Saxagliptin metformin double-layer tablet and preparation method thereof

A technology of metformin and metformin hydrochloride, which is applied in pharmaceutical formulations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc. Improve the effect of marketing efforts, close connection, and mild operating conditions

Inactive Publication Date: 2019-03-08
瀚晖制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Since metformin and saxagliptin are complementary in diabetes treatment mechanism, when these two drugs are used in combination, the therapeutic effect of the drug can be enhanced, so metformin and saxagliptin will be made into a compound preparation in the prior art, but Saxagliptin is an alkaline drug, and metformin hydrochloride is an acidic drug, and the drug release mechanisms of the two are also completely different. If they are mixed directly, the drug itself may be degraded, affecting the normal performance of the drug and affecting the drug. Drug Stability of Compound Preparations

Method used

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  • Saxagliptin metformin double-layer tablet and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] The preparation technology of saxagliptin metformin bilayer tablet follows the steps:

[0042] 1. Preparation of Metformin Granules:

[0043] 1) Take by weighing metformin hydrochloride 1000g, carboxymethylcellulose 50g according to prescription quantity, cross 40 mesh sieves respectively, magnesium stearate 10g and micropowder silica gel 7g (silicon dioxide) cross 60 mesh manual sieves;

[0044] 2) Mix metformin, carboxymethylcellulose, hydroxypropylmethylcellulose K100M grade 260g, hypromellose K15M CR grade 130g and micropowder silica gel for 40min with a hopper mixer, add magnesium stearate (internal ) 5g mixed for 6min;

[0045] 3) The mixed material is granulated by a dry granulator, the granulation speed: 200rpm, the granulation screen aperture: 0.9mm;

[0046] 4) Blending: Add the remaining 5 g of magnesium stearate (additional) and mix for 4 minutes.

[0047] 2. Preparation of saxagliptin granules:

[0048] 1) Weigh 138g microcrystalline cellulose 101 and 6...

Embodiment 2

[0060] The preparation technology of saxagliptin metformin bilayer tablet follows the steps:

[0061] 1. Preparation of Metformin Granules:

[0062] 1) Take by weighing metformin hydrochloride 500g, sodium carboxymethyl cellulose 25g according to prescription quantity, cross 50 mesh sieves respectively, magnesium stearate 5g and micropowder silica gel 3.5g (silicon dioxide) cross 70 mesh manual sieves;

[0063] 2) Mix metformin, sodium carboxymethylcellulose, 130g of hydroxypropylmethylcellulose K100M grade, 60g of hydroxypropylmethylcellulose K15M CR grade and micropowder silica gel with a hopper mixer for 60min, add magnesium stearate (inner Add) 2.5g and mix for 4min;

[0064] 3) The mixed material is granulated by a dry granulator, the granulation speed: 400rpm, the granulation screen aperture: 0.7mm;

[0065] 4) Total blending: add the remaining 2.5 g of magnesium stearate (additional) and mix for 6 minutes.

[0066] 2. Preparation of saxagliptin granules:

[0067] 1)...

Embodiment 3

[0079] The preparation technology of saxagliptin metformin bilayer tablet follows the steps:

[0080] 1. Preparation of Metformin Granules:

[0081] 1) Take by weighing metformin hydrochloride 600g, sodium carboxymethyl cellulose 30g according to prescription quantity, pass through 40 mesh sieves respectively, magnesium stearate 6g and micropowder silica gel 4g (silicon dioxide) pass 60 mesh manual sieves;

[0082] 2) Mix metformin, sodium carboxymethylcellulose, 150g of hydroxypropylmethylcellulose K100M grade, 50g of hydroxypropylmethylcellulose K15M CR grade and micropowder silica gel with a hopper mixer for 50min, add magnesium stearate (inner Add) 3g and mix for 5min;

[0083] 3) The mixed material is granulated by a dry granulator, the granulation speed: 300rpm, the granulation screen aperture: 0.8mm;

[0084] 4) Total blending: add the remaining 3 g of magnesium stearate (additional) and mix for 5 minutes.

[0085] 2. Preparation of saxagliptin granules:

[0086] 1)...

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Abstract

The invention provides a saxagliptin metformin double-layer tablet and a preparation method thereof. The saxagliptin metformin double-layer tablet mainly comprises metformin particles and saxagliptinparticles; the metformin particles mainly comprise the following components in parts by mass: 500-1000 parts of metformin hydrochloride, 25-50 parts of carboxymethyl cellulose, 3.5-7 parts of silicondioxide, 190-390 parts of hydroxypropyl methylcellulose, and 5-10 parts of magnesium stearate; and the saxagliptin particles mainly comprise the following components in parts by mass: 2.5-5.4 parts ofsaxagliptin monohydrate, 138-142 parts of microcrystalline cellulose, 30-60 parts of lactose, 3-6 parts of hydroxypropyl methylcellulose, and 0.5-2 parts of magnesium stearate. According to the saxagliptin metformin double-layer tablet disclosed by the invention, raw materials and auxiliary materials are effectively compounded, so that the double-layer tablet prepared after compounding has the advantages of stable drug effect, high safety and low cost.

Description

technical field [0001] The invention relates to the field of preparation of saxagliptin-metformin compound medicament, in particular to a saxagliptin-metformin double-layer tablet and a preparation method thereof. Background technique [0002] 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 2 diabetes. [0003] Metformin, a biguanide hypoglycemic drug, can improve blood sugar tolerance in patients with type 2 diab...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/24A61K31/403A61K47/38A61K47/04A61K47/26A61P3/10A61K31/155
CPCA61K9/2009A61K9/2018A61K9/2054A61K9/209A61K31/155A61K31/403A61P3/10A61K2300/00
Inventor 蔡邱华董福霞杜加秋任倩
Owner 瀚晖制药有限公司
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