CN109498490A - One kind dentifrice composition containing Artesunate and preparation method thereof - Google Patents

One kind dentifrice composition containing Artesunate and preparation method thereof Download PDF

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Publication number
CN109498490A
CN109498490A CN201811538066.0A CN201811538066A CN109498490A CN 109498490 A CN109498490 A CN 109498490A CN 201811538066 A CN201811538066 A CN 201811538066A CN 109498490 A CN109498490 A CN 109498490A
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China
Prior art keywords
parts
artesunate
preparation
oil
added
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Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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CN201811538066.0A
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Chinese (zh)
Inventor
王霞
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Dandong Epoch Biological Medicine Science And Technology Co Ltd
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Dandong Epoch Biological Medicine Science And Technology Co Ltd
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Priority to CN201811538066.0A priority Critical patent/CN109498490A/en
Publication of CN109498490A publication Critical patent/CN109498490A/en
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/4973Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
    • A61K8/498Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom having 6-membered rings or their condensed derivatives, e.g. coumarin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34Alcohols
    • A61K8/347Phenols
    • 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

Abstract

One kind white lotion preparation method of dentifrice composition containing Artesunate of the invention, by weight ratio, water material: 17-20 parts of sorbierite, PEG-600 is 4-8 parts, 0.3-0.45 parts of saccharin, 0.6-0.8 parts of EDTA-2 sodium, 20-24 parts of deionized water to raw material;Oil plant: 0.5-1.2 parts of eugenol, 0.6-0.9 parts of menthol, 1.0-3.0 parts of oil of badian, 1.0-2.5 parts of Artesunate, 1-1.5 parts of essence;Powder: 35-42 parts of calcium monohydrogen phosphate, 2-5 parts of silica, 1.0-1.5 parts of sodium carboxymethylcellulose, 2.4-3.0 parts of lauryl sodium sulfate (K12);Above-mentioned water material, oil plant, powder respectively after mixing, be pumped into three-in-one Manufacturing medicine extract machine stir evenly it is obtained.The bacteriostasis of Artesunate can be given full play to, oral lichen planus, canker sore, gingivitis disease is effectively relieved.

Description

One kind dentifrice composition containing Artesunate and preparation method thereof
Technical field
The present invention relates to dentifrice composition, especially a kind of toothpaste group for improving oral mucosa and gingiva tissue inflammation Close and preparation method thereof.
Technical background
Oral lichen planus is common in oral cavity two sides inner wall, the positions such as tongue, lip, gum, palate, and initial stage shows as affected part presentation White linear, dendroid, ring-type or netted striped, with congested rubescent, rotten to the corn around progression of the disease striped.Often missed by people Common canker sore is considered, to affect treatment adversely.In addition, lichen planus of mouth not instead of bacterium infection, a kind of cell Denaturation is invalid with antibiotic treatment.
Oral lichen planus disease incidence, which has, in recent years increases trend, however many people are to the knowledge of lichen planus not right and wrong Often understand so that it is benign be changed into it is pernicious, when affected part formed hickie when should then be vigilant canceration.
Canker sore is commonly called as " aphtha ", is a kind of common ulcerative damages illness for betiding mucous membrane of mouth, is more common in The positions such as lip inside, tongue, tongue abdomen, cheek mucous membrane, vestibular ditch, soft palate, the mucous membrane at these positions lack keratinization layer or angling compared with Difference.Tongue ulcer refers to the canker sore for betiding tongue, tongue abdomen position.Sharp ache when canker sore is broken out, local cusalgia are bright Aobvious, serious person also will affect diet, speak, and cause very big inconvenience to daily life.
Gingivitis is limited to the lesion of gingiva tissue, wherein most commonly seen is marginal gingivitis, also known as marginality gum Scorching, simple gingivitis, belongs to " only gingivitis related with plaque ", is the most common disease in bacterial plaque gingivitis.Gum Inflammation be predominantly located at free gum and gum nipple, that is, the gingivitis that the big daily life of a family is said.
Beautiful jade is stung compared with the curative effect having had using antimalarial chlorination to oral lichen planus, but its toxic side effect is heavier, Therefore clinical application is very restricted.
Artesunate is the derivative of artemisinine, and qinghaosu is the extract of sweet wormwood, so Artesunate is in pharmacology Same qinghaosu in effect has the effect of class chlorine.Currently, Artesunate is clinically used to treat oral lichen planus, be with Oral or injection mode medication.
CN106880554A discloses a kind of sweet wormwood toothpaste and preparation method thereof, and the sweet wormwood raw material of toothpaste is by weight percentage It is calculated as: rubbing agent 18-25%, adhesive 0.3-0.6%, moisturizer 54-64%, foaming agent 2-7%, sweetener 0.05-0.2%, anti-corrosion Agent 0.1-0.4%, sodium pyrophosphate 0.3-0.6%, essence 1-2%, qinghaosu or Artesunate 0.1-0.3%, surplus are sweet wormwood grass Extracting solution.The preparation method of the patent is that Artesunate and qinghaosu are added in moisturizer sorbierite, propylene glycol, PEG-1450 In, it is directly added into true control Manufacturing medicine extract machine, lotion is obtained after subsequent preparation process.There is sterilization, antibacterial, antibacterial function in the hope of being made The toothpaste that can, prevent bleeding gums, prevent calculus dentalis and plaque from acting on.
Above-mentioned patent is since qinghaosu and Artesunate are insoluble in water and alcohol compound, and qinghaosu and sweet wormwood amber Ester exists in the form of molecule, could play a role to the oral mucosa of illness, this is also that Artesunate is clinically made into needle The reason of agent and oral medication mode.There is Artesunate in granular form cannot glue mucosa absorption by the oral cavity of illness, so Qinghaosu and Artesunate are added in alcohol liquid during above-mentioned prior art preparation and handled, not by qinghaosu and sweet wormwood amber Ester dissolution, but has dispersed qinghaosu and Artesunate in alcohol liquid, that is, be not achieved qinghaosu and Artesunate be dissolved into it is transparent Liquid, qinghaosu and Artesunate are prepared still with graininess there are in alcohol liquid, being a kind of precipitable mixed liquor of muddiness Toothpaste, Artesunate still exists with particle, so qinghaosu and Artesunate cannot be by oral focus mucosa absorptions, in tooth It is very little to the osmosis of oral focus mucous membrane with qinghaosu existing for graininess and Artesunate in cream, it does not play Effect, cannot play the improvement therapeutic effect to oral focus mucous membrane.
In addition, aforementioned patents disclose qinghaosus and Artesunate to have bacteriostasis, but it also adds preservative benzoic acid, institute To have reason to query whether the bacteriostasis of the patent has bacteriostasis property disclosed in it.
Summary of the invention
The object of the present invention is to provide a kind of dentifrice compositions containing Artesunate and preparation method thereof, can give full play to sweet wormwood amber The bacteriostasis of ester, oral lichen planus, canker sore, gingivitis disease is effectively relieved.
The present invention solves the hydrophily of Artesunate by special preparation method, keeps Artesunate soluble in water, then match With eugenol, the toothpaste being prepared can give full play to the drug action of Artesunate and eugenol, can achieve Artesunate Oral cavity cure the disease area medication effect, make toothpaste have the function of effectively alleviating the disease of cari oris mucosa.
The present invention white lotion preparation method of dentifrice composition containing Artesunate:
Raw material is by weight ratio
Water material:
17-20 parts of sorbierite, 4-8 parts of PEG-600,0.3-0.45 parts of saccharin, 0.6-0.8 parts of EDTA-2 sodium, deionized water 20- 24 parts.
Oil plant:
It is 0.5-1.2 parts of eugenol, 0.6-0.9 parts of menthol, 1.0-3.0 parts of oil of badian, 1.0-2.5 parts of Artesunate, fragrant It is 1-1.5 parts smart.
Powder:
35-42 parts of calcium monohydrogen phosphate, 2-5 parts of silica, 1.0-1.5 parts of sodium carboxymethylcellulose, lauryl sodium sulfate (K12) 2.4-3.0 part.
Preparation method:
(1) prepared by water material: it is put into deionized water in water phase tank, PEG-600, EDTA-2 sodium, saccharin is added in the state of stirring, Stirring and dissolving is uniform, and sorbierite is then added and stirs evenly liquid, for use;
(2) preparation of oil plant: Artesunate is added in oil of badian, is evenly stirred until transparent liquid, is then added fourth Fragrant phenol, menthol, essence are stirred even liquid, for use;
(3) prepared by powder: calcium monohydrogen phosphate, sodium carboxymethylcellulose, lauryl sodium sulfate, silica are stirred It is even, for use;
(4) cream processed: above-mentioned water material, oil plant, powder are pumped under vacuum in three-in-one Manufacturing medicine extract machine, after mixing evenly, blowing obtains Product.
The preparation method of the transparent lotion of present invention dentifrice composition containing Artesunate:
Raw material is by weight ratio
Water material:
56-58 parts of sorbierite, 3-5 parts of PEG-600,0.3-0.5 parts of saccharin, 0.5-0.8 parts of EDTA-2 sodium, deionized water 9-12 Part.
Oil plant:
It is 0.5-1.2 parts of eugenol, 0.6-1.0 parts of menthol, 1.5-3.0 parts of oil of badian, 1.0-2.5 parts of Artesunate, fragrant It is 1-1.5 parts smart.
Powder: 6-19 parts of silica 1,0.7-1.0 parts of sodium carboxymethylcellulose, 2.4-3.0 parts of lauryl sodium sulfate.
Preparation method:
(1) prepared by water material: it is put into deionized water in water phase tank, PEG-600, EDTA-2 sodium, saccharin is added in the state of stirring, Stirring and dissolving is uniform, and sorbierite is then added and stirs evenly liquid, for use;
(2) preparation of oil plant: Artesunate is added in oil of badian, is evenly stirred until transparent liquid, is then added fourth Fragrant phenol, menthol, essence are stirred even liquid, for use;
(3) prepared by powder: silica, sodium carboxymethylcellulose, lauryl sodium sulfate, silica are uniformly mixed, For use;
(4) cream processed: above-mentioned water material, oil plant, powder are pumped under vacuum in three-in-one Manufacturing medicine extract machine, after mixing evenly, blowing obtains Product.
Select to use oil of badian of the present invention dissolves artesunate, forms transparency liquid, makes artesunate with molecule shape Formula is dissolved in oil of badian, and uniform emulsus is formed under the emulsification of lauryl sodium sulfate (surfactant) Liquid is uniformly blended into lotion of toothpaste, and in this way when brushing teeth, Artesunate molecule can penetrate into oral cavity affected mucosal membrane, directly It is applied to focal zone, the drug action of Artesunate can be given full play to.
So preparation method provided by the invention solves the problems, such as the hydrophily of Artesunate, keep artesunate molten In Xie Yushui, the drug action of Artesunate has been given full play to, ensure that Artesunate acts on the curative effect of oral lichen planus.
Select to use oil of badian of the present invention can not only dissolve Artesunate, change the hydrophily of Artesunate, again Synergistic function can be played with eugenol, enhance the antibacterial intensity of eugenol and antibacterial time, that is, increase eugenol dialogue Intensity is killed in color candida albicans, staphylococcus aureus, streptococcus suppression.
The present invention has improvement therapeutic effect well to oral problems such as canker sore, oral lichen planus, gingivitis. Meanwhile the present invention does not add any preservative additionally, it is highly-safe by natural bacteriostatic ability.
Oil of badian is extracted from the fruit or branches and leaves of Chinese anise (alias anise, aniseed, spiced illiciumverum) A kind of more complex natural perfume material oil of the ingredient come.
Oil of badian is for colourless or faint yellow volatility oily liquids, and main component is anethole, safrole, eucalyptus Leaf oil element, anisaldehyde, fenchone, benzoic acid, palmitinic acid, terpinol etc. have antibacterial, increasing leukocyte, analgesia, insecticidal activity With free radical resisting oxidation, gram-negative bacteria such as hay bacillus, Escherichia coli, comma bacillus and typhoid bacillus, pair are hurt Cold bacillus, shigella dysenteriae etc. also have bacteriostasis, act on similar to 50 units of streptomycin sulphate/ml;To the antibacterial of fungi Effect is greater than 1% benzoic acid and salicylic acid.So select oil of badian that can not only dissolve to dissolution Artesunate, and And itself also has sufficient contribution to the antibacterial of fungi.
In addition, the Chinese medicine property of oil of badian and the Chinese medicine property of Artesunate are arranged in pairs or groups and are used, to oral lichen planus The Chinese medicine adjustment effect that patient plays qi-regulating, removes dryness, has booster action to healing.
Eugenol is primarily present in basil oil and in the oil of Cinnamomum basyleaves, is the ingredient of a variety of aromatic oil.Fourth Fragrant phenol has an inhibiting effect to Candida albicans, staphylococcus aureus, streptococcus, and with antiviral, analgesia, surface anesthesia Pharmacological action can be applied to the treatment of oral Candida and canker sore.
The bacteriostasis of oil of badian is not only utilized in the present invention, more mainly applies oil of badian and Artesunate The similar effect of mixing can be played.Oil of badian and eugenol cooperate, and can use oil of badian to gram-negative bacteria Bacteriostasis property, can be promoted eugenol to Candida albicans, staphylococcus aureus, streptococcic antibacterial intensity and it is antibacterial when Between.Artesunate and the application of eugenol matched combined can sufficiently have compared with raising bacteriostasis, Oral Lichen tongue fur is effectively relieved Tinea, canker sore, gingivitis disease.
Specific embodiment
White lotion embodiment 1-5, raw material is by weight ratio
White lotion example 1-5 sense organ and physical and chemical index testing result:
Transparent lotion embodiment 1-5 raw material is by weight ratio
Transparent lotion example 1-5 sense organ and physical and chemical index testing result:
It is total that white lotion product of the invention carries out total number of bacterial colonies, coli-group, pathogenic pyogenic baeceria, fungus colony Number, bacteriostatic test (Escherichia coli, staphylococcus aureus, Candida albicans), stability test (Candida albicans) detection: The survey report of Guangzhou industrial microorganism inspection center detects number XJ120180945, and particular content is as follows.
Microorganism detection result:
Detection project Testing result Standard value
Total number of bacterial colonies (CFU/g) <20 ≤200
Fungus colony sum (CFU/g) <20 ≤100
Escherichia coli It is not detected It must not detect
Staphylococcus aureus It is not detected It must not detect
Hemolytic streptococcus It is not detected It must not detect
Pseudomonas aeruginosa It is not detected It must not detect
Detection method: according to GB15979-2002 " Disposable Sanitary Accessory standard " Appendix B;
Testing conditions: environment temperature: 24 DEG C, relative humidity: 52%.
Bacteriostasis rate detection:
Bacteriostasis rate test method: referring to GB15979-2002 " Disposable Sanitary Accessory sanitary standard " appendix C 4 into Row test, action time 2min, 5min, 10min and 20min, test are repeated 3 times.24 DEG C of experimental temperature.
Stability test result:
Stability test test method: referring to GB15979-2002 " Disposable Sanitary Accessory sanitary standard " appendix C 6 It is tested, original packing sample is placed in 37-40 DEG C of insulating box 3 months, keep relative humidity > 75%.
Conclusion: suppression of the sample in 37 DEG C of 3 months accelerated tests, to Escherichia coli, staphylococcus aureus, Candida albicans Bacterium rate reaches standard value as defined in GB15979-2002 " Disposable Sanitary Accessory sanitary standard " appendix C 4, and the product is to big Enterobacteria, staphylococcus aureus, Candida albicans bacteriostasis rate bacteriostasis at room temperature at least keep 2 years.
Acute eye irritation test:
Method: according to " disinfection technology standard " (version 2.3.4 acute eye irritation test in 2002).By 100ml sample stoste Instillation rabbit side eye conjunctiva is intracapsular, and another branch hole is as normal control.After eye drip for 24 hours, 48h, 72h observe result.By " disinfection Technical specification " table 2-13 scoring in (version in 2002);
Conclusion: product stoste belongs to the stimulus intensity of rabbit eyes nonirritant.
Transparent lotion product of the invention carries out total number of bacterial colonies, coli-group, pathogenic pyogenic baeceria, fungus colony Sum, bacteriostatic test (Escherichia coli, staphylococcus aureus, Candida albicans), stability test (Candida albicans) inspection It surveys:
See the survey report of Guangzhou industrial microorganism inspection center, detects number XJ120180942.
Embodiment measure of merit
Three groups of crowds (age 30-55), every group of 25 people brush teeth or smear twice for one day.Test effect is as follows:

Claims (4)

1. a kind of white lotion preparation method of dentifrice composition containing Artesunate, it is characterized in that:
Raw material is by weight ratio
Water material:
17-20 parts of sorbierite, PEG-600 be 4-8 parts, 0.3-0.45 parts of saccharin, 0.6-0.8 parts of EDTA-2 sodium, deionized water 20- 24 parts;
Oil plant:
It is 0.5-1.2 parts of eugenol, 0.6-0.9 parts of menthol, 1.0-3.0 parts of oil of badian, 1.0-2.5 parts of Artesunate, fragrant It is 1-1.5 parts smart;
Powder:
35-42 parts of calcium monohydrogen phosphate, 2-5 parts of silica, 1.0-1.5 parts of sodium carboxymethylcellulose, lauryl sodium sulfate (K12) 2.4-3.0 part;
Preparation method:
(1) prepared by water material: it is put into deionized water in water phase tank, PEG-600, EDTA-2 sodium, saccharin is added in the state of stirring, Stirring and dissolving is uniform, and sorbierite is then added and stirs evenly liquid, for use;
(2) preparation of oil plant: Artesunate is added in oil of badian, is evenly stirred until transparent liquid, is then added fourth Fragrant phenol, menthol, essence are stirred even liquid, for use;
(3) prepared by powder: calcium monohydrogen phosphate, sodium carboxymethylcellulose, lauryl sodium sulfate, silica are stirred It is even, for use;
(4) cream processed: above-mentioned water material, oil plant, powder are pumped under vacuum in three-in-one Manufacturing medicine extract machine, after mixing evenly, blowing obtains Product.
2. the dentifrice composition containing Artesunate obtained such as claim 1 preparation method.
3. a kind of preparation method of the transparent lotion of dentifrice composition containing Artesunate, it is characterized in that:
Raw material is by weight ratio
Water material:
56-58 parts of sorbierite, PEG-600 be 3-5 parts, 0.3-0.5 parts of saccharin, 0.5-0.8 parts of EDTA-2 sodium, deionized water 9-12 Part;
Oil plant:
It is 0.5-1.2 parts of eugenol, 0.6-1.0 parts of menthol, 1.5-3.0 parts of oil of badian, 1.0-2.5 parts of Artesunate, fragrant It is 1-1.5 parts smart;
Powder: 6-19 parts of silica 1,0.7-1.0 parts of sodium carboxymethylcellulose, 2.4-3.0 parts of lauryl sodium sulfate;
Preparation method:
(1) prepared by water material: it is put into deionized water in water phase tank, PEG-600, EDTA-2 sodium, saccharin is added in the state of stirring, Stirring and dissolving is uniform, and sorbierite is then added and stirs evenly liquid, for use;
(2) preparation of oil plant: Artesunate is added in oil of badian, is evenly stirred until transparent liquid, is then added fourth Fragrant phenol, menthol, essence are stirred even liquid, for use;
(3) prepared by powder: silica, sodium carboxymethylcellulose, lauryl sodium sulfate, silica are uniformly mixed, For use;
(4) cream processed: above-mentioned water material, oil plant, powder are pumped under vacuum in three-in-one Manufacturing medicine extract machine, after mixing evenly, blowing obtains Product.
4. the dentifrice composition containing Artesunate obtained such as claim 3 preparation method.
CN201811538066.0A 2018-12-16 2018-12-16 One kind dentifrice composition containing Artesunate and preparation method thereof Pending CN109498490A (en)

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Application Number Priority Date Filing Date Title
CN201811538066.0A CN109498490A (en) 2018-12-16 2018-12-16 One kind dentifrice composition containing Artesunate and preparation method thereof

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Application Number Priority Date Filing Date Title
CN201811538066.0A CN109498490A (en) 2018-12-16 2018-12-16 One kind dentifrice composition containing Artesunate and preparation method thereof

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Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1771904A (en) * 2005-10-25 2006-05-17 汪正华 New use of sweet wormwood herb
US20070269537A1 (en) * 2003-02-10 2007-11-22 Bioderm Research Skin Condition Improvement Including Acne, Rosacea, and Topical Wounds by Artemisia Annua Extract via Iron Siderophore Trojan Horse Delivery System
CN106214505A (en) * 2016-08-10 2016-12-14 辛成业 Artemisine composition or a combination thereof thing new opplication in mouth care
CN106236612A (en) * 2016-08-27 2016-12-21 广东罗浮山国药股份有限公司 A kind of toothpaste and preparation method thereof
CN106880554A (en) * 2017-03-14 2017-06-23 四川蓝伯特生物科技股份有限公司 A kind of sweet wormwood toothpaste and preparation method thereof

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070269537A1 (en) * 2003-02-10 2007-11-22 Bioderm Research Skin Condition Improvement Including Acne, Rosacea, and Topical Wounds by Artemisia Annua Extract via Iron Siderophore Trojan Horse Delivery System
CN1771904A (en) * 2005-10-25 2006-05-17 汪正华 New use of sweet wormwood herb
CN106214505A (en) * 2016-08-10 2016-12-14 辛成业 Artemisine composition or a combination thereof thing new opplication in mouth care
CN106236612A (en) * 2016-08-27 2016-12-21 广东罗浮山国药股份有限公司 A kind of toothpaste and preparation method thereof
CN106880554A (en) * 2017-03-14 2017-06-23 四川蓝伯特生物科技股份有限公司 A kind of sweet wormwood toothpaste and preparation method thereof

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
宁保明 等: "《化学药品对照品图谱集-热分析》", 31 August 2014, 中国医药科技出版社 *

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