Preparation of ticagrelor or pharmaceutical salt thereof

A technology for ticagrelor and preparations, which is applied in the directions of non-active ingredient medical preparations, medical preparations containing active ingredients, and pill delivery, etc., can solve problems such as no conformational change and signal transmission, and achieve good reproducibility , High degree of industrialization, good stability

Active Publication Date: 2016-11-09
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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  • Preparation of ticagrelor or pharmaceutical salt thereof
  • Preparation of ticagrelor or pharmaceutical salt thereof
  • Preparation of ticagrelor or pharmaceutical salt thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0081] 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.

[0082] 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

...

Embodiment 2

[0090] 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.

[0091] 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

[0100] 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.

[0101] 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

-

15...

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Abstract

The invention relates to a preparation of ticagrelor or a pharmaceutical salt thereof. Specifically, the invention relates to the improved preparation of ticagrelor or the pharmaceutical salt thereof for administration for once daily. The ticagrelor plasma concentration of a tested person can reach about more than 0.2 [mu]g / mL within 2 hours; the ticagrelor plasma concentration of the tested person can still reach about more than 0.2 [mu]g / mL 12 hours later after the drug is taken; and the maximum plasma concentration (Cmax) of the ticagrelor or the pharmaceutical salt thereof between about 0.2 [mu]g / mL-about 0.8 [mu]g / mL is generated in the tested person. The preparation of ticagrelor or the pharmaceutical salt thereof can make the administration times reduced, thereby improving the administration compliance of patients, reducing the risks of myocardial infarction or stroke caused by acute thrombosis caused because the patients miss taking ticagrelor.

Description

technical field [0001] 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 [0002] 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: [0003] [0004] This product is used for patients with acute coronary syndrome (unstable angina, non-ST-segment elevation myocardial infarction or ST-segment elevation myocardial infarction), including patients receiving drug therapy and percutaneous coronary intervention (PCI), to reduce Incidence of thrombotic cardiovascular events. Compared with clopidogrel, this product can...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/519A61P9/10A61P7/02
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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