Ticagrelor pharmaceutical composition and preparation method thereof

A technology of ticagrelor and its mixture, which is applied in the field of ticagrelor oral pharmaceutical composition and its preparation, and can solve the problems of increasing safety risks and degradation impurities

Active Publication Date: 2015-03-18
SICHUAN HAISCO PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] On the other hand, studies have shown that ticagrelor decreases steadily under hot and hu

Method used

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  • Ticagrelor pharmaceutical composition and preparation method thereof
  • Ticagrelor pharmaceutical composition and preparation method thereof
  • Ticagrelor pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0124] Preparation of ticagrelor crystal form A

[0125] Under stirring, dissolve 2g of ticagrelor in 3ml of N,N-dimethylformamide at 25-30°C, and then add dropwise to 30ml of methyl tert-butyl ether cooled to 0-10°C. Continue to stir and crystallize at this temperature for 2 hours, filter, wash the filter cake with n-hexane, then dry under reduced pressure at 40-45°C for 6 hours, and then dry under reduced pressure at 80-85°C to obtain ticagrelor crystal form A, 1.71g.

[0126] The measured X-ray powder diffraction pattern is shown in figure 1 , The measured value is shown in the following table (take the measured value corresponding to the diffraction peak with a relative intensity greater than 1%):

[0127]

Embodiment 2

[0129] Preparation of ticagrelor crystal form A

[0130] Under stirring, dissolve 2g of ticagrelor in 5ml of N,N-dimethylformamide at 20-25°C, then add to 30ml of n-heptane, lower the temperature to 5-10°C, and continue to stir and crystallize for 5 hours After filtering, the filter cake was washed with n-heptane, then dried under reduced pressure at 50-55°C for 5 hours, and then dried under reduced pressure at 70-75°C to obtain ticagrelor crystal form A, 1.65 g. The measured X-ray powder diffraction pattern and figure 1 similar.

Embodiment 3

[0132] Ticagrelor tablets and preparation method thereof

[0133] Composition of prescription:

[0134]

[0135] Preparation:

[0136] 1. Dry the microcrystalline cellulose, mannitol, sodium carboxymethyl starch and magnesium stearate in Table 3 above at about 85°C for 12 hours, and set aside.

[0137] 2. Add the sodium carboxymethyl starch and mannitol twice in equal amounts, mix for 10 minutes, and rotate at 10 rpm to obtain mixture (I).

[0138] 3. Mix ticagrelor crystal form A (D90 less than 100μm) with the above mixture (I) for 10 minutes at a speed of 10 revolutions per minute to obtain mixture (II).

[0139] 4. Mix the above mixture (II) and microcrystalline cellulose for 10 minutes at a speed of 10 revolutions per minute to obtain a mixture (III).

[0140] 5. Add magnesium stearate to the above mixture (III) and mix for 10 minutes at a speed of 10 rpm to obtain mixture (IV).

[0141] 6. Press the mixture (IV) into tablets, and control the tablet weight within ±5% of the average ta...

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Abstract

The invention relates to a tablet composition of anticoagulation medicament ticagrelor and a preparation method of the tablet composition. The tablet composition comprises ticagrelor, a filling agent, a disintegrating agent, a lubricating agent and/or an adhesive. The tablet composition is characterized in that a tablet is prepared by virtue of a direct compression method or a dry granulation compression method. The preparation method has the beneficial effects that the operation steps are simple, the controllability of process parameters is good, and the process repeatability is good; meanwhile, the crystal type transform and impurity increase which can be caused in damp and hot processes of ticagrelor are avoided; the prepared ticagrelor tablet has a similar in vitro dissolution behavior with a primarily researched preparation. Therefore, the ticagrelor tablet is stable and controllable in quality and good in treatment effect and safety.

Description

Technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and specifically relates to a ticagrelor oral pharmaceutical composition and a preparation method thereof. Background technique [0002] Ticagrelor, also known as ticagrelor, is chemically named (1S,2S,3R,5S)-3-[7-{[(1R,2S)-2-(3,4-difluorobenzene Yl)cyclopropyl]amino)-5-propylthio-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy) -1,2-Cyclopentanediol, the chemical structure is shown in formula I: [0003] [0004] Ticagrelor is a cyclopentyltriazolopyrimidine compound and is the first reversible P2Y12 platelet inhibitor. It is mainly used to reduce acute coronary syndrome (unstable angina, non-ST-segment myocardial infarction, ST-segment myocardial infarction) The incidence of thrombotic cardiovascular events in patients; it can also be used to reduce cardiovascular death, myocardial infarction and ischemic stroke in patients (>50 years of age) diagnosed with peripher...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/28A61K9/36A61K31/519A61P7/02
Inventor 向志祥黄智龙江智勇周仕川何夏凯罗杰李方群程睿钱春霞李学超袁道义郑伟
Owner SICHUAN HAISCO PHARMA CO LTD
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