Oral tablet containing trelagliptin succinate and preparation method thereof

A technology of trilagliptin succinate and oral tablet is applied in the field of oral tablet containing trilagliptin succinate and its preparation field, which can solve the problem that the crude drug of trilagliptin succinate is easy to aggregate and is not suitable for commercialization Production, granulation and other problems are not good, to achieve good in vitro dissolution behavior, to solve the effect of poor fluidity and stable quality

Active Publication Date: 2015-08-12
ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The purpose of the present invention is to overcome the easy aggregation of trexagliptin succinate crude drug, poor fluidity, poor granulation effect after granulation, thereby causing problems in the tableting process, and is not suitable for commercial production

Method used

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  • Oral tablet containing trelagliptin succinate and preparation method thereof
  • Oral tablet containing trelagliptin succinate and preparation method thereof
  • Oral tablet containing trelagliptin succinate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047]

[0048] Note: Trexagliptin succinate particle size d0.9=79μm

[0049] The preparation method is as follows: mix troxagliptin succinate, mannitol, microcrystalline cellulose, hydroxypropyl cellulose, and croscarmellose sodium and sieve to obtain mixed powder 1; mix powder 1, part The magnesium stearate is mixed for later use to obtain mixed powder 2; the mixed powder 2 is dry-granulated by a dry granulator to obtain dry granules of troxagliptin succinate; the dry granules of troxagliptin succinate and remaining stearin Magnesium acid mixed evenly, compressed into tablets.

[0050] Comparative Example 1, Comparative Example 2, and Example 1 were placed naked under high-temperature and high-humidity conditions, and the related substances on day 0 and day 10 were investigated. The results are shown in Table 1.

[0051] Table 1: Related Substance Results

[0052]

Embodiment 2

[0055]

[0056] Note: Trexagliptin succinate particle size d0.9=79μm

[0057] The preparation method is as follows: mix troxagliptin succinate, mannitol, microcrystalline cellulose, hydroxypropyl cellulose, and croscarmellose sodium and sieve to obtain mixed powder 1; mix powder 1, part The magnesium stearate is mixed for later use to obtain mixed powder 2; the mixed powder 2 is dry-granulated by a dry granulator to obtain dry granules of troxagliptin succinate; the dry granules of troxagliptin succinate and remaining stearin Magnesium acid mixed evenly, compressed into tablets.

Embodiment 3

[0059]

[0060] The preparation method is as follows: mix troxagliptin succinate, mannitol, microcrystalline cellulose, hydroxypropyl cellulose, and croscarmellose sodium and sieve to obtain mixed powder 1; mix powder 1, part The hard sodium fumarate is mixed and set aside to obtain mixed powder 2; the mixed powder 2 is dry-granulated by a dry granulator to obtain troxagliptin succinate dry granules; the troxagliptin succinate dry granules and the remaining Hard sodium fumarate is mixed evenly and pressed into tablets.

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Abstract

The invention provides an oral tablet containing trelagliptin succinate and a preparation method thereof. The tablet do not contain flow aids such as micro-powder silica gel and comprises 35-50 percent by weight of trelagliptin succinate, the trelagliptin succinate tablet cores are prepared by tabletting trelagliptin succinate granules and lubricating agents, and filling agents only exist in the tabletting trelagliptin succinate granules. The trelagliptin succinate tablet prepared by the method disclosed by the invention is stable and controllable in quality, the poor phenomena such as low liquidity in the granulation process and phenomena such as sticking, adhesion, tablet capping and layering during tabletting are avoided, and the oral tablet is suitable for commercialized production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an oral tablet containing trexagliptin succinate and a preparation method thereof. Background technique [0002] Type II diabetes has become an increasingly popular disease, and its high-frequency complications (such as diabetic foot, blindness, renal failure, etc.) not only affect the quality of life of patients, but may also lead to shortened life span. [0003] Trexagliptin succinate is a once-weekly dipeptidyl peptidase IV (DPP-4) inhibitor that controls blood sugar levels through selective and sustained inhibition of DPP-4. DPP-4 is an enzyme that triggers the inactivation of incretins (glucagon-like peptide-1 (GLP-1) and diabetes-dependent insulinotropic polypeptide (GIP), which are It plays an important role in regulation.Inhibition of DPP-4 can increase blood glucose level-dependent insulin secretion, thereby controlling blood glucose levels. [0004] The c...

Claims

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Application Information

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IPC IPC(8): A61K9/28A61K31/513A61K47/10A61K47/38A61P3/10
Inventor 施祥杰陈浩屠后为胡功允
Owner ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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