Anti-ischemic herbal meliloti and method thereof

 

The invention relates to medicine. The drug has anticoagulant, antioxidant, act-protective, neuroprotective, analgesic, capillary, antiulcerative, antiexudative, antiproliferative, wound healing, immunomodulatory action based on the extractives of clover grass medicinal in the following ratio of components, extractives of 0.1 - 40 wt. %; 20-95% ethyl alcohol or purified water - the rest. Spend the extraction of vegetable raw materials by the method of fractional maceration purified water at 80-90oWith or by percolation with ethanol of different concentrations within 1-168 h at a ratio of raw material: solvent 1: (5-100) followed by condensation of an alcohol or water extract of extractives in the form of coumarins and flavonoids and drying to obtain a dry extract. The invention provides maximum extraction of extractive substances, as well as preserve them over the long term. 3 S. and 1 C.p. f-crystals, 2 tab.

The invention relates to medicine, namely the creation of an anti-ischemic drug with wide spectrum of action based on vegetable raw materials and the method of its production, rnym, analgesic, capillary, antiulcerative, antiexudative, anti-proliferative, wound healing, immune modulating action on the basis of extractives (biologically active substances) in the form of coumarins and flavonoids of clover grass drug Herba Melilotus officinalis (L) Pall., the family of legumes - Fabaceae (Leguminosae) used for the prevention and treatment of ischemic damage of the cardiovascular system, causing poor circulation in the cardiovascular system, dizziness, hypertension, diabetes, giperlipedemia, cardiovascular disease, cerebral insufficiency, neurosensory disorders, peripheral vascular disease, as well as used to maintain good blood circulation, including in the brain, arms, legs.

Brain sensitivity to hypoxia ischemia is on the first place, the urgency of the search for new non-toxic substances of plant origin which increase the resistance of the brain to ischemia due to an increase in diseases caused by disorders of cerebral circulation.

Well-known domestic anti-ischemic herbal preparation with antihypoxic and nootropic effect on the basis of axih leaves and stems, followed by filtration and evaporation under vacuum. The drug contains a 9.5 22,74% extractives and is used for prophylaxis and treatment of cerebral circulation.

The drug has a narrow spectrum of pharmacological activity.

The closest solution according to the first invention is an anti-ischemic herbal drug TANAKAN (France) - based extractives leaves Gingo biloba antioxidant, antihypoxic effect, used for the treatment of cerebral and peripheral blood circulation.

Disadvantage - expensive foreign drug and narrow spectrum of pharmacological activity.

In the analyzed literature not found closest solution from a known source information according to the second invention.

It is known that the herb of melilot drug Herba Melilotus officinalis (L) Pall. , of the legume family - Fabaceae (Leguminosae) has long been used in folk medicine as a drug for the prevention and treatment of various diseases caused by poor blood circulation in the cardiovascular system. Medicinal raw materials are the tops of flowering shoots with leaves that can accumulate during flowering biologically active substances - coumarins, flavanone - the creation of new domestic anti-ischemic drug with broad spectrum of pharmacological activity on the basis of extractives in the form of coumarins and flavonoids of clover grass drug Herba Melilotus officinalis (L) Pall. , of the legume family - Fabaceae (Leguminosae), as well as enabling the use of rational technology of manufacturing of the drug, providing not only the maximum extraction of biologically active substances from plant material, but also maintaining them over a long period of time without changes.

The problem is solved in that the anti-ischemic drug MELILOTI on the basis of the extractive substances of vegetable raw materials, according to the invention, contains extractives of clover grass drug Herba Melilotus officinalis (L) Pall., the family of legumes-Fabaceae( Leguminosae) - coumarins and flavonoids, ethyl alcohol or purified water in the following ratio, wt%: Extractives of 0.1 - 40 20-95% ethyl Alcohol or purified water - the Rest of the problem is solved in that a method for producing anti-ischemic drug MELILOTI with anticoagulant, antigipoksicheskim, antioxidant, act-protective, neuroprotective, analysis, immunomodulatory effects, according to the invention, as the plant materials used fresh or dried herb of melilot drug Herba Melilotus officinalis (L) Pall., the family of legumes - Fabaceae (Leguminosae), collected during flowering, and the extraction was carried out by the method of fractional maceration purified water at a temperature of 80-90oC for 1-168 h at a ratio of raw material:solvent 1:(5-100), obtained by removing extractives cleanse, followed by separation of the amount of extractives in the form of coumarins and flavonoids. When this extraction is performed by the method of double maceration for 2.5 h with constant stirring at a ratio of raw materials - extractant 1:20, with the water extract of extractives unite.

The problem is solved as well by the fact that the method of obtaining anti-ischemic drug MELILOTI with anticoagulant, antigipoksicheskim, antioxidant, act-protective, neuroprotective, analgesic, capillary, antiulcerative, antiexudative, anti-proliferative, wound healing, immunomodulatory effects, according to the invention, as the plant materials used freshly picked and what about the time of flowering, and the extraction was carried out by the method of percolation 20-95% ethyl alcohol for 1-168 h at a ratio of raw material:solvent 1:(5-100), obtained by removing extractives cleanse, followed by separation of the amount of extractives in the form of coumarins and flavonoids.

While cleaning extraction extractives carried out by filtration, purified extract of extractives is condensed at a temperature of 90oC up to 5-30% of air-dry matter, however, the selection of the amount of extractives in the form of coumarins and flavonoids exercise of condensed extract of extractives by drying at a temperature of 60oC to obtain the dry extract.

The proposed group of inventions combined to form a single inventive concept, the second and third inventions are intended for first. All inventions solve the same task with achieving the same technical result.

Eksperimentalno found that as a result of this claimed as the invention of the technology can achieve the maximum degree of extraction of extractive substances in the form of coumarins and flavonoids from grass clover medicinal Herba Melilotus officinalis (L) Pall., the family of legumes - Fabaceae(Legumi, antihypoxic, anti-oxidant, act-protective, neuroprotective, analgesic, capillary, antiulcerative, antiexudative, anti-proliferative, wound healing, immunomodulatory activity and can be used for the prevention and treatment of circulatory disorders in the cardiovascular system, dizziness, hypertension, diabetes, hyperlipidemia, cardiovascular diseases for the treatment of cerebral insufficiency, neurosensory disorders, peripheral vascular disease, as well as to maintain good blood circulation, including in the brain, arms, legs. (The results of the pharmacological characteristics of the drug MELILOTI presented in the description of the drug and in tables 1-2).

As follows from the above review of the prior art, the claimed anti-ischemic drug MELILOTI on the basis of extractives - coumarins and flavonoids of clover grass drug Herba Melilotus officinalis (L) Pall., the family of legumes - Fabaceae (Leguminosae) with a wide spectrum of pharmacological activity and how to obtain it are new, they are not known from publicly available sources of information not derived explicitly from known modern level is of the invention is illustrated below by examples of implementation of the invention in St. Petersburg chemical-pharmacological Academy.

Example 1 Threshed grass clover medicinal Herba Melilotus officinalis (L) Pall., legume in the amount of 50 g is loaded into the extractor with water steam jacket and pour 600 ml of boiling purified water, stirred for 1.5 h, keeping the temperature to 80 or 90oC. Upon expiration of the time water removing extractives drained, raw squeeze and pour 400 ml boiling water and stirred under the same conditions for 1 hour After the double maceration of raw material which is obtained by water extraction of the combined filter. The resulting aqueous extract is a brown liquid, bitter taste with a spicy coumarin smell, containing 40% of extractives in the form of coumarins and flavonoids in purified water. The aqueous extract is packaged in a sterilized glass tacony of orange glass, sealed in plastic tubes, each bottle is placed in a cardboard pack packaged together with instructions for use, bundles are placed in boxes and are labeled.

Example 2 Alcohol extractant different concentrations are prepared in a reactor with a stirrer. In the reactor serves 96% ethyl alcohol and there served in the required amount of purified water. Threshed grass live ethyl appropriate concentration before the mirror, infused for 24 h, then permalert mainly 20% ethanol for 48 h until complete depletion of plant material, when the ratio of raw material:solvent 1:5. Then the resulting alcoholic extract purified from ballast substances by filtration and poured into the sump. The resulting alcoholic extract of extractives is a brown liquid, bitter taste with a spicy (coumarin) smell. Anti-ischemic drug Meliloti - tincture, containing 40% of extractives in the form of coumarins and flavonoids in 20% ethyl alcohol, which is Packed in glass bottles of orange glass, sealed in plastic tubes, the vial is placed in a pack together with instructions for use, bundles stacked in boxes and nakliyat labels.

The drug MELILOTI - tincture containing 10% extractives in the form of coumarins and flavonoids in 95% ethyl alcohol, which is Packed in glass bottles of orange glass, sealed in plastic tubes, the vial is placed in a pack together with instructions for use, bundles stacked in boxes and nakliyat labels.

Example 3 Threshed grass clover medicinal Herba Melilotus officinalis (L) entrale before the mirror, infused for 24 h, then permalert mainly 20% ethyl alcohol for 168 h until complete depletion of plant material, when the ratio of raw material: solvent 1:100. Then the resulting alcoholic extract purified from ballast substances by filtration and poured into the sump. The resulting alcoholic extract of extractives is a brown liquid, faint bitter taste with a spicy (coumarin) smell. Anti-ischemic drug Meliloti - tincture matrix homeopathic, contains 0.1% of extractives in the form of coumarins and flavonoids in 20% ethyl alcohol, which is Packed in glass bottles of orange glass, sealed in plastic tubes, the vial is placed in a pile with the statement, bundles stacked in boxes and are labeled.

Example 4 Selection of the amount of extractives in the form of coumarins and flavonoids from the alcoholic extract of different concentration or water extraction carried out with the concentration of the extract at a temperature of 90oWith in a vacuum rotary evaporator to 5-30% of air-dry matter, get a thick extract, representing viscous liquid, brown in color, bitter taste with a spicy (who do have dry extract, a powder light brown in color, spicy (coumarin) smell, bitter taste. Dry and dense extracts can be used for manufacturing of various dosage forms: tablets, capsules, granules, etc. (9).

Example 5 the Amount of extractives in the drug MELILOTI determined as follows: 5 ml of the preparation was placed in a weighted Boxing, is evaporated on a water bath and dried 3 hours at a temperature of 105oC, then cooled in a desiccator for 30 min and weighed.

Example 6 the resulting preparation MELILOTI identify the following way. One part of the alcohol extract of different concentration or water extraction of extractive substances are placed in a flask, add powder of zinc and concentrated hydrochloric acid, heated on a boiling water bath until the pink colouring (flavonoids), adding to another part of the alcoholic extract of different concentration or water extract of extractives solution of sodium hydroxide and diazotized sulfonylurea acid by heating on a water bath appears orange (coumarins).

Pharmacological studies of the drug MELILOTI
(presented in tables 1-2)
The first is LILITIN. It is established that for mice when intraabdominal administration of the investigational product LD50was 4300 mg/kg Maximum dose in oral administration was not more than 6000 mg/kg of the drug. This mortality was not observed. When examining the spectrum of antihypoxic activity found that the drug has a pronounced effect in a wide range of doses on models with a single intraperitoneal injection. On the activity of the drug MELILOTI not inferior, and in some cases superior to the reference product GUTIMIN and close to the drug TANAKAN. The drug Gutimin - antihypoxic drug. Drug TANAKAN widely used in case of insufficiency of cerebral blood flow (dyscirculatory encephalopathy), disorders of peripheral blood circulation, antioxidant and antihypoxic drug. Preparation MELITTIN at doses of 60-120 mg/kg on his activity was not inferior by prophylactic oral administration of the drug TANAKAN. The results of biochemical studies were confirmed by histological study of identical areas of hippocam and new cortex of rat brain. The results of our experiments indicate that the drug MELILOTI able to shunt the respiratory chain at nascosto Occidental of activity of the drug MELILOTI suggest he has a wide range of therapeutic effects. The drug has low toxicity after a single dose. With long-term administration of the drug in therapeutic and toxic doses in laboratory animals had no toxic effects on major body systems of animals. To establish the anticoagulant properties of the drug MELILOTI determined the clotting time of the blood of animals after a course of chemotherapy. Experiments conducted on rats male body weight 170-230, Animals were kept on a standard diet. Each group consisted of 10 animals. Pre-determined initial clotting time of the blood of animals. Drugs administered orally. From the dry extracts prepared solution of purified water and alcohol extraction was previously dealcoholization and diluted with purified water. The dry extract was administered at a dose of 40 mg/kg of alcoholic extract to 10 ml/kg Volume of the injected solution was 10 ml/kg of Comparators: Venelin (pill) and coumarin (standard sample) was also administered orally. From the Comparators prepared thin suspension using emulsifier tween-80. The volume of injected solution was 10 ml/kg Control group received water purified. Similarly conducted studies of simultaneous peroral the project for the blood were measured by the stopwatch immediately after blood collection in rats of lower gum and 1 ml. End of coagulation was evaluated visually. The obtained data testify to the anticoagulant properties of the drug MELILOTI. The combination of anticoagulation, antihypoxic, anti-oxidant, act-protective, neuroprotective, analgesic, capillary, antiulcerative, antiexudative, anti-proliferative, wound healing, immune-modulating effects allows us to speak about the prospects of anti-ischemic drug MELILOTI. The above detailed description of examples of the practical implementation of invention leave no doubt as to their feasibility is an integral part of all elements of technological methods of manufacture of the drug from a plant long known and well-developed modern pharmacology. Conducted pharmacological research and development of technology have confirmed the consistent achievement of the goals, created anti-ischemic drug MELILOTI has anticoagulant antihypoxic, anti-oxidant, neuroprotective, analgesic, capillary,anti-inflammatory, immunomodulatory activity and can be used for the prevention and treatment of disorders of krooo is simple diseases, cerebral insufficiency, neurosensory disorders, peripheral vascular disease, as well as to maintain good blood circulation, including in the brain, arms, legs.


Claims

1. Anti-ischemic drug on the basis of the extractive substances of plant material, characterized in that it contains extractives of clover grass drug Herba Melilotus officinalis (L) Pall., the family of legumes - Fabaceae(Leguminosae) - coumarins and flavonoids, ethyl alcohol or purified water in the following ratio, wt.%:

Extractives of 0.1 - 40

20-95% ethyl Alcohol or purified water Rest

2. The method of obtaining anti-ischemic drug, possess anticoagulant, anti-hypoxic, antioxidant, act-protective, neuroprotective, analgesic, capillary, antiulcerative, antiexudative, anti-proliferative, wound healing, immunomodulatory effects, including extraction of plant materials, characterized by the fact that they use fresh or dried, threshed grass clover medicinal Herba Melilotus officinalis (L) Pall., the family of legumes - Fabaceae (Leguminosae), sobrano the img src="https://img.russianpatents.com/chr/176.gif">With over 1-168 h at a ratio of raw material : solvent 1 : (5-100), obtained by removing extractives cleanse, followed by separation of the amount of extractives in the form of coumarins and flavonoids.

3. The method according to p. 2, characterized in that the extraction carried out mainly by the method of double maceration for 2.5 h with constant stirring at a ratio of raw material : solvent 1 : 20, with the water extract of extractives unite.

4. The method of obtaining anti-ischemic drug, possess anticoagulant, anti-hypoxic, antioxidant, act-protective, neuroprotective, analgesic, capillary, antiulcerative, antiexudative, anti-proliferative, wound healing, immunomodulatory effects, including extraction of plant materials, characterized by the fact that they use fresh or dried, threshed grass clover medicinal Herba Melilotus officinalis (L) Pall., the family of legumes - Fabaceae (Leguminosae), collected during flowering, and the extraction was carried out by the method of percolation 20-95% ethyl alcohol for 1-168 h at a ratio of raw material : solvent 1 : (5-100), obtained by removing extractives from the eyes of the

 

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