WO2024016109A1 - Oral care composition of tea active substance and method for preparing same - Google Patents
Oral care composition of tea active substance and method for preparing same Download PDFInfo
- Publication number
- WO2024016109A1 WO2024016109A1 PCT/CN2022/106245 CN2022106245W WO2024016109A1 WO 2024016109 A1 WO2024016109 A1 WO 2024016109A1 CN 2022106245 W CN2022106245 W CN 2022106245W WO 2024016109 A1 WO2024016109 A1 WO 2024016109A1
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- WO
- WIPO (PCT)
- Prior art keywords
- composition
- tea
- sodium
- oral
- cleaning
- Prior art date
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- 239000000203 mixture Substances 0.000 title claims abstract description 49
- 238000000034 method Methods 0.000 title claims abstract description 10
- 239000013543 active substance Substances 0.000 title claims description 4
- 241001122767 Theaceae Species 0.000 title abstract 5
- 235000013824 polyphenols Nutrition 0.000 claims abstract description 42
- 150000008442 polyphenolic compounds Chemical class 0.000 claims abstract description 41
- 238000004140 cleaning Methods 0.000 claims abstract description 32
- 239000000126 substance Substances 0.000 claims abstract description 25
- 239000004094 surface-active agent Substances 0.000 claims abstract description 23
- 210000000214 mouth Anatomy 0.000 claims abstract description 21
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- 235000019640 taste Nutrition 0.000 claims abstract description 12
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- 230000002401 inhibitory effect Effects 0.000 claims abstract description 11
- 239000003755 preservative agent Substances 0.000 claims abstract description 11
- 235000013355 food flavoring agent Nutrition 0.000 claims abstract description 8
- 239000000022 bacteriostatic agent Substances 0.000 claims abstract description 6
- 150000001875 compounds Chemical class 0.000 claims abstract description 5
- 230000002335 preservative effect Effects 0.000 claims abstract description 5
- 235000013616 tea Nutrition 0.000 claims description 61
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- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 34
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 27
- 235000001014 amino acid Nutrition 0.000 claims description 20
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 claims description 16
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 claims description 16
- 229940041616 menthol Drugs 0.000 claims description 16
- DATAGRPVKZEWHA-YFKPBYRVSA-N N(5)-ethyl-L-glutamine Chemical compound CCNC(=O)CC[C@H]([NH3+])C([O-])=O DATAGRPVKZEWHA-YFKPBYRVSA-N 0.000 claims description 14
- 150000001413 amino acids Chemical class 0.000 claims description 14
- 235000011187 glycerol Nutrition 0.000 claims description 14
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 13
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 13
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- YBHILYKTIRIUTE-UHFFFAOYSA-N berberine Chemical compound C1=C2CC[N+]3=CC4=C(OC)C(OC)=CC=C4C=C3C2=CC2=C1OCO2 YBHILYKTIRIUTE-UHFFFAOYSA-N 0.000 claims description 11
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- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims description 10
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
- A61K8/97—Cosmetics 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
Definitions
- the present application relates to the field of oral care, and specifically to a composition for cleaning and inhibiting bacteria on the inner surface of the oral cavity and a preparation method thereof.
- the oral microbial community is a collection of microorganisms that colonize the human oral cavity, and most of them perform microbial physiological functions in the form of biofilms.
- a variety of oral infectious diseases can be induced, including caries, pulp apical disease, periodontal disease, wisdom tooth pericoronitis, jaw osteomyelitis, etc., seriously endangering oral health.
- the oral microbiome is closely related to systemic diseases such as oral tumors, diabetes, rheumatoid arthritis, cardiovascular disease, and premature birth.
- the oral mucosa is exposed to various pathogens (bacteria, viruses, etc.).
- chlorhexidine has the risk of allergy.
- long-term use of oral care products containing chlorhexidine will cause the oral mucosa and teeth to turn yellow. Fluoride may cause tooth deformity and softening, causing tooth enamel to lose its luster and become stained with yellow spots. In severe cases, it may also cause tooth hypoplasia and loss of normal shape. Therefore, there is an urgent need to develop a product with good antibacterial effect, broad spectrum, non-irritating, harmless to humans and animals, and not affected by the environment, organic matter, acid, alkali and other physical and chemical factors.
- Tea is a unique product of China. Chinese people have a long history of drinking tea, and the national awareness of tea is very high. Research has found that the active ingredients in tea have broad-spectrum inhibitory effects on microorganisms (including bacteria, fungi and viruses). Based on this, this application aims to provide a composition for oral surface cleaning and antibacterial composition composed of tea extract as the main component, so as to solve the problems of irritation, sensitization and side effects existing in existing oral cleaning and antibacterial products. .
- a composition for cleaning and inhibiting bacteria on the inner surface of the oral cavity includes by weight: tea polyphenols 0.05-0.49wt%, surfactant, and inclusion complex containing tea polyphenols 0.01-1.19wt% .
- inclusion compound in the composition is hydroxypropyl- ⁇ -cyclodextrin and the surfactant is an amino acid surfactant.
- the amino acid surfactant is selected from one or more of sodium lauroyl alanine, sodium cocoyl alanine, sodium lauroyl sarcosinate and any N-acyl amino acid salts. kind.
- the composition further includes one or more of an auxiliary bacteriostatic agent, a spirit-enhancing substance, a flavoring agent, a pH adjuster, an antifreeze agent, and a preservative.
- the auxiliary bacteriostatic agent includes one or more of amino acid surfactant 0.01-0.15wt%, berberine 0.005-0.010wt%, green tea extract 0.01-0.20wt%, lemon extract 0.01-0.20wt% ;
- Flavoring agents include sorbitol 2.00 ⁇ 8.00wt%, xylitol 0.05 ⁇ 2.00wt%, essence ⁇ 3.00wt%, glycerol 2.00 ⁇ 24.00wt% and one or more substances that can improve the taste; improve
- the psychoactive substances include one or more of ⁇ -cyclodextrin-contained menthol 0.01-1.20wt%, tea polysaccharide 0.01-1.20wt%, and theanine 0.01-0.05wt%; the antifreeze is glycerol 2.00-1.20wt%. 24.00wt%; the preservative 0.20-0.40wt% includes one or more of sodium ascorbate, sodium benzoate, potassium sorbate
- berberine is 0.005-0.008wt%
- green tea extract is 0.05-0.18wt%
- lemon extract is 0.05-0.18wt%
- the pH is adjusted to 5.00-8.00 using a pH adjuster.
- the composition includes, by weight: 0.05wt% tea polyphenols, 0.12wt% amino acid surfactant, and 0.01wt% hydroxypropyl- ⁇ -cyclodextrin.
- a method for preparing an oral surface cleaning and antibacterial composition including the following steps:
- solution 2 Dissolve predetermined weight portions of glycerin, sorbitol, preservatives, and xylitol in water to form solution 2;
- preparing solution 1 also includes the following steps:
- oral cleaning products comprising the above compositions and the use of any of the compositions in oral cleaning products.
- the present application further provides a method for cleaning the oral cavity of humans or animals, by contacting any of the above compositions with the inner surface of the oral cavity.
- Tea polyphenols are a type of polyhydroxy compounds contained in tea, mainly catechins (flavanols), flavones and flavonols, anthocyanins, phenolic acids and depsiphenolic acids, and polymeric phenols. A complex of similar compounds. Tea polyphenols have broad-spectrum and highly efficient antibacterial effects both in vivo and in vitro. Tea polyphenols exert their antibacterial effects mainly by specifically coagulating bacterial proteins, destroying bacterial cell membrane structures, and combining with bacterial DNA, thereby changing the physiological state of bacteria. The purpose of inhibiting its growth is that the antibacterial effect of tea polyphenols is very selective and can inhibit the growth of harmful bacteria and maintain the balance of normal flora.
- tea polyphenols are antibacterial, they can also maintain the integrity of the oral mucosa, enhance the toughness and permeability of capillaries, enhance the resistance of blood vessels, quickly heal oral mucosal ulcers, reduce mucosal bleeding, and protect the oral mucosa.
- Hydroxypropyl- ⁇ -cyclodextrin is a hydrophilic derivative formed by the condensation of ⁇ -cyclodextrin and 1,2-propylene oxide. Hydroxypropyl- ⁇ -cyclodextrin has a special three-dimensional ring structure with "hydrophobic inside and hydrophilic outside". The hydrophobic cavity can enclose the drug, thereby improving the water solubility, stability and antioxidant of the guest molecule. , resist photolysis, or achieve sustained release and three-dimensional separation effects. It is used to encapsulate tea polyphenols and reduce the bitterness caused by the combination of phenolic substances and proteins in the oral cavity through sustained release.
- Tea polysaccharide is an acidic glycoprotein combined with a large number of mineral elements.
- the protein part is mainly composed of about 20 common amino acids. Tea polysaccharide has the effects of antioxidant, lowering blood sugar, lowering blood lipids, and regulating intestinal flora. It also has obvious effects in anticoagulation, preventing thrombosis, protecting blood phase, and enhancing the body's non-specific immunity.
- Theanine is a unique free amino acid in tea. It is the main ingredient in tea that promotes body fluids and sweetness. It also has the health-care effects of relieving fatigue, relaxing the body and mind, lowering blood pressure and improving learning and memory abilities.
- Tea polyphenols and berberine can also effectively prevent a variety of viral infections. Many studies have proven that berberine can reduce the risk of influenza virus and hepatitis B virus infection; tea polyphenols can inhibit various stages of the influenza virus growth cycle, and tea polyphenols also It can inhibit the attachment or invasion of viruses, such as SARS virus, human herpes virus, adenovirus, etc., by interacting with the receptor protein or envelope structure on the virus surface.
- viruses such as SARS virus, human herpes virus, adenovirus, etc.
- N-acyl amino acid salt surfactants such as sodium lauroyl sarcosinate, sodium lauroyl alanine and sodium cocoyl alanine are new green and environmentally friendly surfactants derived from renewable substances. They are different from other traditional surfactants. In comparison, sodium lauroyl sarcosinate, sodium lauroyl alanine, and sodium cocoyl alanine have better wettability, foaming, antibacterial, anti-corrosion, and antistatic capabilities. N-acyl amino acid salt surfactants such as sodium lauroyl sarcosinate, sodium lauroyl alanine and sodium cocoyl alanine are non-toxic and harmless, mild and non-irritating to the oral cavity.
- the degradation products are amino acids and fatty acids, which are harmful to the oral cavity.
- amino acid surfactants use their surface activity and bacteriostasis at the same time to qualitatively adsorb at the interface to achieve cleaning, antibacterial, antitoxic and other effects.
- N-acyl amino acid salt surfactants have good effects in the oral cavity. Inhibits the action of lactic acid bacteria that convert glucose into lactic acid.
- Beta cyclodextrin menthol can be directly dissolved in an aqueous system without ethanol to help dissolve it, giving it a refreshing mint feel without the irritation caused by alcohol.
- Flavoring agents can further improve or shield the bitter taste and astringent irritation of tea polyphenols.
- Preservatives can effectively protect tea polyphenols from oxidation and maintain the antibacterial effect of the product.
- the tea polyphenols in the oral cleaning antibacterial composition provided by this application have broad-spectrum antibacterial effects, without the need to add other antibacterial agents, the ingredients are safe, and the taste is relieved through the effect of the auxiliary material hydroxypropyl- ⁇ -cyclodextrin irritating.
- adding preservatives can solve the problem of the impact of tea polyphenols on the antibacterial effect after oxidation.
- this application further adds auxiliary antibacterial agents such as berberine, which enhance the effect of tea polyphenols in preventing various viral infections.
- the cleaning and antibacterial composition in this application is non-irritating to mucous membranes, has broad-spectrum antibacterial properties, low onset concentration, fast action, stable performance, is easily soluble in water, and is environmentally friendly. It has the same antibacterial properties as chemicals. It has the same bacterial effect, but it is more natural, healthier and more in line with the consumption habits of Chinese people.
- Figure 1 is a schematic diagram of the antibacterial effect of Example 1 and Example 2 of the present application on Staphylococcus aureus;
- Figure 2 is a schematic diagram of the antibacterial effect of Example 3, Example 4, Example 5 and Example 6 of the present application on Staphylococcus aureus;
- Figure 3 is a schematic diagram of the antibacterial effect of Comparative Example 1 of the present application on Staphylococcus aureus;
- Figure 4 is a schematic diagram of the antibacterial effect of Comparative Example 2 of the present application on Staphylococcus aureus;
- Figure 5 shows the antibacterial effect of oral care product 1 on the market on Staphylococcus aureus
- Figure 6 shows the antibacterial effect of oral care product 2 on the market on Staphylococcus aureus
- Figure 7 shows the antibacterial effect of 3 oral care products on the market on Staphylococcus aureus
- Figure 8 shows the antibacterial effect of 4 oral care products on the market on Staphylococcus aureus
- Figure 9 shows the antibacterial effect of 5 oral care products on the market on Staphylococcus aureus
- Figure 10 shows the antibacterial effect of 6 oral care products on the market on Staphylococcus aureus.
- an embodiment means that a particular feature, structure or characteristic described in connection with the embodiment can be included in at least one embodiment of the present application.
- the appearances of this phrase in various places in the specification are not necessarily all referring to the same embodiment, nor are separate or alternative embodiments mutually exclusive of other embodiments. Those skilled in the art understand, both explicitly and implicitly, that the embodiments described herein may be combined with other embodiments.
- the antibacterial substance is 0.05wt% tea polyphenols
- Excipients including:
- the antibacterial substance is 0.05wt% tea polyphenols
- Excipients including:
- the preparation process is the same as the above embodiment.
- preparing solution 1 it also includes adding a predetermined weight portion of berberine and green tea extract.
- the antibacterial substance is 0.49wt% tea polyphenols
- Excipients including:
- the preparation process is the same as the above embodiment.
- the antibacterial substance is 0.20wt% tea polyphenols
- Excipients including:
- the preparation process is the same as the above embodiment.
- preparing solution 1 it also includes adding a predetermined weight portion of lemon extract.
- the antibacterial substance is 0.30wt% tea polyphenols
- Excipients including:
- the preparation process is the same as the above embodiment.
- the antibacterial substance is 0.10wt% tea polyphenols
- Excipients including:
- the preparation process is the same as the above embodiment.
- the oral inner surface cleaning and antibacterial composition of this comparative example includes the following components:
- the antibacterial substance is 0.04wt% tea polyphenols
- Excipients including:
- the preparation process is the same as the above embodiment.
- the oral inner surface cleaning and antibacterial composition of this comparative example includes the following components:
- the antibacterial substance is 0.50wt% tea polyphenols
- Excipients including:
- test samples are as follows: Examples 1-6, Control 1 (water, sorbitol, propylene glycol, PEG-40 hydrogenated castor oil, tea extract, dipotassium glycyrrhizate, menthol, sucralose, hydroxyphenyl Methyl ester, sodium benzoate, flavoring, CI 19140, CI 42090);
- Control 2 water, glycerin, propylene glycol, sorbitol, poloxamer 407, flavor (containing tea extract), saccharin sodium, cetylpyridinium chloride (0.075%), sodium fluoride (0.05%), Potassium sorbate, menthol, CI19140, CI42051);
- Control 3 water, glycerin, sorbitol, PEG-40 hydrogenated castor oil, xylitol, cherry blossom extract, yeast fermentation product extract, tea extract, peppermint extract, probiotics (paracheese milk) bacilli), menthol, citric acid, methylparaben, chlorogalactose, domiphene, flavor);
- Control 4 water, sorbitol, glycerin, sodium chloride, methyl paraben, sodium benzoate, essence, menthol, lactobacilli, lysozyme, plant peptides, propolis extract, honeysuckle flower extract, Bletilla striata Root extract, Dendrobium officinale extract, hydrogenated castor oil, citric acid);
- Control 5 water, ethanol, sorbitol, thymol, eucalyptol, methyl salicylate, menthol, sodium benzoate, benzoic acid, poloxamer 407, sodium saccharin, CI 42053, food flavors);
- Control 6 (contains 0.6 g of chlorhexidine gluconate and 0.1 g of metronidazole per 500 ml; excipients are: glycerin, polysorbate 80, polyethylene glycol-400, concentrated mint water, ethanol, saccharin sodium, pigment, essence, purified water).
- Test strain Staphylococcus aureus ATCC6538
- Test method According to the antibacterial ring test requirements in the Disinfection Technical Specifications (2002 Edition), 4 test samples and 1 negative control sample are placed on each bacteria-contaminated plate, for a total of 5 pieces. Use sterile forceps to take a sample piece and place it on the surface of the plate. The centers of each sample should be at least 25mm apart and at least 15mm apart from the edge of the flat plate. After the patch is placed, use sterile tweezers to gently press the sample piece to make it stick to the surface of the plate. Cover the plate, place it in a 37°C incubator, and incubate for 16 to 18 hours to observe the results. Use a vernier caliper to measure the diameter of the inhibition ring (including the patch) and record it. The test was repeated three times. The bactericidal activity was evaluated based on the presence and size of the inhibition zone.
- CK all represent sterile water, and the numbers represent examples.
- the diameter of the inhibitory ring is greater than 7mm, it is judged to have antibacterial effect; if the diameter of the inhibitory ring is less than or equal to 7mm, it is judged to have no antibacterial effect.
- Test samples Examples 1-6, Comparative Examples 1-2, Control 3 (water, glycerol, sorbitol, PEG-40 hydrogenated castor oil, xylitol, cherry blossom extract, yeast fermentation product extract , tea extract, peppermint extract, probiotics (Lactobacillus paracasei), menthol, citric acid, methyl paraben, chlorogalactose, domiphene, flavor);
- Control 4 water, sorbitol, glycerin, sodium chloride, methyl paraben, sodium benzoate, essence, menthol, lactobacilli, lysozyme, plant peptides, propolis extract, honeysuckle flower extract, Bletilla striata Root extract, Dendrobium officinale extract, hydrogenated castor oil, citric acid);
- Control 5 water, ethanol, sorbitol, thymol, eucalyptol, methyl salicylate, menthol, sodium benzoate, benzoic acid, poloxamer 407, sodium saccharin, CI 42053, food flavors);
- Control 6 (contains 0.6 g of chlorhexidine gluconate and 0.1 g of metronidazole per 500 ml. Excipients are: glycerin, polysorbate 80, polyethylene glycol-400, concentrated mint water, ethanol, saccharin sodium, pigment, Fragrance, purified water).
- Test strain Staphylococcus aureus ATCC6538
- test method According to the GB 15979-2002 Hygienic Standard for Disposable Hygiene Products, C4 dissolution antibacterial (anti)bacterial product antibacterial performance test method, each test sample acts on Staphylococcus aureus for 2min, 5min, 10min, 20min, calculated The antibacterial rates are as follows:
- the product has antibacterial effect.
- the antibacterial rate is greater than or equal to 90%, and the product has strong antibacterial effect.
- Test samples Examples 1-6, Comparative Examples 1-2.
- a score of 4-5 means the mouthwash tastes comfortable, has a suitable tea flavor, is mild and non-irritating;
- a score of 3-4 indicates that the mouthwash tastes average and has the obvious bitterness of tea, which is within an acceptable range
- a score of less than 3 means that the mouthwash has a distinctly bitter taste and is unacceptable.
- the cleaning and antibacterial composition provided in this application can achieve an antibacterial effect close to that of chemical products by relying only on the natural active substance tea polyphenols in tea. It can prevent the occurrence of dental caries and periodontitis by inhibiting bacterial growth. It is safe and has no side effects. It inhibits bacteria and does not cause harm to the oral mucosa. Tea polyphenols and berberine also have certain antiviral effects, which can reduce the risk of viral infection from the oral cavity to a certain extent, enabling oral care compositions to effectively protect against influenza virus, coronavirus, hepatitis B virus, human herpes virus and other viruses.
- the composition in this application is an alcohol-free formula and has a refreshing mint feeling without the irritation caused by alcohol. It completely solves the problems of poor safety and irritating taste of existing chemical products, and is suitable for preparing antibacterial, safe and natural oral care products with suitable taste.
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Abstract
The present application pertains to the field of oral hygiene and care, and particularly provides a composition for cleaning the inner surface of the oral cavity and inhibiting bacteria thereon, comprising: 0.05-0.49 wt% of tea polyphenol, a surfactant, and 0.01-1.19 wt% of an inclusion compound that includes tea polyphenol, and comprising one or more of an auxiliary bacteriostatic agent, a refreshing substance, a flavoring agent, a pH regulator, an anti-freezing agent, and a preservative. The present application further provides a method for preparing the composition and use of the composition. The present application uses tea polyphenol, an active ingredient in tea, as the main bacteriostatic component, adds cleaning and auxiliary bacteriostatic components to ensure the effective bacteriostatic effect of the composition, and eliminates the irritating taste by means of component combination, thus having wide market prospects.
Description
本申请涉及口腔护理领域,具体涉及口腔内表面清洁抑菌的组合物及其制备方法。The present application relates to the field of oral care, and specifically to a composition for cleaning and inhibiting bacteria on the inner surface of the oral cavity and a preparation method thereof.
口腔微生物群落是定植于人体口腔的微生物集合,多以生物膜形式行使微生物生理学功能。当微生物群落与宿主间生态关系失衡时,可诱发多种口腔感染性疾病,包括龋病、牙髓根尖周病、牙周病、智齿冠周炎、颌骨骨髓炎等,严重危害口腔健康。更为重要的是,口腔微生物群落与口腔肿瘤、糖尿病、类风湿性关节炎、心血管疾病及早产等系统性疾病紧密相关。口腔黏膜作为人体免疫系统的第一道防线,会接触到各种病原体(细菌和病毒等),因此,清洁口腔中的食物残渣和抑制病原菌是非常重要的抗感染方法。目前,常用黏膜表面的清洁抑菌产品多为用化学品抑菌,例如,酒精、甲硝唑、氯已定、单氟磷酸钠、苯扎溴铵和H
2O
2等。但化学品都有一定的刺激性不适合免疫力弱者(如患免疫系统疾病)、过敏者、老人、孕妇及哺乳期妇女、小孩和黏膜表面有创伤的病人或动物使用,例如酒精会导致口腔干燥,破坏保持口腔湿润的黏液保护层,并引发刺痛感;氯己定存在过敏的风险,其次长期使用含氯己定的口腔护理产品会使口腔黏膜与牙齿发黄。氟可能会导致牙齿畸形、软化,牙釉质失去光彩并且带有黄色斑点,严重者还会导致牙齿发育不全、失去正常形态等。因此,亟需开发一种抑菌效果好、广谱、无刺激和对人、畜无害以及不受环境、有机物、酸、碱及其它物理、化学因素影响的产品。
The oral microbial community is a collection of microorganisms that colonize the human oral cavity, and most of them perform microbial physiological functions in the form of biofilms. When the ecological relationship between the microbial community and the host is imbalanced, a variety of oral infectious diseases can be induced, including caries, pulp apical disease, periodontal disease, wisdom tooth pericoronitis, jaw osteomyelitis, etc., seriously endangering oral health. . More importantly, the oral microbiome is closely related to systemic diseases such as oral tumors, diabetes, rheumatoid arthritis, cardiovascular disease, and premature birth. As the first line of defense of the human immune system, the oral mucosa is exposed to various pathogens (bacteria, viruses, etc.). Therefore, cleaning food residues in the oral cavity and inhibiting pathogenic bacteria are very important anti-infection methods. At present, most of the commonly used cleaning and antibacterial products for mucosal surfaces use chemical antibacterial agents, such as alcohol, metronidazole, chlorhexidine, sodium monofluorophosphate, benzalkonium bromide, and H 2 O 2 . However, chemicals are irritating to a certain extent and are not suitable for use by people with weak immunity (such as those suffering from immune system diseases), allergies, the elderly, pregnant and lactating women, children, and patients or animals with trauma to the mucosal surface. For example, alcohol can cause oral Drying, destroying the protective layer of mucus that keeps the mouth moist, and causing a stinging sensation; chlorhexidine has the risk of allergy. Secondly, long-term use of oral care products containing chlorhexidine will cause the oral mucosa and teeth to turn yellow. Fluoride may cause tooth deformity and softening, causing tooth enamel to lose its luster and become stained with yellow spots. In severe cases, it may also cause tooth hypoplasia and loss of normal shape. Therefore, there is an urgent need to develop a product with good antibacterial effect, broad spectrum, non-irritating, harmless to humans and animals, and not affected by the environment, organic matter, acid, alkali and other physical and chemical factors.
发明内容Contents of the invention
茶是中国特有产品,国人喝茶历史悠久,国民对茶的认知度非常高。经研究发现茶叶中的活性成分对微生物(包括细菌、真菌和病毒)具有广谱的抑制作用。基于此,本申请旨在提供一种以茶叶提取物为主要成分组成的用 于口腔内表面清洁并抑菌的组合物,以解决现有口腔清洁抑菌产品存在的刺激、致敏和副作用等问题。Tea is a unique product of China. Chinese people have a long history of drinking tea, and the national awareness of tea is very high. Research has found that the active ingredients in tea have broad-spectrum inhibitory effects on microorganisms (including bacteria, fungi and viruses). Based on this, this application aims to provide a composition for oral surface cleaning and antibacterial composition composed of tea extract as the main component, so as to solve the problems of irritation, sensitization and side effects existing in existing oral cleaning and antibacterial products. .
根据本申请一个方面,用于口腔内表面清洁抑菌的组合物,按重量分数包括:茶多酚0.05~0.49wt%、表面活性剂、包合茶多酚的包合物0.01~1.19wt%。According to one aspect of the present application, a composition for cleaning and inhibiting bacteria on the inner surface of the oral cavity includes by weight: tea polyphenols 0.05-0.49wt%, surfactant, and inclusion complex containing tea polyphenols 0.01-1.19wt% .
进一步地,组合物中的包合物为羟丙基-β-环糊精以及表面活性剂为氨基酸表面活性剂。Further, the inclusion compound in the composition is hydroxypropyl-β-cyclodextrin and the surfactant is an amino acid surfactant.
根据本申请中的一些实施例,氨基酸表面活性剂选自月桂酰丙氨酸钠、椰油酰丙氨酸钠、月桂酰肌氨酸钠及任何N-酰基氨基酸盐类中的一种或多种。According to some embodiments in this application, the amino acid surfactant is selected from one or more of sodium lauroyl alanine, sodium cocoyl alanine, sodium lauroyl sarcosinate and any N-acyl amino acid salts. kind.
根据本申请中的一些实施例,组合物还包括辅助抑菌剂、提振精神的物质、矫味剂、pH调节剂、防冻剂、防腐剂中的一种或多种。According to some embodiments in this application, the composition further includes one or more of an auxiliary bacteriostatic agent, a spirit-enhancing substance, a flavoring agent, a pH adjuster, an antifreeze agent, and a preservative.
具体地,辅助抑菌剂包括氨基酸表面活性剂0.01~0.15wt%、黄连素0.005~0.010wt%、绿茶提取物0.01~0.20wt%、柠檬提取物0.01~0.20wt%中的一种或多种;矫味剂包括山梨醇2.00~8.00wt%、木糖醇0.05~2.00wt%、香精≤3.00wt%、甘油2.00~24.00wt%及任何可改善口感的物质中的一种或多种;提振精神的物质包括β环糊精包合的薄荷醇0.01~1.20wt%、茶多糖0.01~1.20wt%、茶氨酸0.01~0.05wt%中的一种或多种;防冻剂为甘油2.00~24.00wt%;防腐剂0.20~0.40wt%包括抗坏血酸钠、苯甲酸钠、山梨酸钾、羟苯甲酯中的一种或多种;pH调节剂包括碳酸钠和/或碳酸氢钠。Specifically, the auxiliary bacteriostatic agent includes one or more of amino acid surfactant 0.01-0.15wt%, berberine 0.005-0.010wt%, green tea extract 0.01-0.20wt%, lemon extract 0.01-0.20wt% ; Flavoring agents include sorbitol 2.00~8.00wt%, xylitol 0.05~2.00wt%, essence ≤3.00wt%, glycerol 2.00~24.00wt% and one or more substances that can improve the taste; improve The psychoactive substances include one or more of β-cyclodextrin-contained menthol 0.01-1.20wt%, tea polysaccharide 0.01-1.20wt%, and theanine 0.01-0.05wt%; the antifreeze is glycerol 2.00-1.20wt%. 24.00wt%; the preservative 0.20-0.40wt% includes one or more of sodium ascorbate, sodium benzoate, potassium sorbate, and methyl paraben; the pH adjuster includes sodium carbonate and/or sodium bicarbonate.
进一步地,黄连素为0.005~0.008wt%、绿茶提取物为0.05~0.18wt%、柠檬提取物为0.05~0.18wt%,用pH调节剂将pH调节到5.00-8.00。Further, berberine is 0.005-0.008wt%, green tea extract is 0.05-0.18wt%, lemon extract is 0.05-0.18wt%, and the pH is adjusted to 5.00-8.00 using a pH adjuster.
根据本申请的某个实施例,组合物按重量分数,包括:茶多酚0.05wt%、氨基酸表面活性剂0.12wt%、羟丙基-β-环糊精0.01wt%。According to a certain embodiment of the present application, the composition includes, by weight: 0.05wt% tea polyphenols, 0.12wt% amino acid surfactant, and 0.01wt% hydroxypropyl-β-cyclodextrin.
根据本申请另一方面,还提供了口腔内表面清洁抑菌组合物的制备方法,包括以下步骤:According to another aspect of the present application, a method for preparing an oral surface cleaning and antibacterial composition is also provided, including the following steps:
取预定重量份的植物活性物质茶多酚、茶氨酸、茶多糖、β环糊精薄荷 醇和羟丙基-β-环糊精,溶解于水中,形成溶液1;Take a predetermined weight portion of plant active substances tea polyphenols, theanine, tea polysaccharide, β-cyclodextrin menthol and hydroxypropyl-β-cyclodextrin, and dissolve them in water to form solution 1;
取预定重量份的甘油、山梨醇、防腐剂、木糖醇溶解于水中,形成溶液2;Dissolve predetermined weight portions of glycerin, sorbitol, preservatives, and xylitol in water to form solution 2;
在溶液2中加入氨基酸表面活性剂和香精,均匀混合后加入所述溶液1,补足水,调节pH,灭菌,即得。Add amino acid surfactant and essence to solution 2, mix evenly, then add solution 1, add water, adjust pH, and sterilize to obtain.
进一步地,制备溶液1,还包括以下步骤:Further, preparing solution 1 also includes the following steps:
添加预定重量份的黄连素;和/或Add a predetermined weight portion of berberine; and/or
添加预定重量份的柠檬提取物;和/或Add a predetermined weight portion of lemon extract; and/or
添加预定重量份的绿茶提取物。Add a predetermined weight portion of green tea extract.
进一步地,包含以上组合物的口腔清洁产品和任一所述组合物在口腔清洁产品中的应用。Further, oral cleaning products comprising the above compositions and the use of any of the compositions in oral cleaning products.
本申请还进一步提供了一种清洁人或动物口腔的方法,将上述任一组合物与口腔内表面接触。The present application further provides a method for cleaning the oral cavity of humans or animals, by contacting any of the above compositions with the inner surface of the oral cavity.
茶多酚是茶叶中所含的一类多羟基类化合物,主要为儿茶素类(黄烷醇类)、黄酮及黄酮醇类、花青素类、酚酸及缩酚酸类、聚合酚类等化合物的复合体。茶多酚在体内外均具有广谱高效的抗菌作用,茶多酚发挥自身抗菌作用主要是通过特异性地凝固细菌蛋白、破坏菌体细胞膜结构、与菌体DNA结合,从而改变细菌生理状态达到抑制其生长目的,茶多酚的抑菌作用有很强的的选择性,可抑制有害菌群的生长,维持正常菌群平衡。另外,茶多酚在抑菌的同时还具有维持口腔黏膜完整性,增强毛细血管的韧性、渗透性,增强血管的抵抗力,快速愈合口腔黏膜溃疡,减轻黏膜出血,保护口腔黏膜的功能。Tea polyphenols are a type of polyhydroxy compounds contained in tea, mainly catechins (flavanols), flavones and flavonols, anthocyanins, phenolic acids and depsiphenolic acids, and polymeric phenols. A complex of similar compounds. Tea polyphenols have broad-spectrum and highly efficient antibacterial effects both in vivo and in vitro. Tea polyphenols exert their antibacterial effects mainly by specifically coagulating bacterial proteins, destroying bacterial cell membrane structures, and combining with bacterial DNA, thereby changing the physiological state of bacteria. The purpose of inhibiting its growth is that the antibacterial effect of tea polyphenols is very selective and can inhibit the growth of harmful bacteria and maintain the balance of normal flora. In addition, while tea polyphenols are antibacterial, they can also maintain the integrity of the oral mucosa, enhance the toughness and permeability of capillaries, enhance the resistance of blood vessels, quickly heal oral mucosal ulcers, reduce mucosal bleeding, and protect the oral mucosa.
羟丙基-β-环糊精(Hydroxypropyl-β-cyclodextrin)是β-环糊精与1,2-环氧丙烷缩合而成的亲水性衍生物。羟丙基-β-环糊精有1个“内疏水、外亲水”的特殊立体环状结构,疏水空腔可以对药物进行包合,从而提高客体分子的水溶性、稳定性和抗氧化、抗光解能力,或达到缓释和立体分离效果。用来包埋茶多酚通过缓释作用降低酚类物质与口腔内蛋白质结合形成 的苦涩感。Hydroxypropyl-β-cyclodextrin is a hydrophilic derivative formed by the condensation of β-cyclodextrin and 1,2-propylene oxide. Hydroxypropyl-β-cyclodextrin has a special three-dimensional ring structure with "hydrophobic inside and hydrophilic outside". The hydrophobic cavity can enclose the drug, thereby improving the water solubility, stability and antioxidant of the guest molecule. , resist photolysis, or achieve sustained release and three-dimensional separation effects. It is used to encapsulate tea polyphenols and reduce the bitterness caused by the combination of phenolic substances and proteins in the oral cavity through sustained release.
茶多糖是一种酸性糖蛋白,并结合有大量的矿质元素。其中蛋白部分主要由约20种常见的氨基酸组成。茶多糖具有抗氧化、降血糖、降血脂、调节肠道菌群的作用,同时在抗凝、防血栓形成,保护血相和增强人体非特异性免疫能力等方面均有明显效果。Tea polysaccharide is an acidic glycoprotein combined with a large number of mineral elements. The protein part is mainly composed of about 20 common amino acids. Tea polysaccharide has the effects of antioxidant, lowering blood sugar, lowering blood lipids, and regulating intestinal flora. It also has obvious effects in anticoagulation, preventing thrombosis, protecting blood phase, and enhancing the body's non-specific immunity.
茶氨酸是茶叶中特有的游离氨基酸,是茶叶中生津润甜的主要成分,另外还具有消解疲劳、旷怡身心、降低血压和提高学习记忆能力的保健作用。Theanine is a unique free amino acid in tea. It is the main ingredient in tea that promotes body fluids and sweetness. It also has the health-care effects of relieving fatigue, relaxing the body and mind, lowering blood pressure and improving learning and memory abilities.
茶多酚和黄连素还可以有效预防多种病毒感染,多项研究已证明黄连素可以降低流感病毒和乙肝病毒的感染风险;茶多酚可以抑制流感病毒生长周期的各个阶段,茶多酚还可以通过与病毒表面的受体蛋白或包膜结构相互作用来抑制病毒的附着或侵入,如SARS病毒,人类疱疹病毒,腺病毒等。Tea polyphenols and berberine can also effectively prevent a variety of viral infections. Many studies have proven that berberine can reduce the risk of influenza virus and hepatitis B virus infection; tea polyphenols can inhibit various stages of the influenza virus growth cycle, and tea polyphenols also It can inhibit the attachment or invasion of viruses, such as SARS virus, human herpes virus, adenovirus, etc., by interacting with the receptor protein or envelope structure on the virus surface.
月桂酰肌氨酸钠、月桂酰丙氨酸钠和椰油酰丙氨酸钠等N-酰基氨基酸盐类表面活性剂是可再生物质来源的新型绿色环保表面活性剂,与其他传统表面活性剂相比,月桂酰肌氨酸钠、月桂酰丙氨酸钠和椰油酰丙氨酸钠等有更好的润湿性、起泡性、抗菌、抗蚀、抗静电能力等特点。月桂酰肌氨酸钠、月桂酰丙氨酸钠和椰油酰丙氨酸钠等N-酰基氨基酸盐类表面活性剂无毒无害,对口腔温和无刺激,降解产物为氨基酸和脂肪酸,对环境基本无影响;氨基酸表面活性剂同时利用其表面活性和抑菌性,在界面处发生定性吸附达到清洁、抗菌、抗毒等功效,比如,N-酰基氨基酸盐类表面活性剂在口腔内具有抑制使葡萄糖变为乳酸的乳酸菌的作用。作为口腔产品的重要成分,还具有与其他成分很好的配伍性,起到清洁口腔以及清新口气的效果。N-acyl amino acid salt surfactants such as sodium lauroyl sarcosinate, sodium lauroyl alanine and sodium cocoyl alanine are new green and environmentally friendly surfactants derived from renewable substances. They are different from other traditional surfactants. In comparison, sodium lauroyl sarcosinate, sodium lauroyl alanine, and sodium cocoyl alanine have better wettability, foaming, antibacterial, anti-corrosion, and antistatic capabilities. N-acyl amino acid salt surfactants such as sodium lauroyl sarcosinate, sodium lauroyl alanine and sodium cocoyl alanine are non-toxic and harmless, mild and non-irritating to the oral cavity. The degradation products are amino acids and fatty acids, which are harmful to the oral cavity. There is basically no impact on the environment; amino acid surfactants use their surface activity and bacteriostasis at the same time to qualitatively adsorb at the interface to achieve cleaning, antibacterial, antitoxic and other effects. For example, N-acyl amino acid salt surfactants have good effects in the oral cavity. Inhibits the action of lactic acid bacteria that convert glucose into lactic acid. As an important ingredient in oral products, it also has good compatibility with other ingredients and has the effect of cleaning the mouth and freshening breath.
β环糊精薄荷醇可以在无乙醇助溶的水相体系直接溶解,具有薄荷清凉感且没有酒精带来的刺激感。Beta cyclodextrin menthol can be directly dissolved in an aqueous system without ethanol to help dissolve it, giving it a refreshing mint feel without the irritation caused by alcohol.
矫味剂可进一步改善或屏蔽茶多酚的苦涩味和收敛刺激性。Flavoring agents can further improve or shield the bitter taste and astringent irritation of tea polyphenols.
防腐剂可以有效保护茶多酚不被氧化,维持产品抑菌功效。Preservatives can effectively protect tea polyphenols from oxidation and maintain the antibacterial effect of the product.
发明有益效果Invent beneficial effects
本申请所提供的口腔清洁抑菌组合物中的茶多酚具有广谱抑菌作用,无需添加其他抑菌剂,成分安全,并通过辅料羟丙基-β-环糊精的作用缓解了口感上的刺激性。同时,添加防腐剂可解决茶多酚氧化后对抑菌功效的影响问题,此外,本申请进一步加入黄连素等辅助抑菌剂,它们增强了茶多酚在预防多种病毒感染方面的作用。本申请中的清洁抑菌组合物对黏膜无刺激性,并具有广谱抑菌,起效浓度低,作用速度快,性能稳定,易溶于水和环境友好等优点,与化学品达到的抑菌效果相当,但是更天然、更健康、更符合国人的消费习惯。The tea polyphenols in the oral cleaning antibacterial composition provided by this application have broad-spectrum antibacterial effects, without the need to add other antibacterial agents, the ingredients are safe, and the taste is relieved through the effect of the auxiliary material hydroxypropyl-β-cyclodextrin irritating. At the same time, adding preservatives can solve the problem of the impact of tea polyphenols on the antibacterial effect after oxidation. In addition, this application further adds auxiliary antibacterial agents such as berberine, which enhance the effect of tea polyphenols in preventing various viral infections. The cleaning and antibacterial composition in this application is non-irritating to mucous membranes, has broad-spectrum antibacterial properties, low onset concentration, fast action, stable performance, is easily soluble in water, and is environmentally friendly. It has the same antibacterial properties as chemicals. It has the same bacterial effect, but it is more natural, healthier and more in line with the consumption habits of Chinese people.
构成本申请的一部分的附图用来提供对本申请的进一步理解,本申请的示意性实施例及其说明用于解释本申请,并不构成对本申请的不当限定。在附图中:The drawings that form a part of this application are used to provide a further understanding of this application. The illustrative embodiments and descriptions of this application are used to explain this application and do not constitute an improper limitation of this application. In the attached picture:
图1为本申请实施例1和实施例2对金黄色葡萄球菌的抑菌效果示意图;Figure 1 is a schematic diagram of the antibacterial effect of Example 1 and Example 2 of the present application on Staphylococcus aureus;
图2为本申请实施例3、实施例4、实施例5和实施例6对金黄色葡萄球菌的抑菌效果示意图;Figure 2 is a schematic diagram of the antibacterial effect of Example 3, Example 4, Example 5 and Example 6 of the present application on Staphylococcus aureus;
图3为本申请对比例1对金黄色葡萄球菌的抑菌效果示意图;Figure 3 is a schematic diagram of the antibacterial effect of Comparative Example 1 of the present application on Staphylococcus aureus;
图4为本申请对比例2对金黄色葡萄球菌的抑菌效果示意图;Figure 4 is a schematic diagram of the antibacterial effect of Comparative Example 2 of the present application on Staphylococcus aureus;
图5为市场上口腔护理产品1对金黄色葡萄球菌的抑菌效果图;Figure 5 shows the antibacterial effect of oral care product 1 on the market on Staphylococcus aureus;
图6为市场上口腔护理产品2对金黄色葡萄球菌的抑菌效果图;Figure 6 shows the antibacterial effect of oral care product 2 on the market on Staphylococcus aureus;
图7为市场上口腔护理产品3对金黄色葡萄球菌的抑菌效果图;Figure 7 shows the antibacterial effect of 3 oral care products on the market on Staphylococcus aureus;
图8为市场上口腔护理产品4对金黄色葡萄球菌的抑菌效果图;Figure 8 shows the antibacterial effect of 4 oral care products on the market on Staphylococcus aureus;
图9为市场上口腔护理产品5对金黄色葡萄球菌的抑菌效果图;Figure 9 shows the antibacterial effect of 5 oral care products on the market on Staphylococcus aureus;
图10为市场上口腔护理产品6对金黄色葡萄球菌的抑菌效果图。Figure 10 shows the antibacterial effect of 6 oral care products on the market on Staphylococcus aureus.
以下结合附图和实施例,对本申请的具体实施方式进行更加详细的说明,以便能够更好地理解本申请的方案以及其各个方面的优点。然而,以下描述的具体实施方式和实施例仅是说明的目的,而不是对本申请的限制。不应将此理解为本申请的制备方法仅仅限于上述所列举方法。The specific embodiments of the present application will be described in more detail below with reference to the accompanying drawings and examples, so that the solutions of the present application and the advantages of each aspect thereof can be better understood. However, the specific embodiments and examples described below are for illustrative purposes only and are not intended to limit the application. This should not be understood to mean that the preparation method of the present application is limited to the methods listed above.
在本文中提及“实施例”意味着,结合实施例描述的特定特征、结构或特性可以包含在本申请的至少一个实施例中。在说明书中的各个位置出现该短语并不一定均是指相同的实施例,也不是与其它实施例互斥的独立的或备选的实施例。本领域技术人员显式地和隐式地理解的是,本文所描述的实施例可以与其它实施例相结合。Reference herein to "an embodiment" means that a particular feature, structure or characteristic described in connection with the embodiment can be included in at least one embodiment of the present application. The appearances of this phrase in various places in the specification are not necessarily all referring to the same embodiment, nor are separate or alternative embodiments mutually exclusive of other embodiments. Those skilled in the art understand, both explicitly and implicitly, that the embodiments described herein may be combined with other embodiments.
下面参考具体实施例,对本申请进行说明。The present application will be described below with reference to specific embodiments.
称取预定重量份的茶多酚、羟丙基-β-环糊精、辅助抑菌剂和提振精神的物质混合后,充分溶解于去离子水中,形成溶液1;Weigh and mix predetermined weight portions of tea polyphenols, hydroxypropyl-β-cyclodextrin, auxiliary bacteriostatic agents and energy-boosting substances, then fully dissolve them in deionized water to form solution 1;
再取预定重量份的防冻剂、矫味剂和防腐剂溶解于去离子水中,形成溶液2;Then take predetermined weight portions of antifreeze, flavoring agents and preservatives and dissolve them in deionized water to form solution 2;
然后,在溶液2中加入氨基酸表面活性剂和香精,均匀混合后加入上述溶液1,补足水,用pH调节剂调节pH,经过滤灭菌处理,获得口腔内表面清洁抑菌溶液。Then, add amino acid surfactant and essence to solution 2, mix evenly, add the above solution 1, add water, adjust the pH with a pH adjuster, and undergo filtration and sterilization to obtain a cleaning and antibacterial solution for the inner surface of the oral cavity.
实施例1Example 1
本实施例的口腔内表面清洁抑菌组合物包括以下组分:The oral inner surface cleaning and antibacterial composition of this embodiment includes the following components:
抑菌物质,为0.05wt%的茶多酚;The antibacterial substance is 0.05wt% tea polyphenols;
辅料,包括:Excipients, including:
称取以下预定重量份的原料:茶多酚0.05wt%、茶氨酸0.01wt%、茶多糖0.01wt%、β环糊精薄荷醇0.01wt%和羟丙基-β-环糊精0.01wt%混合后,溶解于去离子水中,形成溶液1;Weigh the following raw materials in predetermined weight portions: tea polyphenols 0.05wt%, theanine 0.01wt%, tea polysaccharide 0.01wt%, β-cyclodextrin menthol 0.01wt% and hydroxypropyl-β-cyclodextrin 0.01wt After % mixing, dissolve in deionized water to form solution 1;
再取预定重量份的甘油2.00wt%、山梨醇8.00wt%、苯甲酸钠0.20wt%、抗坏血酸钠0.20wt%、木糖醇0.05wt%溶解于去离子水中,形成溶液2;Then take predetermined weight portions of glycerol 2.00wt%, sorbitol 8.00wt%, sodium benzoate 0.20wt%, sodium ascorbate 0.20wt%, and xylitol 0.05wt% and dissolve them in deionized water to form solution 2;
在溶液2中加入月桂酰丙氨酸钠0.01wt%和薄荷香精0.10wt%,均匀混合后加入所述溶液1,补足水,用碳酸氢钠调节pH 6.12,经过滤灭菌处理,获得口腔内表面清洁抑菌的溶液。Add sodium lauroyl alanine 0.01wt% and peppermint essence 0.10wt% to solution 2, mix evenly and then add solution 1, add water, adjust the pH to 6.12 with sodium bicarbonate, and filter and sterilize to obtain the oral cavity Surface cleaning and bacteriostatic solution.
实施例2Example 2
制备流程同理于实施例1。The preparation process is the same as in Example 1.
本实施例的口腔内表面清洁抑菌组合物包括以下组分:The oral inner surface cleaning and antibacterial composition of this embodiment includes the following components:
抑菌物质,为0.05wt%的茶多酚;The antibacterial substance is 0.05wt% tea polyphenols;
辅料,包括:Excipients, including:
实施例3Example 3
制备流程同理于上述实施例。制备溶液1时,还包括加入预定重量份的黄连素和绿茶提取物。The preparation process is the same as the above embodiment. When preparing solution 1, it also includes adding a predetermined weight portion of berberine and green tea extract.
本实施例的口腔内表面清洁抑菌组合物包括以下组分:The oral inner surface cleaning and antibacterial composition of this embodiment includes the following components:
抑菌物质,为0.49wt%的茶多酚;The antibacterial substance is 0.49wt% tea polyphenols;
辅料,包括:Excipients, including:
实施例4Example 4
制备流程同理于上述实施例。The preparation process is the same as the above embodiment.
本实施例的口腔内表面清洁抑菌组合物包括以下组分:The oral inner surface cleaning and antibacterial composition of this embodiment includes the following components:
抑菌物质,为0.20wt%的茶多酚;The antibacterial substance is 0.20wt% tea polyphenols;
辅料,包括:Excipients, including:
实施例5Example 5
制备流程同理于上述实施例。制备溶液1时,还包括加入预定重量份的柠檬提取物。The preparation process is the same as the above embodiment. When preparing solution 1, it also includes adding a predetermined weight portion of lemon extract.
本实施例的口腔内表面清洁抑菌组合物包括以下组分:The oral inner surface cleaning and antibacterial composition of this embodiment includes the following components:
抑菌物质,为0.30wt%的茶多酚;The antibacterial substance is 0.30wt% tea polyphenols;
辅料,包括:Excipients, including:
实施例6Example 6
制备流程同理于上述实施例。The preparation process is the same as the above embodiment.
本实施例的口腔内表面清洁抑菌组合物包括以下组分:The oral inner surface cleaning and antibacterial composition of this embodiment includes the following components:
抑菌物质,为0.10wt%的茶多酚;The antibacterial substance is 0.10wt% tea polyphenols;
辅料,包括:Excipients, including:
对比例1Comparative example 1
制备流程同理于上述实施例。The preparation process is the same as the above embodiment.
本对比例的口腔内表面清洁抑菌组合物包括以下组分:The oral inner surface cleaning and antibacterial composition of this comparative example includes the following components:
抑菌物质,为0.04wt%的茶多酚;The antibacterial substance is 0.04wt% tea polyphenols;
辅料,包括:Excipients, including:
对比例2Comparative example 2
制备流程同理于上述实施例。The preparation process is the same as the above embodiment.
本对比例的口腔内表面清洁抑菌组合物包括以下组分:The oral inner surface cleaning and antibacterial composition of this comparative example includes the following components:
抑菌物质,为0.50wt%的茶多酚;The antibacterial substance is 0.50wt% tea polyphenols;
辅料,包括:Excipients, including:
抑菌作用检测一Antibacterial effect test one
测试样品如下:实施例1-6、对照物1(水,山梨(糖)醇,丙二醇, PEG-40氢化蓖麻油,茶叶提取物,甘草酸二钾,薄荷醇,三氯半乳糖,羟苯甲酯,苯甲酸钠,食用香精,CI 19140,CI 42090);The test samples are as follows: Examples 1-6, Control 1 (water, sorbitol, propylene glycol, PEG-40 hydrogenated castor oil, tea extract, dipotassium glycyrrhizate, menthol, sucralose, hydroxyphenyl Methyl ester, sodium benzoate, flavoring, CI 19140, CI 42090);
对照物2(水,甘油,丙二醇,山梨(糖)醇,泊洛沙姆407,香精(含茶叶提取物),糖精钠,西吡氯铵(0.075%),氟化钠(0.05%),山梨酸钾,薄荷醇,CI19140,CI42051);Control 2 (water, glycerin, propylene glycol, sorbitol, poloxamer 407, flavor (containing tea extract), saccharin sodium, cetylpyridinium chloride (0.075%), sodium fluoride (0.05%), Potassium sorbate, menthol, CI19140, CI42051);
对照物3(水,甘油,山梨(糖)醇,PEG-40氢化蓖麻油,木糖醇,樱花花提取物,酵母发酵产物提取物,茶叶提取物,薄荷提取物,益生菌(副干酪乳杆菌),薄荷醇,柠檬酸,羟苯甲酯,三氯半乳糖,度米芬,香精);Control 3 (water, glycerin, sorbitol, PEG-40 hydrogenated castor oil, xylitol, cherry blossom extract, yeast fermentation product extract, tea extract, peppermint extract, probiotics (paracheese milk) bacilli), menthol, citric acid, methylparaben, chlorogalactose, domiphene, flavor);
对照物4(水,山梨(糖)醇,甘油,氯化钠,羟苯甲酯,苯甲酸钠,香精,薄荷脑,乳酸杆菌,溶菌酶,植物多肽,蜂胶提取物,忍冬花提取物,白芨根提取物,铁皮石斛提取物,氢化蓖麻油,柠檬酸);Control 4 (water, sorbitol, glycerin, sodium chloride, methyl paraben, sodium benzoate, essence, menthol, lactobacilli, lysozyme, plant peptides, propolis extract, honeysuckle flower extract, Bletilla striata Root extract, Dendrobium officinale extract, hydrogenated castor oil, citric acid);
对照物5(水,乙醇,山梨(糖)醇,麝香草酚,桉叶油素,水杨酸甲酯,薄荷醇,苯甲酸钠,苯甲酸,泊洛沙姆407,糖精钠,CI 42053,食用香精);Control 5 (water, ethanol, sorbitol, thymol, eucalyptol, methyl salicylate, menthol, sodium benzoate, benzoic acid, poloxamer 407, sodium saccharin, CI 42053, food flavors);
对照物6(每500毫升含葡萄糖酸氯己定0.6克、甲硝唑0.1克;辅料为:甘油,聚山梨酯80,聚乙二醇-400,浓薄荷水,乙醇,糖精钠,色素,香精,纯化水)。Control 6 (contains 0.6 g of chlorhexidine gluconate and 0.1 g of metronidazole per 500 ml; excipients are: glycerin, polysorbate 80, polyethylene glycol-400, concentrated mint water, ethanol, saccharin sodium, pigment, essence, purified water).
测试菌种:金黄色葡萄球菌ATCC6538Test strain: Staphylococcus aureus ATCC6538
测试方法:根据消毒技术规范(2002年版)中抑菌环实验要求,每个染菌平板贴放4片试验样片,1片阴性对照样片,共5片。用无菌镊子取样片贴放于平板表面。各样片中心之间相距25mm以上,与平板的周缘相距15mm以上。贴放好后,用无菌镊子轻压样片,使其紧贴于平板表面。盖好平皿,置37℃温箱,培养16h~18h观察结果。用游标卡尺测量抑菌环的直径(包括贴片)并记录。试验重复3次。以抑菌圈的有无及抑菌圈大小评价杀菌活性。Test method: According to the antibacterial ring test requirements in the Disinfection Technical Specifications (2002 Edition), 4 test samples and 1 negative control sample are placed on each bacteria-contaminated plate, for a total of 5 pieces. Use sterile forceps to take a sample piece and place it on the surface of the plate. The centers of each sample should be at least 25mm apart and at least 15mm apart from the edge of the flat plate. After the patch is placed, use sterile tweezers to gently press the sample piece to make it stick to the surface of the plate. Cover the plate, place it in a 37°C incubator, and incubate for 16 to 18 hours to observe the results. Use a vernier caliper to measure the diameter of the inhibition ring (including the patch) and record it. The test was repeated three times. The bactericidal activity was evaluated based on the presence and size of the inhibition zone.
测试结果如附图1-10所示,并统计如下表:The test results are shown in Figure 1-10, and the statistics are as follows:
表1抑菌环测试结果Table 1 Antibacterial ring test results
根据上表所示的结果,结合附图1-10所示,CK均代表无菌水,数字代表实施例。According to the results shown in the above table, combined with those shown in Figures 1-10, CK all represent sterile water, and the numbers represent examples.
注:根据标准抑菌环直径大于7mm者,判为有抑菌作用;抑菌环直径小于或等于7mm者,判为无抑菌作用。Note: According to the standard, if the diameter of the inhibitory ring is greater than 7mm, it is judged to have antibacterial effect; if the diameter of the inhibitory ring is less than or equal to 7mm, it is judged to have no antibacterial effect.
抑菌作用检测二Antibacterial effect test 2
测试样品:实施例1-6,对比例1-2,对照物3(水,甘油,山梨(糖)醇,PEG-40氢化蓖麻油,木糖醇,樱花花提取物,酵母发酵产物提取物,茶叶提取物,薄荷提取物,益生菌(副干酪乳杆菌),薄荷醇,柠檬酸,羟苯甲酯,三氯半乳糖,度米芬,香精);Test samples: Examples 1-6, Comparative Examples 1-2, Control 3 (water, glycerol, sorbitol, PEG-40 hydrogenated castor oil, xylitol, cherry blossom extract, yeast fermentation product extract , tea extract, peppermint extract, probiotics (Lactobacillus paracasei), menthol, citric acid, methyl paraben, chlorogalactose, domiphene, flavor);
对照物4(水,山梨(糖)醇,甘油,氯化钠,羟苯甲酯,苯甲酸钠,香精,薄荷脑,乳酸杆菌,溶菌酶,植物多肽,蜂胶提取物,忍冬花提取物,白芨根提取物,铁皮石斛提取物,氢化蓖麻油,柠檬酸);Control 4 (water, sorbitol, glycerin, sodium chloride, methyl paraben, sodium benzoate, essence, menthol, lactobacilli, lysozyme, plant peptides, propolis extract, honeysuckle flower extract, Bletilla striata Root extract, Dendrobium officinale extract, hydrogenated castor oil, citric acid);
对照物5(水,乙醇,山梨(糖)醇,麝香草酚,桉叶油素,水杨酸甲酯,薄荷醇,苯甲酸钠,苯甲酸,泊洛沙姆407,糖精钠,CI 42053,食用香精);Control 5 (water, ethanol, sorbitol, thymol, eucalyptol, methyl salicylate, menthol, sodium benzoate, benzoic acid, poloxamer 407, sodium saccharin, CI 42053, food flavors);
对照物6(每500毫升含葡萄糖酸氯己定0.6克、甲硝唑0.1克。辅料 为:甘油,聚山梨酯80,聚乙二醇-400,浓薄荷水,乙醇,糖精钠,色素,香精,纯化水)。Control 6 (contains 0.6 g of chlorhexidine gluconate and 0.1 g of metronidazole per 500 ml. Excipients are: glycerin, polysorbate 80, polyethylene glycol-400, concentrated mint water, ethanol, saccharin sodium, pigment, Fragrance, purified water).
测试菌种:金黄色葡萄球菌ATCC6538Test strain: Staphylococcus aureus ATCC6538
测试方法:根据GB 15979-2002一次性使用卫生用品卫生标准中,C4溶出性抗(抑)菌产品抑菌性能试验方法,各测试样品对金黄色葡萄球菌作用2min、5min、10min、20min,计算抑菌率如下:Test method: According to the GB 15979-2002 Hygienic Standard for Disposable Hygiene Products, C4 dissolution antibacterial (anti)bacterial product antibacterial performance test method, each test sample acts on Staphylococcus aureus for 2min, 5min, 10min, 20min, calculated The antibacterial rates are as follows:
表2抑菌率测试结果Table 2 Antibacterial rate test results
注:根据标准抑菌率50%~90%,产品有抑菌作用,抑菌率大于等于90%,产品有较强抑菌作用。Note: According to the standard antibacterial rate of 50% to 90%, the product has antibacterial effect. The antibacterial rate is greater than or equal to 90%, and the product has strong antibacterial effect.
口感检测Taste test
测试样品:实施例1-6,对比例1-2。Test samples: Examples 1-6, Comparative Examples 1-2.
测试方法:Test Methods:
采用民意调查评分法,挑选100名20~70岁人群(性别不限)作为试用对象,分别试用测试样品,对样品进行口感评价。Using the public opinion survey scoring method, 100 people aged 20 to 70 years old (gender is not limited) were selected as trial subjects, and the test samples were tried separately to evaluate the taste of the samples.
评分标准:Grading:
总分为5Total score 5
4-5分表示漱口水口感舒适,茶味浓淡适宜,温和不刺激;A score of 4-5 means the mouthwash tastes comfortable, has a suitable tea flavor, is mild and non-irritating;
3-4分表示漱口水口感一般,有明显茶的苦涩感,可接受范围;A score of 3-4 indicates that the mouthwash tastes average and has the obvious bitterness of tea, which is within an acceptable range;
3分以下表示漱口水苦涩感明显,难以接受。A score of less than 3 means that the mouthwash has a distinctly bitter taste and is unacceptable.
测试结果:Test Results:
如下表所示:As shown in the following table:
表3口腔护理组合物口感测试评分结果区间人数占比结果Table 3 Oral care composition taste test score result interval number of people proportion results
测试对象Test object | 4-5分4-5 points |
3-4分3-4 |
3分以下3 points or less |
实施例1Example 1 | 86%86% | 14%14% | 0%0% |
实施例2Example 2 | 92%92% | 8%8% | 0%0% |
实施例3Example 3 | 63%63% | 28%28% | 9%9% |
实施例4Example 4 | 61%61% | 25%25% | 14%14% |
实施例5Example 5 | 80%80% | 16%16% | 4%4% |
实施例6Example 6 | 89%89% | 11%11% | 0%0% |
对比例1Comparative example 1 | 77%77% | 23%twenty three% | 0%0% |
对比例2Comparative example 2 | 66%66% | 13%13% | 21%twenty one% |
总结说明:本申请提供的清洁抑菌组合物,仅依靠茶叶中的天然活性物质茶多酚就可以达到接近于化学产品的抑菌效果,通过抑制细菌生长可以 预防龋齿和牙周炎的发生,安全无副作用,在抑菌的同时不会对口腔黏膜造成伤害。茶多酚与黄连素还具有一定的抗病毒作用,能够在一定程度上降低病毒从口腔感染的风险,实现了口腔护理组合物对流感病毒,冠状病毒,乙肝病毒,人类疱疹病毒等多种病毒感染的预防;添加月桂酰丙氨酸钠、椰油酰丙氨酸钠、月桂酰肌氨酸钠表面活性剂可以更好地清洁口腔和清新口气以及辅助茶多酚抑菌;另外利用羟丙基-β-环糊精包裹茶多酚和添加多种矫味剂消除了茶多酚造成的苦涩感,再添加β环糊精薄荷醇、茶多糖、茶氨酸使整体口感温和清香,还能提神醒脑,最后通过添加防腐剂解决了茶多酚在使用中易氧化影响抑菌效果的问题。Summary: The cleaning and antibacterial composition provided in this application can achieve an antibacterial effect close to that of chemical products by relying only on the natural active substance tea polyphenols in tea. It can prevent the occurrence of dental caries and periodontitis by inhibiting bacterial growth. It is safe and has no side effects. It inhibits bacteria and does not cause harm to the oral mucosa. Tea polyphenols and berberine also have certain antiviral effects, which can reduce the risk of viral infection from the oral cavity to a certain extent, enabling oral care compositions to effectively protect against influenza virus, coronavirus, hepatitis B virus, human herpes virus and other viruses. Prevention of infection; adding sodium lauroyl alanine, sodium cocoyl alanine, and sodium lauroyl sarcosinate surfactants can better clean the mouth and freshen breath and assist tea polyphenols in antibacterial; in addition, use hydroxypropylene Base-β-cyclodextrin wraps tea polyphenols and adds a variety of flavoring agents to eliminate the bitterness caused by tea polyphenols, and then adds β-cyclodextrin menthol, tea polysaccharide, and theanine to make the overall taste mild and fragrant, and also adds It can refresh the mind. Finally, by adding preservatives, the problem that tea polyphenols are easily oxidized during use and affects the antibacterial effect is solved.
由于β环糊精薄荷醇可以在无乙醇助溶的水相体系直接溶解,本申请中的组合物为无酒精配方,具有薄荷清凉感但无酒精带来的刺激性。彻底解决了现有化学产品的安全性差与口感刺激的问题,适合用于制备抑菌,安全天然,口感适宜的口腔护理产品。Since β-cyclodextrin menthol can be directly dissolved in an aqueous phase system without ethanol as a solubilizer, the composition in this application is an alcohol-free formula and has a refreshing mint feeling without the irritation caused by alcohol. It completely solves the problems of poor safety and irritating taste of existing chemical products, and is suitable for preparing antibacterial, safe and natural oral care products with suitable taste.
显然,上述实施例仅是为清楚地说明本申请所作的举例,而并非对实施方式的限定。对于所属领域的普通技术人员来说,在上述说明的基础上还可以做出其它不同形式的变化或变动。这里无需也无法对所有的实施方式予以穷举。而由此所引申出的显而易见的变化或变动仍处于本申请的保护范围之中。Obviously, the above-mentioned embodiments are only examples to clearly illustrate the present application, and are not intended to limit the implementation. For those of ordinary skill in the art, other different forms of changes or modifications can be made based on the above description. An exhaustive list of all implementations is neither necessary nor possible. The obvious changes or changes derived therefrom are still within the protection scope of this application.
Claims (13)
- 一种用于口腔内表面清洁抑菌的组合物,其特征在于,按所述组合物的重量分数,包括:茶多酚0.05~0.49wt%、表面活性剂、包合茶多酚的包合物0.01~1.19wt%。A composition for cleaning and inhibiting bacteria on the inner surface of the oral cavity, which is characterized in that, according to the weight fraction of the composition, it includes: 0.05 to 0.49 wt% of tea polyphenols, surfactants, and inclusions of tea polyphenols. Material 0.01~1.19wt%.
- 根据权利要求1所述的组合物,其特征在于,所述包合物为羟丙基-β-环糊精;所述表面活性剂为氨基酸表面活性剂。The composition according to claim 1, wherein the inclusion compound is hydroxypropyl-β-cyclodextrin; and the surfactant is an amino acid surfactant.
- 根据权利要求2所述的组合物,其特征在于,所述氨基酸表面活性剂选自月桂酰丙氨酸钠、椰油酰丙氨酸钠、月桂酰肌氨酸钠及任何N-酰基氨基酸盐类中的一种或多种。The composition according to claim 2, wherein the amino acid surfactant is selected from the group consisting of sodium lauroyl alanine, sodium cocoyl alanine, sodium lauroyl sarcosinate and any N-acyl amino acid salt One or more of the categories.
- 根据权利要求1所述的组合物,其特征在于,还包括辅助抑菌剂、提振精神的物质、矫味剂、pH调节剂、防冻剂、防腐剂中的一种或多种。The composition according to claim 1, further comprising one or more of an auxiliary bacteriostatic agent, a spirit-enhancing substance, a flavoring agent, a pH adjuster, an antifreeze agent, and a preservative.
- 根据权利要求4所述的组合物,其特征在于,所述辅助抑菌剂包括氨基酸表面活性剂0.01~0.15wt%、黄连素0.005~0.010wt%、绿茶提取物0.01~0.20wt%、柠檬提取物0.01~0.20wt%中的一种或多种;所述矫味剂包括山梨醇2.00~8.00wt%、木糖醇0.05~2.00wt%、香精≤3.00wt%、甘油2.00~24.00wt%及任何可改善口感的物质中的一种或多种;所述提振精神的物质包括β环糊精包合的薄荷醇0.01~1.20wt%、茶多糖0.01~1.20wt%、茶氨酸0.01~0.05wt%中的一种或多种;所述防冻剂为甘油2.00~24.00wt%;所述防腐剂0.20~0.40wt%包括抗坏血酸钠、苯甲酸钠、山梨酸钾、羟苯甲酯中的一种或多种;pH调节剂包括碳酸钠和/或碳酸氢钠。The composition according to claim 4, wherein the auxiliary bacteriostatic agent includes amino acid surfactant 0.01-0.15wt%, berberine 0.005-0.010wt%, green tea extract 0.01-0.20wt%, lemon extract One or more substances 0.01 to 0.20wt%; the flavoring agents include sorbitol 2.00 to 8.00wt%, xylitol 0.05 to 2.00wt%, essence ≤ 3.00wt%, glycerol 2.00 to 24.00wt% and One or more of any substances that can improve the taste; the spirit-boosting substances include 0.01 to 1.20 wt% of β-cyclodextrin-contained menthol, 0.01 to 1.20 wt% of tea polysaccharide, and 0.01 to 0.01 to 1.20 wt of theanine. One or more of 0.05wt%; the antifreeze is glycerol 2.00~24.00wt%; the preservative 0.20~0.40wt% includes one of sodium ascorbate, sodium benzoate, potassium sorbate, and methyl paraben. One or more; pH adjuster includes sodium carbonate and/or sodium bicarbonate.
- 根据权利要求5所述的组合物,其特征在于,所述黄连素为0.005~0.008wt%、所述绿茶提取物为0.05~0.18wt%、所述柠檬提取物为0.05~0.18wt%。The composition according to claim 5, wherein the berberine is 0.005-0.008wt%, the green tea extract is 0.05-0.18wt%, and the lemon extract is 0.05-0.18wt%.
- 根据权利要求4-6任一所述的组合物,所述pH调节剂将pH调节到5.00-8.00。According to the composition of any one of claims 4-6, the pH adjuster adjusts the pH to 5.00-8.00.
- 根据权利要求1所述的组合物,其特征在于,按所述组合物的 重量分数,包括:茶多酚0.05wt%、氨基酸表面活性剂0.12wt%、羟丙基-β-环糊精0.01wt%。The composition according to claim 1, characterized in that, according to the weight fraction of the composition, it includes: tea polyphenols 0.05wt%, amino acid surfactant 0.12wt%, hydroxypropyl-β-cyclodextrin 0.01 wt%.
- 一种用于口腔内表面清洁抑菌的组合物的制备方法,其特征在于,包括以下步骤:A method for preparing a composition for cleaning and inhibiting bacteria on the inner surface of the oral cavity, which is characterized by comprising the following steps:取预定重量份的植物活性物质茶多酚、茶氨酸、茶多糖、β环糊精薄荷醇和羟丙基-β-环糊精,溶解于水中,形成溶液1;Take a predetermined weight portion of the plant active substances tea polyphenols, theanine, tea polysaccharide, β-cyclodextrin menthol and hydroxypropyl-β-cyclodextrin, and dissolve them in water to form solution 1;取预定重量份的甘油、山梨醇、防腐剂、木糖醇溶解于水中,形成溶液2;Dissolve predetermined weight portions of glycerin, sorbitol, preservatives, and xylitol in water to form solution 2;在溶液2中加入氨基酸表面活性剂和香精,均匀混合后加入所述溶液1,补足水,调节pH,灭菌,即得。Add amino acid surfactant and essence to solution 2, mix evenly, then add solution 1, add water, adjust pH, and sterilize to obtain.
- 根据权利要求9所述的制备方法,其特征在于,所述溶液1,还包括:The preparation method according to claim 9, characterized in that the solution 1 further includes:添加预定重量份的黄连素;和/或Add a predetermined weight portion of berberine; and/or添加预定重量份的柠檬提取物;和/或Add a predetermined weight portion of lemon extract; and/or添加预定重量份的绿茶提取物。Add a predetermined weight portion of green tea extract.
- 包含权利要求1-6任一所述组合物的口腔清洁产品。An oral cleaning product comprising the composition of any one of claims 1-6.
- 权利要求1-6任一所述组合物在口腔清洁产品中的应用。Application of the composition according to any one of claims 1 to 6 in oral cleaning products.
- 一种清洁人或动物口腔的方法,其特征在于,将所述权利要求1-6任一所述的组合物与人或动物的口腔内表面接触。A method for cleaning the oral cavity of humans or animals, characterized by contacting the composition of any one of claims 1 to 6 with the inner surface of the oral cavity of humans or animals.
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