Ticagrelor dispersible tablet and preparation method thereof

A technology for ticagrelor and dispersible tablets, applied in the field of ticagrelor dispersible tablets and their preparation, can solve the problems of low bioavailability of ticagrelor, poor patient compliance with the dissolution rate of ticagrelor, etc. The effect of crystal transformation and impurity increase, good process reproducibility and simple operation steps

Inactive Publication Date: 2018-04-17
ZHENGZHOU TAIFENG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The object of the present invention is to provide a ticagrelor dispersible tablet and a preparation method thereof, aiming at solving the problems of low bioavailability of ticagrelor, dissolution rate of ticagrelor and poor patient compliance

Method used

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  • Ticagrelor dispersible tablet and preparation method thereof
  • Ticagrelor dispersible tablet and preparation method thereof
  • Ticagrelor dispersible tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Ticagrelor dispersible tablets are prepared from the following components, according to the dosage of 1000 tablets

[0032]

[0033] Its preparation method comprises the following steps:

[0034] 1) Micronize ticagrelor to a particle size of <20µm;

[0035] 2) Add sodium carboxymethyl starch and mannitol three times in equal amounts, mix for 15 minutes, and the speed of the mixer is 10 rpm to obtain the mixture (1)

[0036] 3) Add ticagrelor to the mixture (1) obtained in step 2, the mixing time is 15 minutes, the speed of the mixer is 10 rpm, and the mixture (2) is obtained

[0037] 4) Add microcrystalline cellulose to the mixture (2) obtained in step 3, mix for 15 minutes, and the speed of the mixer is 10 rpm to obtain the mixture (3)

[0038] 5) Add magnesium stearate and sodium dodecylsulfonate to the mixture (3) obtained in step 4, mix for 10 minutes, and the speed of the mixer is 10 rpm to obtain the mixture (4)

[0039] 6) Take the mixture (4) obtained in s...

Embodiment 2

[0041] Ticagrelor dispersible tablets are prepared from the following components, according to the dosage of 1000 tablets

[0042]

[0043] Its preparation method comprises the following steps:

[0044] 1) Micronize ticagrelor to a particle size of <20µm;

[0045] 2) The croscarmellose sodium and mannitol were added twice in equal amounts, the mixing time was 10 minutes, the speed of the mixer was 10 rpm, and the mixture (1) was obtained;

[0046] 3) Add ticagrelor to the mixture (1) obtained in step 2, the mixing time is 15 minutes, the speed of the mixer is 10 rpm, and the mixture (2) is obtained;

[0047] 4) Add microcrystalline cellulose to the mixture (2) obtained in step 3, mix for 15 minutes, and the speed of the mixer is 10 rpm to obtain the mixture (3);

[0048] 5) Add magnesium stearate and sodium lauryl sulfonate to the mixture (3) obtained in step 4, mix for 10 minutes, and the speed of the mixer is 10 rpm to obtain the mixture (4);

[0049] 6) Take the mixtu...

Embodiment 3

[0050] Example 3 Ticagrelor dispersible tablets are formulated from the following components, in the amount of 1000 tablets

[0051]

[0052] Its preparation method comprises the following steps:

[0053]1) Micronize ticagrelor to a particle size of <20µm;

[0054] 2) The sodium carboxymethyl starch and mannitol were added twice in equal amounts, the mixing time was 10 minutes, and the speed of the mixer was 10 rpm to obtain the mixture (1);

[0055] 3) Add ticagrelor to the mixture (1) obtained in step 2, the mixing time is 15 minutes, the speed of the mixer is 10 rpm, and the mixture (2) is obtained;

[0056] 4) Add microcrystalline cellulose to the mixture (2) obtained in step 3, mix for 15 minutes, and the speed of the mixer is 10 rpm to obtain the mixture (3);

[0057] 5) Add magnesium stearate and sodium lauryl sulfonate to the mixture (3) obtained in step 4, mix for 10 minutes, and the speed of the mixer is 10 rpm to obtain the mixture (4);

[0058] 6) Take the mi...

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PUM

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Abstract

The invention relates to a ticagrelor dispersible tablet for patients with acute coronary syndrome, including patients receiving drug therapy and percutaneous coronary intervention (PCI) treatment. The ticagrelor is used as a raw material, and auxiliary materials are added to prepare ticagrelor dispersible tablets. The dispersible tablet of the present invention disintegrates quickly, absorbs quickly, and has high bioavailability; it is convenient to take; it has less intestinal residue and less side effects; There will be no sticking phenomenon in the process, which is conducive to the realization of industrialized production.

Description

technical field [0001] The invention belongs to the field of ticagrelor preparations, and in particular relates to ticagrelor dispersible tablets and a preparation method thereof. Background technique [0002] Ticagrelor (Ticarelor), also known as ticagrelor, the 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-hydroxyethoxy)- 1,2 Cyclopentanediol. Molecular formula: C 23 h 28 f 2 N 6 o 4 S, molecular weight: 522.57, chemical structural formula as follows: [0003] [0004] Ticagrelor belongs to the cyclopentyltriazolopyrimidine class of compounds and is the first reversible P2Y12 platelet inhibitor. It is a new type of anti-platelet aggregation drug developed by AstraZeneca, which does not require liver activation. Active drug with rapid onset of action; and its reversible binding to platelet receptors, which is very beneficial for reducing the risk of bleeding in p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/519A61K47/36A61K47/38A61P7/02
CPCA61K9/2095A61K9/0056A61K9/2054A61K9/2059A61K31/519
Inventor 杨苗苗沙薇米攀义
Owner ZHENGZHOU TAIFENG PHARMA CO LTD
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