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Sitagliptin pharmaceutical composition and preparation process thereof

A composition and drug technology, applied in drug combination, drug delivery, drug formulation and other directions, can solve the problems of weight difference, poor product stability, sticking and punching, etc.

Pending Publication Date: 2021-05-28
ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] In view of the deficiencies in the prior art, the technical problem to be solved by the present invention is the impurity content, weight difference, poor product stability and sticky punching problems of sitagliptin in the prior art; in the prior art, the medicine is pretreated, such as micropowder Compounding, multiple sieving, wet granulation and other process steps lead to complex production process and high production cost; in addition, the use of common technical means to increase the amount of lubricant can improve sticking and punching, but the stability of the product is significantly reduced

Method used

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  • Sitagliptin pharmaceutical composition and preparation process thereof
  • Sitagliptin pharmaceutical composition and preparation process thereof
  • Sitagliptin pharmaceutical composition and preparation process thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-3 and comparative Embodiment 1-3

[0043] Preparation of Sitagliptin Phosphate Tablets, the material composition is shown in Table 1-2

[0044] Table 1 embodiment 1-3 and the material composition ratio of comparative example 1-2

[0045]

[0046] The material composition ratio of table 2 comparative example 3

[0047]

[0048] The particle size (laser particle size analyzer detection) of active ingredient in the concrete embodiment of table 3

[0049]

[0050] The coating parameter that table 4 specific embodiment uses

[0051]

Embodiment 1-3

[0052] Embodiment 1-3 and comparative example 1-3 processing steps are:

[0053] 1. Sitagliptin phosphate is mixed with microcrystalline cellulose, calcium hydrogen phosphate, and croscarmellose sodium;

[0054] 2. The mixture is then sized by a rotary granulator. The sizes of the sieves of the granulator used in Examples 1 to 3 are 0.8mm, 1.0mm, and 1.2mm, respectively.

[0055] 3. Add the sieved sodium stearyl fumarate and magnesium stearate and continue mixing.

[0056] 4. Tablet pressing.

[0057] 5. Carry out coating according to the coating parameter of table 4, coating material is selected from series.

[0058] The product quality was tested, and the results are shown in Table 5.

[0059] Table 5 Test results of sitagliptin phosphate tablets

[0060]

[0061] Analysis of Table 1-5 results:

[0062] According to embodiment 1-3, the product placed under accelerated conditions for 6 months is surprisingly found that the product stability has a significantly bette...

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Abstract

The present invention discloses a sitagliptin pharmaceutical composition and a preparation process thereof, the sitagliptin pharmaceutical composition comprises an active agent of sitagliptin phosphate or a pharmaceutically acceptable salt thereof as an active ingredient, and by adding a pharmaceutically acceptable additive of the pharmaceutical composition, the sitagliptin pharmaceutical composition is characterized in that the granularity of 90% of the active agent is in the range of 60-300 [mu] m; the pharmaceutical composition is prepared by a direct tabletting method and coating. As for the granularity of the medicine, the stability can be effectively improved, sticking can be improved, and the problem of product degradation impurities can be controlled without grinding or preparing dry particles with other materials by a dry method or a wet method in advance. The invention also relates to a preparation method of the pharmaceutical composition, the preparation method has the characteristics of simple process, low cost, good product stability and the like, the production efficiency is improved to a certain extent, and the preparation method is suitable for commercial production.

Description

technical field [0001] The invention relates to a pharmaceutical preparation and a preparation method thereof, in particular to a pharmaceutical composition of sitagliptin phosphate or a pharmaceutically acceptable salt thereof and a preparation method thereof. Background technique [0002] Sitagliptin, an oral antihyperglycemic drug that is a dipeptidyl peptidase IV (DPP-IV) inhibitor, improves glycemic control in patients with type 2 diabetes by increasing the levels of active incretin hormones. Sitagliptin is a potent and highly selective DPP-IV enzyme inhibitor that does not inhibit DPP-8 or DPP-9, which are closely related to DPP-IV, at therapeutic concentrations. In patients with type 2 diabetes, a single oral dose of this product inhibits DPP-IV enzyme activity within 24 hours, resulting in a 2- to 3-fold increase in circulating concentrations of active GLP-1 and GIP and increased plasma levels of insulin and C-peptide , lowers glucagon levels, lowers fasting blood g...

Claims

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Application Information

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IPC IPC(8): A61K9/30A61K31/4985A61K47/32A61P3/10
CPCA61K9/2095A61K9/284A61K31/4985A61P3/10
Inventor 沈广青章正赞黎昱鑫聂倩兰邵建华
Owner ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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