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Slow-release preparation of ticagrelor

A slow-release preparation, the technology of ticagrelor, is used in medical preparations containing active ingredients, pill delivery, cardiovascular system diseases, etc., which can solve problems such as waste and achieve the effect of avoiding waste.

Inactive Publication Date: 2018-06-29
JIANGSU HENGRUI MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For these patients, it is necessary to purchase immediate-release preparations and sustained-release preparations at the same time, but the immediate-release preparations can only be used once, which will cause a lot of waste

Method used

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  • Slow-release preparation of ticagrelor
  • Slow-release preparation of ticagrelor
  • Slow-release preparation of ticagrelor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Premix ticagrelor with the materials in the prescription, add binders for wet granulation, add magnesium stearate to mix the granules evenly, and then compress and coat the granules to prepare immediate-release tablet cores; according to the prescription information, The immediate-release tablet core is coated with sustained-release material, enteric-coated material and drug-containing layer in turn, and dried. The release of the prepared formulations was evaluated.

[0043]

[0044]

[0045] The chromatographic conditions for the determination of the release rate are: use octadecylsilane bonded silica gel as the chromatographic column filler, use 10ml of phosphate buffer [take 1.0mol / L sodium dihydrogen phosphate solution (adjust the pH value to 3.0 with phosphoric acid), Add water to 480ml, shake well]-acetonitrile (48:52) as mobile phase; column temperature is 55°C; detection wavelength is 242nm. The tailing factor of the ticagrelor peak should not be greater ...

Embodiment 2

[0047] The tablets of prescription 3 and prescription 5 in the embodiment are cut according to the form of 1:1 and 1:3, that is, split into 1 / 2 and 1 / 4. Put all parts of the cut tablet into the dissolution cup, and investigate the dissolution behavior in the dissolution medium of 0.1NHCL with 0.2% Tween 80 at the same time as the commercially available 2 tablets of Belinda, and the dissolution curve figure 2 with image 3 .

[0048] According to the above data, it is shown that the ticagrelor film-controlled sustained-release tablet of the present invention can achieve a certain release in the early stage and a stable release in the later stage in the completed state. The tablet of the present invention has an in vitro dissolution behavior similar to that of the original commercially available immediate-release tablet after cutting and breaking the coating film at different ratios. Therefore, the preparation of the present invention can not only meet the requirement of once...

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Abstract

The invention relates to a slow-release preparation of ticagrelor. Specifically, the slow-release preparation of the ticagrelor, provided by the invention, is suitable for being orally taken one timeevery day; meanwhile, a rapid drug releasing effect can be realized after tablets are damaged. The releasing tablets which are administrated one time every day can reduce the number of times of oral administration, so that the oral drug taking compliance of patients can be improved and risks that myocardial infarction or stroke is caused when acute thrombus formation is caused by the fact that thepatients forget to orally take the ticagrelor are reduced; meanwhile, when the tablets provided by the invention are orally taken for the first time, the tablets can be opened to meet the requirementof giving a load dosage to the patients, so as to rapidly take effect.

Description

technical field [0001] The invention relates to a sustained-release preparation of ticagrelor, which is suitable for oral administration once a day and can achieve the effect of rapid drug release after the tablet is broken. 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 even...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519A61K9/22A61P9/10
CPCA61K9/2059A61K9/209A61K31/519
Inventor 陈昊卢韵潘晓晨张强
Owner JIANGSU HENGRUI MEDICINE CO LTD
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