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Coposition containing chlopidogrel and antithrombotic agent active component

Technology of an active ingredient, clopidogrel, in the field of compositions containing active ingredients of clopidogrel and an antithrombotic agent

Inactive Publication Date: 2003-07-30
SANOFI AVENTIS SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The results obtained predict the therapeutic importance of the combination of ticlopidine and aspirin in some types of acute thrombosis, especially after surgery, but are not sufficient to draw conclusions from them on the role of atherosclerosis. Indication of secondary prophylaxis against disease or endarterectomy or vascular accidental injury with metallic endarterectomy

Method used

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Experimental program
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Embodiment Construction

[0036] The combination of active ingredients according to the invention is the subject of pharmaceutical research. As mentioned above, studies were conducted on experiments for agglutination of rabbit platelets with collagen (Born et al., J. Physiol., 1963, 168, 178-95). Briefly, 2.5-3 kg of New Zealand rabbits were treated for 3 days with ticlopidine (100 mg / kg / day) by the oral route or with clopidogrel (10 mg / kg) by the intravenous route. One hour after the last dose, animals were treated with aspirin (1 mg / kg) by intravenous route.

[0037] Five minutes after aspirin administration, the animal was anesthetized with ether, and a 2 ml blood sample was taken from the middle ear artery and mixed with 0.2 ml of 3.8% sodium citrate aqueous solution. Blood samples were centrifuged at 500g for 10 minutes at 15°C to obtain platelet-rich plasma. The number of platelets was then adjusted to 106 cells / [mu]l with the aid of platelet-depleted plasma obtained by centrifugation of antico...

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PUM

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Abstract

The invention relates to a pharmaceutical composition containing an association of active principles, wherein the active principles are clopidogrel and aspirin, said two constituents being present in a free form or in the form of a pharmaceutically acceptable salt.

Description

field of invention [0001] The subject of the present invention is a new combination of active ingredients consisting of clopidogrel and aspirin with antiplatelet aggregation activity, as well as pharmaceutical compositions containing them. [0002] The active ingredient constituting the composition exists in its free state or in the form of a pharmaceutically acceptable salt. Background of the invention [0003] Over the past decade, research on the role of platelets in the progression of atherosclerosis-related diseases (myocardial infarction, angina, brain attacks, peripheral arterial disease, etc.) interest of. The demonstrated role of platelets in arterial thrombosis led to the development of several drugs that inhibit these functions of platelets, while the discovery that ADP played a fundamental role in the thrombosis process led to the development of ticlopidine, a potent Potential antithrombotic drugs. Such thieno[3,2-c]pyridine derivatives are disclosed in patent...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/435A61K31/00A61K31/4353A61K31/4365A61K31/60A61K31/612A61K31/616A61P5/36A61P5/44A61P7/00A61P7/02
CPCA61K31/621A61K31/60A61P25/00A61P5/36A61P5/44A61P7/00A61P7/02A61P9/00A61P9/10A61K31/435A61K2300/00
Inventor A·伯纳特J-M·赫伯特P·萨特
Owner SANOFI AVENTIS SA