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Ticagrelor sustained-release tablet system and preparation method thereof

A technology for ticagrelor and sustained-release tablets, which is applied in the field of medicine and can solve problems such as half-life of only 12 hours and difficulty in development

Inactive Publication Date: 2012-09-12
SHENZHEN HUALIKANG BIOLOGICAL MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Although ticagrelor has shown superiority over clopidogrel in clinical studies, ticagrelor also has an obvious disadvantage: the half-life of ticagrelor is only 12 hours
Generally speaking, formulation products with more than 20 doses of oral drugs are more difficult to develop, while sustained-release formulation products with more than 20 doses are more difficult to develop

Method used

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  • Ticagrelor sustained-release tablet system and preparation method thereof
  • Ticagrelor sustained-release tablet system and preparation method thereof
  • Ticagrelor sustained-release tablet system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Ticagrelor Sustained Release Tablet System Formula Composition:

[0032]

[0033] The particle size of ticagrelor: 30 μm.

[0034] To prepare ticagrelor extended-release tablets:

[0035] Mix ticagrelor, lactose, and hypromellose first, add appropriate amount of water to granulate; fully dry the prepared granules at 50-60°C, and mix the sieved granules with magnesium stearate and micropowder silica gel Post-compression to make ticagrelor matrix sustained-release tablets.

Embodiment 2

[0037] Ticagrelor Sustained Release Tablet System Formula Composition:

[0038]

[0039] The particle size of ticagrelor: 15 μm.

[0040] To prepare ticagrelor extended-release tablets:

[0041] Mix ticagrelor, lactose, and hypromellose first, add appropriate amount of water to granulate; fully dry the prepared granules at 50-60°C, and mix the sieved granules with magnesium stearate and micropowder silica gel Post-compression to make ticagrelor matrix sustained-release tablets.

Embodiment 3

[0043] Ticagrelor Sustained Release Tablet System Formula Composition:

[0044]

[0045] The particle size of ticagrelor: 5 μm.

[0046] To prepare ticagrelor extended-release tablets:

[0047] Mix ticagrelor, lactose, and hypromellose first, add appropriate amount of water to granulate; fully dry the prepared granules at 50-60°C, mix the sieved granules with magnesium stearate, and press into tablets , made of ticagrelor matrix sustained-release tablets.

[0048] With 900ml adding 1% sodium dodecyl sulfate (SDS) pH6.8 phosphate buffer saline as stripping medium, constant temperature is to 37 ℃, in the paddle method that 50 turns, embodiment 1 to embodiment 3 are measured, stripping Curve see attached figure 1 .

[0049] from figure 1 It shows that the ticagrelor sustained-release tablet of the present invention makes the drug continuously effective within 12-24 hours, and can release slowly under physiological conditions, so that the patient can take it once a day, an...

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Abstract

The invention provides a ticagrelor sustained-release tablet system and a preparation method of the ticagrelor sustained-release tablet system. The preparation method comprises the following steps of: firstly uniformly mixing 10-60% of ticagrelor, 5-60% of a filler and 5-60% of high molecular polymer in percentage by weight, adding a granulating solution to granulate; fully drying the obtained granules at a temperature of 50-60 DEG C, uniformly mixing the sieved granules with 0.25-10% of a lubricant and / or 0-10% of a flow aid, carrying out tabletting to obtain the ticagrelor matrix type sustained-release tablets, wherein the granulating solution is preferably water, an alcohol-water solution or absolute ethyl alcohol; the granule size of the ticagrelor is below 100 micrometers; and the content of the ticagrelor is 50-300mg in the preparation process. The ticagrelor matrix type sustained-release tablet system provided by the invention has the advantages that a patient can take the ticagrelor once a day to ensure that the drug dependence of the patient can be improved and the risk of myocardial infarction or apoplexy caused by acute thrombosis due to a dose of the ticagrelor missing of the patient is reduced.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a ticagrelor sustained-release tablet system and a preparation method thereof. Background technique [0002] Ticagrelor, also known as ticagrelor, is an oral anti-platelet aggregation drug developed by AstraZeneca. Ticagrelor was approved by the European Union in December 2010 for reducing the occurrence of thrombotic events in patients with acute coronary syndrome (ACS), and its trade name is Brilique in the European market. The drug was approved by the US FDA on July 20, 2011, and its trade name is Brilinta. Ticagrelor is a novel, selective anticoagulant and the first reversible binding P2Y12 adenosine diphosphate receptor (ADP) antagonist that can reversibly act on vascular smooth muscle cells (VSMC) The purine 2 receptor subtype P2Y12 on ADP has obvious inhibitory effect on platelet aggregation caused by ADP, and can effectively improve the symptoms of patients with acute coronary h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/519A61K47/38A61K47/34A61P7/02
Inventor 王泽人
Owner SHENZHEN HUALIKANG BIOLOGICAL MEDICINE
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