KR20170028638A - Pharmaceutical compositions for preventing or treating osteoporosis comprising an extract of Allium hookeri - Google Patents
Pharmaceutical compositions for preventing or treating osteoporosis comprising an extract of Allium hookeri Download PDFInfo
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- KR20170028638A KR20170028638A KR1020150125496A KR20150125496A KR20170028638A KR 20170028638 A KR20170028638 A KR 20170028638A KR 1020150125496 A KR1020150125496 A KR 1020150125496A KR 20150125496 A KR20150125496 A KR 20150125496A KR 20170028638 A KR20170028638 A KR 20170028638A
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- extract
- bone
- osteoporosis
- alcohol
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- 230000001681 protective effect Effects 0.000 description 1
- HELXLJCILKEWJH-NCGAPWICSA-N rebaudioside A Chemical compound O([C@H]1[C@H](O)[C@@H](CO)O[C@H]([C@@H]1O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)O[C@]12C(=C)C[C@@]3(C1)CC[C@@H]1[C@@](C)(CCC[C@]1([C@@H]3CC2)C)C(=O)O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O HELXLJCILKEWJH-NCGAPWICSA-N 0.000 description 1
- 235000019204 saccharin Nutrition 0.000 description 1
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- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 description 1
- 235000011888 snacks Nutrition 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
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- 235000019654 spicy taste Nutrition 0.000 description 1
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- 229940032147 starch Drugs 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 229960004793 sucrose Drugs 0.000 description 1
- 150000005846 sugar alcohols Chemical class 0.000 description 1
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- 239000000375 suspending agent Substances 0.000 description 1
- 235000019605 sweet taste sensations Nutrition 0.000 description 1
- 235000019640 taste Nutrition 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 229960003604 testosterone Drugs 0.000 description 1
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- 210000001519 tissue Anatomy 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- 201000008827 tuberculosis Diseases 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
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- 235000013311 vegetables Nutrition 0.000 description 1
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/88—Liliopsida (monocotyledons)
- A61K36/896—Liliaceae (Lily family), e.g. daylily, plantain lily, Hyacinth or narcissus
- A61K36/8962—Allium, e.g. garden onion, leek, garlic or chives
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/105—Plant extracts, their artificial duplicates or their derivatives
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2200/00—Function of food ingredients
- A23V2200/30—Foods, ingredients or supplements having a functional effect on health
- A23V2200/306—Foods, ingredients or supplements having a functional effect on health having an effect on bone mass, e.g. osteoporosis prevention
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
- A61K2236/30—Extraction of the material
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Abstract
The present invention relates to a process for the preparation of Allium The present invention relates to a pharmaceutical composition for the prevention and treatment of osteoporosis which contains as an active ingredient an extract of osteoporosis and hookeri , The triple extract of the present invention can be effectively used as a pharmaceutical composition for the prevention and treatment of osteoporosis.
Description
The present invention relates to a pharmaceutical composition for preventing and treating osteoporosis comprising Allium hookeri as an active ingredient.
The bone is a special tissue that combines internal cellular components called calcified hard surface and bone marrow. The combination of these two physiologically distinct structures is due to the lifelong bone remodeling process, which is characterized by osteoclasts in the bone marrow due to hormones or physical stimuli applied to the bone. (JS, Natl ., 215, < RTI ID = 0.0 & gt ; 215), & lt ; / RTI > pp. 25-31, 2000). In addition, bone is responsible for preserving the bone mass and structure required as a physical support of body, and play an important role in maintaining blood levels of calcium, such as a storage bin, such as calcium (Ca 2 +). In order to perform this function, it is necessary that the bone is always in harmony with the degradation and reconstruction, and in this process, the bone is absorbed and formed together with the bone formation. When such an equilibrium relationship between bone resorption and bone formation is broken, osteoporosis may occur, in which bone resorption is relatively higher than bone formation, whereby bone density or bone mass is decreased and bone strength is not maintained.
Osteoporosis is a disease in which fracture and morphological deformation are easily caused by a small impact due to a decrease in overall bone mass due to structural weakening of the bone, and this patient shows a primary decrease in the space occupied by the bone marrow and the thickness of the cortex (Reilly , DT and Burstein, AH, J. Bone Joint Surg ., 56, 1001-1022, 1994).
Osteoporosis can be classified into various types depending on its type and cause, including type I osteoporosis due to menopause and type II osteoporosis due to aging (Dempster, DW, Lindsay, R., Lancet, 341, 797-801,1993). Although many studies have not been conducted on the causes of osteoporosis, Type I and Type II osteoporosis are caused by endocrine disorders in many cases. In addition, calcium, phosphate and vitamin D (Sambrook, P. et al., N. Engl . J. Med ., 328, 1747-1752, 1993; Marie, PJ et al . , J. Clin . Endourinol . Metab ., 69 , 272-279, 1989; Krane, SM and Holiok, MF, in Harrison ' s Principles of Internal Medioin , vol.2, 2172-2183, 1994).
Because Type I and Type II osteoporosis are diseases that occur over decades, it is not sufficient to take several simple drugs for a short period of time to treat them. Estrogen or testosterone has been generally used as a treatment for osteoporosis. Calcium, phosphate, fluoride, ipriflavone, vitamin D and calcitonin have been reported to be used as therapeutic agents. However, It is necessary to develop a new therapeutic agent for osteoporosis that has no adverse effects on the human body.
In addition, up to now, a therapeutic agent for osteoporosis, which inhibits osteoclast function and suppresses excessive bone resorption, has been mainly developed, but it is difficult to restore the risk of fracture due to reduction of bone mass only by inhibiting bone resorption. Drugs should be developed.
Allium hookeri are distributed in southern China, India, Bhutan, Sri Lanka, etc. in East Asia and grow in forests, wetlands and grasslands of 1400 m to 4200 m above sea level. It is also called "Root Leek". It is also called "玄 菜" because its taste and shape are similar to ginseng. It is also called "三 菜" because it has three flavors of bitter taste, sweet taste and spicy taste. The height of the plant is about 0.6 to 1 m, and it is known that the roots, leaves and flowers of the three-leafed plants can be used for food and medicinal use.
Accordingly, the present inventors have made efforts to find a substance effective for the prevention and treatment of osteoporosis, and confirmed that the bone strength, bone density, bone weight and bone mineral content are increased in ovariectomized rats (rats) The present invention has been accomplished on the basis that it is useful for prevention and treatment of osteoporosis.
An object of the present invention is to provide a pharmaceutical composition for preventing and treating osteoporosis, which contains Allium hookeri as an active ingredient.
In order to achieve the above object, the present invention is three (Allium The present invention provides a pharmaceutical composition for the prevention and treatment of osteoporosis, which comprises an extract of Hookeria as an active ingredient.
Further, the present invention provides a health functional food for prevention and improvement of osteoporosis, which comprises a tea leaf extract as an active ingredient.
The present invention relates to a process for the preparation of Allium The present invention relates to a pharmaceutical composition for the prevention and treatment of osteoporosis, which comprises, as an active ingredient, a bone extract, a hookeri extract, and the like. In ovariectomized rats fed with a tuberous extract, bone strength, bone density, The triple extract of the present invention can be effectively used as a pharmaceutical composition for the prevention and treatment of osteoporosis.
Fig. 1 shows the results of immunohistochemical staining of the Allium hookeri ) extract group and the control group.
FIG. 2 is a graph showing the bone density (g / cm 3) of the triple extract-fed group and the control group in ovariectomized rats.
Fig. 3 is a graph showing the bone weights (g) in the group fed with the tuberculosis extract and the control group in the ovariectomized rats.
FIG. 4 is a graph showing the bone mineral content (g / 100 g) in the group fed with the tuberous extract and the control group in the ovariectomized rats.
Hereinafter, the present invention will be described in detail.
The present invention relates to a process for the preparation of Allium The present invention provides a pharmaceutical composition for the prevention and treatment of osteoporosis, which comprises an extract of Hookeria as an active ingredient.
The above-mentioned tubular extract is preferably prepared by a manufacturing method comprising the following steps, but not limited thereto:
1) extracting the triplets by adding an extraction solvent;
2) filtering the extract of step 1);
3) Concentrating the filtrate obtained in step 2) under reduced pressure and then drying to prepare a triplex extract.
In the above method, the triplex of step 1) can be used without limitation such as cultivated or marketed, and any of leaves, roots, stems and branches can be used, and the present invention is not limited thereto. It is most preferable to use the leaves of the trifoliate leaves or the leaves of the plants associated with the same.
In the above method, it is preferable that the extraction solvent of step 1) be water, alcohol, alcohol, or a mixture thereof and an organic solvent. As the alcohol, C 1 to C 2 lower alcohol is preferably used, and as the lower alcohol, ethanol or methanol is preferably used. As the extraction method, it is preferable to use shaking extraction, Soxhlet extraction or reflux extraction, but it is not limited thereto. The extraction solvent is preferably added by 5 to 30 times the amount of the dried triplets, more preferably 10 to 20 times. The extraction temperature is preferably 20 占 폚 to 100 占 폚, more preferably 20 占 폚 to 40 占 폚, and most preferably room temperature, but is not limited thereto. The extraction time is preferably 10 to 48 hours, more preferably 15 to 30 hours, most preferably 24 hours, but is not limited thereto. The number of times of extraction is preferably 1 to 5 times, more preferably 3 to 4 times, and most preferably, 3 times, but is not limited thereto.
The above-mentioned triple extract is preferably a 40 to 95% alcohol extract, more preferably a 50 to 90% alcohol extract, a 60 to 80% alcohol extract, and most preferably less than 40% May not exhibit the desired osteoporosis mitigation effect, and in the case of the extract of the alcohol extract of 80% or more, the production cost of the tubular extract may be increased, which is not good.
The above-mentioned triple extract has an osteoporosis relieving effect by increasing bone strength, bone density, bone weight and bone mineral content.
In a specific example of the present invention, the present inventors prepared triacylglycerol extracts using trifoliate leaves and fed them to ovariectomized rats (rats). As a result, compared to the control group not consuming the trifoliate extracts, (See FIGS. 1 to 4), the tubular extract of the present invention can be effectively used as a pharmaceutical composition for the prevention and treatment of osteoporosis.
The composition of the present invention may further comprise a pharmaceutically acceptable carrier. The term " pharmaceutically acceptable "as used herein means that the composition is free of toxicity to cells or humans exposed to the composition. Compositions comprising a pharmaceutically acceptable carrier can be of various oral or parenteral formulations. In the case of formulation, it can be prepared using diluents or excipients such as fillers, extenders, binders, humectants, disintegrants, surfactants and the like which are usually used. The carriers, excipients and diluents include lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, acacia rubber, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methylcellulose, microcrystalline cellulose, But may be at least one selected from the group consisting of polyvinylpyrrolidone, physiological saline, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and mineral oil, dextrin, calcium carbonate, propylene glycol and liquid paraffin, But are not limited to, ordinary carriers, excipients or diluents. The components may be added independently or in combination with the active ingredient triple extract.
Solid formulations for oral administration may include tablets, pills, powders, granules, capsules, and the like, which may contain one or more excipients, such as starch, calcium carbonate, sucrose, Lactose, gelatin, and the like. In addition to simple excipients, lubricants such as magnesium stearate, talc, and the like may also be used. Liquid preparations for oral administration include suspensions, solutions, emulsions, syrups and the like. Various excipients such as wetting agents, sweeteners, fragrances, preservatives and the like may be included in addition to water and liquid paraffin, which are simple diluents commonly used. have. Formulations for parenteral administration may include sterile aqueous solutions, non-aqueous solutions, suspensions, emulsions, freeze-dried preparations, and suppositories. Examples of the non-aqueous solvent and the suspending agent include propylene glycol, polyethylene glycol, vegetable oil such as olive oil, and injectable ester such as ethyl oleate. As the base of the suppository, witepsol, macrogol, tween 61, cacao paper, laurin, glycerogelatin and the like can be used.
The pharmaceutical composition of the present invention may also be in the form of tablets, pills, powders, granules, capsules, suspensions, solutions, emulsions, syrups, sterile aqueous solutions, non-aqueous solutions, suspensions, emulsions, Or a pharmaceutically acceptable salt thereof.
The pharmaceutical composition of the present invention can be administered in a pharmaceutically effective amount. There is no particular restriction on the dosage, and it may vary depending on the body's absorption, body weight, age, sex, health condition, diet, administration time, administration method, excretion rate, severity of disease and the like. The pharmaceutical composition of the present invention is prepared in consideration of an effective dose range, and the unit dosage formulations thus formulated are classified according to the judgment of the expert who monitors or observes the administration of the drug, if necessary, Or may be administered several times at a predetermined time interval. Preferably, the composition of the present invention may be administered at a dose of 0.5 to 5000 mg / kg, preferably 50 to 500 mg / kg, more preferably 50 mg / kg, based on the amount of the tubercle leaf extract per day, The above administration may be carried out once a day or several times.
Further, the present invention provides a health functional food for prevention and improvement of osteoporosis, which comprises a tea leaf extract as an active ingredient.
The above-mentioned tubular extract is preferably prepared by a manufacturing method comprising the following steps, but not limited thereto:
1) extracting the triplets by adding an extraction solvent;
2) filtering the extract of step 1);
3) Concentrating the filtrate obtained in step 2) under reduced pressure and then drying to prepare a triplex extract.
In the above method, the triplex of step 1) can be used without limitation such as cultivated or marketed, and any of leaves, roots, stems and branches can be used, and the present invention is not limited thereto. It is most preferable to use the leaves of the trifoliate leaves or the leaves of the plants associated with the same.
In the above method, it is preferable that the extraction solvent of step 1) be water, alcohol, alcohol, or a mixture thereof and an organic solvent. As the alcohol, C 1 to C 2 lower alcohol is preferably used, and as the lower alcohol, ethanol or methanol is preferably used. As the extraction method, it is preferable to use shaking extraction, Soxhlet extraction or reflux extraction, but it is not limited thereto. The extraction solvent is preferably added by 5 to 30 times the amount of the dried triplets, more preferably 10 to 20 times. The extraction temperature is preferably 20 占 폚 to 100 占 폚, more preferably 20 占 폚 to 40 占 폚, and most preferably room temperature, but is not limited thereto. The extraction time is preferably 10 to 48 hours, more preferably 15 to 30 hours, most preferably 24 hours, but is not limited thereto. The number of times of extraction is preferably 1 to 5 times, more preferably 3 to 4 times, and most preferably, 3 times, but is not limited thereto.
The above-mentioned triple extract is preferably a 40 to 95% alcohol extract, more preferably a 50 to 90% alcohol extract, a 60 to 80% alcohol extract, and most preferably less than 40% May not exhibit the desired osteoporosis mitigation effect, and in the case of the extract of the alcohol extract of 80% or more, the production cost of the tubular extract may be increased, which is not good.
The above-mentioned triple extract has an osteoporosis relieving effect by increasing bone strength, bone density, bone weight and bone mineral content.
In a specific example of the present invention, the present inventors prepared triacylglycerol extracts using trifoliate leaves and fed them to ovariectomized rats (rats). As a result, compared to the control group not consuming the trifoliate extracts, (See FIGS. 1 to 4), the tubular extract of the present invention can be effectively used as a health functional food for prevention and improvement of osteoporosis.
The health functional food of the present invention can be used as it is or in combination with other food or food ingredients, and can be suitably used according to conventional methods.
There is no particular limitation on the kind of the health functional food. Examples of the food to which the above-mentioned tangerine-derived extract can be added include dairy products including meat, sausage, bread, chocolate, candy, snack, confectionery, pizza, ramen, other noodles, gums, ice cream, various soups, drinks, tea, , An alcoholic beverage, and a vitamin complex, all of which include health functional foods in a conventional sense.
The health functional beverage composition of the present invention may contain various flavors or natural carbohydrates as an additional ingredient such as ordinary beverages. Such natural carbohydrates are monosaccharides such as glucose and fructose, disaccharides such as maltose and sucrose, and polysaccharides such as dextrin and cyclodextrin, and sugar alcohols such as xylitol, sorbitol and erythritol. Examples of sweeteners include natural sweeteners such as tau martin and stevia extract, synthetic sweeteners such as saccharin and aspartame, and the like. The ratio of the natural carbohydrate is generally about 0.01 to 0.04 g, preferably about 0.02 to 0.03 g per 100 g of the composition of the present invention.
In addition to the above, the health functional food of the present invention may contain various nutrients, vitamins, electrolytes, flavors, colorants, pectic acids and salts thereof, alginic acid and its salts, organic acids, protective colloid thickeners, pH adjusters, stabilizers, Alcohols, carbonating agents used in carbonated drinks, and the like. It may also contain flesh for the production of natural fruit juices, fruit juice drinks and vegetable drinks. These components may be used independently or in combination. The proportion of such an additive is not critical but is generally selected in the range of 0.01 to 2 parts by weight per 100 parts by weight of the composition of the present invention.
Hereinafter, the present invention will be described in detail with reference to Examples and Experimental Examples.
However, the following Examples and Experimental Examples are merely illustrative of the present invention, and the content of the present invention is not limited by the following Examples and Experimental Examples.
< Example 1> Triptych Extract preparation
Samcheon was purchased from the morphological evaluation of Sunchang Agricultural Technology Center in Jeollabuk-do, and the leaves were washed with water and freeze-dried (PVTFD 10R, Ilsin Lab, Yangzhou, Korea) Twenty times as much as 70% fermented juice was added to 100 g of the sample, and the mixture was repeatedly stirred twice at room temperature for 24 hours (Jeio tech sk-71, Lab companion, Daejeon, Korea). The extract was filtered under reduced pressure using ADVANTEC paper No. 6 (ADVANTEC Co., Tokyo, Japan) and concentrated using a vacuum concentrator (EYELA N-1000, Riakikai Co., Ltd., Tokyo, Japan) Lyophilized and used for the experiment.
< Experimental Example 1> In an ovariectomized animal model Triptych Identification of osteoporosis relief effect of extract
The ovariectomized model rat (rat) oocyte extract-induced osteoporosis relieving effect of the present invention was confirmed.
Specifically, the ovariectomized animal model was obtained by ovariectomized rats (Korean Central Laboratory Animal Room) ovariectomized by SD female rats (rat), and used for the experiment. The tubular extract of Example 1 was divided into 100 Kg / kg, and control group, which did not receive the extract of tubercle bark, for 12 weeks. Then, bone strength, bone density, bone weight and bone mineral content were measured. The bone strength was analyzed using a texture analyzer (System microsystems, UK). The bone strength was measured constantly at the mid-point of the bone with a pre-speed of 0.6 mm / sec, a test speed of 0.6 mm.sec, and a force of 0.005 kg. The bone mineral density (BMD) and bone mineral content (BMC) contents were measured using an animal-specific bone mineral density measuring device (
As a result, as shown in 1 to 4, it was confirmed that bone strength, bone density, bone mass and bone mineral content were increased in ovariectomized rats fed with tubercle leaf extract (FIGS. 1 to 4).
Claims (7)
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