Ticagrelor sustained-release preparation

A technology of ticagrelor and preparation, applied in the field of medicine, can solve problems such as poor compliance, myocardial infarction or stroke, and increase the risk of acute thrombosis in patients

Active Publication Date: 2014-01-22
BEIJING KANG LISHENG PHARMA TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This is a challenge for non-compliant patients
It has also been found in practice that about 20% of patients treated with clopidogrel did not follow the doctor's advice. These patients are even less likely to strictly follow the prescribed dose when using ticagrelor. Direct withdrawal of the drug is likely to increase the risk of acute thrombosis in patients. lead to heart attack or stroke

Method used

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  • Ticagrelor sustained-release preparation
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1: Preparation of Ticagrelor Sustained Release Tablets

[0022]

[0023] Preparation process: pass the main drug and auxiliary materials through a 100-mesh sieve. Mix the main drug in the immediate-release part and the auxiliary materials except magnesium stearate evenly, make soft material with 70% ethanol, granulate with 16 mesh, dry at 60°C, granulate with 16 mesh, and add magnesium stearate as the instant release part. Release part of the granules; mix the main drug in the slow-release part and the excipients except magnesium stearate evenly, make soft material with 70% ethanol, granulate with 16 mesh, dry at 50°C, granulate with 16 mesh, add stearin Magnesium sulfate was used as the sustained-release part granules; this bilayer sustained-release tablet of ticagrelor was prepared on a bilayer tablet press.

Embodiment 2

[0024] Example 2: Preparation of Ticagrelor Sustained Release Tablets

[0025]

[0026] Preparation process: pass the main drug and auxiliary materials through a 100-mesh sieve. Mix the main drug in the slow-release part and the excipients except magnesium stearate evenly, make soft material with 70% ethanol, granulate with 16 mesh, dry at 50°C, granulate with 16 mesh, add magnesium stearate and press into tablets As the sustained-release part; the hypromellose in the immediate-release part is made into a 5% aqueous solution, the main drug is added and suspended evenly, and the immediate-release part is wrapped on the sustained-release part by coating equipment.

Embodiment 3

[0027] Embodiment 3: Preparation of ticagrelor sustained-release capsules

[0028]

[0029] Preparation process: pass the main drug and auxiliary materials through a 100-mesh sieve. Mix the main drug in the quick-release part with lactose and microcrystalline cellulose evenly, make hypromellose into a 3% aqueous solution as a binder, and use extrusion spheronization equipment to prepare quick-release pellets; The main drug in the mixture is mixed evenly with hypromellose and microcrystalline cellulose, and 70% ethanol is used as a binder to prepare slow-release pellets with extrusion and spheronization equipment; the two kinds of pellets are respectively coated with film, and mixed Then pack into capsules.

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Abstract

The invention relates to a sustained-release preparation composed of ticagrelor, a pharmaceutically acceptable sustained-release material, and other pharmaceutically acceptable auxiliary materials. The sustained-release preparation has an immediate-release part and a sustained-release part. The preparation can be double-part tablets obtained by compression by using a double-part tabletting machine, or tablets with the sustained-release medicine as a tablet core and the immediate-release medicine as outer coating, or sustained-release capsules composed of the immediate-release part and the sustained-release part. With the sustained-release preparation provided by the invention, medicine effect is fast, and medicine effective concentration can be maintained for a long time. Therefore, an ideal treatment effect can be provided.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a sustained-release preparation of ticagrelor. Background technique [0002] Ticagrelor (Ticagrelor; previously used code: ADZ6140, ARC126532, also translated as ticagrelor), belongs to cyclopentyl triazolopyrimidine compounds, chemical name is (1S, 2S, 3R, 5S)-3-[ 7-[(1R,2S)-2-(3,4-difluorophenyl)cyclopropylamino]-5-(thiopropyl)-3H-[1,2,3]triazole[4,5- d] pyrimidin-3-yl]-5-(2-hydroxyethoxy)cyclopentane-1,2-diol, English chemical name: (1S, 2S, 3R, 5S)-3-(7-( (1R,2S)-2-(3,4-difluorophenyl)cyclopropylamino)-5-propylthio-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-5-(2 -hydroxyethoxy)cyclopentane-1,2-diol; molecular formula: C 23 h 28 f 2 N 6 o 4 S; molecular weight: 522.574; CAS registration number: 274693-27-5 is a new drug for the treatment of acute coronary syndrome (acute coronary syndrome, ACS) developed by British AstraZeneca pharmaceutical company (AstraZeneca). The drug was ap...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519A61K9/16A61K9/22A61K9/52A61K47/48A61K47/40A61P9/10
Inventor 程刚
Owner BEIJING KANG LISHENG PHARMA TECH DEV
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