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Preparation method of composite trelagliptin succinate tablets

A technology of troxagliptin succinate and compound succinic acid is applied in the field of medicine to achieve the effects of treating hyperglycemia, less toxic and side effects, and less dosage

Active Publication Date: 2019-02-15
HONG KONG JOWA & HUAYUAN GRP CHUZHOU PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the treatment methods of drugs are accompanied by various risks, and the dosage is positively correlated with the toxic and side effects of the drug. Therefore, it is necessary to provide a therapeutic drug that can not only have a significant therapeutic effect, but also reduce the dosage and reduce the toxic and side effects.

Method used

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  • Preparation method of composite trelagliptin succinate tablets

Examples

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Comparison scheme
Effect test

Embodiment 1

[0043] A kind of preparation method of composite troxagliptin succinate tablet, the preparation of troxagliptin succinate raw material, comprises the following steps:

[0044] Step 1: Intermediate 2-[(6-chloro-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl)methyl]-4-fluorobenzyl Nitrile preparation:

[0045] Add 10.8kg of ethyl acetate, 2.4kg of 2-bromomethyl-4-fluorobenzonitrile, 1.74kg of 6-chloro-3-methyluracil, and 2.27kg of triethylamine to the 20L reactor in sequence; start stirring and heating The device is heated to an internal temperature of 60-70°C; the temperature range in the reaction kettle is controlled to 60-70°C, and the reaction time is 1.5-2.5 hours.

[0046] Reaction end point control method: use thin-layer chromatography, choose petroleum ether: ethyl acetate = 3: 1 (PE: EA = 3: 1) as the developer ratio, develop color under ultraviolet light, until the raw material spots disappear, it is regarded as The reaction is complete;

[0047] After the reactio...

Embodiment 2

[0079] A kind of preparation method of composite troxagliptin succinate tablet, the preparation of troxagliptin succinate raw material, comprises the following steps:

[0080] Step 1: Intermediate 2-[(6-chloro-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl)methyl]-4-fluorobenzyl Nitrile preparation:

[0081] Add 9.6kg of ethyl acetate, 1.9kg of 2-bromomethyl-4-fluorobenzonitrile, 1.24kg of 6-chloro-3-methyluracil, and 1.87kg of triethylamine to the 20L reactor in sequence; start stirring and heating The device is heated to an internal temperature of 60-70°C; the temperature range in the reaction kettle is controlled to 60-70°C, and the reaction time is 1.5-2.5 hours.

[0082] Reaction end point control method: use thin-layer chromatography, choose petroleum ether: ethyl acetate = 3: 1 (PE: EA = 3: 1) as the developer ratio, develop color under ultraviolet light, until the raw material spots disappear, it is regarded as The reaction is complete;

[0083]After the reaction ...

Embodiment 3

[0115] A kind of preparation method of compound troxagliptin succinate tablet, the preparation of troxagliptin succinate raw material, comprises the following steps:

[0116] Step 1: Intermediate 2-[(6-chloro-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl)methyl]-4-fluorobenzyl Nitrile preparation:

[0117] Add 11.3kg of ethyl acetate, 2.9kg of 2-bromomethyl-4-fluorobenzonitrile, 2.24kg of 6-chloro-3-methyluracil, and 2.57kg of triethylamine to the 20L reactor in sequence; start stirring and heating The device is heated to an internal temperature of 60-70°C; the temperature range in the reaction kettle is controlled to 60-70°C, and the reaction time is 1.5-2.5 hours.

[0118] Reaction end point control method: use thin-layer chromatography, choose petroleum ether: ethyl acetate = 3: 1 (PE: EA = 3: 1) as the developer ratio, develop color under ultraviolet light, until the raw material spots disappear, it is regarded as The reaction is complete;

[0119] After the reaction...

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Abstract

The invention provides a preparation method of composite trelagliptin succinate tablets. Preparation of trelagliptin succinate raw materials comprises the step of separately sieving 50 g-230 g of trelagliptin succinate raw materials, 300 g-1380 g of apocynum venetum plaster powder, 30 g-86 g of mannitol, 2 g-58 g of microcrystalline celluloses, 1.8 g-37 g of croscarmellose sodium and 3.2 g-54 g ofsodium stearyl fumarate by using a sieve with meshes of 60, wherein the trelagliptin succinate raw materials and the apocynum venetum plaster powder are added according to the ratio of 1: (5-7), theuse amount of drugs and the toxic and side effects of the drugs are reduced obviously, and an effect of treating diabetes is remarkable.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a preparation method of compound troxagliptin succinate tablet. Background technique [0002] Diabetes is currently the top five leading cause of death worldwide. Especially in Asia, the number and compound growth rate of diabetic patients will rise rapidly. Although there are many types of diabetes drugs on the market, experts point out that with the progression of type 2 diabetes, the function of pancreatic beta cells gradually declines or even fails. The hypoglycemic efficacy of traditional treatments, whether it is insulin secretagogues or sensitizers, depends on the existence of pancreatic β-cell function. [0003] Therefore, more and more patients, especially those in the middle and advanced stages, have increasingly difficult to control their blood sugar levels. For such patients, insulin-independent hypoglycemic drugs may provide a more effective treatment option. Ho...

Claims

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Application Information

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IPC IPC(8): A61K31/513A61K36/24A61P3/10C07D401/04A61K9/20
CPCA61K9/2054A61K31/513A61K36/24A61P3/10C07D401/04A61K2300/00
Inventor 管悦琴余星云罗雪峰
Owner HONG KONG JOWA & HUAYUAN GRP CHUZHOU PHARMA CO LTD
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