Hypolipidemic and anti-sclerotic therapeutic and prophylactic
The invention relates to the field of generating plant to normalize cholesterol metabolism, prevention and treatment of atherosclerosis. Hypolipidemic and anti-sclerotic therapeutic tool based on medicinal plants contains clover, lovage and alfalfa with a ratio of clover : lovage : Lucerne 2:1:1 respectively. Therapeutic agent may be in the form of liquid extract or in the form of a dry extract, or mixture of dry extracts, or tableted or encapsulated forms. Reception means reduces cholesterol in the blood to normal in 68% of patients. 3 C.p. f-crystals.
The invention relates to the pharmaceutical industry, namely to funds on the basis of medicinal plants, designed to normalize cholesterol metabolism, prevention and treatment of atherosclerosis.
As is known, the increase in the content of cholesterol in blood serum plays a significant role in the development of atherosclerosis, so lately attach great importance to the correction of disturbed cholesterol metabolism.
Along with chemical lekarskou these plants produced a large amount of health care resources, in varying degrees, to reduce cholesterol in the blood and regulating lipid, namely cholesterol exchange.
Known dry extract of the rhizomes and roots of dioskoreya nipponskaya - polysporin , which has a moderate hypocholesterolemic effect.
According to the patent of Russian Federation №2011383 known tool that has hypolipidemic and protivoateroskleroticheskim action, obtained by extraction meal of sea-buckthorn berries after receiving sea buckthorn oil; in another patent of the RF No. 2043111 described therapeutic and prophylactic cholesterolreducing actions on the basis of dry, thick or liquid extract of grass Russian Thistle Salsola collina Pall.
In the patent of Russian Federation №2144373 as a means with hypocholesterolemic action proposed syrup from the ethanol extract of hibiscus petals, and in the patent of Russian Federation №2164145 for regulation of lipid metabolism, in particular for the prevention of arteriosclerosis, a seed extract of millet; in the application of the Russian Federation No. 2000109723 offer to reduce cholesterol and regulate lipid metabolism of plant Sterol, RF patent No. 2177798 for the same purpose - extract of grains of oats.
Known composition according to the patent of Russian Federation №2211043 for prigeon, prevention and treatment of atherosclerosis, containing oil, pine nuts and vitamins.
From the patent of the Russian Federation No. 2108802 known application for the prevention of hypercholesterinemia ointment, which includes 25% tincture of the roots of elecampane 40% ethanol.
It is also known many drug charges possess hypolipidemic and protivoateroskleroticheskim action, such as RF patents №№2163132, 2171679, 2204403. Disadvantages charges usually are a large number of components, and therefore it is difficult to predict their interaction and mutual influence.
Pyatigorsk state pharmaceutical Academy works were carried out to study the hypolipidemic and anti-sclerotic properties of red clover (red), which together with the state enterprise “Pharmaceutical factory”, Volgograd, was developed by clover extract liquid (Extractum Trifolii fluidum), 70% alcohol, which is recommended for use as anti-sclerotic tool (prototype).
In addition to the liquid extract of clover Pyatigorsk state pharmaceutical Academy in collaboration with the Institute of Experimental medicine of the Russian Academy of medical Sciences (St. Petersburg) was developed sclerotic and gipolipidemiceski).
Object of the invention is the expansion of health care resources based on red clover.
The technical result - obtaining new funds on the basis of red clover with lipid-lowering and anti-sclerotic properties.
The problem is solved in that the proposed treatment-and-prophylactic means to normalize cholesterol metabolism of medicinal plants containing clover, lovage and alfalfa at a ratio of 2:1:1 respectively. Therapeutic and prophylactic agent is a liquid extract, dry extract, or a mixture of dry extracts in pill or capsule form.
It is known that the main cause of atherosclerosis is a disorder of lipid metabolism, and flavonoids perform the role of natural antioxidants in the regulation of processes of lipid peroxidation in the cells. This determines the possibility of use as etiopathogenetic means plants containing flavonoids, have shown protective properties for the treatment of atherosclerosis. Such plants as proven by the latest research, are clover and alfalfa [2, 3].
Also the STI, cardiosclerosis. While cardio is important not only decrease cholesterol in the serum, but also the maintenance (supply) of the heart muscle. One such natural cardiotonics is lovage.
The claimed technical solution is proposed to use grass clover from the sort of meadow (red) (Trifolium pratense L.), as it is universally introduced to the culture and its resource base is virtually unlimited. According to the State Pharmacopoeia of the USSR (the global Fund of the USSR. General methods of analysis. Medicinal plant raw materials / the USSR Ministry of health. - Ed. 2nd supplementary - M.: Medicine, 1989. - Vol.2. - S. 400) main pharmacological activity of clover due to flavonoid compounds. Total flavonoid complexes clover reduce cholesterol and triglycerides in the blood, are lipid-lowering activity.
Lucerne sowing (Medicago sativa L.) as medicinal plants included in the State register of medicinal products (official publication from November 1, 1998). This plant is the same as clover, introduced in the cultural field.
Alfalfa is a natural bioregulator. The roots of this widespread plants penetrate the soil to a depth of 30-40 m, so this is one of the most bugkfa - and beta-carotene, essential amino acids, flavonoids, organic acids, humic substances, monosaccharides, calcium, copper, iron, magnesium, phosphorus, potassium, sodium, sulfur, zinc. The amino acid composition of alfalfa is very rich and well balanced. The use of alfalfa increases the elasticity of arteries, lowers the level of cholesterol in the blood by its preferential binding in the gastrointestinal tract, prevents the development of atherosclerosis.
The lovage pharmacy or drug (Levisticum officinale) contains a large amount of essential oils in all parts of the plant, but in different quantities - more than just dry the roots and rhizomes of 0.6 to 1.0%. It includes terpineol, cineole, carvacrol and other terpenoids. The roots were also found bergapten, resinous substances, starch and sucrose, angelic acid.
In folk medicine lovage is used primarily as a diuretic and heart. Drugs lovage possess cardiotonic effect, strengthen the cordial tone, they are swelling cardiac nature of the nervous diseases [3, 4].
In the present tool lovage is used as a heart cardiac tonic that can support the heart when the cardiosclerosis.
On the creation, alfalfa and lovage, in the ratio 2:1:1, respectively, as they complement the action of each other and create a cumulative effect, amplifying the hypolipidemic and anti-sclerotic effect of the proposed drug, which has been proved in experimental and clinical trials and study the specific activity of the drug, conducted Pyatigorsk state pharmaceutical Academy.
The main index, allowing to identify the inventive tool is, the total content of flavonoids as the main groups of active substances. Quantitative content and the ratio of the components of the formulation proposed dosage forms selected so that the content of the main active substances (flavonoids) remains constant. Set the lower limit of the content of the amount of flavonoids in the tool - 0,03% rutin.
Select the patient of the dosage form produced according to individual characteristics: if you cannot drink alcohol-containing preparations, use pills or capsules.
The invention is illustrated is not limiting the invention, examples of industrial implementation tools.
Red clover herb 7,0-10,5
The lovage pharmacy roots 3,5-5,25
Alfalfa seed grass 3,5-5,25
Red clover extract of 0.8-1.2
The lovage pharmacy extract of 0.4-0.6
Alfalfa seed extract 0,4-0,6
The extract obtained is a clear liquid from light brown to dark brown color with a specific smell. The content of extractives not less than 2 wt.%. The content of total flavonoids rutin not less than 0.03 wt.%.
Example 2. Tablets.
In the preparation of tablets using dry extracts components are prepared separately, or dry extract, obtained as described in example 1 liquid extract. To eliminate excessive hygroscopicity and improved ability to pelletizing the composition is added in the required amounts of microcrystalline cellulose and auxiliary substances, such as calcium stearate or magnesium and Aerosil, the components are taken in the following amounts, wt.%:
Aerosil Not more than 3.3
Calcium stearate is Not more than 1.0
Microcrystalline cellulose To 100
Tablets are gray-green in color with inclusions, faint odor and a bitter-sour taste. The content of total flavonoids rutin is not less than 0.45 wt.%. Tablets can be coated with soluble shell, manufactured in a known manner from known components.
Example 3. The capsule.
Another, more modern, preparative form of the proposed drug gelatin capsules containing powder of the proposed structure.
To obtain capsules mixed extracts in number, wt.%:
Red clover extract 25-50
The lovage pharmacy extract 25-50
Alfalfa seed extract 25-50
Auxiliary substances To 100
The resulting powder has a gray-green color with inclusions, faint odor and a bitter-sour taste. The content of total flavonoids rutin is not less than 0.45 wt.%.
The tool shows good hypolipidemic activity and is recommended for the treatment and prevention of atherosclerosis. The applicant was held Kli. the useful effect of the use of the invention is that expanding the range of domestic treatment-and-prophylactic preparations based on vegetable raw materials.
Industrial production invented tools under the trade name “Heteroclitic” carry on known equipment, using known means, therefore, a technical solution has industrial applicability. The tool is recommended to take adults and children over 12 years: 20-30 drops in a glass of water 2-3 times a day. Taking 25-30 days. For long-term and sustainable results it is recommended to take 3-4 courses per year.
The composition and manufacturing techniques allow to obtain a high-quality product with therapeutic effect, satisfy the security requirements SanPiN 188.8.131.528-01. When storage conditions in accordance with GOST 29189-91 product preserves the organoleptic, physico-chemical and microbiological indicators within the requirements of GOST.
Sources of information
1. Mashkovsky M. D. Medicines. - M.: Medicine. - 1987, T. 2 S. 92.
2. Babaskin B. C. and other Antiarrhythmic properties of flavonoids of some representatives of legumes. Tr. IV Rossier red as a source of biologically active substances, has anti-sclerotic effect. Medicinal substances. Rostov - on-don: Publishing house. Growth. University, 1979, S. 145-151.
4. Gammerman A. F. and other Medicinal plants. - M.: Higher school, 1990.
5. Popov A. P. Medicinal plants in folk medicine. - Kiev: Health, 1969, S. 138.
1. Hypolipidemic and anti-sclerotic therapeutic tool based on medicinal plants containing clover, characterized in that it further comprises the lovage and alfalfa with a ratio of clover:lovage:Lucerne 2:1:1 respectively.
2. Therapeutic and prophylactic under item 1, characterized in that it is a liquid extract.
3. Therapeutic and prophylactic under item 1, characterized in that it is a dry extract, or a mixture of dry extracts.
4. Therapeutic and prophylactic under item 1, characterized in that it has a tableted or encapsulated form.
R1means alkyl with 1, 2, 3, 4, 5, 6, 7 or 8 C-atoms; CandH2A-phenyl, where a = 0, which is unsubstituted or substituted by 1-3 substituents selected from the group consisting of F, Cl, Br, J, CF3, metoxygroup; CdH2d(C3-7-cycloalkyl, where d = 0; R2and R3independently from each other denote hydrogen, F, Cl, J, C=N; COR6where R6denotes hydrogen, alkyl with 1, 2, 3, 4, 5, 6, 7 or 8 C-atoms, OR30where R30- alkyl with 1, 2, 3, 4, 5, 6, 7 or 8 C-atoms; OR7where R7denotes hydrogen, alkyl with 1, 2, 3, 4, 5, 6, 7 or 8 C-atoms; phenyl; or R2and R3, independently of one another, denote CqH2q-phenyl, where q=0; or R2and R3independently from each other mean-SOnR22where n stands for zero, R22- alkyl with 1, 2, 3, 4, 5, 6, 7 or 8 C-atoms; R4and R5independently of one another denote hydrogen, alkyl with 1, 2, 3, 4, 5, 6, 7 or 8 C-atoms, F, Cl, Br, J, CF3and their physiologically acceptable salts; and to medicines, inhibiting Na+dependent Cl-/HCO-3- exchange rate is
where: A means-OR1-C(O)N(R1R2or-N(R1R21; each X, Y and Z independently represents N or C(R19); each U represents N or C(R5), provided that U is N only when X represents N, and Z and Y denote CR19; each W represents N or CH; V denotes: (1) N(R4); (2) C(R4)H; or (3) the groupdirectly related to the group -(C(R14R20)n-A,denotes a 5-6-membered N-heterocyclyl, optionally containing 6-membered ring additional heteroatom selected from oxygen, sulfur and NR6where R6denotes hydrogen, optionally substituted phenyl, 6-membered heterocyclyl containing 1-2 nitrogen atom, optionally substituted 5-membered heterocyclyl containing 1-2 nitrogen atom, aminosulfonyl, monoalkylammonium, dialkylaminoalkyl,1-6alkoxycarbonyl, acetyl, etc
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.