Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Implant or insert
Patent
1998-08-12
1999-11-23
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Implant or insert
424427, 424434, 424436, 424456, 424465, 424489, 514165, 514301, A61F 1300, A61F 902, A61K 964, A61K 920, A61K 914
Patent
active
059895780
DESCRIPTION:
BRIEF SUMMARY
The subject of the present invention is a new combination of active ingredients with anti-platelet aggregation activity consisting of clopidogrel and aspirin, and pharmaceutical compositions containing them.
The active ingredients constituting the combination are present in the free state or in the form of one of their pharmacologically acceptable salts.
During the last decade, there has been a lot of interest in the study of the role played by the platelets in the development of diseases associated with atherosclerosis (myocardial infarction, angor, cerebral attack, peripheral arterial diseases and the like). The well-established role of the platelets in arterial thrombosis has allowed the development of numerous medicaments which inhibit the functions of the platelets and the discovery of the essential role of ADP in the thrombotic process has led to the development of ticlopidin, a potent antithrombotic agent. This thieno[3,2-c]pyridine derivative is described in Patent FR 73 03503. Ticlopidin selectively inhibits the platelet aggregation induced by ADP as well as that of other agonists, mediated by ADP [Feliste et al., Thromb. Res., 1987, 48, 403-415).
In multicentre double-blind clinical studies, ticlopidin proved to be significantly more effective than aspirin or a placebo in the prevention of cerebral attack in patients having a high risk of vascular accidents (Gent et al., Lancet, 1989, 8649, 1215-1220; Hass et al., N. Eng. J. Med., 1989, 321, 501-507). It also proved significantly more effective than the placebo in patients exhibiting a high risk of central or peripheral vascular accidents (Janzon et al., Scand. J. Int. Med., 1990, 227, 301-308).
Although it is known, to date, that aspirin and ticlopidin act via two different mechanisms of action, numerous studies have compared the efficacy of these two medicaments and it is only very recently that a few studies have suggested that ticlopidin, administered in combination with aspirin, could be of great interest in relation to acute thrombosis, as a replacement of current poorly effective treatments, in patients in whom a metallic endovascular prostheses had been implanted (Van Belle et al., Cor. Art. Dis., 1995, 6, 341-345).
The combination of ticlopidin and aspirin is claimed in patent FR 75 12084 for its use as anti-platelet aggregation agent endowed with a haemodynamic effect which is considerably qualitatively and quantitatively superior to that of ticlopidin alone. These results were demonstrated with the aid of pharmacological studies which related to the platelet aggregation inhibiting properties by making measurements of the platelet aggregation induced by ADP or collagen. The results which were obtained are predictive of a therapeutic importance of the ticlopidin-aspirin combination in some types of acute thrombosis following in particular some surgical operations but are not sufficient to deduce therefrom an indication in the secondary prevention of vascular accidents in atherometous disease or alternatively in endarterectomy or fitting of metallic endovascular prostheses.
It is moreover known that other combinations of anti-platelet aggregation agents, such as for example the combination aspirin-dipyridamole, have been the subject of clinical studies against dipyridamole alone or aspirin alone in the study of the prevention of cerebral vascular accident or of occlusion of the vascular shunt in patients. The conclusion of these studies was that the aspirin-dipyridamole combination does not possess any significant beneficial effect greater than that observed with dipyridamole alone or aspirin alone in the secondary prevention of cerebral atherothrombotic ischaemia or towards thrombosis (Acta. Neurol. Scand., 1987, 76(6), 413-421; Thrombosis, 1994, Alert No. 12; Thrombosis, 1994, Alert No. 9. Thrombosis, 1993, Alert No. 9; Thrombosis, 1993, Alert No. 2).
The fitting of metallic endovascular prostheses at the coronary and carotid level can be considered today as an important therapeutic advance in the prevention and treatment of central and
REFERENCES:
Herbert, J.M. Clopidgorel and antiplatelet therapy. Expert Opinion Investigating Drugs. 1994. 3(5):449-455. XP 000610730.
Expert Opin. Invest. Drugs, 1994, 3/5 (449-455), United Kingdom, Herbert, J. M. Clopidogrel and antiplatelet therapy.
Bernat Andre
Herbert Jean Marc
Savi Pierre
Alexander Michael D.
Berman Alysia
Page Thurman K.
Sanofi
LandOfFree
Associations of active principles containing clopidogrel and an does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Associations of active principles containing clopidogrel and an , we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Associations of active principles containing clopidogrel and an will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1218420