Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Reexamination Certificate
2000-05-31
2001-10-02
Weber, Jon P. (Department: 1651)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
C514S078000
Reexamination Certificate
active
06297218
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates to the use of phospholipid complexes of oligomeric proanthocyanidins containing from 2 to 7 catechin units extracted from
Vitis vinifera
for the preparation of medicaments for the treatment and the prophylaxis of atherosclerosis, and of myocardial and cerebral infarctions.
BACKGROUND OF THE INVENTION
The extracts of
Vitis vinifera
are already known and used in the therapy of cardiovascular disorders connected with venous insufficiency, in the treatment of impaired conditions of capillary permeability and resistance and in cicatrization. These extracts, which can be obtained from the seeds of the plant as described in British patent application 1,541,469 or in French patent application 2,092,743, are a mixture of polyphenols such as epicatechin and its polymerization products, in part esterified at the C-3 hydroxyl of the monomer with gallic acid. The phospholipid complexes of the extracts of
Vitis vinifera
are described in U.S. Pat. No. 4,963,527 and are at present commercially available under the trademark LEUCOSELECT. The extracts of
Vitis vinifera
detailed in the prior art are obtained by extraction with acetone, usually using an acetone-water mixed solution.
SUMMARY OF THE INVENTION
The present invention is directed to a method for the treatment of atherosclerosis or of myocardial or cerebral infarctions and an anti-atherosclerotic medicament therefor. The method for the treatment of atherosclerosis or of myocardial or cerebral infarctions includes administering a therapeutically effective amount of an extract of
Vitis vinifera
, preferably in a phospholipid complex, to a patient in need of such treatment. Advantageously, the extract can contain oligomeric proanthocyanidins having from about 2 to about 7 catechin units. In one embodiment, the unitary dosage and/or the therapeutically effective amount of the medicament ranges from 50 mg to 500 mg. In another embodiment, the unitary dosage and/or the therapeutically effective amount of the medicament can range from 266 mg to 500 mg.
In a preferred embodiment, the medicament is in the form of an orally administrable composition. Alternately or additionally, a pharmaceutically acceptable carrier, adjunct, or excipient may also be present. Preferably, the pharmaceutically acceptable carrier is a soft or hard gelatin capsule or a tablet. More preferably, the capsule or tablet may be administrable orally.
Another aspect of the present invention relates to an anti-atherosclerotic medicament that includes a therapeutically effective amount of one or more of the extracts or phospholipid complexes described herein. In a preferred embodiment, the medicament is in the form of an orally administrable composition. Alternatively or additionally, a pharmaceutically acceptable carrier, adjunct, or excipient may also be present. Preferably, the pharmaceutically acceptable carrier is a soft or hard gelatin capsule or a tablet.
DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
It has now surprisingly been found that the complexes prepared according to U.S. Pat. No. 4,963,527 exert, when administered systemically, preferably by the oral route, a marked anti-atherosclerotic activity and effect both in animals and in humans.
More specifically, it has been found that the phospholipid complexes of oligomeric proanthocyanidins containing from 2 to 7 catechin units extracted from
Vitis vinifera
, prevent or reduce the formation of atherosclerotic plaques in a dose-dependent relationship.
Such an activity was evidenced in rabbits fed with hypercholesterolemic diet, so as to induce atherosclerotic lesions similar to the human ones at the vascular level, particularly at the aortic arch, ventral aorta, carotids, and cerebral vessels. In a comparative model, a normal, or control, diet was compared to two hypercholeseterolemic diets, one without and one with the above mentioned phospholipid complexes. It was found that the phospholipid complexes may have changed the macroscopic and microscopic vascular condition, compared with untreated animals, by reducing both the number of atheromatous plaques and their severity, with a surprising vascular-tissular benefit. In another atherosclerosis model, the purpose of which was to examine cerebral protection, the vasal lumen of rabbit internal carotid was surgically reduced, while administering a hypercholesterolemic diet rich in saturated fats. As a result, a decrease in carotid obstruction was exhibited, as well as a reduction of vessel wall thickness, and an increased survival rate of the animals was evidenced. Furthermore, in atherosclerotic patients, a reduction in carotid obstruction due to atheromatous plaques and an improved carotid flow were observed, as evaluated by Doppler ultrasonography.
The phospholipid complexes of the proanthocyanidins extracted from
Vitis vinifera
can be used in suitable oral formulations, for example, such as tablets and soft or hard gelatin capsules, at dosages preferably from 50 mg to 500 mg, or alternately from 266 mg to 500 mg, administered preferably two to three times a day, depending on the severity of the ailment to be treated. The preparation of the pharmaceutical formulations can be carried out according to conventional techniques and may optionally include pharmaceutically acceptable carriers, adjuncts, or excipients.
REFERENCES:
patent: 4963527 (1990-10-01), Bombardelli et al.
patent: 5484594 (1996-01-01), Frangi et al.
patent: 5607965 (1997-03-01), Kondo et al.
patent: 0713706 A (1996-05-01), None
patent: 2092743 (1970-06-01), None
patent: 1541469 (1979-02-01), None
Lust, J. The Herb Book; pp. 659, 1974.*
K. Tebib, et al., “Antioxidant Effects of Dietary Polymeric Grape Seed Tannins in Tissues of Rats Fed a High Cholesterol-Vitamin E-Deficient Diet,”Food Chemistry,vol. 59, No. 1, pp. 135-141 (1997).
E. Bombardelli, et al., “Biological Activity of Procyanidins fromVitis Vinifera L.,” Biofactors,vol. 6, No. 4, pp. 429-431 (1997).
Bombardelli Ezio
Morazzoni Paolo
Indena SpA
Patten Patricia D.
Pennie & Edmonds LLP
Weber Jon P.
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