The use of phospholipid complexes of extracts of vitis vinifera as protivoateroskleroticheskim agents

 

The invention relates to medicine. The proposed use of phospholipid complexes of oligomeric proanthocyanidins for therapeutic and prophylactic treatment of atherosclerosis and treatment of atherosclerosis. The invention prevents the formation of atherosclerotic plaques. 2 S. and 3 C.p. f-crystals, 1 table.

The 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 drugs for the treatment and prevention of atherosclerosis and myocardial infarction and brain.

Extracts of Vitis vinifera already known and used in the treatment of cardiovascular disorders associated with venous insufficiency, for treating disorders permeability and resistance of the capillaries and scarring. These extracts, which can be obtained from the seeds of plants, as described in GB-A-1541469 or in FR-A-2092743 are a mixture of polyphenols such as epicatechin and its polymerization products, partially esterified by Gallic acid on the C-3 hydroxyl monomer. Phospholipid complexes of extracts of Vitis vinifera described in U.S. patent US-4963527 and currently commercially available PAYE in accordance with US-4963527, upon systemic administration, preferably oral, display a marked protivoateroskleroticheskim activity for both animals and humans.

More defined, found that phospholipid complexes of oligomeric proanthocyanidins containing from 2 to 7 catechin units extracted from Vitis vinifera, prevent or reduce the formation of atherosclerotic plaques dose-dependent manner.

Such activity was detected in rabbits, which were kept on a diet with a high content of cholesterol, in order to induce atherosclerotic lesions, similar lesions in humans, on the vascular level, particularly in the aortic arch, abdominal aorta, carotid arteries and cerebral vessels. In these models the above-mentioned phospholipid complexes change the state of the macro - and microscopic blood vessels, reducing, compared with untreated animals, as the number of atherosclerotic plaques and the severity of the process affects the beneficial effect on blood vessels and tissue. In another model of atherosclerosis, created with the purpose of studying the possibilities for protection of the brain, which was surgically reduced vascular lumen of the internal carotid artery of the rabbit, despite the introduction of hyperhaline vascular walls, and increased life expectancy of animals. In addition, patients suffering from atherosclerosis, see reducing obstruction of the carotid artery due to atherosclerotic plaques, and improved blood flow in the carotid artery, measured by Doppler ultrasound echography.

Phospholipid complexes of proanthocyanidins extracted from Vitis vinifera, can be used in appropriate oral compositions, such as tablets, soft and hard gelatin capsules at doses ranging from 50 to 500 mg two to three times a day, depending on the severity of the disease that is being treated. Preparation of pharmaceutical compositions can be effected in accordance with conventional techniques and excipients.

The following examples illustrate the invention in more detail.

Example 1 3 groups, each with 8 new Zealand rabbits were treated as follows: Group 1: Control, normal diet Group 2): a Diet high in cholesterol (0.2% cholesterol) Group 3: a Diet high cholesterol + phospholipid complex of extracts of Vitis vinifera (0.2% cholesterol + 2% Leucoselect).

After 8 weeks, during which measured the levels of cholesterol, LDL/VLDL (glipizide, animals slaughtered.

Estimated number, size and distribution of atherosclerotic lesions in the thoracic aorta and abdominal aorta.

Strips of aorta fixed and stained with Sudan IV for visualization of lesions and evaluation of cholesterol vessels and content of oxidized cholesterol by gas chromatography. The results presented in the table demonstrate that the processing of phospholipid complexes of extracts of Vitis vinifera statistically reduces atherosclerotic lesions, induced by a diet high in cholesterol.

Example 2 Capsules containing 500 mg of phospholipid complex of extracts of Vitis vinifera Composition: Complex extract of Vitis vinifera with soy phosphatidylcholine - 200 mg Lactose - 57 mg Modified starch 40 mg
Magnesium stearate - 3.0 mg
Example 3
Gastro-resistant tablets
Complex extract of Vitis vinifera with soy phosphatidylcholine 250 mg
Microcrystalline cellulose - 118 mg
Precipitated silica 3 mg
Magnesium stearate 4 mg
Anionic polymer of methacrylic acid and its esters - 12 mg
Talc - 8 mg
Magnesium carbonate - 8 mg
Corn starch 5 mg
Arabian gum - 159 mg
Example 4
Partially hydrogenated vegetable oil 100 mg
Soy lecithin - 5 MND


Claims

1. The use of phospholipid complexes of oligomeric proanthocyanidins containing from 2 to 7 catechin units extracted from Vitis vinifera, as an active ingredient for the manufacture of drugs for therapeutic and prophylactic treatment of atherosclerosis.

2. Application under item 1, where a single dose of the drug ranges from 50 to 500 mg of active ingredient.

3. Application under item 1 or 2, where the drug is administered orally.

4. Application under item 3, where the medicinal product is presented in the form of soft or hard gelatin capsules or tablets.

5. A method of treating atherosclerosis, which involves the administration to a patient an effective amount of phospholipid complex extract of Vitis vinifera.

 

Same patents:

The invention relates to medicine and relates to the treatment of metabolic syndrome

The invention relates to pharmaceutical compositions containing the inhibitor nm g COA reductase (E.)-7-[4-(4-forfinal)-6-isopropyl-2-[methyl(methylsulphonyl)amino] pyrimidine-5-yl]-(3R, 5S)-3,5-dihydroxide-6-envoy acid or its pharmaceutically acceptable salt as an active ingredient

The invention relates to the field of medicine and relates to a method of increasing the expression of molecular chaperone cell and/or increasing the activity of molecular chaperones in cells by treating the cells an effective amount of hydroxylamine derivative of the formula (I) or (II), as well as to new derivatives of hydroxylamine and farmkompanijam based on them
The invention relates to medicine, specifically to the preparations for the prevention and treatment of various forms of ischemic heart disease, atherosclerosis, and acute circulatory disorders, cerebral stroke

The invention relates to medicine, namely, neurology, and for the treatment of cerebral vascular shock
The invention relates to medicine, namely cardiology, and for the treatment of alexithymia (violations recognition and describe their own feelings), in patients with angina

The invention relates to benzodiapines General formula I, their derivatives and analogues

-converting enzyme)" target="_blank">

The invention relates to novel ortho-sulfonamidophenylhydrazine heteroaryl hydroxamic acids of the formula

< / BR>
where W and X are both carbon, T is nitrogen, U represents CR1where R1represents hydrogen, or alkyl containing 1-8 carbon atoms, R represents-N(CH2R5)-SO2Z, Q represents -(C=O)-NHOH, with

< / BR>
is a benzene ring, or is a heteroaryl ring of 5 to 6 atoms in the cycle, which may contain 0-2 heteroatoms selected from nitrogen, oxygen and sulfur, in addition to the heteroatom of nitrogen, denoted as W, where benzene or heteroaryl ring may optionally contain one or two substituent R1where permissible; Z is phenyl, which is optionally substituted by phenyl, alkyl with 1-8 carbon atoms, or a group OR2; R1represents halogen, alkyl with 1-8 carbon atoms, alkenyl with 2-6 carbon atoms, perfluoroalkyl from 1 to 4 carbon atoms, phenyl, optionally substituted by 1-2 groups OR2group-NO2group -(CH2)nZ, where Z is a phenyl which allows an alkyl with 1-8 carbon atoms, phenyl, optionally substituted with halogen, or heteroaryl radical containing 5 to 6 atoms in the cycle, including 1-2 heteroatoms selected from nitrogen, oxygen and sulfur; R5represents hydrogen, alkyl with 1-8 carbon atoms, phenyl, or heteroaryl containing 5 to 6 atoms in the cycle, including 1-2 heteroatoms selected from nitrogen, oxygen and sulfur; or their pharmaceutically acceptable salts

The invention relates to a derivative of D-Proline General formula

< / BR>
or

< / BR>
where R is SH, benzyl or phenyl, optionally substituted by a hydroxy-group or a lower alkoxygroup, or a group of the formula

< / BR>
R1is hydrogen or halogen; X represents -(CH2)n-; -CH(R2)(CH2)n-; -CH2O(CH2)n-; CH2NH-; benzyl, -C(R2)=CH-; CH2CH (OH)- or thiazol-2,5-diyl; Y represents-S -; (CH2)n; -O-; -NH-; -N (R2)-; -CH=CH-; -NHC(O)NH-; -N(R2)C(O)N(R2)-; -N[CH2WITH6H3(OCH3)2]-; -N(CH2WITH6H5)-; -N(CH2WITH6H5)C(O)N(CH2WITH6H5)-; -N(alkoxyalkyl)-; -N(cyclooctylmethyl)-; 2,6-pyridyl; 2,5-furanyl; 2,5-thienyl; 1,2-cyclohexyl; 1,3-cyclohexyl; 1,4-cyclohexyl; 1,2-naphthyl; 1,4-naphthyl; 1,5-naphthyl; 1,6-naphthyl or diphenylene; 1,2-phenylene; 1,3-phenylene or 1,4-phenylene, where phenylenebis group optionally substituted by 1-4 substituents selected from the group comprising halogen, lower alkyl, lower alkoxygroup, the hydroxy-group, carboxypropyl, -COO-lower thiazolyl, 2-oxo[1,2,3,5] oxadiazolyl, 5-thioxo[1,2,4]oxadiazolyl and 5-tert-butylsulfonyl[1,2,4] oxadiazolyl; X' represents -(CH2)n-; (CH2)nCH(R2)-; -(CH2)nOCH2-; -NHCH2-; benzyl, -CH= C(R2)-; -CH(OH)CH2or thiazol-2,5-diyl; R2denotes lower alkyl, lower alkoxygroup or benzyl and n = 0-3, their pharmaceutically acceptable salts, mono - and diesters, except (R)-1-[(R)- and (R)-1-[(S)-3-mercapto-2-methylpropionyl] pyrrolidin-2-carboxylic acid; medicinal product with amyloidoses activity, and the method of obtaining these derivatives

The invention relates to medicine, namely the pharmaceutical industry for the production of drugs therapeutic and prophylactic purposes

The invention relates to medicine, in particular to the pharmaceutical industry for the production of drugs therapeutic and prophylactic purposes, and can be used as a preventive and auxiliary means when levels of stress, mental and physical stress

The invention relates to medicine, in particular to the pharmaceutical industry for the production of drugs therapeutic and prophylactic purposes, and can be used as an aid in facilitating the normalization of peripheral (capillary) blood circulation, including brain

The invention relates to medicine, in particular to the pharmaceutical industry for the production of drugs therapeutic and prophylactic purposes, and can be used as a means to reduce the risk of symptoms of menopausal syndrome

The invention relates to medicine, namely to the pharmaceutical industry

The invention relates to medicine, in particular to the pharmaceutical industry for the production of drugs therapeutic and prophylactic purposes, and can be used as an aid in facilitating the regulation of the respiratory system
The invention relates to medicine, in particular to balms to treat impotence, prostatitis and benign prostatic hyperplasia
The invention relates to the field of pharmacology, and relates to biologically active compounds from plant material, which, on the one hand, can be used as biologically active food supplements as a nonspecific measure to increase the body's resistance to adverse influences, prevention of morbidity and normalize the functioning of the body, and on the other hand, can be used as the basis for medicines, in particular for the treatment of cancer

The invention relates to medicine, in particular to the pharmaceutical industry for the production of drugs therapeutic and prophylactic purposes, and can be used for the prevention and adjuvant therapy of hypotension and vascular dystonia

FIELD: medicine, cardiology, phytotherapy, pharmacy.

SUBSTANCE: invention relates to the field in development of an agent of vegetable origin used for improvement of the functional state and prophylaxis of organic alterations in cardiovascular system, in particular, atherosclerosis. The biologically active supplement used for prophylaxis of cardiovascular diseases, in particular, atherosclerosis comprises clover dry extract, haw-thorn flowers powder, ascorbic and nicotinic acids, and accessory substances taken in the definite ratio. The biologically active supplement is made in the form of tablet or capsule. No adverse responses observed in intake of the supplement. The blood cholesterol level was reduced to the normal value in 68% of patients and reducing morbidity with acute respiratory-viral infections has been noticed. In patients with ischemic heart disease with cholesterolemia the improvement of the state is noted on the background of conventional therapy: the moderate reducing the arterial pressure value in its elevation, improved in the state of health, enhanced working capacity, reduced retrosternal pains, ear noise, vertigo, headache.

EFFECT: valuable medicinal properties of supplement.

1 ex

Up!