CN110538084A - Compound for synergistically resisting dental plaque and inhibiting dental ulcer - Google Patents

Compound for synergistically resisting dental plaque and inhibiting dental ulcer Download PDF

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Publication number
CN110538084A
CN110538084A CN201810521373.1A CN201810521373A CN110538084A CN 110538084 A CN110538084 A CN 110538084A CN 201810521373 A CN201810521373 A CN 201810521373A CN 110538084 A CN110538084 A CN 110538084A
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compound
mouthwash
indirubin
indigo
resisting
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张玉波
石育坤
石全贵
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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
    • A61K8/19Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/20Halogens; Compounds thereof
    • A61K8/21Fluorides; Derivatives 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
    • A61K8/19Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/24Phosphorous; Compounds 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
    • A61K8/49Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/4906Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom
    • A61K8/4913Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having five membered rings, e.g. pyrrolidone carboxylic acid
    • A61K8/492Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having five membered rings, e.g. pyrrolidone carboxylic acid having condensed rings, e.g. indol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Chemical & Material Sciences (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Cosmetics (AREA)

Abstract

The invention relates to a compound for synergistically resisting dental plaque and inhibiting dental ulcer and an application method of the compound in mouthwash, chewing gum and toothpaste, and belongs to the field of oral hygiene. The compound comprises indigo, indirubin and inorganic fluoride salt. The raw materials for applying the compound to the mouthwash comprise indigo, indirubin, inorganic fluoride salt, surfactant, sweetener, spice, preservative and deionized water. The preparation method comprises the following steps: sequentially putting inorganic fluoride salt, indigo, indirubin and other auxiliary materials into deionized water, stirring for 20-35min by using vacuum high-speed shearing equipment, and obtaining the mouthwash after the mouthwash is clear and free of precipitates. The compound of the invention has the functions of resisting infection and enhancing immunity, and has the functions of resisting dental plaque and inhibiting dental ulcer. The compound of the invention can be applied to mouth wash, chewing gum and toothpaste.

Description

Compound for synergistically resisting dental plaque and inhibiting dental ulcer
Technical Field
The invention relates to the field of daily oral care, in particular to a compound for resisting dental plaque and inhibiting dental ulcer for an oral cavity.
Background
According to the invention, the compound combination of the inorganic fluoride salt, the indigo and the indirubin has good synergistic effect on inhibiting the growth of dental plaque caused by bacteria and superficial ulcer on oral mucosa.
Indigo has anti-inflammatory and analgesic effects, and can relieve pain after periodontal diseases. Indirubin is a bisindole compound, and has biological effects of resisting bacteria, diminishing inflammation, resisting virus, resisting tumor, enhancing immunity of organism, etc. The indigo and indirubin, as extracts of pure natural herbs, have the advantages of being not easy to generate drug resistance, low in toxicity, free of or low in residue and the like.
At present, no report of toxic and side effects of indigo and indirubin is found, and the medicine can be used for a long time.
The inorganic fluoride salt can inhibit cariogenic bacteria, inhibit enamel and dentin demineralization, and promote remineralization, and has dental plaque inhibiting effect.
The mechanism of the indigo, indirubin and inorganic fluoride salt compound for inhibiting dental plaque is as follows: can directly destroy the surface structure of bacteria under the condition of separation to play the role of bacteriostasis, and can play the role of inhibiting dental plaque through the function of immunity under the state of living body. I.e. has the functions of resisting infection and enhancing immunity.
The compound of the indigo, the indirubin and the inorganic fluoride salt has obvious effects of inhibiting dental plaque, preventing periodontal diseases and treating oral ulcer infected by nonspecific oral mucosa and traumatic oral ulcer.
At present, the anti-dental plaque mouthwash applied to the market mainly contains bactericides, such as chlorhexidine (0.2%) and other antibiotics with broad-spectrum bactericidal action. But chlorhexidine can kill some beneficial bacteria at the same time, easily causes imbalance of oral flora and causes adverse effects on human health.
Inorganic fluoride is currently recognized as a safe, effective anticaries substance commonly used in mouthwashes and toothpastes. However, it is also controversial that fluorine excess causes dental fluorosis, and even that fluorine intake is excessive is said to cause "neurological diseases, endocrine diseases, and even cancer".
According to the invention, inorganic fluoride and indigo are used as effective components for inhibiting bacteria, and indirubin is used as a component for enhancing immunity for compounding, so that a synergistic effect is shown. The efficacy of inorganic fluoride is achieved without reducing its efficacy in enhancing enamel and dentin remineralization and inhibiting plaque upon application of smaller doses of the fluoride. The indigo has synergistic bactericidal effect, and the indirubin has immunity enhancing effect. The compound not only has the function of inhibiting dental plaque, but also has the function of protecting sensitive and even wounded oral mucosa during the process of installing false teeth and correcting teeth, and has the function of preventing oral ulcer caused by the sensitive and even wounded oral mucosa.
Disclosure of Invention
In view of the defects of the prior art, the first object of the present invention is to provide a compound having the functions of resisting dental plaque and enhancing immune suppression of dental ulcer, specifically a compound of indigo blue, indirubin and inorganic fluoride salt.
The inorganic fluoride salt used for implementing the invention can be one of sodium fluoride, sodium monofluorophosphate and stannous fluoride or a compound thereof.
The second purpose of the invention is to provide the application of the compound as a main functional substance in mouthwash, toothpaste and chewing gum.
In the invention, the indigo, the indirubin and the inorganic fluoride salt are compounded, so that the effects of resisting infection and enhancing immunity are increased on the basis of inhibiting dental plaque.
In the invention, the mass ratio of the indigo to the indirubin to the inorganic fluoride is (1-10) to (1-100), and the mass ratio is hereinafter referred to as a compound.
The compound of the invention can be used for mouthwash, toothpaste and chewing gum.
A collutory for synergistically inhibiting dental plaque and dental ulcer is prepared from indigo blue, indirubin, inorganic fluoride salt, surfactant, sweetener, perfume, antiseptic and deionized water.
A mouth wash for synergistically resisting dental plaque and inhibiting dental ulcer, which is prepared by the following steps: sequentially putting inorganic fluoride salt, indigo, indirubin and other auxiliary materials into deionized water, stirring for 20-35min by using vacuum high-speed shearing equipment, and obtaining the mouthwash after the mouthwash is clear and free of precipitates.
In the invention, the mass fraction of the compound in the mouthwash is 0.05-0.3%.
Preferred sweeteners in the above formula are: maltose, lactose, glucose, xylitol, saccharin, etc.
The preferred surfactants in the above formulation are: one or more of sodium dodecyl sulfate, sodium dodecyl benzene sulfonate, ethanol ammonium salt and the like.
The preferred fragrances in the above formula are: one or more of daily essences such as mint spice, lemon spice and the like are compounded.
The preferred preservatives in the above formulation are: sorbic acid, sodium sorbate, benzoic acid, sodium benzoate, etc.
In the invention, the mass fraction of the compound in the toothpaste is 0.5-1.2%.
A toothpaste for synergistically inhibiting dental plaque and dental ulcer comprises indigo blue, indirubin, inorganic fluoride salt, calcium phosphate, glycerin, magnesium aluminum silicate, sorbitol, stannous pyrophosphate, perfume, sweetener and deionized water.
In the invention, the mass fraction of the compound in the chewing gum is 0.08-0.2%.
A chewing gum for synergistically inhibiting dental plaque and dental ulcer is prepared from indigo blue, indirubin, inorganic fluoride salt, resin, granulated sugar, perfume and softener.
The compound of the invention has the functions of resisting infection and enhancing immunity, and is suitable for daily periodontal nursing; prevention of periodontal disease; prevention of dental caries; inhibition of dental plaque and prevention of dental ulcers that it causes during adult denture installation; relieving discomfort of the mouth during denture installation; inhibition of dental plaque and prevention of traumatic oral ulcers caused thereby during correction in children and adults.
Detailed Description
The use of the synergistic antiplaque antiulcer oral formulation of the present invention in mouthwash is illustrated by the following specific examples.
Example 1
The composition is prepared by taking a compound of indigo, indirubin and inorganic fluoride as an effective component, taking deionized water as a carrier, and adding a surfactant, a sweetening agent, a spice and a preservative. The concrete components (by mass fraction) are as follows: sodium monofluorophosphate: 0.03%, indigo 0.02%, indirubin: 0.02%, sodium lauryl sulfate: 0.8%, ethanolammonium salt: 0.2%, lactose: 3%, xylitol 1%, lemon flavor: 0.5%, sodium sorbate: 0.5 percent and the balance of deionized water.
In the formula, inorganic fluoride salt, indigo, indirubin and other substances are sequentially placed into deionized water, and are uniformly stirred for 20min by using vacuum high-speed shearing equipment, so that the mouthwash is obtained after the mouthwash is clear and free of precipitates.
Example 2
The compound for synergistically resisting dental plaque and inhibiting dental ulcer is used as an effective component, a carrier is deionized water, and a surfactant, a sweetening agent, a spice and a preservative are matched to form the compound. The concrete components (by mass fraction) are as follows: sodium fluoride: 0.04%, indigo 0.04%, indirubin: 0.03%, sodium dodecylbenzenesulfonate: 1%, xylitol: 1.5%, glucose 2%, lemon flavor: 0.8%, sodium benzoate: 0.2 percent and the balance of deionized water.
In the formula, functional substances such as inorganic fluoride salt, indigo, indirubin and the like and auxiliary materials are sequentially put into deionized water, and are uniformly stirred for 25min by using vacuum high-speed shearing equipment, so that the mouthwash is obtained after the mouthwash is clear and free of precipitates.
Example 3
The compound for synergistically resisting dental plaque and inhibiting dental ulcer is used as an effective component, a carrier is deionized water, and a surfactant, a sweetening agent, a spice and a preservative are matched to form the compound. The concrete components (by mass fraction) are as follows: sodium fluoride: 0.08%, indigo 0.03%, indirubin: 0.03%, sodium dodecyl benzene sulfonate 0.6%, ethanol ammonium salt 0.4%, maltose: 2%, xylitol: 2%, mint flavor: 0.2%, sodium sorbate: 0.3 percent and the balance of deionized water.
In the formula, functional substances such as inorganic fluoride salt, indigo, indirubin and the like and auxiliary materials are sequentially put into deionized water, and are uniformly stirred for 35min by using vacuum high-speed shearing equipment, so that the mouthwash is obtained after the mouthwash is clear and free of precipitates.
Example 4
The compound for synergistically resisting dental plaque and inhibiting dental ulcer is used as an effective component, a carrier is deionized water, and a surfactant, a sweetening agent, a spice and a preservative are matched to form the compound. The concrete components (by mass fraction) are as follows: stannous fluoride: 0.06%, indigo 0.03%, indirubin: 0.05%, sodium dodecylbenzenesulfonate: 1%, glucose: 2%, xylitol 2%, mint flavor: 0.2%, sodium sorbate: 0.3 percent and the balance of deionized water.
In the formula, functional substances such as inorganic fluoride salt, indigo, indirubin and the like and auxiliary materials are sequentially put into deionized water, and are uniformly stirred for 30min by using vacuum high-speed shearing equipment, so that the mouthwash is obtained after the mouthwash is clear and free of precipitates.
Example 5
This example is a comparative example, containing only sodium fluoride or sodium monofluorophosphate, without the combination of indigo and indirubin, wherein the specific components (by mass fraction) are: sodium fluoride: 0.04%, sodium dodecylbenzenesulfonate: 0.8%, xylitol 3%, lemon flavor: 0.6%, sodium benzoate: 0.2 percent and the balance of deionized water.
In the formula, functional substances such as inorganic fluoride salt, indigo, indirubin and the like and auxiliary materials are sequentially put into deionized water, and are uniformly stirred for 30min by using vacuum high-speed shearing equipment, so that the mouthwash is obtained after the mouthwash is clear and free of precipitates.
The combination with experimental studies shows that the mouthwash has the effect of inhibiting the growth of bacteria in vitro and the effect of inhibiting dental ulcer.
Activating strains to be detected (Porphyromonas gingivalis, Streptococcus mutans, Actinomyces viscosus and Staphylococcus aureus) on a suitable plate, preparing into bacterial suspension, and storing in a refrigerator at 4 deg.C for use. Soaking a sterilized filter paper sheet with the diameter of 8mm in the mouthwash of the embodiments 1 and 2 for 10min, uniformly coating 0.5mL of each suspension of the bacteria to be tested on the surface of an LB solid culture medium, and after the culture medium is absorbed, sticking the filter paper sheet containing the compound mouthwash on a bacteria-containing flat plate, wherein 3 filter paper sheets are stuck to each dish; using a filter paper impregnated with the filter paper of example 5 (comparative example) as a control, the size of the zone of inhibition was measured after incubation at 25 ℃ for 2 hours.
Table 1 zone diameters of inhibition for different bacteria in examples 1, 2, 5
Table 1 shows that the mouthwash containing the indigo, indirubin and inorganic fluoride compound has a significant bacteriostatic effect compared with the mouthwash containing inorganic fluoride alone.
164 patients (2014-2017) with dental ulcer after orthodontic treatment who are treated by an oral clinic are selected, the age is 18-50 years, 85 men and 79 women have good health conditions of the whole body, and the whole mouth is not less than 20 functional teeth. Antibiotics and hormones are not taken within three months, and no systemic diseases exist. They were randomly divided into an observation group (82 cases) and a control group (82 cases). During the treatment period, the observation group used 10-15ml of the compound mouthwash of experimental example 1 each time and gargled for 3 minutes, and then gargled 3 times daily without the rinse. The control group was rinsed with example 5, the comparative example, daily for 3 minutes and three times daily.
The therapeutic effect judgment standard is as follows: after the medicine is taken for 3 days, the red swelling of the patient is partially removed, the pain is not felt, and the ulcer is basically healed, so that the medicine is judged to be effective; after 7 days of administration, the patient is judged to be effective because the red swelling is partially removed, no pain is caused, and the ulcer is obviously healed, and after 7 days of treatment, the patient is judged to be ineffective because the red swelling is not removed, the pain is caused, and the ulcer is not healed or even aggravated. The total effective rate is the effective rate plus the significant efficiency.
Inhibition rate of oral ulcer: the patient of the observation group used the mouthwash formulated according to example 1, and the patient of the control group used the mouthwash formulated according to example 5, i.e. the comparative example. 82 patients in an observation group are observed, wherein 50 patients with obvious effect, 25 patients with effective effect and 7 patients with ineffective effect have a total effective rate of 91.4 percent; 82 patients in the control group, wherein 16 patients with significant effect, 25 patients with effective effect and 41 patients with ineffective effect have a total effective rate of 50.0%.
Evaluation of the effect of canker sore: p is less than 0.05, has statistical difference and reliable total effective rate.
Example 6
The following description of the "synergistic antiplaque antiulcer oral formulation" of the present invention in chewing gum is provided in connection with the specific examples. Mixing resin, granulated sugar, spice and softener at a weight ratio of 1: 2: 1 to obtain mixture A; mixing sodium fluoride, indigo and indirubin together according to the weight ratio of 5: 2 to obtain a mixture B; and pouring the B into the A according to the mass of 0.1 percent of the A, uniformly mixing, extruding in a forming device to form a semi-finished product, finally coating sugar coat, cutting and forming.
Example 7
The following description of the application of the synergistic antiplaque and antiulcer oral composition of the present invention in toothpaste is provided in conjunction with the following specific examples, and the composition is formulated in terms of mass percent according to table 2. Dissolving sorbitol, stannous pyrophosphate, xylitol and magnesium aluminum phosphate in a premixing pot by using deionized water until the mixture is uniform, adding the mixture into a paste making pot, adding glycerol into the paste making pot, and uniformly stirring; adding stannous fluoride, indigo, indirubin and calcium phosphate into a paste making pot, adding spice, stirring with a scraper, homogenizing, stirring, and grinding; simultaneously, the vacuum pumping is carried out until the vacuum degree reaches-0.096 Mpa, and the time is about 50 minutes. After kneading and grinding, a small amount of paste is beaten out for inspection, the paste is uniform and bubble-free, then the paste is put into a paste storage pot for aging, the paste is naturally cooled to the normal temperature, meanwhile, the materials are fully expanded to form a homogeneous adhesive body, and the aging time is about 120 minutes.
Table 2 toothpaste formulations containing the compound
Composition (I) Mass percent Composition (I) Mass percent Composition (I) Mass percent
Stannous fluoride 0.55% Calcium phosphate 43.00% Sorbitol 19.50%
Indigo blue 0.05% Glycerol 9.00% Stannous pyrophosphate 1.10%
Indirubin 0.10% Magnesium aluminum silicate 0.50% Xylitol, its preparation method and use 0.20%
Perfume 1.00% Deionized water 25.0%
The above detailed descriptions of the compound for inhibiting dental ulcer and inhibiting dental plaque and the preparation method thereof according to the embodiments of the present invention are provided, and the principle and the embodiments of the present invention are illustrated herein by using specific examples, and the description of the above embodiments is only for the purpose of understanding the method of the present invention and the core idea thereof, and is not intended to limit the present invention, and any modifications, equivalents, improvements, etc. made within the spirit and principle of the present invention should be included in the scope of the present invention.

Claims (10)

1. An oral synergistic antiplaque and antiulcer oral formulation comprising: indigo, indirubin and inorganic fluoride salts.
2. The formulation according to claim 1, wherein said inorganic fluoride salt comprises one or a combination of sodium fluoride, sodium monofluorophosphate, stannous fluoride.
3. The compound of claim 1, wherein the mass ratio of the indigo to the indirubin to the inorganic fluoride is (1-10) to (1-100).
4. A formulation according to claims 1 to 3, characterized in that it can be used in mouthwashes, toothpastes, chewing gums.
5. The compound according to claims 1-4 is used for preparing mouthwash for resisting dental plaque and inhibiting dental ulcer, and is characterized in that raw materials of the mouthwash comprise indigo blue, indirubin, inorganic fluoride salt, surfactant, sweetener, spice, preservative and deionized water.
6. The compound mouthwash for resisting dental plaque and inhibiting dental ulcer according to claims 1-4 is characterized in that the mass fraction of the compound in the mouthwash is 0.05-0.3%.
7. The compound mouthwash for resisting dental plaque and inhibiting dental ulcer according to claims 1 to 6 is prepared by sequentially putting inorganic fluoride salt, indigo, indirubin and other auxiliary materials into deionized water, stirring for 20-35min by using a vacuum high-speed shearing device, and obtaining the mouthwash after the mouthwash is clear and free of precipitates.
8. The compound according to claims 1-4 is used for toothpaste for resisting dental plaque and inhibiting dental ulcer, and is characterized in that the toothpaste comprises the following raw materials: indigo, indirubin, inorganic fluoride salts, calcium phosphate, glycerin, magnesium aluminum silicate, sorbitol, stannous pyrophosphate, flavors, sweeteners and deionized water.
9. The compound according to claims 1-4 is used for toothpaste for resisting dental plaque and inhibiting dental ulcer, and the compound accounts for 0.5-1.2% of the toothpaste by mass.
10. A chewing gum containing the compound according to claims 1-4 for resisting dental plaque and inhibiting dental ulcer is characterized in that raw materials of the chewing gum comprise indigo, indirubin, inorganic fluoride salt, resin, granulated sugar, spice and softener, and the mass fraction of the compound in the chewing gum is 0.08-0.2%.
CN201810521373.1A 2018-05-28 2018-05-28 Compound for synergistically resisting dental plaque and inhibiting dental ulcer Pending CN110538084A (en)

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Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020068094A1 (en) * 1998-06-30 2002-06-06 Hajime Aga Physiologically active exract
CN101249056A (en) * 2008-01-11 2008-08-27 美晨集团股份有限公司 Anti-inflammation gargle water and method of preparing the same
CN107582486A (en) * 2017-09-26 2018-01-16 西安罗格斯生物科技有限公司 It is a kind of to be used for oral hygiene spray that is antibacterial, removing removing abnormal flavor in oral cavity, firm tooth, tooth-whitening

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020068094A1 (en) * 1998-06-30 2002-06-06 Hajime Aga Physiologically active exract
CN101249056A (en) * 2008-01-11 2008-08-27 美晨集团股份有限公司 Anti-inflammation gargle water and method of preparing the same
CN107582486A (en) * 2017-09-26 2018-01-16 西安罗格斯生物科技有限公司 It is a kind of to be used for oral hygiene spray that is antibacterial, removing removing abnormal flavor in oral cavity, firm tooth, tooth-whitening

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
林丽霞等: "《牛仔产品艺术加工》", 28 February 2014, 东华大学出版社 *
王永午等: "《现代儿科药物治疗学》", 30 September 1998, 人民军医出版社 *

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Application publication date: 20191206