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A jelly-like mouthwash with anti-caries, antibacterial and strong root tooth-fixing effects

A tooth-strengthening and mouthwash technology, which is applied to medical preparations containing active ingredients, antibacterial drugs, organic chemistry, etc., can solve the problems of caries-free prevention and tooth-strengthening, and achieve enhanced anti-caries effect, The preparation process is simple and convenient, and the effect of improving the anti-inflammatory and analgesic effects

Active Publication Date: 2020-08-18
中寰健康科技(无锡)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Aiming at the problems in the above-mentioned prior art, especially for the problems that traditional mouthwash can only freshen breath or non-specifically kill cariogenic microorganisms in the oral cavity, but usually do not have the effects of preventing dental caries and strengthening teeth, the present invention provides a A mouthwash that integrates anti-caries, antibacterial, and tooth-strengthening effects, and has low toxicity and good user experience. It is expected to replace the existing mouthwash on the market and protect people's dental health. A new type of oral care product

Method used

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  • A jelly-like mouthwash with anti-caries, antibacterial and strong root tooth-fixing effects
  • A jelly-like mouthwash with anti-caries, antibacterial and strong root tooth-fixing effects
  • A jelly-like mouthwash with anti-caries, antibacterial and strong root tooth-fixing effects

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1: (S)-2-(1,3-dimethyl-2-oxo-1,2-dihydroquinoxaline-6-sulfonamido)-3-(methylthio)-N- Preparation of (5-nitrothiazol-2-yl) propionamide (compound LX-S-06)

[0038]

[0039] Preparation of intermediate 3-methylquinoxalin-2(1H)-one (1)

[0040] Weigh 10.81g (0.10mol) of o-phenylenediamine into a 500mL round bottom flask, add 250mL of absolute ethanol, and stir until completely dissolved to obtain a light yellow solution. 12.77 g (0.11 mol) of ethyl pyruvate was added dropwise to the solution with stirring at room temperature. After about 10 minutes, a large amount of solids were generated instantaneously, and the reaction was continued for 5 hours, and the reaction ended. After filtration, the solid was collected and recrystallized with ethanol. After vacuum drying, a light white cotton wool-like product was obtained. The yield was 90.4%, m.p.=241.0-242.7°C.

[0041] Preparation of intermediate 1,3-dimethylquinoxalin-2(1H)-one (2)

[0042] Weigh 8.01g (0.05mo...

Embodiment 2

[0051] Example 2: (R)-methyl(2-(1-methyl-3-(((5-nitrothiazole-2-)amino)methyl)-2-oxo-1,2-dihydroquinone Preparation of oxaline-6-sulfonamido)-3-phenylpropionyl) carbamate (compound LX-S-18)

[0052]

[0053]Intermediate (R)-methyl 2-(1,3-dimethyl-2-oxo-1,2-dihydroquinoxaline-6-sulfonamido)-3-phenylpropanoic acid methyl ester (6 ) preparation

[0054] The preparation method of the intermediate (6) is the same as that of the intermediate (4) in Example 1, and the yield is 69%. M.p=151.0~153.0℃, 1 H-NMR (DMSO-d 6 ,400MHz,ppm):δ2.473(s,3H,N=CCH 3 ), 2.751 (dd, J=9.0, 13.8Hz, 1H, CH 2 ), 2.93 (dd, J=6.0, 13.8Hz, 1H, CH 2 ),3.34(s,3H,OCH 3 C=O),3.63(s,3H,NCH 3 ), 4.08(d, J=7.8Hz, 1H, CH), 7.05-7.14(m, 5H, 5ArH), 7.57(d, J=9.0Hz, 1H, ArH), 7.69(dd, J=2.4, 9.0 Hz,1H,ArH),7.85(d,J=2.4Hz,1H,ArH),8.63(d,J=9.0Hz,1H,NH).ESI-MS:416.7[M+H] + .

[0055] Intermediate (R)-Methyl 2-(3-bromomethyl)-1-methyl-2-oxo-1,2-dihydroquinoxaline-6-sulfonamido)-3-phenylpropionic acid Preparat...

Embodiment 3

[0059] Embodiment three: the antibacterial activity test of compound LX-S-06

[0060] Preparation of Streptococcus mutans

[0061] (1) The medium for cultivating Streptococcus mutans is Brain heart infusion medium (brand OXOID, product number CM1135), the main components of which are Brain infusion solids 12.5g / L, Beef heartinfusion solids 5.0g / L , Proteose peptone 10.0g / L, Glucose 2.0g / L, Sodiumchloride 5.0g / L, Di-sodium phosphate 2.5g / L, pH 7.4±0.2. If solid medium is required, add 1.5% agar powder. Sterilize with damp heat at 115°C for 30 minutes, and cool down for use.

[0062] (2) The culture medium for Streptococcus mutans biofilm is brain heart infusion-sucrose medium. The preparation method is to make 20% stock solution of sucrose, filter and sterilize it with a 0.22 μm sterile filter, and add 1% sucrose to the brain-heart infusion medium.

[0063] (3) Streptococcus mutans type strain UA159 and clinical strain UA246 were inoculated on the solid medium of brain hear...

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Abstract

The invention discloses a jelly like mouthwash with functions of preventing decayed teeth and bacteria, enhancing tooth roots, and strengthening teeth. The mouthwash comprises following components inpercentage by weight: 3 to 5% of humectant component, 91 to 95% of solvent, 0.25% to 0.75% of acid-alkali buffering agent, 0.2 to 0.6% of anti-caries component, 0.05 to 0.15% of tooth root enhancing component, 0.2 to 0.6% of flavoring component, 0.1 to 0.2% of anticorrosion component, 0.25 to 0.35% of fragrance, 0.01 to 0.03% of tooth strengthening component, and 0.4 to 0.8% of gel component; wherein the anti-caries component is one or more of LX-S-06, LX-S-18, XQH-2-92, XQH-3-6, and XQH-3-7, and the tooth root enhancing component is quercetin. The functions of preventing decayed teeth and bacteria, enhancing tooth roots, and strengthening teeth are integrated, and the mouthwash is comfortable to use, does not have any toxic or side effect, and is suitable for long-term use.

Description

technical field [0001] The invention relates to the technical field of oral health care, in particular to a mouthwash, in particular to a jelly-shaped mouthwash with anti-caries, antibacterial, tooth-strengthening and a preparation method thereof. Background technique [0002] Caries, commonly known as tooth decay, is a bacterial infectious disease. The etiology of caries can be explained by the "quadruple factor theory", that is, bacteria, oral microenvironment, host and time, which are four interrelated factors. Caries is mainly caused by cariogenic microorganisms. Cariogenic bacteria form plaque biofilms on places that are not easy to clean, such as crowns of teeth, thereby forming a microenvironment that destroys tooth enamel. The predilection sites of dental caries are very hidden, mainly including pits and fissures, adjacent surfaces and neck, and these parts are also difficult to clean with traditional toothbrushing. Oral health can be protected through oral care cl...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K8/9789A61K8/60A61K8/49A61K8/368A61K8/365A61K8/21A61K8/34A61K8/04A61Q11/00A61K31/498A61P1/02A61P31/04C07D417/12
CPCA61K8/042A61K8/21A61K8/345A61K8/365A61K8/368A61K8/49A61K8/498A61K8/60A61K8/97A61K31/498A61Q11/00C07D417/12
Inventor 李荀李星胡玮王川东赵坚丁坤张娴姝郭明珠蒋晓婷
Owner 中寰健康科技(无锡)有限公司
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