CN115040546A - Application of gallnut extract and xylitol - Google Patents

Application of gallnut extract and xylitol Download PDF

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CN115040546A
CN115040546A CN202210172143.5A CN202210172143A CN115040546A CN 115040546 A CN115040546 A CN 115040546A CN 202210172143 A CN202210172143 A CN 202210172143A CN 115040546 A CN115040546 A CN 115040546A
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composition
xylitol
extract
present
hyperesthesia
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秋定何
张润禧
金智亨
金廷恩
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LG H&H Co Ltd
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LG Household and Health Care Ltd
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K35/00Medicinal preparations containing materials or reaction products thereof with undetermined constitution
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    • A23VINDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2200/00Function of food ingredients
    • A23V2200/30Foods, ingredients or supplements having a functional effect on health
    • A23V2200/312Foods, ingredients or supplements having a functional effect on health having an effect on dental health
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    • A23V2250/00Food ingredients
    • A23V2250/60Sugars, e.g. mono-, di-, tri-, tetra-saccharides
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    • A23V2250/6422Xylitol
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    • A61K2800/5922At least two compounds being classified in the same subclass of A61K8/18

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Abstract

The present invention relates to a composition comprising a gallnut extract and xylitol as active ingredients, which has a significant synergistic effect in preventing, ameliorating or treating hypersensitivity, gingival internal bleeding or toothache by suppressing inflammation in the oral cavity, suppressing bleeding and sealing dentinal tubules, has no side effect as a natural product, and can be safely and effectively used in the manufacture of pharmaceuticals, quasi drugs or foods, etc., and to the use of the gallnut extract and xylitol.

Description

Application of gallnut extract and xylitol
Technical Field
The invention relates to a composition containing gallnut extract and xylitol, and application of the gallnut extract and the xylitol in manufacturing the composition.
Background
Tooth hypersensitivity symptoms of teeth are symptoms that teeth are sensitive to external stimuli (temperature change, physical contact, drying of teeth, contact with substances such as chopsticks, osmotic pressure stimulation caused by sweet food or sour food, etc.) and are a phenomenon typically exhibited by hyperesthesia as a disease. In contrast to caries or other pathological causes, hyperesthesia is sensitive to external stimuli and exhibits temporary pain.
There are many theories that account for the hypersensitivity of teeth, but there is currently no single, well-established theory. The most widely accepted theory is the hydrodynamic theory proposed by Brannstrom in 1964. Regardless of the reason for the disappearance of enamel or cementum in the neck of the tooth, dentin thereunder is exposed without being protected from external stimuli, whereby the exposed dentin transmits all stimuli from the outside to nerves within the pulp, making it react more sensitively than usual to the same stimuli, and possibly inducing pain.
The mechanism of occurrence of this hypersensitivity is closely related to the structure of dentin. If physical stimulation, chemical stimulation, thermal stimulation, or the like is applied in a state where the dentinal tubules are directly open to the environment in the oral cavity, the liquid in the dentinal tubules moves inward and outward. It is quite fast and the pressure generated as the liquid moves affects the cells in the dental pulp, makes the cells elongate or contract, so that the change is sensed by the nerves contacting the cells and the stimulus is transmitted to the brain, thereby sensing pain.
Although this type of hyperesthesia is a common symptom experienced by 8 to 57% of adults, there is still a case where a therapeutic agent capable of immediately solving the hyperesthesia is lacking at present. In addition, since teeth cannot be regenerated due to their characteristics, administration of analgesic or anti-inflammatory agents cannot be the fundamental means for solving the hypersensitivity phenomenon.
Currently, there are two common methods of treatment being performed, according to the principle of action, one using nerve blockers to interfere with the signaling of the nerves that transmit pain, and one using various types of dental materials to occlude the dentinal tubules of the exposed dentin. However, the nerve blocking agent has a problem that it has a low pain blocking effect and a temporary effect, and thus it needs to be repeatedly used.
The method of plugging dentinal tubules is a method of filling exposed dentinal tubules with resin or the like or repairing damaged enamel anew by coating fluorine or the like. However, such a treatment has problems in that the clogged dental material is detached over time or symptoms are reproduced due to a gap generated at a boundary portion around the clogged dental material, and in that treatment needs to be performed in dentistry by a professional treatment method.
Therefore, there is a need to develop a product that is easily accessible to the general public and can safely prevent hyperesthetic symptoms in terms of personal hygiene management. In particular, it is still a problem to be solved to develop a material having a sufficient effect from among natural-source ingredients used in the human body which can be stably used in the oral cavity.
Disclosure of Invention
Problems to be solved by the invention
As a result of long-term studies for developing a material capable of safely maintaining oral health in terms of personal hygiene management, particularly capable of preventing and improving sensory hypersensitivity, it was confirmed that when nutgall extract and xylitol are used together, the effect of alleviating, improving or treating dental hypersensitivity, gingival internal bleeding or dental pain caused by sensory hypersensitivity is exhibited, and other side effects are not caused as a natural source component, and the present invention was confirmed.
Accordingly, an object of the present invention is to provide an oral composition which can be safely used in the oral cavity and has an excellent effect of alleviating, treating or improving oral diseases, and more specifically, to provide a composition for preventing, improving or treating hyperesthesia, gingival bleeding or toothache, which comprises a gallnut extract and xylitol.
In addition, the present invention is directed to the use of a gallnut extract and xylitol for the manufacture of the oral composition, and more specifically, to the use of a gallnut extract and xylitol for the manufacture of a composition for preventing, ameliorating or treating hyperesthesia, gingival bleeding or dental pain.
Means for solving the problems
In order to achieve the above object, according to one aspect of the present invention, there is provided a pharmaceutical composition for external use for preventing or improving hyperesthesia, gingival internal bleeding or toothache, comprising a galla chinensis extract and xylitol.
As another mode, there is provided a food additive composition for preventing or improving hyperesthesia, gingival internal bleeding or toothache, comprising a galla chinensis extract and xylitol.
As still another mode, there is provided a pharmaceutical composition for preventing or treating hyperesthesia, gingival bleeding or toothache, comprising a gallnut extract and xylitol.
As still another mode, there is provided an oral hygiene composition for preventing or improving hyperesthesia, gingival internal bleeding or toothache, comprising a gallnut extract and xylitol.
In addition, as an embodiment of the present invention, there is provided a use of a gallnut extract and xylitol for the manufacture of a composition for preventing, improving or treating hyperesthesia, gingival internal bleeding or toothache.
As another mode, there is provided a use of a gallnut extract and xylitol for manufacturing a pharmaceutical external composition for preventing or improving hyperesthesia, gingival internal bleeding or toothache.
As another mode, there is provided a use of the gallnut extract and xylitol for the manufacture of a pharmaceutical composition for preventing or treating hyperesthesia, gingival bleeding or dental pain.
As a further aspect, there is provided the use of an extract of galla chinensis and xylitol in the manufacture of an oral hygiene composition for preventing or ameliorating hyperesthesia, intra-gingival bleeding or dental pain.
As still another mode, there is provided a use of the gallnut extract and xylitol for manufacturing a food additive composition for preventing or improving hyperesthesia, gingival internal bleeding or toothache.
The gallnut extract may be an extract extracted using one or more solvents selected from the group consisting of alcohol (alcohol) having 1 to 6 carbon atoms, acetone (acetone), ether (ether), benzene (benzzene), chloroform (chloroform), ethyl acetate (ethyl acetate), methylene chloride (methylene chloride), hexane (hexane), cyclohexane (cyclohexane), petroleum ether (petroleum ether), and water.
The composition can prevent, ameliorate or treat hypersensitivity by sealing dentinal tubules.
The gallnut extract may be included in an amount of 0.001 to 10 parts by weight and the xylitol may be included in an amount of 0.001 to 10 parts by weight, relative to 100 parts by weight of the composition.
The hypersensitivity may be dentinal hypersensitivity.
Effects of the invention
The composition comprising the gallnut extract and xylitol according to the present invention has an effect of alleviating, improving or treating tooth sensitivity symptoms, gingival internal bleeding or toothache caused by hyperesthesia, does not cause other side effects as a natural source component, and can be effectively used for the manufacture of pharmaceuticals, quasi drugs or foods.
Drawings
Fig. 1 is a result of confirming the PGE2 inhibitory effect when treated with a composition comprising a gallnut extract, a composition comprising xylitol, or a composition comprising a gallnut extract and xylitol according to an embodiment of the present invention, respectively.
Fig. 2 is a result of confirming the results of suppressing the intra-gingival bleeding when treated with the composition comprising a gallnut extract, the composition comprising xylitol, or the composition comprising a gallnut extract and xylitol according to one embodiment of the present invention, respectively.
Fig. 3 is a result of confirming dentinal tubule occluding ability when a toothpaste containing a composition comprising a gallnut extract, a composition comprising xylitol, or a composition comprising a gallnut extract and xylitol according to an embodiment of the present invention, or a toothpaste not containing the above composition, respectively, is treated.
Detailed Description
The present inventors have found that, in the course of studying a safe oral material derived from a natural product, a remarkably excellent synergistic effect can be obtained in the case of containing a nutgall extract and xylitol, as compared with the case of using a single component, in terms of alleviating or treating hypersensitivity, gingival internal bleeding, and dental pain, and have completed the present invention.
The present invention will be further specifically described below.
The present invention relates to a composition for preventing, treating or ameliorating hyperesthesia, gingival internal bleeding or toothache, comprising an extract of Galla chinensis and xylitol.
The composition may be a pharmaceutical topical composition, a pharmaceutical composition, or an oral hygiene composition.
The composition may be a food additive composition.
The present invention also relates to pharmaceutical preparations, foods and pharmaceuticals containing the various compositions.
In addition, the invention relates to the use of Galla rhois extract and xylitol in the manufacture of various said compositions.
In the present invention, Galla chinensis (scientific name: Gallnut) refers to gall produced by the parasite of the aphid family Homoptera Gallnut on the leaf of Rhus chinensis (Galla chinensis) of Anacardiaceae. The medicine is empty, has sour taste, and has astringent, hemostatic, toxic materials clearing away, and antibacterial effects in Chinese medicine, so as to be used for treating diarrhea, rectocele, gastric ulcer, duodenal ulcer, night sweat, spermatorrhea, bloody stool, hematuria, etc. The gallnut contains about 50 to 60% of tannin (tannin) component, and thus is used as a raw material of a hair dye or ink including a tanning agent.
In the present invention, xylitol is a compound having the structure of the following formula 1, and it is known that xylitol has an effect of preventing dental caries by inhibiting dissolution of enamel in teeth by the action of acid generated when sugar is decomposed. Mainly used as a sweetener.
[ structural formula 1]
Figure BDA0003518684340000051
The composition of the present invention is characterized by comprising the galla chinensis extract and xylitol together, thereby preventing, treating or improving hyperesthesia, toothache or gingival internal bleeding. In particular, it was confirmed by specific examples that by simultaneously containing the gallnut extract and xylitol, a significant synergistic effect can be obtained in terms of alleviating or treating the symptoms.
The composition of the present invention may comprise 0.001 to 10 parts by weight of the gallnut extract and 0.001 to 10 parts by weight of xylitol, relative to 100 parts by weight of the total composition. In this case, the synergistic effect based on the combination of the gallnut extract and xylitol is more excellent, and thus a significant effect of preventing, treating, or improving hyperesthesia, toothache, or gingival internal bleeding can be obtained.
The gallnut extract and xylitol may be mixed to contain them in a weight ratio of 1:0.1 to 10. The composition within the range has remarkable effects in inhibiting toothache, improving gingival internal bleeding and dentinal tubule blocking ability.
In the present invention, "hyperesthesia" is a symptom in which teeth sensitively respond to external stimuli (temperature change, physical contact, drying of teeth, contact with substances such as chopsticks, osmotic pressure stimulation caused by sweet food or sour food, etc.), accompanied by tooth hypersensitivity. Hypersensitivity is a symptom that is distinguished from the existing pathological causes of caries or other periodontal diseases, and basically dentin is exposed to the outside, causing sensitive parts to react sensitively. Since symptoms such as tooth sensitivity occur due to exposed dentin, the present invention also includes a preventive, ameliorating or therapeutic effect against tooth sensitivity.
For the treatment or alleviation of hyperesthesia, methods are used to block/interfere with nerve signaling using nerve blockers or to block sensitive sites from external stimuli by closing dentinal tubules. These methods have problems in that the nerve blocking agent has a low effect of blocking pain and acts temporarily, and thus the effect of relief or treatment is not great.
However, the composition of the present invention, which comprises the gallnut extract and xylitol together, has a remarkable synergistic effect in terms of occluding dentinal tubules, thereby being capable of obtaining an excellent effect of improving or treating hyperesthesia.
In this regard, the composition of the present invention may be for preventing, ameliorating or treating hypersensitivity by occluding dentinal tubules, and in the present invention, the hypersensitivity may be dentinal hypersensitivity.
In the present specification, the term "extract" refers to a substance from which an active ingredient or characteristic ingredient is separated by dissolving the substance in a solvent, and specifically, in the present invention, includes: an extract extracted by adding an extraction solvent to a plant; and a separation product separated (fractionation) by adding a separation solvent to the extract extracted and produced with the extraction solvent.
The extraction solvent may be one or more selected from the group consisting of water, an organic solvent, a subcritical fluid, and a supercritical fluid. The organic solvent may be a polar solvent, a non-polar solvent, a mixed solvent of a polar solvent and a non-polar solvent, or water. Specifically, the solvent may be any one selected from the group consisting of alcohol (alcohol) having 1 to 6 carbon atoms, acetone (acetone), ether (ether), benzene (bezene), chloroform (chloroform), ethyl acetate (ethyl acetate), methylene chloride (methylene chloride), hexane (hexane), cyclohexane (cyclohexane), petroleum ether (petroleum ether), and water.
As a preferable example, it may be an ethanol extract, more specifically, an aqueous ethanol extract of 30 to 80%. In this case, by combining with xylitol, a significant synergistic effect is exhibited in terms of alleviating hyperesthesia, toothache, or gingival internal bleeding.
The method for producing the extract of the present invention may be a method generally used in the art to which the present invention pertains, and the right of the present invention is not limited to a specific extraction method.
Therefore, the gallnut extract of the present invention includes an extract extracted by adding a solvent to gallnuts and an isolate separated by adding a separation solvent again to the extract.
In one embodiment of the present invention, ethanol is preferably used as the extraction solvent, since it is confirmed that a composition comprising a combination of ethanol extract of gallnut and xylitol has a remarkable synergistic effect in suppressing PGE2 associated with toothache, improving gingival bleeding and tooth sensitivity, and sealing dentinal tubules.
The extract can be produced according to a conventional method for producing an extract. More specifically, it can be performed by a method of adding an extraction solvent to the extraction target from which impurities are removed and performing an extraction process. The extraction process may be cold soaking extraction, hot soaking extraction, pressure extraction or ultrasonic pulverizing extraction.
The separation solvent may be water, butanol, ethyl acetate, chloroform, hexane or a mixture of these. The isolate may be an extract produced by the extraction method, and specifically, may be an isolate obtained by further performing a separation process on a crude extract. The separation solvent may be a solvent selected from the group consisting of ethyl acetate, diethyl ether, chloroform, benzene, hexane, dichloromethane, and a mixed solvent thereof. More specifically, the separation process may be carried out by adding a separation solvent to the crude extract to carry out separation to obtain a layered isolate. In addition, a layered isolate can be obtained by performing separation by adding a separation solvent to the isolate again.
After the extraction process or the separation process, the extract or the isolate may be subjected to a reduced pressure filtration process or further concentration and/or freeze-drying, thereby concentrating or removing the solvent. The extract obtained can be kept in a deep freezer (deep freezer) until use.
The separation may use techniques such as solvent separation, silica gel chromatography (silica gel chromatography), preparative high performance liquid chromatography (prep-HPLC) to produce a specific isolate in which the active substance is concentrated.
In this specification, "prevention" refers to all actions that inhibit or delay the onset of a disease or condition. In the present invention, it means to delay the onset of inflammation, the occurrence of gingival internal congestion or bleeding due to some cause, or the onset of symptoms due to hypersensitivity caused by exposure to dentin, or to suppress the onset of such symptoms.
In the present specification, "improvement" refers to all actions that improve or beneficially modify the state of a disease or condition, and in the present invention, refers to improvement of symptoms caused by the occurrence of inflammation, the occurrence of gingival congestion or bleeding due to some cause, or hypersensitivity due to exposure to dentin.
In the present specification, "treatment" refers to all actions that delay, halt or reverse the progression of a disease or condition, and in the present invention, refers to halting, reducing, alleviating, eliminating or reversing the occurrence of inflammation, the occurrence of intra-gingival congestion or bleeding due to some cause, or the symptoms caused by hypersensitivity due to exposure to dentin.
In one embodiment of the present invention, it was confirmed that the occurrence of inflammation, the occurrence of congestion or bleeding in the gum can be suppressed, or the toothache, the bleeding in the gum, or the sensory hypersensitivity can be prevented or treated by the treatment with the gallnut extract and xylitol, or by the occlusion of dentinal tubules of the dentin.
Thus, the present invention can provide the use of the Galla chinensis extract and xylitol for the production of pharmaceutical compositions and pharmaceutical products for preventing or ameliorating hyperesthesia, gingival internal bleeding or dental pain, and can also provide the use of the Galla chinensis extract and xylitol for the production of pharmaceutical compositions or pharmaceutical products for preventing or treating hyperesthesia, gingival internal bleeding or dental pain.
In addition, the composition of the present invention may be a composition for dentinal tubule occlusion, a pharmaceutical composition for preventing or treating hyperesthesia or dentinal hyperesthesia.
The pharmaceutical composition includes a composition intended for a human subject and a composition intended for an animal other than a human subject, and the pharmaceutical composition intended for an animal other than a human subject includes all animal drugs, pharmaceutical intermediates, and pharmaceutical products other than drugs.
In addition to the above active ingredients, the compositions of the present invention may also contain more than one active ingredient having the same or similar function. The prophylactic or therapeutic effect of the composition of the present invention can be further enhanced if additional ingredients are included. When the above components are added, the stability of the combination, the ease of formulation, and the stability of the active ingredients can be considered. Said additional ingredients may be included in an amount of from more than 0.0001% to less than 10% by weight relative to the total weight of the composition. For example, it may be 0.0001% by weight or more and 1% by weight or less, 0.0001% by weight or more and 0.1% by weight or less, 0.0001% by weight or more and 0.001% by weight or less, 0.001% by weight or more and 10% by weight or less, 0.001% by weight or more and 1% by weight or less, 0.001% by weight or more and 0.1% by weight or less, 0.01% by weight or more and 10% by weight or less, 0.01% by weight or more and 1% by weight or less. The content range can be adjusted according to requirements such as stability and ease of formulating the composition of the present invention.
In addition, the pharmaceutical composition of the present invention may further comprise a pharmaceutically acceptable carrier.
The pharmaceutically acceptable carrier may further include, for example, a carrier for oral administration or a carrier for non-oral administration. The carrier for oral administration may include lactose, starch, cellulose derivatives, magnesium stearate, stearic acid, and the like. The carrier for parenteral administration may include water, an appropriate oil, saline, an aqueous glucose solution, ethylene glycol, and the like. In addition, stabilizers and preservatives may also be included. As suitable stabilizers there are antioxidants such as sodium bisulfite, sodium sulfite or ascorbic acid. As suitable preservatives there are benzalkonium chloride, methyl or propyl p-hydroxybenzoate and chlorobutanol. As other pharmaceutically acceptable carriers, reference may be made to the carriers described in the following documents: remington's Pharmaceutical Sciences,19th ed., Mack Publishing Company, Easton, PA, 1995.
The pharmaceutical compositions of the present invention may be administered to mammals, including humans, by a method. For example, the administration may be oral or non-oral, and as a non-oral administration method, intravenous, intramuscular, intraarterial, intramedullary, intradural, intracardiac, transdermal, subcutaneous, intraperitoneal, intranasal, intestinal, topical, sublingual or intrarectal administration is possible, but not limited thereto.
The pharmaceutical composition of the present invention may be formulated into oral administration preparations or non-oral administration preparations according to the administration routes as described above. In the case of being formulated, the formulation may be prepared using one or more buffers (e.g., saline or PBS), carbohydrates (e.g., glucose, mannose, sucrose, or dextran, etc.), antioxidants, bacteriostats, chelating agents (e.g., EDTA or glutathione), fillers, extenders, binders, adjuvants (e.g., aluminum hydroxide), suspending agents, thickening agents, wetting agents, disintegrating agents or surfactants, diluents, or excipients.
Solid preparations for oral administration include tablets, pills, powders, granules, liquids, gels, syrups, slurries, suspensions, capsules, and the like, and these solid preparations can be prepared by mixing at least one or more excipients, for example, starch (including corn starch, wheat starch, rice starch, potato starch, and the like), Calcium carbonate (Calcium carbonate), Sucrose (Sucrose), Lactose (Lactose), dextrose, sorbitol, mannitol, xylitol, erythritol, maltitol, cellulose, methyl cellulose, sodium carboxymethyl cellulose, hydroxypropyl methyl cellulose, gelatin, and the like, with the pharmaceutical composition of the present invention. For example, after mixing the active ingredient with a solid excipient, these are pulverized and appropriate adjuvants are added, followed by processing into a mixture of granules, thereby obtaining a tablet or a sugar-coated tablet.
In addition to simple excipients, lubricants such as magnesium stearate, talc are also used. The liquid preparations for oral administration include suspensions, solutions for internal use, emulsions, syrups and the like, and may contain various excipients such as wetting agents, sweeteners, aromatics, preservatives and the like in addition to water or liquid paraffin, which are generally used simple diluents.
In addition, as a disintegrating agent, cross-linked polyvinylpyrrolidone, agar, alginic acid, sodium alginate, or the like may be added according to circumstances, and an anti-agglomerating agent, a lubricant, a wetting agent, a fragrance, an emulsifier, a preservative, or the like may be further included.
In the case of parenteral administration, the pharmaceutical composition of the present invention may be formulated into a dosage form in the form of injection, transdermal preparation and nasal inhalation preparation according to a method known in the art, together with a suitable parenteral carrier. In the case of the injection, it must be sterilized and protected from contamination by microorganisms such as bacteria and fungi. In the case of an injection, as examples of suitable carriers, there may be mentioned water, ethanol, polyhydric alcohols (e.g., glycerin, propylene glycol, and liquid polyethylene glycol, etc.) and mixtures of these and/or solvents or dispersion media including vegetable oils, but not limited thereto.
When the pharmaceutical composition of the present invention comprises an effective amount of the active ingredient, it can provide an effect of preventing, ameliorating or treating hyperesthesia, gingival internal bleeding or toothache. In the present specification, the "effective amount" refers to an amount showing a reaction higher than that in the negative control group, and preferably means an amount sufficient for preventing, ameliorating or treating hypersensitivity, gingival bleeding or toothache. The gallnut extract and the xylitol can be contained in the pharmaceutical composition of the invention by 0.01 to 99.99 percent, and the rest can be occupied by pharmaceutically allowable carriers. The effective amounts of the Galla rhois extract or its isolate and xylitol contained in the pharmaceutical composition of the present invention may vary depending on the form of the composition in which it is formulated, etc.
The total effective amount of the pharmaceutical composition of the present invention may be administered to a patient in a single dose (single dose), or may be administered by a fractionated therapy (fractionated treatment protocol) in which multiple doses (multiple doses) are administered over a long period of time. The pharmaceutical composition of the present invention may vary the content of the effective ingredient depending on the severity of the disease. For example, the administration may be carried out in one or more divided doses, preferably in an amount of 0.001 to 100mg, more preferably in an amount of 0.01 to 10mg per 1kg body weight per day, based on the Galla chinensis extract and xylitol. However, the effective dose of the Galla chinensis extract and xylitol to a patient is determined not only by the route of administration and the number of treatments of the pharmaceutical composition, but also by various factors such as the age, body weight, health status, sex, severity of the disease, diet and excretion rate of the patient, and therefore, considering this, one of ordinary skill in the art can determine an appropriate effective dose according to the specific use of the Galla chinensis extract and xylitol for treating or improving hypersensitivity, gingival bleeding or toothache. The pharmaceutical composition according to the present invention is not particularly limited in its dosage form, administration route, and administration method as long as the pharmaceutical composition exhibits the effects of the present invention.
The pharmaceutical composition for preventing or treating hyperesthesia, gingival internal bleeding or toothache of the present invention can be used alone or in combination with surgery, radiotherapy, hormone therapy, chemotherapy or a method using a biological response modifier.
The composition for preventing or treating hyperesthesia, gingival internal bleeding or toothache of the present invention can be provided as a pharmaceutical external product containing a gallnut extract and xylitol as active ingredients. In this regard, the composition of the present invention may be a pharmaceutical external composition for preventing or improving hyperesthesia, gingival internal bleeding or toothache and a pharmaceutical external comprising the same. The external medicine can be directly applied to the skin or the oral cavity. In the case where the composition of the present invention is used as an external preparation, the composition may further contain any auxiliary agent generally used in the field of dermatology, such as a fatty material, an organic solvent, a solubilizer, a thickener, a gelling agent, a softener, an antioxidant, a suspending agent, a stabilizer, a foaming agent, a fragrance, a surfactant, water, an ionic emulsifier, a nonionic emulsifier, a filler, a metal ion blocking agent, a chelating agent, a preservative, a vitamin, a blocking agent, a wetting agent, essential oils, a dye, a pigment, a hydrophilic activator, a lipophilic activator, or a lipid vesicle. In addition, the ingredients may be introduced in amounts commonly used in the dermatological field.
In the case where the composition of the present invention is provided as a topical agent, it may be in the form of a liquid, ointment, patch, gel, cream, spray, or the like, but is not limited thereto.
According to an embodiment of the present invention, the external pharmaceutical product of the present invention may include an oral care product including toothpaste, water in the mouth, and an oral spray, ointment, pack agent, wet cloth agent, patch agent, transdermal absorbent, and the like.
In one embodiment of the present invention, it was confirmed that the treatment with the gallnut extract and xylitol has the effects of alleviating hypersensitivity, gingival internal bleeding, or dental pain and improving hypersensitivity by occluding dentinal tubules, and that when the active ingredient according to the present invention is used in an oral care product, the symptoms of hypersensitivity, gingival internal bleeding, or dental pain and the symptoms caused by these symptoms can be improved. Therefore, the pharmaceutical external composition may be an oral hygiene composition for preventing or improving hyperesthesia, gingival internal bleeding or toothache. Further, there can be provided use of Galla chinensis extract and xylitol for manufacturing an oral hygiene composition for preventing or improving sensory hypersensitivity, gingival internal bleeding or toothache.
The composition for external pharmaceutical use of the present invention may be prepared by adding the extract of Galla chinensis and xylitol directly or by using the extract of Galla chinensis and xylitol together with other ingredients for external pharmaceutical use according to a conventional method. The mixing amount of the effective ingredient may be appropriately determined depending on the purpose of use (preventive, health care or therapeutic treatment).
The pharmaceutical composition and the food composition of the present invention can be applied to the pharmaceutical composition and the pharmaceutical product of the present invention.
In another aspect, the composition of the present invention relates to a food composition for preventing or improving hyperesthesia, gingival bleeding or toothache.
The food composition may be a health functional food composition.
The food composition may be a food additive composition.
In addition to foods intended for humans, the food composition includes foods intended for animals other than humans, and the foods intended for animals other than humans include, for example, animal feeds, animal feed (food) additives, animal supplementary foods, and the like to which feed management laws are applied.
In one embodiment of the present invention, it was confirmed that the symptoms of hypersensitivity including toothache, gingival bleeding or tooth hypersensitivity including tooth hypersensitivity can be improved by inhibiting inflammation, inhibiting bleeding and occluding dentinal tubules when treated with the gallnut extract and xylitol.
Thus, the present invention also provides the use of the gallnut extract and xylitol for the manufacture of a food composition or food for preventing or ameliorating hyperesthesia, gingival bleeding or dental pain.
The food composition of the present invention includes all forms of functional foods (functional foods), nutritional supplements (nutritional supplements), health foods (health foods), food additives (food additives), and feeds, and is intended for ingestion by animals including humans and domestic animals.
Food compositions of the above-mentioned kind may be manufactured in various forms according to conventional methods well known in the art. The general food can be produced by adding the above-mentioned nutgall extract and xylitol to a beverage (including alcoholic beverages), fruit and processed foods thereof (e.g., canned fruits, bottled foods, jams, marmalade, etc.), fish, meat and processed foods thereof (e.g., ham, sausage, beef with salt, etc.), bread and pasta (e.g., udon, buckwheat noodles, pasta, macaroni, etc.), fruit juice, various drinks, cookies, caramel, dairy products (e.g., butter, cheese, etc.), edible vegetable oils and fats, margarine, vegetable proteins, steamed foods, frozen foods, various seasonings (e.g., doenjang, soy sauce, etc.), etc., but is not limited thereto.
In addition, the nutritional supplement can be produced by adding the gallnut extract and xylitol to capsules, tablets, pills, and the like, but is not limited thereto.
In addition, as a health functional food, for example, the galla chinensis extract and xylitol themselves can be liquefied, granulated, encapsulated, and powdered to be made into tea, juice, and drink forms, and can be drunk (health drink) for ingestion. In addition, in order to use the gallnut extract and xylitol in the form of a food additive, they may be manufactured and used in the form of a powder or a concentrated solution. Alternatively, the Galla rhois extract and xylitol may be mixed together with additional known active ingredients and then made into the form of a composition.
In the case where the food composition of the present invention is used as a health drink composition, the health drink composition may contain various flavors or natural carbohydrates, etc. as additional ingredients, as in conventional drinks. The above natural carbohydrates may include: monosaccharides such as glucose, fructose; disaccharides, such as maltose, sucrose; polysaccharides, such as dextrin, cyclodextrin; and sugar alcohols such as xylitol, sorbitol, erythritol, and the like. The sweetener can be natural sweetener such as thaumatin and stevia extract; synthetic sweeteners such as saccharin, aspartame, and the like. The natural carbohydrate ratio is generally about 0.01 to 0.04g, preferably about 0.02 to 0.03g per 100mL of the composition of the invention.
The gallnut extract and xylitol may be contained as an active ingredient in a food composition for preventing or improving hypersensitivity, gingival internal bleeding or toothache in an amount effective to achieve the effect of preventing or improving hypersensitivity, gingival internal bleeding or toothache, preferably 0.002 to 20% by weight relative to the total weight of the entire composition, but are not particularly limited. The food composition of the present invention can be manufactured by mixing the gallnut extract and xylitol together with additional other active ingredients.
In addition to the above, the health food of the present invention may contain various nutrients, vitamins, electrolytes, flavoring agents, coloring agents, pectic acids, pectates, alginic acids, alginates, organic acids, protective colloid thickeners, pH regulators, stabilizers, preservatives, glycerin, alcohols, or carbonating agents, etc. In addition to these, the health food of the present invention may further contain pulp used for manufacturing natural fruit juice, fruit juice beverages, or vegetable beverages. These components may be used alone or in admixture thereof. The ratio of these additives, although not critical, is generally selected in the range of 0.0001 to 0.1 parts by weight per 100 parts by weight of the composition of the present invention.
Hereinafter, the present invention will be described in more detail by examples. While the invention is susceptible of various modifications and alternative forms, specific embodiments and details are set forth below only to aid in the understanding of the invention, and are not intended to limit the invention to the specific forms disclosed. It should be understood that the scope of the present invention includes all modifications, equivalents, and alternatives falling within the spirit and technical scope of the present invention.
[ examples ]
Example 1 preparation of Galla rhois extract
The Galla chinensis extract is obtained by adding 50% ethanol at a ratio of 1:10 (sample: solvent) to pulverized or minced dried sample of Galla chinensis, heating to 60 deg.C and extracting for about 3 hours, and then filtering and concentrating the extracted solution. In order to use the gallnut extract obtained as described above in the experiment, it was dissolved in purified water for use.
Experimental example 1 PGE2 inhibitory Effect as a marker of pain and inflammation
In order to confirm the effect of preventing and ameliorating dental pain in a composition comprising a gallnut extract or a composition comprising a gallnut extract and xylitol, the inhibitory effect of PGE2 as a marker of pain and inflammation was confirmed.
First, human macrophages (THP-1) were cultured in RPMI medium containing 10% FBS at 1.5X 10 5 cells/mL were plated onto 24-well plates (well plates) at 37 ℃ and 5% CO 2 Cultured under the conditions of (1) for 24 hours. Then, a sample containing 500ppm of a Galla chinensis extract, a sample containing 500ppm of xylitol, or a mixed sample containing 250ppm of a Galla chinensis extract and 250ppm of xylitol (Galla chinensis extract: xylitol in a 1:1 weight ratio) were treated, respectively, and after 1 hour, 1. mu.g/mL of LPS (lipopolysaccharide) as an inflammation stimulus was treated and further cultured for 23 hours. The amount of PGE2 in the cell culture solution was confirmed by using a PGE2 ELISA assay kit (seimer feishol), thereby confirming the PGE2 inhibitory effect of each sample.
As shown in fig. 1, the gallnut extract alone-treated group showed about 38% of the inhibitory effect of PGE2 and the xylitol alone-treated group showed about 17% of the inhibitory effect of PGE2, when compared with the control group treated with LPS only. However, PGE2 was inhibited by about 75% in the group treated with nutgall extract and xylitol at the same time. From this, it was found that the PGE 2-inhibiting effect was significantly increased when the gallnut extract and xylitol were mixed, in particular, as compared with the case where the gallnut extract alone was used.
Therefore, it is found that the mixture of the gallnut extract and xylitol has a remarkable effect of suppressing toothache as compared with the single-component treated group.
Experimental example 2 hemorrhage suppressing Effect
In order to find the effect of the composition of the gallnut extract, the composition of xylitol, and the mixed composition of the gallnut extract and xylitol on preventing and improving bleeding, experiments were performed using the blood vessels of the urinary membrane of the chorionic membrane of a fertilized egg.
First, fertilized eggs incubated over 10 days were irradiated with a vertical lamp, the shell on one side of the air cell was broken, and the urinary membrane of the chorion was removed, followed by pretreatment with water as a control group and each sample. As experimental groups, a sample containing 1 wt% of the gallnut extract, a sample containing 1 wt% of xylitol, and a sample containing both 0.5 wt% of the gallnut extract and 0.5 wt% of xylitol were used, respectively. After 30 seconds, the blood vessels were stimulated by treatment with 5% Sodium Lauryl Sulfate (Sodium Lauryl Sulfate), and the degree of bleeding was confirmed every 30 seconds.
[ Table 1]
Figure BDA0003518684340000141
As is clear from the results shown in fig. 2 and table 1, bleeding occurred more frequently in the control group after only 30 seconds, whereas bleeding did not occur in the 1% of the gallnut extract after 30 seconds, and bleeding did not occur in the group treated with the gallnut extract and xylitol together even after 1 minute. In particular, the bleeding suppressing effect in the group treated with xylitol together was significantly superior to that when only the gallnut extract was used. Therefore, it is known that the mixture of the gallnut extract and xylitol has a significant effect in preventing, treating, or improving gingival bleeding.
Experimental example 3 inhibitory Effect on dental hypersensitivity
In order to know the effect of the gallnut extract or the composition comprising the gallnut extract and xylitol on preventing or improving tooth hypersensitivity, a subject was selected and subjected to clinical trials.
First, a control toothpaste was prepared using sodium carboxymethylcellulose, sodium lauryl sulfate, glycerin, colloidal silicon dioxide, silicas, sodium cocoyl isethionate, doxycycline (dodicin), sweetener, flavoring agent, coloring agent, and the like, which are commonly used in the manufacture of toothpaste,
the experimental group toothpastes were manufactured in such a manner that the control group toothpastes contained 0.01 wt% of the gallnut extract, 0.01 wt% of xylitol, and 0.005 wt% of the gallnut extract and 0.005 wt% of xylitol, respectively, with respect to the total toothpaste compositions.
The subjects were 40 volunteers who agreed to participate in the test as the persons having dentin hypersensitivity teeth, and 80 teeth were counted as the total subjects. In addition, 20 of the subjects were male, 20 were female, and the age was between 20 and 50 years. Subjects were not allowed to know the toothpaste contents and the total experimental period was set to 2 weeks.
The experiment is performed by a method of measuring the response of the subject after application of a temperature stimulus. Before the experiment, the sensitive part of the dentin hypersensitive tooth of each test subject was examined in advance, cold water of about 5 ℃ was dropped on the sensitive part of the tooth with a dropper, and after the evaluation was performed according to the criteria shown in table 2 below, the control group toothpaste was required to be used three times a day for 2 weeks, the test group toothpaste was required to be used three times a day for 2 weeks, and after 2 weeks, cold water of about 5 ℃ was dropped with a dropper and the evaluation was performed. Statistical treatment the stimulation scores before and after 2 weeks of experiment were tested by the corresponding specimen T-test (paired Student-T test), and the response scores after 2 weeks to temperature stimulation are shown in table 3 below (scoring criteria for the experimental subjects after stimulation).
[ Table 2]
Score of Content providing method and apparatus
0 Has no discomfort
1 Slightly uncomfortable or cold
2 Very cool
3 Pain (due to cold or dampness)
[ Table 3]
Figure BDA0003518684340000161
As shown in the above table 3, the experimental group using the toothpaste comprising the gallnut extract or the toothpaste comprising the gallnut extract and xylitol suppressed the tooth sensitivity phenomenon after 2 weeks, compared to the control group. In addition, the toothpaste comprising the gallnut extract and xylitol had a more excellent effect of suppressing tooth sensitivity than the toothpaste comprising the gallnut extract alone. Therefore, it is known that the galla chinensis extract or the composition comprising the galla chinensis extract and xylitol has a significant effect on the treatment, prevention or improvement of dental hypersensitivity.
EXAMPLE 4 evaluation of dentinal tubule blocking Capacity (dentine coverage)
In order to fundamentally treat hyperesthesia that causes tooth hypersensitivity symptom or the like, an experiment was conducted to confirm whether or not the composition according to the present invention has an effect of occluding dentinal tubules.
As a control toothpaste, a toothpaste was made containing sodium carboxymethylcellulose, sodium lauryl sulfate, glycerin, colloidal silicon dioxide, silicas, sodium cocoyl isethionate, doxine, sweetener, fragrance, and colorant.
The experimental group toothpaste according to the present invention was manufactured such that the control group toothpaste contained 0.01 wt% of the gallnut extract (comparative example 1), 0.01 wt% of xylitol (comparative example 2), and 0.005 wt% of the gallnut extract and 0.005 wt% of xylitol (example 1), respectively, with respect to the total toothpaste composition.
After the toothpaste composition was dispersed in the artificial saliva at a weight ratio of 1:3 (toothpaste composition: artificial saliva), an image of the dentinal tubule blocking effect of the toothpaste was taken using a differential scanning microscope, and the result was confirmed. Specifically, dentinal tubules were exposed by grinding the surface of a caries specimen, and then the specimen whose surface was delimed with a citric acid solution was repeatedly treated with a control group of toothpaste and artificial saliva or a test group of toothpaste and artificial saliva, respectively, 20 times.
The treated sample was washed with distilled water, dried, and observed with a scanning electron microscope Image (SEM Image). The SEM Image results were evaluated under the following 6 point standard, and 3 points or more were judged to be effective.
[ evaluation standards ]
6: after the surface is completely covered, a multi-layer (multi-layer) is formed.
5: the dentinal tubules were blocked, completely covering the dentinal surface.
4: penetrate into the interior of the dentinal tubules and cover a portion of the surface.
3: the surface of dentinal tubules and dentin is covered by more than 50%.
2: deposits were observed on the surface of dentinal tubules and dentin, and were covered by 50% or less.
1: the dentinal tubules were not occluded.
[ Table 4]
Figure BDA0003518684340000171
As shown in the above table 4 and fig. 3, it was confirmed that in the case of the experimental group containing the gallnut extract and xylitol together, the dentinal tubule occluding ability was significantly improved as compared to the group of the gallnut extract alone. Therefore, considering that the composition of the present invention can alleviate hypersensitivity of teeth by closing dentinal tubules, it is known that the effect of improving, treating or preventing hyperesthesia is high.

Claims (7)

1. Use of an extract of Galla rhois and xylitol in the manufacture of a composition for preventing, ameliorating or treating hyperesthesia, gingival internal bleeding or dental pain.
2. The use of Galla rhois extract and xylitol according to claim 1, wherein,
the Galla chinensis extract is extracted with at least one solvent selected from the group consisting of C1-6 alcohol, acetone, diethyl ether, benzene, chloroform, ethyl acetate, dichloromethane, hexane, cyclohexane, petroleum ether and water.
3. The use of Galla rhois extract and xylitol according to claim 1, wherein,
the composition prevents, ameliorates or treats hyperesthesia by sealing dentinal tubules.
4. The use of Galla rhois extract and xylitol according to claim 1, wherein,
the composition comprises 0.001 to 10 parts by weight of a gallnut extract and 0.001 to 10 parts by weight of xylitol, relative to 100 parts by weight of the composition.
5. The use of Galla chinensis extract and xylitol according to claim 1, wherein,
the hyperesthesia is dentinal hyperesthesia.
6. The use of Galla rhois extract and xylitol according to claim 1, wherein,
the composition is a pharmaceutical composition, a pharmaceutical composition or an oral hygiene composition.
7. The use of Galla rhois extract and xylitol according to claim 1, wherein,
the composition is a food additive composition.
CN202210172143.5A 2021-02-25 2022-02-24 Application of gallnut extract and xylitol Pending CN115040546A (en)

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