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Stable linagliptin medicine composition

A technology of linagliptin and its composition, which is applied in the field of linagliptin pharmaceutical composition and its preparation, can solve the problem that linagliptin does not give further prompts, etc., and achieves the method is simple, reliable in quality, The effect of stable product quality

Inactive Publication Date: 2016-11-23
TIANJIN HANRUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, how to obtain a more excellent dissolution rate through the dissolution adjustment formula and process adjustment of linagliptin, how to select suitable process conditions to avoid problems such as degradation of linagliptin, the prior art has not given. Further hint, in view of this, propose this invention

Method used

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  • Stable linagliptin medicine composition
  • Stable linagliptin medicine composition
  • Stable linagliptin medicine composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Linagliptin pharmaceutical composition is made into the prescription composition of 1000 tablets as follows:

[0055] Linagliptin 5g

[0056] Mannitol 122g

[0057] 18g pregelatinized starch

[0058] Cornstarch 20g

[0059] Copovidone 5g

[0060] Magnesium Stearate 1g

[0061] Film coating agent 5g

[0062] Preparation

[0063] 1) Drying linagliptin, mannitol, pregelatinized starch and cornstarch, pulverizing, passing through a 100-mesh sieve, and dissolving copovidone in pure water to produce granulation liquid;

[0064] 2) Take the prescribed amount of excipients and mix them evenly with linagliptin, then add an appropriate amount of granulation liquid to make a soft material, pass through a 20-mesh sieve and granulate to obtain linagliptin wet granules;

[0065] 3) drying the wet granules of linagliptin at 40°C until the water content is less than 5%, to obtain dry granules of linagliptin;

[0066] 4) Pass the dry granules of linagliptin through a 20-mesh sie...

Embodiment 2

[0068] Linagliptin pharmaceutical composition is made into the prescription composition of 1000 tablets as follows:

[0069] Linagliptin 5g

[0070] Mannitol 108g

[0071] 18g pregelatinized starch

[0072] Cornstarch 25g

[0073] Copovidone 5g

[0074] Magnesium Stearate 1g

[0075] Film coating agent 5g

[0076] The preparation method is the same as in Example 1.

Embodiment 3

[0078] Linagliptin pharmaceutical composition is made into the prescription composition of 1000 tablets as follows:

[0079] Linagliptin 5g

[0080] Mannitol 157g

[0081] 18g pregelatinized starch

[0082] Cornstarch 15g

[0083] Copovidone 5g

[0084] Magnesium Stearate 1g

[0085] Film coating agent 5g

[0086] The preparation method is the same as in Example 1.

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Abstract

The invention discloses a stable linagliptin medicine composition and a preparation method thereof. According to the formula, besides active components, through selection on a diluent and a disintegrating agent in special composition with ratio of all components being controlled, the linagliptin has excellent stability and bioavailability.

Description

technical field [0001] The invention relates to a stable linagliptin pharmaceutical composition and a preparation method thereof. Background technique [0002] Linagliptin, a selective dipeptidyl peptidase IV (DPP-IV) inhibitor, can significantly control blood sugar with only once-daily oral administration, risk of hypoglycemia, cardiovascular events and weight gain Lower, the market prospect is better. Linagliptin is a purine derivative, and its compound structure contains a substituted quinazoline group and a 3-aminopiperidine group, and its structure is shown in the following formula (1): [0003] [0004] (1) [0005] Chemical name: 8-[(3R)-3-amino-1-piperidinyl]-7-(2-butynyl)-3,7-dihydro-3-methyl-1-[(4-methyl base-2-quinazolinyl)methyl]-1H-purine-2,6-dione [0006] Molecular formula: C 25 h 28 N 8 o 2 [0007] Molecular weight: 472.54 [0008] Through the research on the prior art, the stability problem of the linagliptin preparation is still a problem that...

Claims

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Application Information

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IPC IPC(8): A61K31/522A61K47/36A61K47/38A61P3/10A61K31/155
Inventor 严洁
Owner TIANJIN HANRUI PHARMA
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