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Formulation of ticagrelor or pharmaceutically acceptable salt thereof

A technology for ticagrelor and preparations, which is applied in the field of preparations of ticagrelor or its pharmaceutically acceptable salts, can solve the problems of no conformational change and signal transmission, and achieve good reproducibility, good stability, and industrialization high effect

Inactive Publication Date: 2020-08-18
JIANGSU HENGRUI MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the difference is that the interaction between ticagrelor and the platelet P2Y12 ADP receptor is reversible, without conformational changes and signal transmission, and the platelet function in the blood also recovers rapidly after drug withdrawal

Method used

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  • Formulation of ticagrelor or pharmaceutically acceptable salt thereof
  • Formulation of ticagrelor or pharmaceutically acceptable salt thereof
  • Formulation of ticagrelor or pharmaceutically acceptable salt thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0082] Polyoxyethylene, sodium alginate, and Kollidon SR were used as skeleton materials to prepare sustained-release tablets, and hypromellose in CN1102657629A was used to prepare ticagrelor sustained-release tablets for comparative study, and the release rate was evaluated.

[0083] Element Prescription 1 Prescription 2 Prescription 3 Prescription 4 Prescription 5 Prescription 6 Prescription 7 Ticagrelor 180mg 180mg 180mg 180mg 180mg 180mg 180mg PEO N80 100mg - - - - - - PEO N10 - 50mg - - - - Kollidon SR - - 50mg - - - - sodium alginate - - - 50mg - - - HPMC K4M - - - - 100mg - - HPMC K100LV - - - - - 100mg 150mg lactose 100mg 100mg 100mg 100mg 100mg 100mg 100mg microcrystalline cellulose 165mg 165mg 165mg 165mg 165mg 115mg 115mg Magnesium stearate 5mg 5mg 5mg 5mg 5mg 5mg 5mg

[0084] Ticagrelor...

Embodiment 2

[0091] Considering that ticagrelor is almost insoluble in water, and there is a phenomenon of incomplete dissolution in the later stage when it is directly mixed with sustained-release materials, in order to make the release rate in vitro more controllable and meet the requirements for later release, the present invention proposes "immediate release first and then The design idea of ​​"sustained release" is that firstly, the solid dispersion technology is used to increase the release rate of the raw material, so that the raw material can be released quickly; then the solid dispersion is mixed with the sustained release material, and compressed into tablets to prepare ticagrelor sustained release tablets.

[0092] Using povidone and copovidone as carriers respectively, the solid dispersion was prepared by solvent method, and the prepared solid dispersion was uniformly mixed with polyoxyethylene, microcrystalline cellulose, and magnesium stearate, and pressed into tablets to prepa...

Embodiment 3

[0101] The solid dispersion of ticagrelor was mixed with sodium alginate, Kollidon SR, and polyoxyethylene as sustained-release matrix materials to prepare sustained-release formulation compositions, and the release behavior of the formulations was investigated.

[0102] Element Prescription 14 Prescription 15 Prescription 16 Prescription 17 Prescription 18 Prescription 19 Prescription 20 Prescription 21 Ticagrelor 180mg 180mg 180mg 180mg 180mg 180mg 180mg 180mg Copovidone 180mg 180mg 180mg 180mg 180mg 180mg 180mg 180mg PEO N80 - - 75mg 75mg 150mg 112.5mg - PEO 205 - - - - - - - 100mg PEO N60K - - - - - - - 50mg Kollidon SR 75mg 150mg - 75mg 112.5mg 112.5mg - 112.5mg sodium alginate - - 150mg - 150mg - lactose 75mg - - - - - - - microcrystalline cellulose 233.5 mg 233.5 mg 233.5 mg 233.5 mg 196.0mg 121...

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Abstract

The invention relates to a formulation of ticagrelor or a pharmaceutically acceptable salt thereof. In particular, the present invention relates to an improved formulation of ticagrelor, or a pharmaceutically acceptable salt thereof, administered once a day. The present invention can achieve a plasma concentration of ticagrelor of greater than about 0.2 [mu] g / mL within 2 hours in a subject; and aplasma concentration of ticagrelor of greater than about 0.2 [mu] g / mL can still be achieved after administration in a subject for 12 hours; and generating a maximum plasma concentration (Cmax) of ticagrelor or a pharmaceutically acceptable salt thereof between about 0.2 [mu] g / mL and about 0.8 [mu] g / mL in the subject. According to the preparation of the ticagrelor or the medicinal salt thereof,the administration frequency can be reduced, so that the administration compliance of a patient can be improved, and the risk of myocardial infarction or stroke caused by acute thrombosis due to missing administration of the ticagrelor by the patient is reduced.

Description

[0001] This application is a divisional application of a Chinese patent application with the application number 201610278846.0, the application date is April 28, 2016, and the invention title is "a preparation of ticagrelor or its pharmaceutically acceptable salt". technical field [0002] The invention relates to a preparation of ticagrelor or a pharmaceutically acceptable salt thereof, which is suitable for oral administration once a day. Background technique [0003] Ticagrelor, a platelet aggregation inhibitor, is a novel cyclopentyltriazole pyrimidine (CPTP) oral antiplatelet drug. Chemical name: 1S,2S,3R,5S)-3-[7-{[(1R,2S)-2-(3,4-difluorobenzene)cyclopropyl]amino}-5-(propylthio )-3H-[1,2,3]-triazolo[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy)cyclopentane-1,2-diol, Molecular formula is C 23 h 28 f 2 N 6 o 4 S, the structural formula is as follows: [0004] [0005] This product is used for patients with acute coronary syndrome (unstable angina, non-ST-segment el...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/24A61K9/22A61K9/52A61K31/519A61K47/02A61K47/10A61K47/26A61K47/32A61K47/36A61K47/38A61P9/10
CPCA61K9/2027A61K9/2054A61K9/2086A61K31/519A61K47/32A61K47/10A61K47/38A61K47/26A61K47/02A61K47/36A61K9/2031A61K9/2059A61K9/4808A61P9/10A61K9/205
Inventor 陈昊潘晓晨卢韵
Owner JIANGSU HENGRUI MEDICINE CO LTD
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