60-mesh sieve, and after the raw and auxiliary materials are mixed evenly, a soft material is made with 80% ethanol solution, granulated with a 20-mesh sieve, dried at 40°C, and dried for 18 Mesh sieve for granulation, and set aside; in addition, rosiglitazone, lactose, calcium hydrogen phosphate, and acrylic resin RS100 were sieved and mixed three times, and the granules were sized in the same way. The above two granules are weighed in proportion respectively, and after adding magnesium stearate, they are compressed into double-layer sustained-release tablets.

Embodiment 2

[0020] Example 2 Compound metformin hydrochloride rosiglitazone film-coated sustained-release tablet

[0021] prescription:

[0022]

[0023]

[0024] Preparation:

[0025] Pass metformin hydrochloride and rosiglitazone through a 100-mesh sieve, and set aside; take metformin hydrochloride, mix evenly with 300 g of microcrystalline cellulose, make a soft material with 3% povidone K-30 aqueous solution, granulate with a 20-mesh sieve, and dry. 18-mesh sieve for granulation, and set aside; take another rosiglitazone, mix well with the remaining microcrystalline cellulose, calcium hydrogen phosphate, and silicon dioxide, and prepare granules by the same method as above, and set aside; mix the two granules and add hard Magnesium fatty acid, mixed evenly, tableted; configured in 8% EC aqueous dispersion solution, stirred evenly, and set aside; opened the coating granulator, and put the tablet into it. Adjust the air inlet pressure and temperature, adjust the rotating speed o...

Embodiment 3

[0026] Example 3 Compound Metformin Hydrochloride Rosiglitazone Sustained-release Pellet Capsules

[0027] prescription:

[0028]

[0029] Preparation:

[0030] Pass metformin hydrochloride, rosiglitazone, HPMC-K4M, and HPMC-K10M through a 60-mesh sieve, add 60% ethanol solution to make a wet soft material, extrude strips with a length of about 3-5cm in 12-20 mesh aperture, and rotate at the bottom of the turntable Adjust to 600-1200rpm, spheronize for about 5 minutes, fluidize and dry, fill in capsule shells, and get ready.

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PUM

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Abstract

The invention relates to a sustained-release preparation of compound metformin hydrochloride rosiglitazone and a preparation method thereof; wherein, rosiglitazone and metformin hydrochloride have slow releasing characteristic in an in-vitro dissolution test, the rosiglitazone is released by 10-30 percent for a first hour, and is released by 60-80 percent for a fourth hour, and is released by morethan 80 percent for an eighth hour; the metformin hydrochloride is released by 15-40 percent for a first hour, is released by 50-70 percent for a fourth hour, and is released by more than 75 percentfor an eighth hour. The formula is mild and has prolonged action of glucose reduction, so as to avoid adverse reaction such as hypoglycemia and gastrointestine malaise, reduce taking times (one or twotimes each day), and improve compliance of a patient. The invention discloses the in-vitro drug-releasing characteristic of the sustained-release preparation and the preparation method thereof.

Description

technical field [0001] The invention relates to a slow-release preparation of compound metformin hydrochloride rosiglitazone and a preparation method thereof. Background technique [0002] Metformin hydrochloride does not promote insulin secretion. Its hypoglycemic effect is mainly to promote the uptake of glucose by adipose tissue, increase the anaerobic glycolysis of muscle tissue, increase the utilization of glucose, and reduce the absorption of glucose through the digestive tract. [0003] Rosiglitazone has the effect of lowering blood sugar by increasing the sensitivity of tissues to insulin and improving the utilization of glucose by cells. It can significantly reduce the levels of fasting blood sugar, insulin and C-peptide, and also significantly reduce postprandial blood sugar and insulin. effect. The level of glycosylated hemoglobin (HbAlc) was significantly reduced. Its mechanism of action is related to the specific activation of a nuclear receptor: peroxisome pr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4439A61K31/155A61K9/00A61P3/10
Inventor (请求不公开姓名)
Owner 北京利乐生制药科技有限公司
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