CN106214505A - Artemisine composition or a combination thereof thing new opplication in mouth care - Google Patents
Artemisine composition or a combination thereof thing new opplication in mouth care Download PDFInfo
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- CN106214505A CN106214505A CN201610650893.3A CN201610650893A CN106214505A CN 106214505 A CN106214505 A CN 106214505A CN 201610650893 A CN201610650893 A CN 201610650893A CN 106214505 A CN106214505 A CN 106214505A
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
- A61K31/366—Lactones having six-membered rings, e.g. delta-lactones
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/28—Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
- A61K36/282—Artemisia, e.g. wormwood or sagebrush
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- 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
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/4973—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
- A61K8/498—Cosmetics 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
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
- A61Q17/005—Antimicrobial preparations
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Abstract
The present invention relates to a kind of new opplication of defined artemisine composition or a combination thereof thing, i.e. new opplication in mammalian mouth nursing field.Its by provide correct dyskeratosis, antiinflammatory, ease pain, stop blooding, wound healing, antibacterium, a series of benefits such as antifungal, eliminate or alleviate mammalian mouth defective mode, to strengthen health and the beauty in oral cavity.Described benefit is proved by substantially preventing or alleviate mammal dental plaque, gingivitis, periodontitis, oral keratosis, sensitivity of tooth, oral ulcer, dental caries, oral cavity pathogen propagation etc..Described benefit is by realizing to administration artemisine composition or a combination thereof thing or the oral care composition such as health-oriented products, daily chemical products, health product or the medicine that comprise artemisine composition or a combination thereof thing.The present invention by the Enlargement of artemisine composition or a combination thereof thing in field of oral care so that it is given play to bigger usefulness for public healthy causes.
Description
Technical field
The present invention relates to a kind of new opplication of defined artemisine composition or a combination thereof thing, i.e. at mammal mouth
The new opplication of chamber nursing field includes, i.e. by correct dyskeratosis, antiinflammatory, ease pain, stop blooding, wound healing, antibacterium, antifungal etc.
A series of comprehensive effects preventions useful to mammalian mouth, postpone and/or treat mammal dental plaque, gingivitis,
The defective modes such as periodontitis, oral keratosis, sensitivity of tooth, oral ulcer, dental caries, oral cavity pathogen propagation, eliminate or alleviate
The symptoms such as red swelling of gingiva pain that they are caused, gingival hemorrhage, dental pain, ulcer, halitosis.By will be containing safely and effectively
The artemisine composition of amount or oral care composition such as health-oriented products, daily chemical products, health product or the medicine etc. of a combination thereof thing
It is administered to need, on the mammal of this kind of effect, these methods and benefit to be realized.
Background technology
Along with the high speed development of economy and society, the health perception of people is greatly promoted, and oral health has obtained unprecedented
Pay attention to.The requirement of oral care product is improved by people the most day by day, is especially embodied in the requirement with safety functional to it.
Perplex public oral problem at present and be mainly periodontitis, dental caries, oral ulcer, gingival hemorrhage, red swelling of gingiva burning pain, tooth
Tooth sensitivity, halitosis etc..Therefore with toothpaste, collutory, oral film agent, oral spray, oral cavity ointment, chewing gum on market
Deng the oral care product for representative, mostly with the addition of to solve the active component of various oral problem.But these compositions
Being mostly synthetic source, user has query to its safety.Advocate natural today pursuing nature, can efficient solution
Certainly the active component of the natural origin of various oral problem, little with its toxic and side effects, green, environmental protection, safety high times
Also constantly increased by public expectations and its consumption demand.
Arteannuin is the present that Chinese Traditional Medicine gives the people of the world, to preventing and treating the infectious diseases such as malaria, safeguarding the world
People's health is significant.Within 2015, slaughter cry of a deer researcher and obtain Nobel prize's soul, table because of arteannuin
Understand the whole world accreditation to artemisine composition, be that China's traditional medicine culture goes to the world, by the people of the world recognized into
A monument in journey.At present artemisine composition has become the study hotspot of countries in the world, to its antitumor, parasiticide,
The effect such as systemic lupus erythematosus conducts in-depth research.But above research is all around drug research and launches
, deeply excavate the elite in pools of traditional Chinese medicine for response country, give full play to the unique advantage of Chinese medicine, advance Chinese medicine existing
Dai Hua, promotes the call that Chinese medicine goes to the world, and artemisine composition is carried out extensively by applicant in line with rigorous realistic attitude
Pharmacodynamics screening research, to making artemisine composition preferably be serviced by society.
Applicant carries out Pharmacodynamics screening widely with Herba Artemisiae Annuae and artemisine composition or a combination thereof thing, and has surprisingly found that
Herba Artemisiae Annuae and artemisine composition or a combination thereof thing have on mammalian mouth antiinflammatory, stop blooding, ease pain, antibacterial, correct abnormal
Keratinization, promotion oral mucosa healing etc. have the ORAL CARE ACTIVE of notable benefit.Therefore applicants have discovered that safe and effective amount
Herba Artemisiae Annuae extract and artemisine composition and the artemisine component composition containing safe and effective amount can to oral disease or
Oral cavity defective mode provides preventative or therapeutic treatment.Such as, applicant has been found that artemisine composition or a combination thereof thing
There is prevention, postpone and/or treat mammal periodontitis；Prevent, postpone and/or treat going out of mammalian mouth ulcer
Existing；Prevent, postpone and/or treat mammalian gums scorching；Keep the cleaning of mammalian mouth, prevent, postpone and/or treat
The mammalian mouth defective mode that antibacterial, fungus etc. are caused；By antiinflammatory, ease pain, stop blooding, antibacterium, antifungal, correction
A series of effect useful to mammalian mouth such as dyskeratosis, eliminates or alleviates mammalian mouth defective mode thus carry
For the oral health strengthened and beauty.More than find to advance the innovation of daily chemical products, health-oriented products and medicine, and will
Public physical and mental healths and daily life are produced far-reaching influence.
Summary of the invention
The first aspect of the invention is to provide a kind of new opplication of defined artemisine composition or a combination thereof thing,
I.e. at the new opplication of field of oral care；The second aspect of the invention is to provide a kind of oral care composition, and it comprises
The artemisine composition of safe and effective amount or a combination thereof thing and stomatology and other active additives pharmaceutically acceptable and substrate；
The third aspect of the invention is that providing a kind of eliminates or alleviate mammalian mouth defective mode to provide the oral cavity strengthened
Healthy with beautiful method, described method include to artemisine composition defined in administration or a combination thereof thing or this
The oral care composition of invention.
Artemisine composition as herein described or a combination thereof thing refer to arteannuin and derivant thereof and correlative and they
Salt includes but not limited to, arteannuin, dihydroarteannuin, artesunate, sodium artesunate, Artemether, arteether, arteannuin C13
Derivant, arteannuin C12Derivant, arteannuin C4Derivant, deoxidation bridge arteannuin structure related compound, demethylation arteannuin
Structure related compound, de-ketonic oxygen arteannuin structure related compound, steroid arteannuin structure related compound, lactams are blue or green
Artemisin structure related compound, open loop arteannuin structure related compound, 4,5-epoxy carbon for arteannuin structure related compound,
Arteannuin structure simplifies thing, other arteannuin structure related compound and their salts；Or the group containing artemisine composition
Compound or extract include but not limited to, Chinese medicine Herba Artemisiae Annuae (ARTEMISIAE ANNUAE HERBA) and goods, plant Artemisia annua
(Artemisia annuaL.) and goods, other Compositae artemisias (Artemisia Linn. Sensu stricto, excl. Sect. Seriphidium Bess.) plant and goods, Herba Artemisiae Annuae tissue culture medium, artemisinin mother liquid etc.；Or be selected from
The arbitrary composition of mentioned component.The source of artemisine composition or a combination thereof thing can be to synthesize or naturally include but not limit
, molecular design, biosynthesis, histiocyte cultivation complete synthesis in, natural product extraction, chemistry, fungal transformation, metabolic pathway
Etc. approach.
Oral cavity as herein described refers to oral cavity and the accessory organ thereof of mammal, includes but not limited to oral cavity, tooth, saliva
Liquid gland, mucosa, gingiva, lip, tongue, palate, pharynx etc..
The new opplication of field of oral care as herein described refers to by correcting dyskeratosis, antiinflammatory, easing pain, stop blooding, more
A series of comprehensive effect useful to mammalian mouth such as wound, antibacterium, antifungal, prevents, postpones and/or treat suckling
Animal dental plaque, gingivitis, periodontitis, oral keratosis, sensitivity of tooth, oral ulcer, dental caries, oral cavity pathogen propagation etc. are no
Good state, and eliminate or alleviate red swelling of gingiva pain that they are caused, gingival hemorrhage, dental pain, ulcer, halitosis, oral cavity
The symptoms such as mucosal hyperplasia is coarse, oral leukoplakia comes off.
Artemisine composition that oral care composition as herein described refers to comprise safe and effective amount or a combination thereof thing and
Various health-oriented products that stomatology is formed with other active additives pharmaceutically acceptable and substrate, cosmetics of everyday use, medicine, guarantor
Strong product etc. include but not limited to, toothpaste, dentifrice, collutory, chewing gum, buccal tablet, throat lozenge, powder, spray, ointment, patch
Membrane, gel, pill, tablet, capsule, granule, effervescent, slow releasing agent etc. and other oral care implements.
Safe and effective amount as herein described refers to that the person skilled of this area rationally judges to use artemisine composition
Or a combination thereof thing be enough to produce significant beneficial effect, and this amount be enough to again avoid serious untoward reaction, i.e. provides reasonably
Effective hazard ratio, its content is preferably from about 0.0001%～90%, even more preferably about 0.005%～36%, most preferably about 0.05%～17%
Wherein said percentage ratio be by composition quality be in terms of 100%.
Oral cavity as herein described defective mode refers to that the oral cavity caused by the intrinsic factor of body or extrinsic factor is raw
The healthy state weakened with aesthetic appearance of reason includes but not limited to, periodontitis, gingivitis, oral ulcer, halitosis, dental caries, tooth bacterium
Speckle, gingival hemorrhage redness, dental pain, hyperplasia of oral mucosa are coarse, oral leukoplakia comes off.
The oral health of enhancing as herein described and beauty refer to make oral cavity owing to oral cavity defective mode is mitigated or eliminated
Physiological health and aesthetic appearance recover or further enhance to include but not limited to,
A) by correcting dyskeratosis effect prevention, postponing and/or treat mammalian mouth leukoderma, oral lichen planus etc.
By the hyperkeratotic conditions caused by dyskeratosis；
B) prevented by antiinflammatory action, postpone and/or treat mammalian gums inflammation, periodontitis, oral ulcer hyperemia redness etc.
Oral inflammation disease；
C) mammalian tooth sensitivity pain, gingiva pain, canker sore pain, aphtha pain is eliminated or alleviates by analgesic activity
The oral cavity defective modes such as pain；
D) eliminated by anastalsis or to alleviate mammalian gums hemorrhage, the oral cavity defective modes such as aphtha is hemorrhage；
E) eliminated by wound healing effect or alleviate mammalian mouth ulcer, the oral cavity defective mode such as aphtha；
F) prevented by antibacterium, antifungic action, to postpone and/or treat mammal halitosis, dental caries, dental plaque, oral cavity true
The mammalian mouth defective modes such as bacterium infection；
G) by correct dyskeratosis, antiinflammatory, ease pain, stop blooding, antibacterium, antifungal etc. a series of comprehensively to mammal mouth
The effect that chamber is useful, eliminates or alleviates mammalian mouth defective mode thus provide the oral health of enhancing with beautiful.
As herein described using refers to be included but not limited to by various route of administration, and rinsing the mouth, partial smearing, local are applied
Artemisine composition as herein described or a combination thereof thing or oral care composition effect as herein described is made by, the mode such as oral
In oral cavity.
Other active additives as herein described and substrate refer to known in the field in current mouth care daily use chemicals use
Product, medicine, health product, healthy product have been applied or the wide model in addition to artemisine composition and combinations thereof thing of possible application
Other the optional active additives enclosed and substrate include but not limited to, surfactant, preservative, abrasivus, wetting agent, increasing
Thick dose, caries preventive agent, desensitizer, hemorrhage, corrosion inhibiter, stabilizer, sweeting agent, spice, pigment, coloring agent, adhesive, disintegrate
Agent, filler, lubricant, wetting agent, osmotic pressure regulator, fluidizer, correctives, suspending agent, coating material, excipient, oil
Lipid substrate, emulsion-type substrate, hydrophilic or water-soluble base, gel-type vehicle, propellant, absorbent, diluent, flocculant are with anti-
Flocculant, filter aid, release blocker, microcapsule, microsphere, liposome, ester gum substrate, interfacial agent etc. and their group
Close.
Stomatology as herein described refers to described compositions with pharmaceutically acceptable and be applicable to and suckling containing component
Animal oral cavity contacts, and does not has excessive toxicity, incompatibility, unstability, atopic reaction etc.；Or be applicable to passing through
Various route of administration contact with mammalian organism, and do not have excessive toxicity, incompatibility, unstability, allergia anti-
Should wait.
The acceptable substrate of pharmacology as herein described refers to that described substrate will not produce impact to pharmacological experiment, can
With appropriate dispersion artemisine composition or a combination thereof thing, and as the negative control group in experiment.
By following limiting examples specific embodiments of the present invention will be further described and carry out now
Illustrating, example is served only for explaining the present invention, is not intended to limit the scope of the present invention.Content described herein is only this
Basic explanation under spirit and range of condition, its object is to make those skilled in the art it will be appreciated that the present invention
Content is also implemented according to this, it is impossible to only limit the scope of the claims of the present invention with following example, to according to technical solution of the present invention
Those of ordinary skill for, according to disclosed spirit, the present invention is carried out any equivalent transformation or modification,
Protection scope of the present invention all should be belonged to.
Embodiment 1: Herba Artemisiae Annuae toothpaste.
Following component can be made into arteannuin toothpaste by the existing production technology of toothpaste.
Embodiment 2: arteannuin chewing gum.
Following component can be made into arteannuin chewing gum by the existing production technology of chewing gum.
Experimental example 1: artemisine composition of the present invention or the antiinflammatory action of a combination thereof thing
Artemisine composition or a combination thereof thing disperse with the acceptable substrate of pharmacology.Take Kunming mouse 24, be randomly divided into 2
Group, i.e. Matrix controls group and 2% artemisine composition or a combination thereof thing group, often organize each 12.Dimethylbenzene 0.05mL is applied to mice
Auris dextra, after stimulation respectively at 15min, 30min, 45min administer locally to the substrate of each group of equivalent and 2% artemisine composition or its
Compositions, 60min break neck put to death animal, cut left and right auricular concha, take at the same position of two ears respectively with the card punch of diameter 8mm
Lower auricle weighs quality, compares with each group of auricular concha swelling of calculating of poor quality of two auricles.
Table 1. artemisine composition or a combination thereof thing xylol acutely inflamed impact of induced mice auricular concha (mean ±
SD)
P < 0.01, compares with Matrix controls group
Being had antiinflammatory action by artemisine composition seen from table 1 or a combination thereof thing, there were significant differences with Matrix controls group.
Experimental example 2: artemisine composition of the present invention or the analgesic activity of a combination thereof thing
Artemisine composition or a combination thereof thing disperse with the acceptable substrate of pharmacology.Take Kunming mouse 30, be randomly divided into 2
Group, i.e. Matrix controls group and 2% artemisine composition or a combination thereof thing group, often organize each 15.Administer locally to the substrate of each group of equivalent
After being administered with 2% artemisine composition or a combination thereof thing, preservative film covers, and unties after immobilization with adhesive tape 30min, cleans with normal saline
Medicine, then wipe dry with dry absorbent cotton, give the 2.5% formalin 30 μ L that mice right metapedes butt hemostasis is newly prepared immediately.Injection first
After aldehyde, immediate record every mice licks, in licking first and stinging incubation period of right metapedes and 10min, the number of times stinging right metapedes.
Table 2. artemisine composition or a combination thereof thing PARA FORMALDEHYDE PRILLS(91,95) cause the impact (mean ± SD) of mice pain
| Group | Number of elements | Incubation period/s | Sufficient number of times is licked in 10min |
| Matrix controls group | 15 | 7.9±1.55 | 25.4±5.2 |
| 2% artemisine composition or a combination thereof thing group | 15 | 13.2±3.25 | 14.9±5.4 |
P < 0.01, compares with Matrix controls group
Being had analgesic activity by artemisine composition seen from table 2 or a combination thereof thing, there were significant differences with Matrix controls group.
Experimental example 3: artemisine composition of the present invention or the anastalsis of a combination thereof thing
Artemisine composition disperses with the acceptable solvent of pharmacology.Take Kunming mouse 24, be randomly divided into 2 groups, i.e. substrate
Matched group and 2% artemisine composition or a combination thereof thing group, often organize each 12.Being fixed on by mice in Mus cylinder, tail tip 2cm soaks
Steep in 2% artemisine composition or a combination thereof thing solution or solvent, administration time 30min, after the 2h of interval, repeat administration 1 time.
Last is administered after 30min, cuts off mice in order to cutting at tail point 1.5cm, starts to count when recording hemorrhage when blood flows out naturally
Between, the cotton balls weighed in advance with oneself every 5 seconds draws drop of blood, naturally stops (depletion of blood when cotton balls is inhaled) until hemorrhage.Count as the following formula
Calculate each treated animal amount of bleeding: amount of bleeding=initial cotton balls weight (mg) of band blood cotton balls weight one.
The anastalsis (mean ± SD) that mice is docked by table 3. artemisine composition or a combination thereof thing
| Group | Number of elements | Bleeding time/s | Amount of bleeding/mg |
| Matrix controls group | 12 | 124.7±11.68 | 45.3±12.1 |
| 2% artemisine composition or a combination thereof thing group | 12 | 113.1±12.77 | 25.3±8.7 |
P < 0.05, compares with Matrix controls group
Being had anastalsis by artemisine composition seen from table 3 or a combination thereof thing, there were significant differences with Matrix controls group.
Experimental example 4: artemisine composition of the present invention or the antibacterial actions of a combination thereof thing
Antibacterial group is observed after 48h with or without colony growth through cultivating, with the medicine least concentration of the aseptic elder that is born as medicine
Low Mlc (MIC).
Table 4. artemisine composition or a combination thereof thing are to common causative antibacterial minimum inhibitory concentration
| Strain name | MIC/g% |
| Staphylococcus aureus | 1.1 |
| Streptococcus mutans | 1.2 |
| Bacillus pyocyaneus | 1.1 |
| Lactobacillus | 1.0 |
By artemisine composition seen from table 4 or a combination thereof thing to common causative antibacterial, especially cause the deformation chain of oral disease
Coccus and lactobacillus have certain inhibitory action.
Experimental example 5: artemisine composition of the present invention or the antifungic action of a combination thereof thing
Fungus group is observed the bacterium scope of dibbling after cultivating 72h and is not increased, and tapers into dry, for bacterial strain by Drug inhibition
Least concentration (MIC).
Table 5. artemisine composition or a combination thereof thing are to common oral fungus minimum inhibitory concentration
| Strain name | MIC/g% |
| Pityrosporum furfur | 0.9 |
| Candida albicans | 0.9 |
| Epidermophyton | 1.1 |
By artemisine composition seen from table 5 or a combination thereof thing, common oral mykoses there is certain inhibitory action.
Experimental example 6: the keratinization regulation effect of artemisine composition of the present invention or a combination thereof thing
Artemisine composition or a combination thereof thing disperse with the acceptable substrate of pharmacology.Take Kunming mouse 30, male and female half and half,
It is randomly divided into matrix group and 2% artemisine composition or a combination thereof thing group.The substrate of the 2 groups of mice every day of partial smearing equivalent respectively
After being administered with 2% artemisine composition or a combination thereof thing, preservative film covers, and unties after immobilization with adhesive tape 30min, cleans with normal saline
Medicine, then wipe dry with dry absorbent cotton, continuous 21 days, one day 2 times.Put to death animal in the 22nd day, at root of the tail 2cm, take rat-tail table
Skin, fixes paraffin embedding with 10% formalin, and HE dyes, at the tail scale of each mice of light Microscopic observation.All scale epidermises
Having continuous rows of granular cell person, be referred to as the scale having granular layer to be formed, granular cell is flat in epidermis or rhombus cell
Formed, in endochylema, be full of thick deep basophilia, the HE dyeing cutin granule transparent in avy blue.Counting rat-tail epidermis 100
Scale there is granular layer form number.
The impact (mean ± SD) that mice rat-tail granular cell is formed by table 6. artemisine composition or a combination thereof thing
| Group | Number of elements | In every 100 scales of rat-tail, granular layer forms number |
| Matrix controls group | 15 | 7.3±1.1 |
| 2% artemisine composition or a combination thereof thing group | 15 | 13.8±1.7 |
P < 0.05, compares with Matrix controls group
The effect promoting keratinization, correcting dyskeratosis is had, with Matrix controls group by artemisine composition seen from table 6 or a combination thereof thing
There were significant differences.
Experimental example 7: artemisine composition of the present invention or a combination thereof thing therapeutical effect to Gingivitis model
Artemisine composition or a combination thereof thing disperse with the acceptable substrate of pharmacology.Take SD rat 36, male and female half and half, at random
It is divided into normal group, matrix group, 2% artemisine composition or a combination thereof thing group.Matrix group and 2% artemisine composition or a combination thereof thing
The vertical gingivitis animal model of establishment is by after rat anesthesia, and in the gingival sulcus of center, left maxillary second molar cheek side, injection fat Han 1mg/mL is many
The normal saline 15 μ L of sugar, injects 1 time, continuous 4 days every day, within every 6 days, observes the change of gingiva, measure buccal gingiva after starting modeling
Ditch is visited and is examined the degree of depth (PD), record maximum and gingival index (GI).Within 7th day, rise, matrix group and 2% artemisine composition or its group
Compound group mice injects the substrate of equivalent and 2% artemisine composition or a combination thereof thing every day in the gingival sulcus suffering from tooth, and 3
It once carries out conventional raising and observes gingiva state.After 25 days, animal is put to death after medication, take the tooth of left maxillary second molar
Gum tissue, 40g/L formaldehyde fixes, routine paraffin wax embedding preparation section, checks inflammatory reaction shape after HE dyeing under optical microscope
Condition.Occurring in that gingiva hyperemia is red and swollen after matrix group and 2% artemisine composition or a combination thereof thing group modeling, gingiva is soft, visits and examines out
Blood, visits during 25d and examines the degree of depth and reach 2mm.PD and the GI comparative result of each group rat is shown in Table 7.2% artemisine composition or a combination thereof thing
Group topical after red swelling of gingiva substantially alleviate, hemorrhage minimizing, Matrix controls group then has no that inflammation is alleviated.Pathological study
Matrix controls group cell infiltration increases, vasodilation；2% artemisine composition or a small amount of cell infiltration of a combination thereof thing group.With
Upper result display artemisine composition or a combination thereof thing have alleviates the effect alleviating mammalian gums inflammation.
Table 7. artemisine composition or a combination thereof thing therapeutical effect (mean ± SD) to Gingivitis model
| Group | Number of elements | Gingival sulcus is visited and is examined the degree of depth (PD)/mm | Gingival index (GI) |
| Normal group | 12 | 0.43±0.17 | 0.00±0.00 |
| Matrix controls group | 12 | 2.12±0.61 | 1.87±0.41 |
| 2% artemisine composition or a combination thereof thing group | 12 | 0.88±0.66 | 0.91±0.36 |
3 groups of PD values and GI value carry out the most all there is significant difference (P < 0.01)
Experimental example 8: artemisine composition of the present invention or the wound healing effect to rabbit Oral ulcer model of a combination thereof thing
Artemisine composition or a combination thereof thing disperse with the acceptable substrate of pharmacology.Take new zealand rabbit 16, be randomly divided into base
Matter group and 2% artemisine composition or a combination thereof thing group.Take a glass tubing and be perpendicularly fixed at rabbit oral mucosal surface, in pipe
Injected slurry volume mark is the glacial acetic acid 0.2ml of 30%, dips in out glacial acetic acid with cotton swab after 30s.Measure after 24h with or without edema, mucosa
Ulcer area also observes inflammatory congestion situation, and carry out classification.Grade scale: 0 grade: without blush around ulcer, without edema；1 grade；
Slightly blush around ulcer；2 grades: have blush around ulcer, without edema；3 grades；There is blush around ulcer, have edema.2 treated animals
Every day, the substrate of partial smearing equivalent respectively was total to 3d with 2% artemisine composition or a combination thereof thing.Take rabbit observation inflammation in d4 to fill
Blood situation is also put to death after measuring ulcer area, takes the formalin that mucous membrane tissue volume fraction at ulcer is 10% and fixes, carries out
Pathologic diagnosis.Matrix group is shown in Table 8 with 2% artemisine composition or a combination thereof thing group ulcer area with inflammation grade.Matrix group
The all visible pitting defect in perusal mucosa face, diameter is about 5.0～5.5mm；Surface has more canescence or lark scorching
Property sphacelus；Seeing obvious ulcer under mirror, scope is relatively big, skin surface squamous epithelial cancer is downright bad, come off and have more slough and
Inflammatory exudate；Under ulcer, connective tissue is also shown in obvious necrosis；A large amount of mononuclear cells, eosinophilic granulocyte, neutral inflammatory cell and
The inflammatory infiltrations such as lymphocyte, as deep as Submucosa.2% artemisine composition or a combination thereof thing group, be shown in the most individually tiny depression
District；See under mirror at former ulcer that slough and inflammatory exudation be relatively light or nothing；Surface covers thin layer squamous epithelial cancer, upper subcutaneous a small amount of inflammation
Sexual cell infiltrates, and sees granulation tissue and proliferation of fibrous tissue.Result above display artemisine composition or a combination thereof thing have slow
Solve mammalian mouth ulcer and promote its effect healed.
Table 8. artemisine composition or the wound healing effect (mean ± SD) to rabbit Oral ulcer model of a combination thereof thing
| Group | Number of elements | Ulcer area/mm before medication2 | Ulcer area/mm after medication2 | Medication proinflammatory classification | Inflammation grade after medication |
| Matrix controls group | 8 | 27.6±3.7 | 12.9±3.4 | 3.0 | 2.3 |
| 2% artemisine composition or a combination thereof thing group | 8 | 28.0±3.9 | 6.1±2.9 | 3.0 | 0.8 |
P < 0.05, compares with Matrix controls group.
Claims (10)
1. artemisine composition or a kind of new opplication of a combination thereof thing, i.e. new opplication in mammalian mouth nursing field,
It is characterized in that described artemisine composition or a combination thereof thing refer to arteannuin and derivant thereof and correlative and their salt
Class includes but not limited to, arteannuin, dihydroarteannuin, artesunate, sodium artesunate, Artemether, arteether, arteannuin C13Spread out
Biological, arteannuin C12Derivant, arteannuin C4Derivant, deoxidation bridge arteannuin structure related compound, demethylation arteannuin are tied
Structure related compound, de-ketonic oxygen arteannuin structure related compound, steroid arteannuin structure related compound, lactams Herba Artemisiae Annuae
Element structure related compound, open loop arteannuin structure related compound, 4,5-epoxy carbon are for arteannuin structure related compound, green grass or young crops
Artemisin structure simplifies thing, other arteannuin structure related compound and their salts；Or the combination containing artemisine composition
Thing or extract include but not limited to, Chinese medicine Herba Artemisiae Annuae (ARTEMISIAE ANNUAE HERBA) and goods, plant Artemisia annua
(Artemisia annuaL.) and goods, other Compositae artemisias (Artemisia Linn. Sensu stricto, excl. Sect. Seriphidium Bess.) plant and goods, Herba Artemisiae Annuae tissue culture medium, artemisinin mother liquid etc.；Or be selected from
The arbitrary composition of mentioned component.
2. contain the oral care composition such as health-oriented products, daily chemical products of artemisine composition or a combination thereof thing, health product or
The new opplication in mammalian mouth nursing field such as medicine, it is characterised in that containing safe and effective amount such as claim 1
Described artemisine composition or a combination thereof thing, and stomatology and other active additives pharmaceutically acceptable and substrate.
3. artemisine composition as described in as arbitrary in right 1～2 or a combination thereof thing or oral care composition are at mammal mouth
The new opplication of chamber nursing field, it is characterised in that the source of artemisine composition or a combination thereof thing can be synthesis or naturally include
But it is not limited to, natural product extraction, complete synthesis, molecular design, biosynthesis, the histiocyte cultivation of chemistry, fungal transformation, generation
Thank to the approach such as path.
4. artemisine composition as described in claims 1 to 3 is arbitrary or a combination thereof thing or oral care composition move in suckling
The new opplication of thing field of oral care, it is characterised in that artemisine composition or a combination thereof thing containing in oral care composition
Amount preferably from about 0.0001%～90%, even more preferably about 0.005%～36%, most preferably about 0.05%～17% wherein said percentage
Than be by composition quality be in terms of 100%.
5. artemisine composition as described in Claims 1 to 4 is arbitrary or a combination thereof thing or oral care composition move in suckling
The new opplication of thing field of oral care, it is characterised in that other active additives that can add and substrate refer to well known in the art
Applied in current mouth care cosmetics of everyday use, medicine, health product, healthy product or the becoming except artemisine of possible application
Point and combinations thereof other optional active additives of wide scope beyond thing and substrate include but not limited to, surfactant,
Preservative, abrasivus, wetting agent, thickening agent, caries preventive agent, desensitizer, hemorrhage, corrosion inhibiter, stabilizer, sweeting agent, spice, color
Element, coloring agent, adhesive, disintegrating agent, filler, lubricant, wetting agent, osmotic pressure regulator, fluidizer, correctives, suspending
Agent, coating material, excipient, greasing base, emulsion-type substrate, hydrophilic or water-soluble base, gel-type vehicle, propellant, suction
Receive agent, diluent, flocculant and deflocculant, filter aid, release blocker, microcapsule, microsphere, liposome, ester gum substrate, interface
Activating agent etc. and their combination.
6. artemisine composition as described in Claims 1 to 5 is arbitrary or a combination thereof thing or oral care composition move in suckling
The new opplication of thing field of oral care, it is characterised in that described oral care composition includes but not limited to, health-oriented products, day
Change articles for use, medicine, health product, toothpaste, dentifrice, collutory, chewing gum, buccal tablet, throat lozenge, powder, spray, ointment, patch
Membrane, gel, pill, tablet, capsule, granule, effervescent, slow releasing agent etc. and other oral care implements.
7. artemisine composition as described in as arbitrary in claim 1～6 or a combination thereof thing or oral care composition move in suckling
The new opplication of thing field of oral care, it is characterised in that described application refers to oral cavity defective mode is mitigated or eliminated and makes oral cavity
Physiological health and aesthetic appearance recover or further enhance to include but not limited to, by correct dyskeratosis, antiinflammatory, analgesia,
A series of comprehensive effect useful to mammalian mouth such as hemostasis, wound healing, antibacterium, antifungal, prevent, postpone and/or
Treatment mammal dental plaque, gingivitis, periodontitis, oral keratosis, sensitivity of tooth, oral ulcer, dental caries, oral cavity pathogen
The defective modes such as propagation, eliminate or alleviate red swelling of gingiva pain that they are caused, gingival hemorrhage, dental pain, ulcer, mouth
The mammalian mouth defective mode such as smelly, hyperplasia of oral mucosa is coarse, oral leukoplakia comes off thus the oral cavity of enhancing is provided
Healthy and beautiful.
8. eliminating or alleviate oral health and a beautiful method that mammalian mouth defective mode strengthens with offer, it is special
Levy and be that described method includes to the arbitrary described artemisine composition of administration right 1～7 or a combination thereof thing or mouth
Chamber care composition.
9. by the arbitrary described artemisine composition of administration such as claim 1～8 or a combination thereof thing or oral cavity
Care composition, obtains the oral health of enhancing with beautiful to eliminate or to alleviate mammalian mouth defective mode.
10. artemisine composition as described in as arbitrary in claim 1～9 or a combination thereof thing or oral care composition move in suckling
The application of thing field of oral care.
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| CN109498490A (en) * | 2018-12-16 | 2019-03-22 | 丹东欣时代生物医药科技有限公司 | One kind dentifrice composition containing Artesunate and preparation method thereof |
| CN110327423A (en) * | 2019-07-29 | 2019-10-15 | 江苏迦南美地生物科技有限公司 | A kind of anti-inflammatory spray of the department of stomatology containing bletilla striata extract ingredient and larynx section |
| CN110613801A (en) * | 2018-06-20 | 2019-12-27 | 株式会社 Lg 生活健康 | Composition for preventing or treating oral diseases comprising Artemisia annua and bamboo salt |
| CN110839796A (en) * | 2019-10-18 | 2020-02-28 | 贵州国圣堂生物科技有限公司 | Sweet wormwood toxin-clearing beverage and preparation method thereof |
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| 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 |
| CN110613801A (en) * | 2018-06-20 | 2019-12-27 | 株式会社 Lg 生活健康 | Composition for preventing or treating oral diseases comprising Artemisia annua and bamboo salt |
| CN110613801B (en) * | 2018-06-20 | 2023-03-28 | 株式会社 Lg 生活健康 | Oral composition for preventing or improving oral diseases and use thereof |
| CN109498490A (en) * | 2018-12-16 | 2019-03-22 | 丹东欣时代生物医药科技有限公司 | One kind dentifrice composition containing Artesunate and preparation method thereof |
| CN110327423A (en) * | 2019-07-29 | 2019-10-15 | 江苏迦南美地生物科技有限公司 | A kind of anti-inflammatory spray of the department of stomatology containing bletilla striata extract ingredient and larynx section |
| CN110839796A (en) * | 2019-10-18 | 2020-02-28 | 贵州国圣堂生物科技有限公司 | Sweet wormwood toxin-clearing beverage and preparation method thereof |
| CN110859790A (en) * | 2019-12-30 | 2020-03-06 | 柳州两面针股份有限公司 | Application of traditional Chinese medicine composition in preparation of oral care product |
| CN110859790B (en) * | 2019-12-30 | 2022-06-24 | 柳州两面针股份有限公司 | Application of traditional Chinese medicine composition in preparation of oral care product |
| CN114949105A (en) * | 2022-06-09 | 2022-08-30 | 云南大唐汉方制药股份有限公司 | Medicinal toothpaste for preventing and treating oral mucositis caused by radiotherapy and chemotherapy |
| CN114949105B (en) * | 2022-06-09 | 2023-07-14 | 云南大唐汉方制药股份有限公司 | Medicinal toothpaste for preventing and treating oral mucositis caused by radiotherapy and chemotherapy |
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