Succinic acid trelagliptin solid preparation and preparation method thereof

A technology for trelagliptin succinate and solid preparation is applied in the field of solid preparation and preparation of trelagliptin succinate, which can solve the problems of poor fluidity of raw materials, increase of impurities, poor compressibility of raw materials, etc., so as to ensure raw materials, improve Effects of stability, improved flow and compressibility

Active Publication Date: 2016-05-25
SHIJIAZHUANG NO 4 PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] The purpose of the present invention is to overcome the deficiencies in the prior art, provide a kind of solid preparation of trexagliptin succinate and preparation method thereof, to solve the deficiencies of poor fluidity of raw materials, n

Method used

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  • Succinic acid trelagliptin solid preparation and preparation method thereof
  • Succinic acid trelagliptin solid preparation and preparation method thereof
  • Succinic acid trelagliptin solid preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0044] Embodiment 1 (1000 pieces amount)

[0045] prescription:

[0046]

[0047]

[0048] making process:

[0049](1) Mix troxagliptin succinate, mannitol, pregelatinized starch, and crospovidone evenly, add purified water, wet granulate, and dry to obtain mixture 1.

[0050] (2) Add magnesium stearate to mixture 1 and mix.

[0051] (3) Compression, coating and packaging.

Embodiment 2

[0052] Embodiment 2 (quantity of 1000 pieces)

[0053] prescription:

[0054]

[0055] making process:

[0056] (1) Mix troxagliptin succinate, mannitol, pregelatinized starch, and crospovidone evenly, add purified water, wet granulate, and dry to obtain mixture 1.

[0057] (2) Add magnesium stearate to mixture 1 and mix.

[0058] (3) Compression, coating and packaging.

Embodiment 3

[0059] Embodiment 3 (quantity of 1000 pieces)

[0060] prescription:

[0061]

[0062] making process:

[0063] (1) Mix troxagliptin succinate, mannitol, pregelatinized starch, and crospovidone evenly, add purified water, wet granulate, and dry to obtain mixture 1.

[0064] (2) Add magnesium stearate to mixture 1 and mix.

[0065] (3) Compression, coating and packaging.

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Abstract

The invention provides a succinic acid trelagliptin solid preparation and a preparation method thereof. The succinic acid trelagliptin solid preparation comprises 13-84wt% of succinic acid trelagliptin and 10-84wt% of mixture of mannitol and pregelatinized starch. The preparation method of the solid preparation is wet granulation and comprises the following concrete processes: (1) uniformly mixing succinic acid trelagliptin, a diluting agent and a disintegrating agent, then adding a wetting agent for wet granulation, and drying to obtain a mixture I; and (2) adding a lubricating agent into the mixture I, totally blending, and tabletting. According to the solid preparation, by wet granulation of the raw materials and auxiliary materials, the problems of loose and light properties and poor liquidity and compressibility of the raw materials are solved; and by adopting the specific auxiliary materials, the generation of impurities of the raw materials under hygrothermal conditions is avoided.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a solid preparation of trexagliptin succinate and a preparation method thereof. Background technique [0002] Dipeptidyl peptidase-4 (DPP-4) can inactivate glucagon-like peptide-1 (GLP-1) secreted from the intestine into the blood, and reduce the glucagon-like peptide-1 (GLP-1) in the blood. 1) at a concentration that reduces blood glucose level-dependent insulin secretion, resulting in an increase in blood glucose levels. Tregelliptin succinate can inhibit the activity of dipeptidyl peptidase-4 (DPP-4), increase the concentration of glucagon-like peptide-1 (GLP-1) in blood, increase blood glucose level-dependent insulin secretion, thereby controlling blood sugar levels. [0003] Trexagliptin succinate, chemical name 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo Generation-1(2H)-pyrimidinyl]methyl]-4-fluoro-benzonitrile succinate, its structur...

Claims

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Application Information

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IPC IPC(8): A61K31/513A61K9/28A61K47/36A61K47/32A61K47/12A61P3/10
CPCA61K9/2059A61K9/28A61K31/513
Inventor 殷殿书赵晓雷魏赛丽闫永娜陈雪桃赵毅莎周康
Owner SHIJIAZHUANG NO 4 PHARMA
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