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Alogliptin-metformin sustained-release tablet and preparation method thereof

A technology of metformin and metformin hydrochloride, which is applied in the directions of pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., to achieve the effect of stable and slow release effect

Inactive Publication Date: 2016-02-03
SHANGHAI SUNTECH PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Patent CN101801351A discloses a preparation method of alogliptin-metformin solid preparation, although it has the advantage of combined medication, but because it is a common tablet, the respective advantages of alogliptin benzoate and metformin cannot be fully utilized

Method used

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  • Alogliptin-metformin sustained-release tablet and preparation method thereof
  • Alogliptin-metformin sustained-release tablet and preparation method thereof
  • Alogliptin-metformin sustained-release tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0097] Embodiment 1: specification 6.25mg alogliptin (equivalent to 8.5mg alogliptin benzoate) and 500mg metformin hydrochloride

[0098] Compound Alogliptin Metformin Sustained Release Tablets (Formulation)

[0099]

[0100] Preparation:

[0101] 1. Drug loading: Dissolve metformin hydrochloride in purified water with a solubility of 300mg / ml; add the adsorbent silicon dioxide to the above metformin hydrochloride solution and stir for 24 hours to make the inner and outer surfaces of the silicon dioxide completely covered by the metformin hydrochloride solution infiltration.

[0102] 2. Curing: Add polyvinylpyrrolidone K30, the binder part of metformin, to the suspension system prepared in step 1 to prepare a suspension with a solid content of about 30%, spray dry it with LPG-10 spray drier, and feed it into the The temperature is 160° C., and the outlet air temperature is 80° C. to obtain solid drug-containing granules.

[0103] 3. Grain sizing: In step 2, the granules ...

Embodiment 2

[0108] Embodiment 2: specification 6.25mg alogliptin (equivalent to 8.5mg alogliptin benzoate) and 1000mg metformin hydrochloride

[0109] Compound Alogliptin Metformin Sustained Release Tablets (Formulation)

[0110] Raw materials

Formula amount (g)

Metformin Hydrochloride Extended Release Fraction

Metformin Hydrochloride

1000

Silica (Aerosil300)

145

Hypromellose K100M

220

Polyvinylpyrrolidone K30

30

Magnesium stearate

8

Subtotal

1403

Alogliptin immediate release portion

Alogliptin Benzoate

8.5

Polyoxyethylene Hydrogenated Castor Oil

8.5

Hypromellose E5

4

Talc powder

4

total

1428

Make 1000 capsules

[0111] Preparation:

[0112] 1. Drug loading: Dissolve metformin hydrochloride in purified water with a solubility of 300mg / ml; add the adsorbent silicon dioxide to the above metformin hydrochlori...

Embodiment 3

[0120] The compound alogliptin metformin sustained-release tablet prepared in embodiment 1 and embodiment 2 adopts Chinese Pharmacopoeia 2005 edition dissolution rate detection method to measure release rate, condition is paddle method, rotating speed is 50 revs / min, and dissolution medium is 37 ℃ 900 ml of pH 6.8 phosphate buffer. The comparative results of the release rates of Example 1 and Example 2 are as follows.

[0121] Metformin release:

[0122] time point (hour)

1

2

4

6

8

10

Example 1 (%)

7

12

30

62

85

97

Example 2 (%)

13

25

52

74

93

96

[0123] Alogliptin Release Rate:

[0124] time point (minute)

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Abstract

The invention provides an alogliptin-metformin sustained-release tablet consisting of a metformin hydrochloride sustained-release portion and an alogliptin benzoate immediate-release portion. The alogliptin-metformin sustained-release tablet comprises the following ingredients by weight percentage as shown in the description. Through series of experiments, the alogliptin-metformin sustained-release tablet provides favorable conditions for rapid absorption of alogliptin benzoate in vivo, and metformin hydrochloride achieves more sustained and stable sustained-release effect. Compared with common preparations, the alogliptin-metformin sustained-release tablet has the advantages that the alogliptin-metformin sustained-release tablet is rapider and more stable in release and can enable a diabetes patient to keep stable blood sugar concentration for the whole day. The alogliptin-metformin sustained-release tablet is taken once per day conveniently and has the combination medication advantage and high clinical application value. A preparation method of the alogliptin-metformin sustained-release tablet is good in reproducibility and stability and suitable for industrial production.

Description

technical field [0001] The invention relates to a pharmaceutical preparation, in particular to a sustained-release preparation, in particular to an alogliptin-metformin sustained-release tablet and a preparation method thereof. Background technique [0002] At present, the global incidence of diabetes is about 6.4%. Type 2 diabetes is common in diabetes and is one of the most difficult diseases to cure, which brings great physical and psychological pain to patients. Obesity caused by overeating and reduced physical activity is the most important environmental factor for type 2 diabetes, and makes individuals with genetic susceptibility to type 2 diabetes prone to the disease. The treatment of type 2 diabetes generally begins with diet control and physical exercise, followed by oral single hypoglycemic drugs to control blood sugar. For many patients, taking a single drug for a long time can not control the disease well, thus many patients need to be treated with two hypoglyc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/513A61K9/36A61K47/44A61K47/38A61K47/36A61K47/32A61P3/10A61K31/155
Inventor 钱晓明黄献华
Owner SHANGHAI SUNTECH PHARMA
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