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White and black special toothpaste

A toothpaste and a special type of technology, applied in dentistry, antibacterial drugs, drug combinations, etc., can solve the problem of insignificant antibacterial effect, achieve the effect of inhibiting the progress of caries, increasing the firmness, and promoting the recovery of cementum

Active Publication Date: 2018-05-29
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

[0007] Aiming at the problems existing in the prior art, especially the insignificant antibacterial effect of traditional toothpaste, the present invention provides a special toothpaste with remarkable effect, simple production, economical and practical, anti-caries antibacterial and strong root-fixing effect. Simultaneously the present invention also provides a kind of method for preparing this anti-caries special toothpaste

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] 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)

[0047]

[0048] Preparation of intermediate 3-methylquinoxalin-2(1H)-one (1)

[0049] 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 under 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.

[0050] Preparation of intermediate 1,3-dimethylquinoxalin-2(1H)-one (2)

[0051] Weigh 8.01g (0.05m...

Embodiment 2

[0060] 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)

[0061]

[0062] Intermediate (R)-methyl 2-(1,3-dimethyl-2-oxo-1,2-dihydroquinoxaline-6-sulfonamido)-3-phenylpropanoic acid methyl ester (6 ) preparation

[0063] 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] + .

[0064] Intermediate (R)-Methyl 2-(3-bromomethyl)-1-methyl-2-oxo-1,2-dihydroquinoxaline-6-sulfonamido)-3-phenylpropionic acid Prepa...

Embodiment 3

[0068] Embodiment three: the antibacterial activity of compound LX-S-06

[0069] Streptococcus mutans and compound preparation

[0070] (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, Beefheartinfusion 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.

[0071] (2) The culture medium for Streptococcus mutans biofilm is brain heart infusion-sucrose medium. The preparation method is that the sucrose is made into 20% stock solution and sterilized by filtering with a 0.22 μm sterile filter, and the final concentration of 1% sucrose is added to the brain-heart infusion medium.

[0072] (3) Streptococcus mutans type strain UA159 and clinical strain UA246 ...

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PUM

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Abstract

The invention discloses a White and Black special toothpaste which is prepared from an antibacterial component, a root reinforcing and tooth strengthening component, a tooth strengthening component, athickening agent, an acid and alkali regulator, a friction component, a moisturizing component, a foaming component, a flavoring component, a desensitizing component and purified water; the white toothpaste also contains a brightening component; the antibacterial component is selected from one or more of LX-S-06, LX-S-18, XQH-2-92, XQH-3-6 and XQH-3-7; the root reinforcing and tooth strengtheningcomponent is quercetin; and the brightening component is prepared from hydrated silica and titanium dioxide. The toothpaste disclosed by the invention can be widely applied to health care of the oralcavity and especially has better effects on preventing and treating decayed teeth and auxiliarily treating periodontal diseases. The toothpaste disclosed by the invention contains safe and stable components, has no harmful stimulation such as damage to normal tissues such as the oral mucosa, can specifically eliminate main cariogenic bacteria, namely streptococcus mutans, in the oral cavity, andhas the effects of preventing and treating caries and does not damage the ecological balance of the oral florae, thereby further maintaining the health balance state of the oral cavity.

Description

technical field [0001] The invention belongs to the technical field of oral health care and relates to a toothpaste, in particular to a "white" plus "black" special toothpaste with the functions of anti-caries, antibacterial and tooth strengthening and a preparation method thereof. Background technique [0002] Caries is a disease of chronic and progressive destruction of dental hard tissue under the influence of various factors, mainly bacteria. The etiology of caries includes bacteria and their plaque biofilm, food, oral microenvironment and time factors. On the basis of etiology, caries can also be referred to as bacterial infectious diseases of dental hard tissues. Although the incidence of caries ranks among the top among common human diseases, caries has not attracted widespread public attention because caries is not life-threatening and is restricted by the level of domestic economic development. It cannot be ignored that the potential risk of dental caries is huge....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K8/92A61K8/73A61K8/49A61K8/29A61K8/26A61K8/25A61K8/24A61K8/20A61K8/21A61Q11/00C07D417/12A61K31/498A61P1/02A61P31/04
CPCA61K8/20A61K8/21A61K8/24A61K8/25A61K8/26A61K8/29A61K8/49A61K8/498A61K8/731A61K8/922A61Q11/00C07D417/12
Inventor 李荀李星胡玮王川东张娴姝蒋晓婷赵坚郭明珠丁坤
Owner 中寰健康科技(无锡)有限公司
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