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Vildagliptin tablet and preparation method thereof

A technology for vildagliptin tablets and tablets, which is applied in the field of pharmaceutical preparations, can solve the problems of increasing material procurement costs, drug production costs, and reducing stability, and achieves the effects of stable quality and simple preparation method.

Inactive Publication Date: 2015-12-30
SHIJIAZHUANG KANGHEWEI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the lubricant magnesium stearate used in it coordinates with the active ingredient to cause degradation reactions of the active ingredient, including ring closure, hydrolysis, etc., resulting in a decrease in its stability during preparation or storage
[0010] CN104161752A lubricant selects sodium stearyl fumarate, and technology is direct compression tablet, to delay drug hydrolysis, but this preparation adopts other lubricants not commonly used, has increased the purchase cost of material and the production cost of medicine

Method used

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  • Vildagliptin tablet and preparation method thereof
  • Vildagliptin tablet and preparation method thereof
  • Vildagliptin tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1 The preparation of vildagliptin crystal form in the tablet of the present invention

[0026] The vildagliptin crude product is dissolved in n-heptane, the weight of the vildagliptin crude product is 100g, the proportion of the n-heptane is 850mL, then dimethylformamide is added dropwise, when it is found that there is solid precipitation Stop the dropwise addition of dimethylformamide, and let the above reaction solution stand still until an off-white solid is obtained. The off-white solid is filtered and vacuum-dried to obtain a white powder, vildagliptin crystalline form 95.8 g, with a yield of 95.8%.

[0027] In the X-ray powder diffraction diagram of this crystal form, the reflection angles 2θ are 5.34, 10.341, 14.438, 15.841, 17.32, 18.301, 18.68, 19.005, 19.577, 20.26, 21.161, 21.859, 22.379, 23.04, 23.5, 24.177, 24.959 There are diffraction peaks at 25.881, 26.641, 27.18, 28.3, 28.999, 29.501, 31.96, 32.258, 33.999, 36.798, 37.38, and 41.297, and the...

Embodiment 2

[0028] Embodiment 2 The preparation of vildagliptin crystal form in the tablet of the present invention

[0029] The vildagliptin crude product is dissolved in n-heptane, the weight of the vildagliptin crude product is 100g, the proportion of the n-heptane is 800mL, then dimethylformamide is added dropwise, when it is found that there is solid precipitation At this time, the dropwise addition of dimethylformamide was stopped, and the above-mentioned reaction solution was allowed to stand still until an off-white solid was obtained. The off-white solid was filtered and vacuum-dried to obtain a white powder, vildagliptin crystal form 94.6g, with a yield of 94.6%.

[0030] The X-ray powder diffraction pattern and DSC pattern of the crystal form of vildagliptin are the same as in Example 1.

Embodiment 3

[0031] Embodiment 3 Preparation of vildagliptin crystal form in the tablet of the present invention

[0032] The vildagliptin crude product is dissolved in n-heptane, the weight of the vildagliptin crude product is 100g, the proportion of the n-heptane is 900mL, then dimethylformamide is added dropwise, when it is found that a solid precipitates At this time, the dropwise addition of dimethylformamide was stopped, and the above reaction solution was allowed to stand still until an off-white solid was obtained. The off-white solid was filtered and vacuum-dried to obtain a white powder which was vildagliptin crystal form 93.7g, with a yield of 93.7%.

[0033] The X-ray powder diffraction pattern and DSC pattern of the crystal form of vildagliptin are the same as in Example 1.

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Abstract

The invention relates to a vildagliptin tablet and a preparation method thereof, belonging to the technical field of medicinal preparations. The vildagliptin tablet is prepare from vildagliptin, a diluent, a disintegrating agent, a lubricant, etc. According to verification results of a great amount of experiments, the vildagliptin tablet prepared in the invention and the preparation method thereof have the following substantial advantages compared with the prior art: vildagliptin amide impurity included in the vildagliptin tablet has stable quality in the processes of acceleration and long-term storage compared with an untreated vildagliptin tablet; and the preparation method is simple and can easily realize industrial mass production.

Description

technical field [0001] The invention relates to a tablet and a preparation method thereof, in particular to a vildagliptin tablet and a preparation method thereof, and belongs to the technical field of pharmaceutical preparations. Background technique [0002] Vildagliptin is a type IV dipeptidyl peptidase (DPP-4) inhibitor, which is a selective, competitive and reversible DPP-4 inhibitor, which combines with DPP-4 to form a DPP-4 complex Inhibiting the activity of this enzyme can increase the concentration of GLP-1 to promote the production of insulin by pancreatic B cells, while reducing the concentration of glucagon, thereby reducing blood sugar, and has no obvious effect on body weight. It has the effects of reducing fasting and postprandial blood sugar levels, postprandial glucagon secretion and improving B cell function. In clinical studies, whether it is used alone or in combination, it has shown good anti-diabetic effect and tolerance, overcoming Some current drugs ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/40C07D207/16A61P3/10
Inventor 刘宏果刘广慧席宁韩天娇田英涛周静
Owner SHIJIAZHUANG KANGHEWEI PHARMA
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