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Ticagrelor tablets and preparation method thereof

A technology of ticagrelor and mannitol, which is applied in the field of medicine, can solve the problems affecting bioavailability and curative effect, affecting the full absorption of drugs, and uneven dissolution, so as to improve bioavailability, easy operation and realization, and dissolution rate fast effect

Active Publication Date: 2015-04-22
HENAN RUNHONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the current commercially available ticagrelor tablets have a low dissolution rate and uneven dissolution, which affects the full absorption of the drug and affects its bioavailability and curative effect.

Method used

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  • Ticagrelor tablets and preparation method thereof
  • Ticagrelor tablets and preparation method thereof
  • Ticagrelor tablets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] The present embodiment ticagrelor tablet is made up of the following components in percentage by weight: ticagrelor 29.1%, mannitol 40.74%, microcrystalline cellulose 20.37%, low-substituted hydroxypropyl cellulose 2.91%, alternating Bihydroxymethylcellulose sodium 2.91%, magnesium stearate 0.97%, film coating premix 3%.

[0046] Among them, the film coating premix was purchased from Shanghai Colorcon Coating Technology Co., Ltd., and the product number was 295B620026.

[0047] The present embodiment prepares 30000 ticagrelor tablets, and its preparation method is: the specific operation steps are as follows:

[0048] 1) Weigh 2.7kg of ticagrelor tablets, 3.78kg of mannitol, 1.89kg of microcrystalline cellulose, 0.27kg of low-substituted hydroxypropyl cellulose, and 0.135kg of croscarmellose sodium, and pass through 100 meshes respectively. After sieving, place in a wet mixing granulator and mix for 3 minutes to obtain a mixed powder;

[0049] 2) Add 2.8 kg of purifie...

Embodiment 2

[0055] The present embodiment ticagrelor tablet is made up of the following components in percentage by weight: ticagrelor 29.55%, mannitol 41.37%, microcrystalline cellulose 20.69%, low-substituted hydroxypropyl cellulose 2.96%, alternating Bihydroxymethylcellulose sodium 2.96%, magnesium stearate 0.99%, film coating premix 1.5%.

[0056] Among them, the film coating premix was purchased from Shanghai Colorcon Coating Technology Co., Ltd., and the product number was 295B620026.

[0057] The present embodiment prepares 30000 ticagrelor tablets, and its preparation method is: the specific operation steps are as follows:

[0058] 1) Weigh 2.7kg of ticagrelor tablets, 3.78kg of mannitol, 1.89kg of microcrystalline cellulose, 0.27kg of low-substituted hydroxypropyl cellulose, and 0.135kg of croscarmellose sodium, and pass through 100 meshes respectively. After sieving, place it in a wet mixing granulator and mix for 5 minutes to obtain a mixed powder;

[0059] 2) Add 3.0 kg of p...

Embodiment 3

[0065] The present embodiment ticagrelor tablet is made up of the following components in percentage by weight: ticagrelor 29.32%, mannitol 41.10%, microcrystalline cellulose 20.54%, low-substituted hydroxypropyl cellulose 2.93%, alternating Bihydroxymethylcellulose sodium 2.93%, magnesium stearate 0.98%, film coating premix 2.2%.

[0066] Among them, the film coating premix was purchased from Shanghai Colorcon Coating Technology Co., Ltd., and the product number was 295B620026.

[0067] The present embodiment prepares 30000 ticagrelor tablets, and its preparation method is: the specific operation steps are as follows:

[0068] 1) Weigh 2.7kg of ticagrelor tablets, 3.78kg of mannitol, 1.89kg of microcrystalline cellulose, 0.27kg of low-substituted hydroxypropyl cellulose, and 0.135kg of croscarmellose sodium, and pass through 100 meshes respectively. After sieving, place in a wet mixing granulator and mix for 4 minutes to obtain a mixed powder;

[0069] 2) Add 2.9 kg of puri...

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Abstract

The invention discloses ticagrelor tablets and a preparation method thereof and belongs to the technical field of medicines. According to the ticagrelor tablets disclosed by the invention, mannitol, microcrystalline cellulose, low-substituted hydroxypropyl cellulose, croscarmellose sodium and magnesium stearate are selected as auxiliary materials and are compounded with the raw material medicine ticagrelor tablets so as to obtain the ticagrelor tablets, and each auxiliary material and the raw material medicine are synergetic in the defined amount range, so that the dissolution rate of the prepared ticagrelor tablets is higher than that of the conventional commercially available tablets. Moreover, the ticagrelor tablets have the same dissolution behavior as the commercially available medicines, the ticagrelor tablets have good absorption effects, and the bioavailability of the ticagrelor tablets is improved. The ticagrelor tablets disclosed by the invention are small in impurity content and are stable in performance under high-temperature illumination conditions. The method for preparing the ticagrelor tablets disclosed by the invention is simple in process flow, easy to operate and implement and suitable for industrial popularization and application.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a ticagrelor tablet and a preparation method thereof. Background technique [0002] Ticagrelor, also known as ticagrelor, its chemical name is: (1S, 2S, 3R, 5S)-3-[7-{[(1R,2S)-2-(3,4-difluorophenyl )cyclopropyl]amino}-5-(propylthio)-3H-[1,2,3]-triazolo[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethyl Oxygen) cyclopentane-1,2-diol, structural formula is as follows: [0003] [0004] Ticagrelor Tablets is an anti-platelet aggregation antithrombotic drug originally developed by AstraZeneca in the United Kingdom. AstraZeneca began to develop ticagrelor in 1999, and the European Society of Cardiology first announced the results of phase III trials of ticagrelor in 2009, describing and comparing its curative effect on patients with acute coronary syndrome in detail. In November 2009, AstraZeneca submitted a new drug application for ticagrelor to the European Union and the US ...

Claims

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Application Information

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IPC IPC(8): A61K9/28A61K31/519A61K47/38A61P7/02A61P9/10
Inventor 靳勇高志亮
Owner HENAN RUNHONG PHARMA
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