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Ticagrelor slow-release preparation as well as preparation and application thereof

A technology for ticagrelor and sustained-release preparations, which is applied in the field of ticagrelor sustained-release preparations, can solve the problems of increased preparation cost, low peak blood drug concentration, prone to wrong administration, etc. Good stability, increase the effect of slow release effect

Inactive Publication Date: 2019-05-28
梁江丽
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The existing Chinese patent document CN108210498 discloses a sustained-release preparation of ticagrelor, comprising an immediate-release layer, a sustained-release coating layer, an enteric coating layer and a drug-containing layer, and the weight of ticagrelor per unit is 160 mg -220mg, take it directly when the sustained-release effect is needed, and cut or split it to take if the immediate-release effect is needed, so that patients who need to take the immediate-release tablet can only buy one kind of sustained-release tablet to avoid waste. However, this method increases The overall preparation cost, and the peak blood concentration is low, it is easy to take the wrong dose, resulting in adverse consequences

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] This example provides a specific implementation of the ticagrelor sustained-release preparation, specifically as follows:

[0030] Take 18g of ticagrelor crude drug, pulverize to 200 mesh, 13.5g of which are used for sustained release layer and 4.5g are used for immediate release layer; 13.5g of ticagrelor and 8.8g of ethyl cellulose are dissolved in 100ml of ethyl acetate To form an oil phase, dissolve 0.2g sodium lauryl sulfate in 200ml of ethyl acetate aqueous solution with a volume fraction of 10% to form a water phase, and slowly drop the oil phase into the water phase under ultrasonic power of 800W, and then add 200ml of water, precipitated 100μm sustained-release microspheres, washed 3 times with pure water, and dried at 40°C to constant weight; 5g aspirin and the ticagrelor sustained-release microspheres, 3.5g chitosan, 2g talc powder, 1g mannitol, 1g sodium carboxymethylcellulose, and 0.005g butylated hydroxyanisole are mixed, and compressed to make 100 sustain...

Embodiment 2

[0034] This example provides a specific implementation of the ticagrelor sustained-release preparation, specifically as follows:

[0035] Take 18g of ticagrelor crude drug and crush it to 200 meshes, 15g of which is used for the slow-release layer and 3g for the immediate-release layer; 15g of ticagrelor and 8.8g of ethyl cellulose are dissolved in 100ml of ethyl acetate to form an oil phase , 0.2g of sodium lauryl sulfate is dissolved in 200ml of ethyl acetate aqueous solution with a volume fraction of 10% to form a water phase, and the oil phase is slowly dropped into the water phase under ultrasonic power of 600W, and then 200ml of water is added, The 200 μm sustained-release microspheres were precipitated, washed 5 times with pure water, and dried at 60° C. to constant weight; 5 g of aspirin and the ticagrelor sustained-release microspheres, 3.5 g of chitosan, 2 g of talcum powder, and 1 g Mannitol, 1g sodium carboxymethylcellulose, and 0.01g butylated hydroxyanisole are m...

Embodiment 3

[0039] This example provides a specific implementation of the ticagrelor sustained-release preparation, specifically as follows:

[0040] Take 24g of ticagrelor crude drug and crush it to 300 meshes, 21g of which is used for the slow-release layer and 3g for the immediate-release layer; 21g of ticagrelor and 8.8g of ethyl cellulose are dissolved in 100ml of ethyl acetate to form an oil phase , 0.2g of sodium lauryl sulfate is dissolved in 200ml of ethyl acetate aqueous solution with a volume fraction of 10% to form a water phase, and the oil phase is slowly dropped into the water phase under ultrasonic power of 800W, and then 300ml of water is added, The slow-release microspheres with a particle size of 150 μm were precipitated, washed 4 times with pure water, and dried at 50° C. to constant weight; 10 g of aspirin and the ticagrelor slow-release microspheres, 3.5 g of chitosan, and 2 g Talcum powder, 1g mannitol, 1g sodium carboxymethylcellulose, and 0.008g butylated hydroxya...

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PUM

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Abstract

The invention belongs to the technical field of ticagrelor and in particular relates to a ticagrelor slow-release preparation as well as preparation and application thereof. The ticagrelor slow-release preparation provided by the invention comprises at least one rapid release layer and at least one slow release layer, wherein each of the rapid release layer and the slow release layer contains theticagrelor; the mass ratio of the content of the ticagrelor in the rapid release layer to the content of the ticagrelor in the slow release layer is 1 to (3 to 7); the ticagrelor slow-release preparation is used as a medicine for anti-platelet treatment; on one hand, the preparation has reasonable plasma drug peak concentration; on the other hand, the residual ticagrelor is slowly released and stable plasma drug concentration is maintained; the anti-platelet treatment effect is good and the bleeding tendency is reduced; the preparation is orally taken once each day and has good patient compliance and high utilization safety; the preparation method of the ticagrelor slow-release preparation has the advantages of simple technology, relatively low cost and good practicability.

Description

technical field [0001] The invention belongs to the technical field of ticagrelor, in particular to a sustained-release preparation of ticagrelor and its preparation and application. Background technique [0002] With the acceleration of the aging process of the population, the incidence of cardiovascular diseases has increased rapidly, and anti-platelet aggregation is an important part of the treatment of cardiovascular and cerebrovascular diseases. Ticagrelor is a platelet aggregation inhibitor, and its clinical efficacy and safety have been verified and supported by the Platelet Inhibition and Patient Outcome Study (PLATO Study) and its multiple subgroup studies. The PLATO study also showed that the curative effect of ticagrelor was significantly better than that of clopidogrel, so it was listed as the first-line recommendation by many domestic and foreign guidelines, and the European guidelines even listed the recommended level of ticagrelor above clopidogrel in the past...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519A61K31/616A61K9/36A61K47/10A61P7/02
Inventor 梁亭梁江丽罗强李军刘宇
Owner 梁江丽
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