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Slow/controlled-release preparation of ticagrelor

A technology of ticagrelor and controlled-release preparations, applied in the field of medicine, can solve the problems of increased risk of myocardial infarction, decrease, and low degree of inhibition, and achieve the effects of reducing peak and valley fluctuations, reducing adverse reactions, and simple production equipment

Inactive Publication Date: 2014-06-18
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, clopidogrel also has some disadvantages: slow onset of action; low degree of inhibition, large individual differences in patient response; irreversible blocking effect on ADP receptor
The half-life of ticagrelor is 12 hours, and it needs to be taken twice a day, which is not suitable for those patients with poor compliance. If the medicine cannot be taken on time according to the doctor's advice, the trough concentration level of platelet inhibition will decrease, and the degree of platelet inhibition will decrease. also weakened
Kleiman and Berger believe that ticagrelor is more suitable for CABG patients, and it is not ideal for patients who need to take anticoagulant drugs for a long time, because immediate withdrawal of the drug may increase the risk of myocardial infarction and stroke

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Preparation of ticagrelor tablets

[0021] 1000 pieces

[0022] Ticagrelor 90g microcrystalline cellulose 100g lactose 60g Sodium carboxymethyl starch 20g Magnesium stearate 8g 5%PVP80% ethanol solution Appropriate amount

[0023] Preparation process: Mix ticagrelor, microcrystalline cellulose, lactose, and sodium carboxymethyl starch in equal amounts, add an appropriate amount of binder to prepare soft materials, pass through a 20-mesh sieve and granulate, dry at 50°C, and granulate , adding magnesium stearate, mixing evenly, and pressing into tablets.

[0024] According to the dissolution test method, use 150ml of hydrochloric acid solution (0.9-1000) as the solvent, and the rotation speed is 75 revolutions per minute. Operate according to the law. The same temperature, the same volume of dissolution medium, filter, add dissolution medium to make a solution containing about 0.3mg per 1ml as the test solution, r...

Embodiment 2

[0027] Preparation of Ticagrelor Sustained Release Tablets

[0028]1000 pieces

[0029] Ticagrelor 90g microcrystalline cellulose 100g lactose 60g Sodium carboxymethyl starch 20g Magnesium stearate 8g 5%PVP80% ethanol solution Appropriate amount

[0030] Preparation process: Mix ticagrelor, hydroxypropyl methylcellulose, and lactose in equal amounts, add an appropriate amount of binder to prepare soft materials, pass through a 20-mesh sieve and granulate, dry at 50°C, granulate, add hard Magnesium fatty acid, mixed evenly, compressed into tablets. The prepared ticagrelor sustained-release tablets have obvious sustained-release properties.

[0031] Determination of release rate of sustained-release tablets:

[0032] According to the dissolution test method, use 150ml of hydrochloric acid solution (0.9-1000) as the solvent, and the speed is 75 revolutions per minute. Operate according to the law. Take an appropriate amount of the ...

Embodiment 3

[0034] Preparation of Ticagrelor Sustained Release Coated Tablets

[0035] 1000 pieces

[0036] Ticagrelor 90g lactose 60g Low-substituted hydroxypropyl cellulose 6g Magnesium stearate 6g Isolation layer coating material Appropriate amount 10% hydroxypropyl methylcellulose solution or ethanol water solution Appropriate amount Sustained release layer coating material Appropriate amount 10% acrylic resin isopropanol-acetone solution 1 Appropriate amount

[0037] Preparation process: prepare soft material by adding ticagrelor, lactose, low-substituted hydroxypropyl cellulose and appropriate amount of wetting agent, granulate, dry, sort through a 16-mesh sieve, add magnesium stearate, mix evenly, and compress into tablets. Coat the material with the isolation layer, dry, and coat with the slow-release coating solution to achieve different slow-release rates.

[0038] Determination of release rate of sustained-release ta...

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PUM

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Abstract

The invention provides a slow / controlled-release preparation of ticagrelor. The slow / controlled-release preparation of ticagrelor is an oral drug. The slow / controlled-release preparation contains ticagrelor or its pharmaceutically acceptable salt. A mass percent of ticagrelor to controlled-release accessory materials is in a range of 1: 0.2 to 1: 20 and preferably, the mass percent is in a range of 1: 0.1 to 1: 10, and a proper amount of other accessory materials are used. The slow / controlled-release base comprises one or more of cellulose, cellulose derivatives, alginate, starch, starch derivatives, polypropylene resins, carboxyvinyl polymers and other controlled-release accessory materials. Compared with a fast-release preparation, the slow / controlled-release preparation of ticagrelor provides a ticagrelor slow / controlled-release preparation system, can be eaten by a patient once each day, can change drug compliance of patients, can reduce the risk of myocardial infarction or stroke caused by acute thrombosis caused by missing of ticagrelor, and provides the easily-prepared slow / controlled-release preparation of ticagrelor or its pharmaceutically acceptable salt.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a sustained and controlled release preparation system of a novel anticoagulant drug ticagrelor. Background technique [0002] Ticagrelor (Brilinta) is a new type of small molecule anticoagulant drug developed by AstraZeneca. It was approved by the European Union in December 2010 and approved by the US FDA in July 2011. Clinical trials have confirmed that this drug, unlike thienopyridine anticoagulant drugs clopidogrel and prasugrel, can reversibly act on the adenosine diphosphate (ADP) receptor subtype P2Y12, and has a significant effect on ADP-induced platelet aggregation. Inhibitory effect, and rapid onset of oral administration, can effectively improve the symptoms of patients with acute coronary syndrome (ACS), especially for patients who need coronary artery bypass grafting (CABG). [0003] Platelets play an important role in the process of arterial thrombosis and atherosclerosis. I...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K9/52A61K31/519A61P7/02
Inventor 严洁李轩
Owner TIANJIN HANKANG PHARMA BIOTECH
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