CN106163497A - Halitosis suppression oral cavity composition - Google Patents

Halitosis suppression oral cavity composition Download PDF

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Publication number
CN106163497A
CN106163497A CN201480077603.XA CN201480077603A CN106163497A CN 106163497 A CN106163497 A CN 106163497A CN 201480077603 A CN201480077603 A CN 201480077603A CN 106163497 A CN106163497 A CN 106163497A
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extract
oral cavity
percentage
cavity composition
halitosis
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张善五
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Spend Ibero American Pharmaceutical Corp
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Spend Ibero American Pharmaceutical Corp
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36Carboxylic acids; Salts or anhydrides thereof
    • A61K8/365Hydroxycarboxylic acids; Ketocarboxylic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783Angiosperms [Magnoliophyta]
    • A61K8/9789Magnoliopsida [dicotyledons]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36Carboxylic acids; Salts or anhydrides thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67Vitamins
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67Vitamins
    • A61K8/678Tocopherol, i.e. vitamin E
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/92Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
    • A61K8/922Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/965Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution of inanimate origin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/59Mixtures
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/59Mixtures
    • A61K2800/592Mixtures of compounds complementing their respective functions
    • A61K2800/5922At least two compounds being classified in the same subclass of A61K8/18
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/80Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof

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Abstract

Relate to a kind of oral cavity composition, this oral cavity composition comprises Radix Scutellariae extract and Herba Schizonepetae extract as neccessary composition, and comprise on this basis containing Fructus Forsythiae extract, the crude drug extract of Flos Lonicerae extract and Radix Platycodonis extract etc., and the most also comprise tocopheryl acetate and malic acid, thus to suppression halitosis, suppression tooth decays disease and suppression periodontal disease has excellent effect, this oral cavity composition is characterised by, comprise: the mixture of the crude drug extract comprising Radix Scutellariae extract and Herba Schizonepetae extract of 0.1 percentage by weight to 5.0 percentage by weights;The tocopheryl acetate of 0.01 percentage by weight to 1.0 percentage by weights;And 0.01 percentage by weight to the malic acid of 1.0 percentage by weights.

Description

Halitosis suppression oral cavity composition
Technical field
The present invention relates to halitosis suppression oral cavity composition, especially, relate to following oral cavity composition: comprise Radix Scutellariae and carry Take thing and Herba Schizonepetae extract as neccessary composition, and comprise on this basis containing Fructus Forsythiae extract, Flos Lonicerae extract and Fructus Citri tangerinae The crude drug extract of stalk extract etc., and the most also comprise tocopheryl acetate (Acetic acid Tocopherol) and malic acid, thus to suppression halitosis, suppression tooth decay disease and suppression periodontal disease has the effect of excellence Really.
Background technology
Decayed tooth is that the carbohydrate in food is present on gum and the microorganism of facing bacterial membrane under gum and metabolism, Cause the disease that the sclerous tissues of tooth destroys from there through the effect of the organic acid locally produced, the prevention to decayed tooth not only exists China, also receives much concern in worldwide.The not direct relation of the life to people although decaying tooth, but it causes food Masticatory function decline, therefore the disease on digestive system brings direct or indirect impact.Decayed tooth is the most multiple in child, In the middle of 5 years old child, the child of up to 85% the most once by or enduring the misery of decayed tooth to the fullest extent.Such decayed tooth is especially by mouth Streptococcus mutans (Streptococcs mutans:S.mutans) in the middle of the microorganism of intracavity and cause, its microorganism lead The decayed tooth initiation mechanism caused is as follows: Streptococcus mutans resides in intraoral facing as Grain-positive facultative anaerobe Bacterial membrane, decomposes the carbohydrate being included in food, particularly glucose, fructose etc., will be in its metabolic process The organic acid as by-product of middle generation, main that lactic acid is released to antibacterial is outer and destroy the enamel of tooth (Jin Zhong trains it He, public's oral cavity health, consultant, pp68-84,1991).
It was reported title, in most cases, halitosis be because of host component and food waste in oral cavity by antibacterial Rot and cause, in the reason of more than 85% is oral cavity.As intraoral reason, there is tongue fur, periodontal disease, uncleanly Many reasons such as oral hygiene state, food debris, improperly dental filling thing, antihygienic artificial tooth, mouth neoplasm, and currently as The most important reason of halitosis and referred tongue fur and periodontal disease.Volatile sulfur compounds (volatile sulfur Compounds:VSC) as the principal element of halitosis, there is hydrogen sulfide (hydrogen sulfide:H2S), methanthiol (methyl Mercaptan:CH3SH), dimethyl sulfide (dimethyl sulfide:CH3SCH3) etc., wherein hydrogen sulfide and methanthiol account for About 90%.Such VSC mainly (especially, is comprised half by by level in gingival sulcus fluid, saliva, the protein that is included in food debris Cystine (cysteine) and methionine (methionine)), peptide, aminoacid etc. be utilized as anaerobic in the oral cavity of substrate The rotten activity of antibacterial and produce.Representational Grain-negative Anaerobic Bacteria has porphyromonas gingivalis (Porphyromonas Gingivalis), middle Prey irrigates bacterium (Prevotella intermedia), fusobacterium nucleatum (Fusobacterium Nucleatum) etc., hydrogen sulfide and the methanthiol of more amount are produced.Its result is, report claims the initiation to halitosis of the periodontal disease antibacterial Play an important role.In a lot of researchs, show that volatile sulfur compounds produces illeffects to periodontal tissue, as VSC pair The produced effect of tissue, is confirmed as follows by experiment: increase the permeability of mucosa, is increased collagen protein (collagen) activity change of decomposition, Gingival Fibroblasts and periodontal ligament cell, the effect etc. postponing wound healing (is weighed Precious prosperousDeng, Korea S's periodontal theory of science collected works 2000).
It is considered as at the disease of chronic inflammatory disease, rheumatoid arthritis, skin as the MMP3 of intracellular stroma protein The such many diseases of skin disease, cancer are related to the important proteolytic enzyme of disorganization and tissue reconstruction, with Polymorphonuclear leukocyte that periodontal disease is relevant, fibroblast, macrophage, epithelial cell etc. are expressed and becomes the former of periodontitis Because of enzyme (Zhao ZhongxiDeng, Korea S's periodontal theory of science collected works 1999).
Periodontitis is the inflammation of the destruction causing the such tooth-supporting tissue of gingiva, periodontal ligament, chilternu and alveolar bone Disease property disease.Periodontitis and interleukin-1 beta (interleukin-1 β: IL-1 β) such cytokine (cytokines) Existence have stronger association.Further, at activation and the periodontitis of physiologically cyclooxygenase (cyclooxygenases:COX) Also there is close association.Especially, before inflammation, the work of COX-2 is induced due to cytokine and bacteriogenic production thing Property (Jin ShanyuIn Korea S's periodontal theory of science collected works 2007).
It addition, the record using various medical herbs since ancient times in order to prevent or treat oral disease can be found, by ginseng Understand according to record, by Mel, Oleum Rosae Rugosae, fire such many retrievable substance migration such as salt, Chinese medicine preparation in oral cavity disease Sick prevention or treatment, but it is a kind of to suppressing halitosis, suppression tooth to decay disease and suppression periodontal in fact to need nonetheless remain for research and development Disease has the oral cavity composition of the effect of excellence.
Summary of the invention
Technical task
In order to solve problem points in conventional art described above and diligent result of study confirms following true and completes The present invention: comprise Radix Scutellariae extract and Herba Schizonepetae extract as neccessary composition, and comprise on this basis containing Fructus Forsythiae extract, The crude drug extract of Flos Lonicerae extract and Radix Platycodonis extract etc., and the most also comprise tocopheryl acetate and Fructus Mali pumilae Acid such that it is able to the oral cavity group of the effect to suppression halitosis, suppression tooth caries disease and suppression periodontal disease with excellence is provided Compound.
Especially, it is an object of the invention to provide the oral cavity composition of a kind of following composition: pH is preferably maintained at 6 to 8, more preferably remain the such neutrality of saliva.
Solve the means of problem
The halitosis suppression oral cavity composition of the present invention comprises: 0.1 percentage by weight comprises Huang to 5.0 percentage by weights The mixture of the crude drug extract of a kind of reed mentioned in ancient books extract and Herba Schizonepetae extract;0.01 percentage by weight is to 1.0 percentage by weights Tocopheryl acetate;And 0.01 percentage by weight to the malic acid of 1.0 percentage by weights.
Be preferably, above-mentioned crude drug extract also comprise 0.1 percentage by weight to 5.0 percentage by weights from by Fructus Forsythiae The extract selected in the group that extract, Flos Lonicerae extract, Radix Platycodonis extract and their mixture of more than two kinds are constituted.
It is preferably, in above-mentioned halitosis suppression oral cavity composition, possesses the pH within the scope of 6 to 8, more preferably structure Become neutrality.
Above-mentioned halitosis suppression oral cavity composition can be paste, especially, can dosage form turn to toothpaste, cleaning agent for mouth cavity or Collutory.
It is preferably, above-mentioned halitosis suppression oral cavity composition is filled in the septate double container of tool.
Invention effect
According to the present invention, having the effect that a kind of oral cavity composition of offer, this oral cavity composition comprises Radix Scutellariae extract And Herba Schizonepetae extract is as neccessary composition, and comprises on this basis and carry containing Fructus Forsythiae extract, Flos Lonicerae extract and Radix Platycodonis Take the crude drug extract of thing etc., and the most also comprise tocopheryl acetate and malic acid, thus to suppressing halitosis, pressing down Tooth processed decays disease and suppression periodontal disease has excellent effect.
Accompanying drawing explanation
Fig. 1 is the interleukin-1 beta of the oral cavity composition representing the present invention with matched group and comparative example in the way of comparing The chart of gene expression inhibition effect.
Fig. 2 is the COX-2 of the oral cavity composition representing the present invention with matched group and comparative example in the way of comparing (COX-2) chart of gene expression inhibition effect.
Detailed description of the invention
Below, referring to the drawings, the specific embodiment of the present invention is specifically described.
The halitosis suppression oral cavity composition of the present invention is characterised by, comprises: 0.1 percentage by weight is to 5.0 weight hundred The mixture of the crude drug extract comprising Radix Scutellariae extract and Herba Schizonepetae extract of proportion by subtraction;0.01 percentage by weight is to 1.0 The tocopheryl acetate of percentage by weight;And 0.01 percentage by weight to the malic acid of 1.0 percentage by weights.
Above-mentioned Flos Lonicerae extract used in the present invention, Fructus Forsythiae extract, Herba Schizonepetae extract, Radix Platycodonis extract can make With the extract extracted by general extracting method well known in the art, it is preferably, can use and pass through hot water extraction procedure Or mixed ethanol or water and ethane and the extract that extracts.
Radix Scutellariae extract in above-mentioned crude drug extract is belonging to the Huang as herbaceos perennial of Labiatae The extract of the root of a kind of reed mentioned in ancient books (Scutellaria baicalensis GEORGE).Enter in various places as above-mentioned herbal Radix Scutellariae Row is cultivated and widely as medicinal, its active ingredient is baicalin (Baicalein), baicalin (Baicalin), Chinese Radix Scutellariae Element (Wogonin), wogonoside (Wogonoside) etc..Bitter in the mouth is cold in nature.Effect is fall excess-fire, therefore, it is possible to improve body heat And it is irritated and very thirsty and when serious, realize in a trance symptom.For from the hyperpyrexia that causes of flu to general infectious disease Hyperpyrexia, antipyretic response is notable.Cough to being caused by lung-heat has significant curative effect, and it is for acute pneumonia or acute bronchitis Hyperpyrexia cough, asthma show significant curative effect.Also it is used in stomach-fire and causes dyspepsia greatly, oral ulcer when more serious And cause stomatitis, thus the symptom of food of cannot taking food, and acute jaundice is also had curative effect.Remove because internal excessive fire is big And the eyeball congestion caused and pain, and it is used in hypertension, headache, epistaxis, metrorrhagia, to skin induced abscess also There is curative effect.Why possess such effect, be because by cold and cool property of medicine fall heat, thus relief of symptoms.Release because of height Burn and cause very thirsty, and eliminate whole body each joint heating and the symptom of pain.Anti-inflammatory is demonstrated in pharmacological evaluation Reaction, resisting pathogenic microbes effect, antipyretic, diuresis, hypotensive activity, reduction blood glucose and hyperlipemia, promotion bile secretion, town It is set for using.
Above-mentioned Herba Schizonepetae extract is the extract of the annual herb plant belonging to Labiatae being called Herba Schizonepetae, the shape of Herba Schizonepetae Shape is similar with Folium Perillae with color, is thus also known as vacation and revives, Herba Schizonepetae edible, but more primarily as medicinal.In the traditional Chinese medical science In, tassel careless and wounded in the battle for the whole strain of Herba Schizonepetae is called Herba Schizonepetae and is used as medical material.Herba Schizonepetae is recorded by Dong-eui-bo-gam book on Chinese herbal medicine As follows: " warm in nature, taste is peppery and bitter, nontoxic.Treatment: optimum syndrome caused by wind pathogen;Pernicious syndrome caused by wind pathogen;Whole body imperception;The headache that caused by typhoid fever and Muscle and the scorching hot pain of bone;Bloody path, migratory arthralgia, scrofula and skin infection.Cultivate in dry land.Delicate fragrance during tender Seedling, taste is peppery, therefore can work as vegetable Edible, the most raw-eaten, it is possible to boil.It addition, endure water when drinking as a tea, can clear the head and improving eyesight.Cut off by flower and seed structure The tassel that becomes and be used as medical material after drying under sunlight.Originally false Soviet Union it is named as, that aroma and flavor being because it and Folium Perillae class Like ".According to the folk prescription of Dong-eui-bo-gam, function and usage and dosage about Herba Schizonepetae are recited as follows: " treatment is had a dizzy spell, and cures mainly Headache.Can decoction or grinds and send use.By same amount of Herba Schizonepetae and Gypsum Fibrosum (firing) grinds, once take 8g and fall Enter in the water boiled with Rhizoma Zingiberis Recens or Herba Alii fistulosi and take after mixing it with water, headache can be controlled.Herba Schizonepetae is made again to dissipate.Perspire.With being decocted in water for oral dose, blood wind can be controlled.Treatment hands Leg cramp.With being decocted in water for oral dose.Dilute crisp and can cold and dressed with sauce eat something rare.Treat and cause mouth because of apoplexy and eye is the most askew and numb and all wind diseases.With It is decocted in water for oral dose.Smashing to pieces and be applied at furuncle with vinegar stirring, effect is notable.Thick soup can be boiled into take.It is boiled into dense with 40g Herba Schizonepetae Soup is taken, and can control the headache caused because of typhoid fever.Perspire and induce sweat.With being decocted in water for oral dose.Treatment metrorrhagia is more than.Burn and retain the property of medicine, will Its grinds, once takes 8g ".
The present invention comprises containing above-mentioned Radix Scutellariae extract and Herba Schizonepetae extract as the crude drug extract of neccessary composition, For effectively suppressing halitosis, it is preferably, on the basis of the gross weight of the halitosis suppression oral cavity composition of the present invention, comprises 0.1 Percentage by weight is to the above-mentioned crude drug extract of the amount within the scope of 5.0 percentage by weights.
The above-mentioned halitosis suppression oral cavity composition of the present invention, on the basis of above-mentioned crude drug extract, also comprises Tocopheryl acetate and malic acid.
Above-mentioned tocopheryl acetate (tocopherol acetate) is as vitamin E acetate, with glass mould vitamin E not With, molecular formula is C31H5203, molecular weight is 472.73, is light yellow viscous liquid.Acetate is not by air, light, ultraviolet etc. The impact of oxidant.Water insoluble, dissolve in acetone, chloroform, ether, dissolve on a small quantity in ethanol.Tocopherol is as vitamin E Oil, not only acts as the effect of natural antioxidant, but also has suppression skin aging and effect of cell regeneration, therefore at skin Skin is mainly applied flexibly with capsule form.Especially, tooth is also possessed such function, adding effective a certain amount of feelings Under condition, the prevention to gingivitis and prevention, periodontal and the gum disease of periodontitis (alveolar abscess) has curative effect.It is preferably, with On the basis of oral cavity composition gross weight is used in the halitosis suppression of the present invention, comprise 0.01 percentage by weight to 1.0 percentage by weights The above-mentioned tocopheryl acetate of the amount within scope.
Above-mentioned malic acid (Malic Acid) is called again hydroxyl succinic acid.It is colourless acicular crystal, and chemical formula is C4H6O5, possess an asymmetric carbon atom, there are tri-kinds of optical isomers of D-, L-and DL-.The L-hydroxyl fourth two of anticlockwise Acid is comprised in the natural fruit such as Fructus Mali pumilae, Fructus Vitis viniferae and vegetable etc..Possessing hygroscopy, molecular weight is 134.09, and proportion is 1.595, fusing point is 100 DEG C, and boiling point is 140 DEG C.Compared with the citric acid belonging to acidic flavoring agent, acid strong, cheap, display Go out the senior tart flavour of gracefulness and refine, and the tart flavour persistent period is longer, improve the appetite of people, for producing in refrigerant beverage Tart flavour.It is again acidic flavoring agent required in the metabolism of the carbohydrate of people, especially, in the oral cavity by acid acid Taste reduces and suppresses halitosis, or act as pH adjusting agent.Being preferably, the halitosis suppression oral cavity composition with the present invention is total On the basis of weight, comprise the above-mentioned malic acid of amount within the scope of 0.01 percentage by weight to 1.0 percentage by weights.
It addition, in order to realize halitosis inhibition, particularly preferably, the halitosis suppression oral cavity composition with the present invention is total On the basis of weight, also comprise in above-mentioned crude drug extract within the scope of 0.1 percentage by weight to 5.0 percentage by weights Amount from the group being made up of Fructus Forsythiae extract, Flos Lonicerae extract, Radix Platycodonis extract and their mixture of more than two kinds The extract selected.
Above-mentioned Fructus Forsythiae extract is the carrying of fruit being called the adopted city Forsyihia viridissima Lindl belonging to Oleaceae of Fructus Forsythiae and congener Take thing.Fructus Forsythiae bitter in the mouth is cold in nature, returns through acting on heart channel, lung meridian, Liver Channel.It addition, possess diaphoresis, heat clearing away effect, promoting pus discharge and removing toxic substances, solution Heat effect, antibacterial, antiinflammatory, generate heat, have a headache, xerostomia, cough, throat pain, abscess tumor, suppression vomiting, expand blood vessel and improve blood The effects such as stream effect.It addition, there is diuresis (being easily drained urine), heart tonifying diuresis (makes heart powerful, is easily drained Urine), heat-clearing and toxic substances removing (fall heat also removes toxin), the effect of detumescence blood stasis dispelling (making abscess detumescence blood stasis dispelling).
Above-mentioned Flos Lonicerae extract is half evergreen liana of the Caprifoliaceae being called Flos Lonicerae, the Radix Rubiae of dicotyledon The extract of mesh plant.Since ancient times, cure mainly: heart plug is very thirsty;Abscess;Skin ulcer or long-term inflammation and evacuation of pus;By dysentery Or the cutaneous necrosis that pyretic toxicity causes;Mumps or conjunctivitis;The inflammation such as tonsil, pharyngolaryngitis, bronchitis, cystitis Disease.According to classic medical book, Caulis Lonicerae taste cold in nature is sweet and micro-hardship, acts on heart channel, lung meridian, heat-clearing and toxic substances removing, and dredging the meridian is right Significant effect, also treatment wound and abscess, furuncle is had in various inflammation diseases.
Above-mentioned Radix Platycodonis extract is the extract of Radix Platycodonis (" Raj, road ").The wild whole regions in China of Radix Platycodonis, often with Radix Platycodonis Caulis et Folium Lactucae Sativae, Radix Platycodonis cold vegetable dish in sauce etc. are edible, and Radix Platycodonis is the most common, one of trichroism vegetable being referred to as on altar.As the saying goes " old Radix Platycodonis is better than wild ginseng ".It practice, as the Radix Platycodonis of excellent basic food does not contain only dietary fiber, but also rich in The aminoacid that minerals and vitamins B1, B2, vitamin C and tyrosine, the tryptophans etc. such as calcium, iron powder, potassium are useful.May is that because of Such nutritional labeling, about the record up to 278 kinds of effect of Radix Platycodonis in Dong-eui-bo-gam.It is many that Radix Platycodonis is belonging to lantern section Year raw herbaceous plant.As crude drug name, also it is called Radix Platycodonis, Radix Talini Paniculati, BAIYAO, stalk grass, RADIX PLATYCODI, profit such as.Mainly root is used Make medical material, take autumn and remove the peel, and dry under sunlight take afterwards the base of a fruit use.Containing the one as saponin in root Platycodin, platycodigenin.Generally, Radix Platycodonis is used for treatment cough and eliminates the phlegm.Especially, the Radix Platycodonis of every 100g contains The saponin of micro-hardship of the main component as Radix Ginseng of about 2g degree, at triterpenoid compound (triterpenoid) class Fructus Gleditsia In the case of glycosides, respiratory illness had curative effect.Increase the mucilage secretion of respiratory apparatus mucosa and reduce phlegm.By Radix Platycodonis and pears The Radix Platycodonis Sucus Pyri mixed is widely used as the preventive drug that the throat enlargement sexuality in winter emits.The famous medicine Cornu Draconis Fossilia of relieving cough and resolving phlegm The main material Radix Platycodonis the most just dissipated.Especially, in the traditional Chinese medical science, Radix Platycodonis treatment evacuation of pus, eliminate the phlegm, tonsillitis, lactogenic, cough-relieving, change Purulence abscess, asthma, and it is phthisical expectorant, the most effective in cure to pleuritis etc..Radix Platycodonis has blood pressure lowering and blood glucose Function, therefore for the bigger hyperpietic of body weight or beneficial for diabetics.Radix Platycodonis increases internal steroid and acid The secretion of (galic acid), reduces internal cholesterol, therefore useful to hyperlipidemia patient.Recently, isolate in Radix Platycodonis The material of suppression tumor, further acknowledges that out antimutagenicity.Also have the fact confirm by by ethyl acetate from the thing of Radix Platycodonis extract Demonstrate stronger antioxidant effect when qualitative response is to hepatoma carcinoma cell, and cell can be protected by oxidative stress, to prevent Cancer.
Additionally, it is preferred that be, the halitosis suppression oral cavity composition of the present invention, on the basis of above-mentioned malic acid, also comprises The citric acid of the amount within the scope of 0.01 percentage by weight to 1.0 percentage by weights.
Above-mentioned halitosis suppression oral cavity composition is preferably used the pH within the scope of 6 to 8, is preferably used and is configured to neutral Amount.
In the present invention, the oral cavity composition of the extract containing the present invention or compound is fabricated to paste and liquid And use, it being preferably, above-mentioned halitosis suppression oral cavity composition is paste, but is not limited to this.
The oral cavity composition of the present invention dosage form can turn to toothpaste, cleaning agent for mouth cavity or collutory.Especially, above-mentioned toothpaste can Comprise the group selected from the group being made up of grinding agent, adhesive, wetting agent, effective ingredient, foaming agent, sweetening material, flavouring agent Compound is as dosage form chemical conversion point, and the dosage form chemical conversion point turning to these toothpaste for dosage form can be to well known to a person skilled in the art Composition.
As above-mentioned grinding agent, from aluminium hydroxide, anhydrous silicic acid, aluminium silicate, the second calcium phosphate, the second hydroxide and nothing Water thing, calcium triphosphate, calcium carbonate, calcium pyrophosphate, insoluble Polymeric sodium metaphosphate., triphosphoric acid magnesium, magnesium carbonate, calcium sulfate, poly-first Base acrylic acid methyl ester., other synthetic resin etc. select one kind or two or more and about 20 percentage by weights with all compositions extremely It (in the case of paste toothpaste, can be that 20 percentage by weights are to 60 weight percent that the amount cooperation of 90 percentage by weights uses Within the scope of Bi).
As above-mentioned adhesive, at carrageenan, various thickening cellulose derivative, xanthan gum, Tragacanth Glue class, polyvinyl alcohol, sodium polyacrylate, polyacrylic acid/maleic acid, carboxy vinyl polymers such as (Tragacanth gum) 1 kind is selected Deng in the organic adhesives such as synthesis polymeric derivative and the mineral-type adhesive such as silicon dioxide, LAPONITE Or two or more and with within the scope of about 0.3 percentage by weight to 5 percentage by weights of all compositions amount coordinate make With.
About above-mentioned wetting agent, when manufacturing paste and liquid composition for oral cavity, as wetting agent, at sorbose Alcohol, glycerol, ethylene glycol, propylene glycol, PTMEG, polypropylene glycol etc. select one kind or two or more and with all compositions pact The amount cooperation of 10% to 70% uses.
It addition, by such sweeting agents such as saccharin sodium, stevioside, aspartame, D-xylose (D-Xylose) etc. with all The 0% to 1% of compositions, the amount within the scope of preferably 0.01 percentage by weight to 0.5 percentage by weight coordinates and uses.
It addition, in the oral cavity composition of the present invention, as the surfactant as foaming ingredient, anion can be used Surfactant, nonionic surfactant, cationic surfactant and/or general stream Buddhist nun gram class (Pluron), Bo Luosha Nurse class (Poloxamer) surfactant.Here, as anion surfactant, sodium lauryl sulfate, the tetradecane can be used Alkyl sodium sulfate, N-sodium lauroyl sarcosine (Sodium N-Lauroylsarcosinate), the N-myristyls such as base sodium sulfate N-sarcosinate (the Sodium N-such as sodium sarcosinate (Sodium N-miristyl sarcosinate) Acylsarcosinate) etc., as nonionic surfactant, sugar fatty acid ester, fatty ester of maltose, breast can be used Sugar fatty acid esters etc. are such comes from the fatty acid ester of sugar, polyoxyethylene hydrogenated Oleum Ricini, polyoxyethylene higher alcohol ether, polyoxy second Alkene poiyoxypropylene copolymer, polyoxyethylene polypropylene fatty acid ester (Polyoxyethylene Polypropylene fatty Acid ester) etc..As cationic surfactant, N-lauryl diamino ethyl glycine (N-Lauryl can be used Di-amino ethyl glycine), N-Semen Myristicae diamino ethyl glycine (N-Myristyl di-amino ethyl Such N-alkyl diamino ethyl glycines (N-Alkyl di-amino ethyl glycine), the N-alkane such as glycine) Base-N-carboxymethyl ammonium glycine betaine (N-Alkyl-N-carboxymethyl ammonium betaine), 2-alkyl-1-ethoxy Imidazolinium betaine sodium (2 Alkyl-1-Hydroxyethyl imidazoline betaine sodium) etc..Further, can make With general stream Buddhist nun gram class, poloxamer class surfactant etc..In this case, as foaming ingredient, main use anion table Face activating agent, typically, the such alkyl sodium sulfate of most widely used sodium lauryl sulfate.It addition, this surfactant Can be used alone a kind or mix two or more and use, use level generally uses 0.01 percentage by weight of all compositions Amount to 0.5 percentage by weight, more preferably uses 0.05 percentage by weight of all compositions to 0.3 weight hundred Amount within the scope of proportion by subtraction.
In addition, the oral cavity composition of the present invention can contain various nutrients, vitamin, mineral (electrolyte), synthesis The spice such as spice and natural perfume material, coloring agent and filler (cheese, chocolate etc.), pectic acid and pectate, alginic acid and Alginate, organic acid, protective colloid thickening agent, stabilizer, preservative, glycerol, ethanol, it is used in the carbon oxygen of soda pop Agent etc..Additionally, the oral cavity composition of the present invention can be containing being used for manufacturing natural water fruit juice and fruice beverage and vegetable beverage Sarcocarp.About such composition, can be used independently or combine and use.The ratio of these additives is the most important, but In the ordinary course of things, select from the scope in 0 to 20 weight portion relative to the compositions in every 100 weight portions of the present invention.
Also can suitably comprise dosage form chemical conversion point in above-mentioned cleaning agent for mouth cavity or collutory, for dosage form, to be melted into these oral cavities clear Clean dose or collutory and the dosage form chemical conversion point that uses can be to well known to a person skilled in the art composition, such as, conduct can be comprised Carrier and rudimentary ethanol, the polyhydric alcohol etc. that keep liquid water, carbon number to be 1 to 4 at normal temperatures, also can comprise other colorings Agent, fragrant agent, flavouring agent, sweetening material etc..
Above-mentioned halitosis suppression oral cavity composition can be filled in the septate double container of tool.It is being filled into such tool In the case of in septate double container, in order to meet the preference degree of consumer, it is filled with the most as follows: with double On the basis of the barrier film of weight container, possess identical composition in both sides, only make color different.
Below, the preferred embodiments of the present invention and comparative example are described.
Below example is only used for illustrating the present invention, and the scope of the present invention is not limited to this.
Embodiment 1 described in table 1 below is the sky comprised containing Radix Scutellariae extract and Herba Schizonepetae extract of the present invention So medicinal substances extract and tocopheryl acetate and malic acid are as the oral cavity composition of neccessary composition, about embodiment 2, except upper On the basis of stating embodiment 1, comprise Fructus Forsythiae extract, Flos Lonicerae extract further with equivalent as crude drug extract And outside the situation of Radix Platycodonis extract, be the oral cavity composition identical with above-described embodiment 1.It addition, about the oral cavity of comparative example 1 Compositions, except not comprising the feelings of Radix Scutellariae extract, Herba Schizonepetae extract, tocopheryl acetate and malic acid in above-described embodiment 1 Outside condition, it is the oral cavity composition identical with above-described embodiment 1.
After weighing exactly with the composition in following table and content and mix, by the manufacturer of general toothpaste Method and be manufactured into toothpaste.
The antimicrbial power test of<experimental example 1>Streptococcus mutans (Streptococcus mutans)
The oral cavity composition dosage form of above-mentioned comparative example 1, embodiment 1 and 2 is melted into toothpaste, and dosage form is turned to the 2g of toothpaste Oral cavity composition dilute and make it suspend in the phosphate buffer through the 9g of sterilization, carried out by following method Experiment.
Table 1
[table 1]
Raw material name Comparative example 1 Embodiment 1 Embodiment 2
Non-crystallising sorbitol 30 30 30
Liquid Macrogol 2 2 2
Carboxymethyl cellulose 1 1 1
Tocopheryl acetate - 0.1 0.1
Saccharin sodium 0.22 0.22 0.22
Malic acid - 0.1 0.1
Calcium phosphate dichloride 0.1 0.1 0.1
Precipitated silica (grinding agent is used) 30 30 30
Precipitated silica (thickening is used) 3 3 3
Sodium lauryl sulfate 1.55 1.55 1.55
Sodium fluoride 0.22 0.22 0.22
Radix Scutellariae extract - 0.5 0.5
Herba Schizonepetae extract - 0.5 0.5
Fructus Forsythiae extract - - 0.5
Flos Lonicerae extract - - 0.5
Radix Platycodonis extract - - 0.5
Yellow 4 (FDC#5) 0.002 0.002 0.002
Green No. 3 (FDC#5) 0.0005 0.0005 0.0005
Toothpaste is fragrant (Flavor) 1.05 1.05 1.05
Titanium dioxide 0.1 0.1 0.1
First sodium phosphate 0.1 0.1 0.1
Sodium triphosphate 0.05 0.05 0.05
Pure water 30.6075 29.4075 27.9075
By the suspension of above-mentioned dilution with BHI (Brain heart infusion) culture medium serial dilution 2 times to 48 Orifice plate (well plate) respectively injectsAnd, in agar culture medium, by 1 Streptococcus mutans (Strept ococcus Mutans, ATCC 25175) bacterium colony (colony) is suspended toBHI culture medium after be injected into above-mentioned dilution additionally 48 orifice plates in, and at 37 DEG C cultivate 24 hours, then with MIC (minimal inhibition concentration) survey Measure antimicrbial power, shown in its result table described as follows 2.
Table 2
[table 2]
Its result understands, according to the crude drug extract comprised containing Radix Scutellariae extract and Herba Schizonepetae extract of the present invention And the oral cavity composition (embodiment 1) of tocopheryl acetate and malic acid and also comprise Fructus Forsythiae on the basis of above-described embodiment 1 and carry Take the oral cavity composition (embodiment 2) of thing, Flos Lonicerae extract and Radix Platycodonis extract compared with the comparative example 1 not comprising these, Antimicrbial power is more excellent.
Antimicrbial power test in<experimental example 2>anerobe
As experimental example 1, the oral cavity composition of comparative example and the 2g of embodiment is diluted to carry out the 9g of sterilization processing Phosphate buffer and make it suspend, and tested by following method.MIC method is held identically with experimental example 1 OK.But, anerobe does not grows when there being oxygen, therefore at the hydrogen (H being supplied to 5%2) and the nitrogen of 95% (N2) anaerobic culture medium (Sheldon Manufactoring Bac 2-2E) in cultivate and tested with it, its Shown in result table described as follows 3.
Table 3
[table 3]
Its result, comprise the oral cavity composition (embodiment 1,2) of the tcm prescription of the present invention on antimicrbial power with comparative example 1 Similar, but to causing the porphyromonas gingivalis of bacterium to display that antimicrbial power as periodontitis, be thus judged as suppression periodontitis There is the effect of excellence.
The activity of<experimental example 3>MMP-3 hinders performance evaluation
Shown in table 4 described as follows, use from the oral cavity composition of above-mentioned comparative example 1 and embodiment 1 and 2, remove fluorination Prescription (comparative example 2, embodiment 3 and 4) outside sodium, sodium lauryl sulfate, spice (flavor), pigment etc. and to MMP-3's Activity hinders performance to be evaluated.
Table 4
[table 4]
Raw material name Comparative example 2 Embodiment 3 Embodiment 4
Non-crystallising sorbitol 30 30 30
Liquid Macrogol 2 2 2
Carboxymethyl cellulose 1 1 1
Tocopheryl acetate - 0.1 0.1
Saccharin sodium 0.22 0.22 0.22
Malic acid - 0.1 0.1
Calcium phosphate dichloride 0.1 0.1 0.1
Radix Scutellariae extract 0.5 0.5
Herba Schizonepetae extract 0.5 0.5
Fructus Forsythiae extract - 0.5
Flos Lonicerae extract - 0.5
Radix Platycodonis extract - 0.5
Titanium dioxide 0.1 0.1 0.1
First sodium phosphate 0.1 0.1 0.1
Sodium triphosphate 0.05 0.05 0.05
Pure water 66.43 65.23 63.73
Hinder performance to cultivate fibroblast to observe the activity of MMP-3, and process with above-mentioned oral cavity composition And implement following experiment.About the Gingival Fibroblasts (Human Gingvial Fibroblast) of people, never tooth The healthy tissue of the people of all scorching case histories is taked and has carried out 1 time and cultivated, and tested with it.At 37 DEG C, 5% Carbon dioxide (CO2) thermostat utilizes containing 10%FBS (Fetal bovine serum: hyclone) (GibcoBRL, Antibiotic (the antibiotics)/antibacterial material (antimyco tics) of USA) and 1% (Penicillin (penicillin)、Amphotericin (amphotericin) D and 100Streptomycin (streptomycin) DMEM (Dulbecco's modified Eagle'smedium) (GibcoBRL, USA) culture medium) Cultivated.The Gingival Fibroblasts of the people for cultivating in the dish of 100 is replaced with the cultivation of the FBS containing 1% Liquid and carried out the cultivation of 24 hours, then utilize phosphate buffer and can single fluorophosphoric acid of toxicity of trigger cell by removing After sodium, sodium lauryl sulfate, methyl parahydroxybenzoate (Methyl ρ-Hydroxybenzoate) and minty note B70097 The concentration of oral cavity composition furnishing 200ppm, 500ppm and add interleukin-1 ' beta ' after carrying out the pretreatment of 30 minutesAnd implement the cultivation of 48 hours (MMP-3).After cultivation, make culture fluid gather and carry out 1500rpm/5 and divide The centrifugation of clock, is only used in supernatant in experiment, and utilize ELISA instrument (Amersham Bioscience, UK) and Measuring MMP-3 activity degree, its result is as shown in table 7.
Table 5
[table 5]
The compositions (embodiment 3) of the tcm prescription comprising Fructus Forsythiae extract, Herba Schizonepetae extract according to the present invention with not The comparative example 2 comprising these is compared effective, it can be seen that Fructus Forsythiae extract, Herba Schizonepetae extract play the main work suppressing composition With.It addition, comprise the compositions of the tcm prescription of Fructus Forsythiae extract, Herba Schizonepetae extract, Flos Lonicerae extract, Radix Platycodonis extract (embodiment 4) MMP-3 inhibition compared with Example 3 is the most excellent, it can be seen that by Flos Lonicerae extract, Radix Platycodonis extract Effect can be more promoted when thing and Fructus Forsythiae extract, Herba Schizonepetae extract are used together.
<experimental example 4>is surveyed as the interleukin-1 ' beta ' of anti-inflammatory index and the expression inhibiting of COX-2 (cox-2) Examination (RT-PCR)
It is injected separately into 1 × 10 to 100 culture dishs6Individual Raw264.7 cell strain, and utilize phosphate buffer joining Removing in polymeric composition can the sodium monofluorophosphate of toxicity of trigger cell, sodium lauryl sulfate, methyl parahydroxybenzoate and thin The concentration of oral cavity composition furnishing 200ppm, 500ppm after lotus perfume (or spice) B70097, and implement 24 hours by LPS induction inflammation Cultivation, then remove culture medium, by cell from culture vessel separate, and use ribonucleic acid extract solution (Invitrogen, CA, USA) and by cell homogenization.Cell is gathered and moves on to centrifugal separating tube after spending 5 minutes, put intoChloroform And stir 15 seconds and place 3 minutes after making it be thoroughly mixed, under 14000rpm, then carry out the centrifugation of 15 minutes.Will bag The supernatant of qiagen rnase moves on to new pipe, and with2-propanol (isopropyl alcohol) mixed. The most again centrifugation and outwell supernatant, precipitate is put into the ethanol of 75%Under 10000rpm Carry out the centrifugation of 5 minutes, then outwell supernatant and the ribonucleic acid of precipitation is dried 20 minutes at normal temperatures.Make to be dried Ribonucleic acid suspend in the distilled water having processed DEPC (Diethylpyrocarbonate, Sigma).To ribonucleic acid After Ding Liang, RT-PreMix (AccuPower RT PreMix, Bioneer) is utilized to synthesize complementary nucleic acid (cDNA).Will Interleukin-1 ' beta ' and COX-2 primer are mixed respectively, so by the complementary nucleic acid of synthesis as template (template) Rear use PCR Premix (AccuPower PCR PreMix, Bioneer) and confirm the expression degree of ribonucleic acid.To close The cDNA become mixes COX-2 primer as template, and use PCR Premix (AccuPower PCR PreMix, Bioneer) the expression degree of ribonucleic acid is confirmed.Use densimeter (densitometer:Image Gauge V3.46, Koshin Graphic Systems, Fuji Photo Film Co., Japan) and implement quantitative analysis.
Its result, as shown in Figures 1 and 2, hindering rate to carry out investigation the relative expression that have passed through the group that LPS processes can Know, as the present invention, comprise the compositions (embodiment 3 of tcm prescription (comprising the prescription of Fructus Forsythiae extract, Herba Schizonepetae extract) And 4) compared with comparative example 2, restrained effectively interleukin-1 ' beta ' and Cyclooxygenase-2 Gene is expressed.Especially, implementing Example 3, in 4, the expression inhibiting rate of COX-2 substantially reduces more than 50% in 500ppm.Can determine whether out such as this from this result The suppression ratio that invention so comprises the oral cavity composition (embodiment 3,4) of tcm prescription is excellent.As can be seen here, as the present invention Comprise the oral cavity composition inhibition highly significant to periodontal antiinflammatory of tcm prescription.
Confirm following situation: the oral cavity composition of the embodiments of the invention 1 comprising tcm prescription suppresses the most effectively Tooth decays disease, halitosis induction bacterium and periodontitis reason bacterium, and effectively suppression directly participate in the MMP-3 of periodontal tissue destruction with Interleukin-1 ' beta ' and Cyclooxygenase-2 Gene as inflammation suppression index are expressed.
Industrial applicability
The present invention may use manufacture health product, especially, the product of such oral cavity composition such as toothpaste or collutory Industry.
Above, described concrete example has only been described in detail by the present invention, but to those skilled in the art It will be clear that various deformation and amendment can be carried out in the range of the technological thought of the present invention, and such deformation and amendment are obviously Fall within the protection domain of appending claims.

Claims (7)

1. a halitosis suppression oral cavity composition, it is characterised in that this halitosis suppression oral cavity composition comprises:
The crude drug extract comprising Radix Scutellariae extract and Herba Schizonepetae extract of 0.1 percentage by weight to 5.0 percentage by weights Mixture;
The tocopheryl acetate of 0.01 percentage by weight to 1.0 percentage by weights;And
The malic acid of 0.01 percentage by weight to 1.0 percentage by weights.
Halitosis suppression oral cavity composition the most according to claim 1, it is characterised in that
Above-mentioned crude drug extract also comprise 0.1 percentage by weight to 5.0 percentage by weights from by Fructus Forsythiae extract, gold silver The extract selected in the group that flower extract, Radix Platycodonis extract and their mixture of more than two kinds are constituted.
Halitosis suppression oral cavity composition the most according to claim 1, it is characterised in that
In above-mentioned halitosis suppression oral cavity composition, pH is in the range of within the scope of 6 to 8.
Halitosis suppression oral cavity composition the most according to claim 3, it is characterised in that
Above-mentioned halitosis suppression oral cavity composition is neutral.
Halitosis suppression oral cavity composition the most according to claim 1, it is characterised in that
Above-mentioned halitosis suppression oral cavity composition is paste.
Halitosis suppression oral cavity composition the most according to claim 1, it is characterised in that
Above-mentioned halitosis suppression oral cavity composition dosage form is turned to toothpaste, cleaning agent for mouth cavity or collutory.
Halitosis suppression oral cavity composition the most according to claim 1, it is characterised in that
Above-mentioned halitosis suppression oral cavity composition is filled in the septate double container of tool.
CN201480077603.XA 2014-04-01 2014-04-03 Halitosis suppression oral cavity composition Pending CN106163497A (en)

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CN1413692A (en) * 2002-11-13 2003-04-30 贵州省安顺制药厂 Medicin spray for treating throat disease and stomatopathy
CN101015512A (en) * 2006-11-30 2007-08-15 广州立白企业集团有限公司 Composition and its application in oral cavity nursing product
KR20110027047A (en) * 2009-09-09 2011-03-16 (주)아모레퍼시픽 Zeolite oral capsule powder and the oral composition containing thereof

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