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Pharmaceutical composition containing clopidogrel

A clopidogrel and composition technology, applied in the directions of drug combinations, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problems of increased bleeding risk, rebound of cardiovascular events, easy to cause bleeding, etc., and achieve the bleeding rate Reduce, enhance anticoagulant activity, inhibit platelet aggregation effect

Active Publication Date: 2009-10-14
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] International experts have reached a consensus that "the more effective the antiplatelet preparation is, the more likely it is to cause bleeding". At the same time, this is also a contradiction in clinical treatment. Clopidogrel has strong anticoagulant activity, effective inhibition of platelet aggregation, and rapid action, but it inevitably leads to the risk of bleeding sex increase
If the drug induces an increased risk of bleeding, even if the bleeding is not severe, it will significantly reduce the patient's compliance. The risk of reduced compliance is important in antiplatelet agents, which may lead to rebound cardiovascular events

Method used

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  • Pharmaceutical composition containing clopidogrel
  • Pharmaceutical composition containing clopidogrel
  • Pharmaceutical composition containing clopidogrel

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Embodiment 1 common tablet

[0013] Proanthocyanidins 25g

[0014] Clopidogrel Bisulfate 25g

[0015] Microcrystalline Cellulose 250g

[0016] Lactose 20g

[0017] 10% starch slurry appropriate amount

[0018] Magnesium Stearate 1.5g

[0019] Preparation process: Weigh the prescribed amount of proanthocyanidins, clopidogrel bisulfate, microcrystalline cellulose, and lactose and mix evenly. In addition, add an appropriate amount of 10% starch slurry to the mixed powder, mix evenly, make soft material, pass through a 18-mesh nylon sieve to make wet granules, and dry at about 60°C. The moisture content of the dry granules should be controlled below 1.5%. Sieve through a 20-mesh sieve, mix with magnesium stearate, and press into tablets.

Embodiment 2

[0020] Embodiment 2 common tablet

[0021] Catechin 5g

[0022] Clopidogrel Hydrochloride 25g

[0023] Starch 400g

[0024] Dextrin 20g

[0025] 50% ethanol appropriate amount

[0026] Magnesium Stearate 2.0g

[0027] Preparation process: Weigh the prescribed amount of catechin, clopidogrel hydrochloride, starch, and dextrin and mix evenly. In addition, an appropriate amount of 50% ethanol is added to the mixed powder, mixed evenly, made into soft material, passed through a 18-mesh nylon sieve to make wet granules, and dried at about 60°C. The moisture content of the dry granules should be controlled below 1.5%. Sieve through a 20-mesh sieve, mix with magnesium stearate, and press into tablets.

Embodiment 3

[0028] Embodiment 3 Dispersible tablets

[0029] Epicatechin 600g

[0030] Clopidogrel 15g

[0031] Croscarmellose Sodium 10g

[0032]Microcrystalline Cellulose 500g

[0033] Polyvinylpyrrolidone 50g

[0034] 5% PVP 60% ethanol solution appropriate amount

[0035] Micronized silica gel 5g

[0036] Preparation process: Weigh epicatechin and clopidogrel according to the prescription, use microcrystalline cellulose as filler, croscarmellose sodium and polyvinylpyrrolidone as disintegrants, 5% PVP 60% ethanol solution It is used as binder, and micronized silica gel is used as flow aid. It is granulated in one step in a fluidized bed, and then compressed into tablets.

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Abstract

The invention provides a pharmaceutical composition containing active procyanidins and clopidogrel or the pharmacologically acceptable salt thereof. The procyanidins and the clopidogrel are used in a combined manner, a more effective method for curing thrombotic diseases is found, after trail for many times, the clopidogrel and the procyanidins (an extract of traditional Chinese medicine) are creatively and effectively combined together, the effect of applying the procyanidins to inhibit the thrombosis in a combined manner is discovered unexpected in the process of applying the clopidogrel to cure the thrombotic diseases, and not only the anticoagulant effect of the clopidogrel is free from the influence of the procyanidins, but also a good effect is achieved in the aspect of reducing the adverse reaction of bleeding after the use of the clopidogrel and the procyanidins in a combined manner, therefore, the risk of bleeding is greatly reduced when the advantages of good anticoagulant activity and fast effect of the clopidogrel during the antiplatelet aggregation are fully exerted, the risk of bleeding of the clopidogrel during the antiplatelet aggregation is effectively reduced and the adverse reaction of the clopidogrel is greatly reduced.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a pharmaceutical composition containing proanthocyanidins and clopidogrel or a pharmacologically acceptable salt thereof as active ingredients. Background technique [0002] Anthocyanin (anthocyanin) belongs to flavonoids in phenolic compounds, is a kind of water-soluble pigment, and is a kind of main coloring substance widely present in plants, which can change color with the acidity and alkalinity of cell fluid (cell fluid If it is acidic, it will be reddish, and if the cell fluid is alkaline, it will be blue), and it is mostly found in plants such as grapes, apples, sorghum and cherries, among which grapes (seeds and skins) are the most abundant. Anthocyanin is one of the main pigments that constitute the color of petals and fruits. It is composed of different amounts of catechin or epicatechin. Free anthocyanins are extremely rare under natural conditions. Proant...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4365A61K31/352A61P7/02
Inventor 赵志全程国良
Owner LUNAN PHARMA GROUP CORPORATION
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