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Pharmaceutical composition containing clopidogrel and carbazochrome sodium sulfonate

A technology of clopidogrel and sodium carboxylate, which is applied in the directions of drug combinations, medical preparations containing active ingredients, pharmaceutical formulations, etc., can solve the problems of rebound of cardiovascular events, reduction of patient compliance, increased bleeding risk, and the like, Achieve good synergistic efficacy, reduce bleeding risk, and inhibit platelet aggregation.

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] However, while clopidogrel has been widely used clinically and achieved good curative effect, its adverse reactions of bleeding have also attracted increasing attention. International experts have reached a consensus that "the more effective the antiplatelet agent is, the easier it is to cause bleeding". Contradictory, clopidogrel has strong anticoagulant activity, is effective in inhibiting platelet aggregation, and acts quickly, but it inevitably leads to an increased risk of bleeding
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 and carbazochrome sodium sulfonate
  • Pharmaceutical composition containing clopidogrel and carbazochrome sodium sulfonate
  • Pharmaceutical composition containing clopidogrel and carbazochrome sodium sulfonate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Embodiment 1 common tablet

[0013] Sodium carbosulfonate 15g

[0014] Clopidogrel Bisulfate 75g

[0015] Microcrystalline Cellulose 250g

[0016] Lactose 20g

[0017] 10% starch slurry appropriate amount

[0018] Magnesium stearate 0.8g

[0019] Preparation process: Weigh the prescription amount of sodium carbosulfate, 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] Sodium carbosulfate 75g

[0022] Clopidogrel Hydrochloride 15g

[0023] Starch 140g

[0024] Dextrin 20g

[0025] 50% ethanol appropriate amount

[0026] Magnesium Stearate 1.0g

[0027] Preparation process: Weigh the prescription amount of sodium carbosulfonate, clopidogrel hydrochloride, starch and dextrin and mix evenly. In addition, add an appropriate amount of 50% ethanol 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 3

[0028] Embodiment 3 Dispersible tablets

[0029] Sodium carbosulfonate 50g

[0030] Clopidogrel 2.5g

[0031] Croscarmellose Sodium 10g

[0032] Microcrystalline Cellulose 150g

[0033] Polyvinylpyrrolidone 5.5g

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

[0035] Micronized silica gel 5g

[0036] Preparation process: Weigh carbosulfonate sodium and clopidogrel according to the prescription, use microcrystalline cellulose as filler, cross-linked carmellose 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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PUM

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Abstract

The invention provides a pharmaceutical composition containing active carbazochrome sodium sulfonate and clopidogrel or the pharmacologically acceptable salt thereof. The invention aims to invent a more effective and low adverse-reaction method for curing thrombotic diseases by using the combined medication of the carbazochrome sodium sulfonate and the clopidogrel. After conscientious trail of the patent applicant for many times, the effect of applying the carbazochrome sodium sulfonate to inhibit the thrombosis in a combined manner is discovered unexpected in the process of applying the clopidogrel to cure the thrombotic diseases, the anticoagulant effect of the clopidogrel is not abated but increased, and the very good synergistic effects are achieved after the combination of the carbazochrome sodium sulfonate and the clopidogrel, 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 caused by the clopidogrel is greatly reduced and the compliance of patients is enhanced.

Description

technical field [0001] The invention belongs to a new pharmaceutical composition, in particular to a pharmaceutical composition containing clopidogrel or a pharmacologically acceptable salt thereof and sodium carbosulfonate as active components. Background technique [0002] Sodium carbosulfonate (Xinanluoxue) is a new generation of hemostatic drug. It is a derivative of Anluoxue. The sodium sulfonate group is introduced into the molecular structure to overcome the low solubility of Anluoxue, which must be assisted by salicylic acid. The disadvantage of dissolving, thus avoiding the salicylic acid reaction that may occur after long-term repeated application. Compared with Anluoxue (adrenochrome hydrazone), sodium carbosulfonate has high water solubility, multiple routes of administration (oral, intramuscular or intravenous injection, intravenous infusion, endoscopic spraying, etc.), and has a fast hemostatic effect. Less adverse reactions, wide range of application, etc., s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/404A61K31/4365A61P7/02A61P9/00
Inventor 赵志全
Owner LUNAN PHARMA GROUP CORPORATION
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