Pharmaceutical composition of ticagrelor and cilostazol, preparation method and application thereof

A technology of cilostazol and ticagrelor, applied in the field of medicine, can solve problems such as myocardial infarction, poor compliance, and inability to compensate for the risk of anticoagulation

Inactive Publication Date: 2015-11-25
北京创世晟源生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007]The half-life of ticagrelor is only about 7 hours, and it needs to be taken twice a day, which is a challenge for patients with poor compliance
After all, patients are unlikely to fully adhere to this dosing regimen, for example, it is estimated that about 20% of patients treated with clopidogrel do not fully adhere to the dosing regimen, and these patients are not likely to be fully adhered to when using ticagrelor Strictly follow the prescribed dose. For ticagrelor, which can be reversed quickly, the missed dose is likely to cause myocardial infarction and stroke soon. Even if ticagrelor is used in combination with aspirin, the half-life of aspirin is only 15- In 20 minutes, the effect of aspirin cannot make up for the risk of decreased anticoagulant effect caused by missed doses
When using ticagrelor, the potential risk of patients accidentally disobeying the dosing regimen is the biggest concern about the use of ticagrelor. In addition, the efficacy of ticagrelor may also exist if it is used for a long time and alone. Uncertainty

Method used

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  • Pharmaceutical composition of ticagrelor and cilostazol, preparation method and application thereof
  • Pharmaceutical composition of ticagrelor and cilostazol, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1. Combination tablet of ticagrelor and cilostazol and its preparation

[0039] prescription:

[0040] Ticagrelor 90g

[0041] Cilostazol 50g

[0042] Mannitol 160g

[0043] Calcium hydrogen phosphate 85g

[0044] Sodium carboxymethyl starch 18g

[0045] Appropriate amount of 2.5% hydroxypropyl cellulose aqueous solution

[0046] Magnesium Stearate 5g

[0047] Preparation method 1: Pass ticagrelor, cilostazol, mannitol, calcium hydrogen phosphate, and sodium carboxymethyl starch through a 100-mesh sieve respectively. After weighing according to the prescription amount, firstly mix ticagrelor and cilostazol uniformly to obtain A mixed powder, which is to be used, and in addition, sodium carboxymethyl starch and calcium hydrogen phosphate are mixed uniformly according to the method of equal addition, and then mixed with Mix mannitol evenly to obtain B mixed powder, then mix A mixed powder and B mixed powder evenly, add 2.5% hydroxypropyl cellulose aqueous sol...

Embodiment 2

[0049] Example 2. Combination tablet of ticagrelor and cilostazol and its preparation

[0050] prescription:

[0051] Ticagrelor 90g

[0052] Cilostazol 60g

[0053] Hydroxypropyl Methyl Cellulose (K 4M )380g

[0054] Mannitol 40g

[0055] Microcrystalline cellulose 30g

[0056] Appropriate amount of 80% ethanol aqueous solution

[0057] Sodium carboxymethyl starch 6g

[0058] Magnesium stearate 4g

[0059] Appropriate amount of 8% polyvinylpyrrolidone aqueous solution

[0060] Preparation method: Pass ticagrelor, cilostazol, hydroxypropyl methylcellulose, mannitol, microcrystalline cellulose, and sodium carboxymethyl starch through a 100-mesh sieve respectively. First mix ticagrelor, cilostazol, hydroxypropyl methylcellulose, mannitol, and microcrystalline cellulose evenly, then use 80% ethanol aqueous solution to make a soft material, pass through a 24-mesh sieve, and granulate at 60°C After drying, use a 20-mesh sieve to granulate to obtain granules, add sodium ca...

Embodiment 3

[0062] Example 3. Combination tablet of ticagrelor and cilostazol and its preparation

[0063] prescription:

[0064] Ticagrelor 90g

[0065] Cilostazol 80g

[0066] Mannitol 160g

[0067] Calcium hydrogen phosphate 85g

[0068] Sodium carboxymethyl starch 18g

[0069] Appropriate amount of 2.5% hydroxypropyl cellulose aqueous solution

[0070] Magnesium Stearate 5g

[0071] Preparation method: with embodiment 1. The mass ratio of ticagrelor to cilostazol is 1.125:1.

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PUM

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Abstract

The invention relates to a pharmaceutical composition of ticagrelor and cilostazol, a preparation method of the pharmaceutical composition, and application of the pharmaceutical composition in medicines. The pharmaceutical composition has the effect of inhibiting or reversing atherosclerosis lipid plaques of artery blood vessel, in particular the effect of inhibiting or reversing atherosclerosis lipid plaques of coronary artery or carotid artery. The composition is able to effectively solve the problem due to interregnum of pharmaceutical function caused by occasionally missing ticagrelor, as well as reduce the possible cardiovascular and cerebrovascular diseases; in addition, the gastrointestinal bleeding can be greatly reduced, and the effect is far more than the effect of the composition of ticagrelor and aspirin.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a therapeutic or preventive pharmaceutical composition, which contains ticagrelor and cilostazol, and is used for the prevention and treatment of heart, brain and blood vessel diseases, as well as its preparation method and its use in medicine application. Background technique [0002] Cardiovascular, cerebrovascular and vascular diseases are diseases with high morbidity, great harm, death, and high disability rate. Cardiovascular and cerebrovascular diseases are essentially vascular lesions, and the main cause of vascular lesions is atherosclerotic plaque in arteries And vascular abnormalities caused by atheromatous lipid plaques, which are the main causes of heart and cerebral ischemia and infarction; about the mechanism of atherosclerosis, there are lipid infiltration, smooth muscle hyperplasia, thrombosis, platelet aggregation and arterial intima injury and other theories, wh...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/519A61P9/10A61P9/00A61P7/02A61K31/4709
Inventor 张耿元王保红白东跃
Owner 北京创世晟源生物科技有限公司
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