CN102058608A - New application of glucosamine in treating dental ulcer - Google Patents
New application of glucosamine in treating dental ulcer Download PDFInfo
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Abstract
The invention relates to new application of glucosamine in treating dental ulcer, wherein the chemical name of the glucosamine is 2amino-2-deoxidation-D-glucose, and the glucosamine is an in vivo synthesized substance. The glucosamine comprises pharmaceutically acceptable salts such as hydrochloride, nitrate, sulfate, phosphate, hydrobromide, mesylate, citrate, and the like. The effective dosage of the glucosamine for treating dental ulcer is 0.01-5g, which is preferable for 0.1-1g, and more preferable for 0.1-0.5g.
Description
Technical field:
The present invention relates to a kind of new purposes of medicine, particularly a kind of new purposes of glucosamine, this new purposes is mainly used in oral ulcer,
Background technology:
Glucosamine, chemical name: 2-amino-2-deoxy-D-glucose is a synthetic material in the human body, is the important nutrient that forms chondrocyte, is the natural tissues composition of healthy articular cartilage.With advancing age, the shortage of the intravital glucosamine of people is more and more serious, and articular cartilage is constantly degenerated and worn and torn.The U.S., Europe and Japanese a large amount of medical researches show: glucosamine can help to repair and safeguard cartilage, and can stimulate the growth of chondrocyte.
Glucosamine treatment function, 1, adapts to disease: knee joint degenerative osteoarthritis, 2, adapt to disease: hyperosteogeny, 3, adapt to disease: meniscus injury, 4, adapt to disease: patella, malacosis, 5, adapt to disease: cervical spondylosis spondylotic radiculopathy, 6, adapt to disease: cervical spondylosis myeloid form, 7, adapt to disease: the cervical spondylosis vertebral artery type, 8, adapt to disease: the cervical spondylosis adrenergic type, 9, adapt to disease: synovitis, 10, adapt to disease: bursitis, 11, adapt to disease: the hands bone
,Arthritis, 12, adapt to disease: sufficient bone, arthritis, 13, adapt to disease: scapulohumeral periarthritis, 14, adapt to disease: tenosynovitis, thecal cyst, 15, adapt to disease: prolapse of lumbar intervertebral disc, 16, adapt to disease: rheumatic
,Arthritis.
Be suitable for the crowd of maintenance, 1, crowd's type: the crowd's scapulohumeral periarthritis of bending over one's desk working for a long time, 2, crowd's type: highly intensive labour crowd, 3, crowd's type: sport people, 4, crowd's type: special occupation crowd glucosamine has 3 main effects: first, repair articular cartilage and surrounding soft tissue thereof that (or reparation) worn and torn already, make articular surface keep smooth; The second, impel the pass internode to generate more knuckle synovia, thereby alleviate interarticular frictional force when walking; The 3rd, antiinflammation can be eliminated arthritic symptom
On market, glucosamine mainly contains two kinds in D-glucosamine hydrochlorate and D-glucosamine sulfate, and in the clinical trial of China, D-glucosamine sulfate is similar to the hydrochlorate therapeutic effect.Glucosamine class osteoarthrosis product can be divided into two classes substantially: the one, add the glucosamine formulations of chemical antibiotic medicine, and be subjected to the strict control of FDA.This class preparation mainly contains glucosamine+ibuprofen, glucosamine+piroxicam.The 2nd, numerous glucosamine class health food manages by the dietary supplement series products.Wherein, glucosamine class health food can be divided into 3 classes again: the one, and simple glucosamine component preparation; The 2nd, the compound formulation of glucosamine+chondroitin sulfate; The 3rd, the compound product that glucosamine+other one-tenth are grouped into is as glucosamine+MSM (the osteoarticular health substance of a kind of protection), glucosamine+bromelain, glucosamine+vitamin D3, glucosamine+hyaluronic acid etc.
Report that glucosamine has antiinflammatory, analgesic effect, treatment rheumatic arthritis and gastric ulcer are had good curative effect; Can participate in the Liver and kidney detoxifcation, performance antiinflammatory liver protection effect; Can suppress the growth of antibacterial.It also is the primary raw material of synthetic cancer therapy drug and antibiotic etc.Also can be used for food, cosmetics and feed additive, purposes is quite extensive.
Oral ulcer is called " aphtha " again, is the superficial ulcer that occurs on the oral mucosa, big I from the grain of rice to the Semen Glycines size, circular or oval, ulcer surface is recessed, congested on every side.Ulcer has characteristics such as periodicity, recurrent and self limiting, good sending out in lip, cheek, lingual margin etc.The cause of disease and mechanism of causing a disease are still indeterminate.Inducement may be local wound, psychentonia, food, medicine, hormonal readiness change and vitamin or trace element deficiency.Systemic disease, heredity, immunity and microorganism may play an important role in its generation, development.Treatment is mainly based on topical therapeutic, and severe patient needs whole body therapeutic.
At present, the medicine of treatment oral ulcer has powders such as Chinese medicine XILEI SAN, BINGPENG SAN, and Western medicine has the membrane of gargarism, aureomycin hydrochloride crystalline ointment and some medicines.The medicine membrane that is used for oral ulcer has sitoesterol film (pharmaceutical factory, the Yellow River), rifamoin membrane (Beijing the 6th pharmaceutical factory), bacteriolyze enzyme membrane (biological pharmaceutical factory, Wuhan), clotrimazole film, Lac regis apis serous coat (Wuhan the 3rd pharmaceutical factory), dexamethasone Chinese medicine and western medicine compound stomatocase-treating films etc., above product has all had necessarily curative effect.
Oral ulcer is one of commonly encountered diseases, frequently-occurring disease, though non-very serious, the course of disease is long, is difficult to cure, and influence is taken food even spoken, and its sickness rate accounts for the 10-15% of the total case of oral cavity outpatient service.Numerous patient's utmost points wish to have a kind of pharmaceutical dosage form easy to use, eutherapeutic.
Summary of the invention:
The present invention finds that unexpectedly glucosamine can have the good curing effect to oral ulcer, therefore the invention provides a kind of new therapeutic use of glucosamine.
The inventor is through long-term conscientious research, and beat all discovery glucosamine is prepared into to paste in the oral cavity in and is coated with preparation and can has the good curing effect to oral ulcer, and does not find its untoward reaction in this product experimentation, safety, effective.Again because of still there not being at present both at home and abroad the report of glucosamine oral administration preparation, so the present invention provides the purposes of glucosamine treatment oral ulcer from another aspect.
Glucosamine of the present invention, comprise pharmaceutically acceptable salt forms such as its hydrochlorate, nitrate, sulfate, phosphate, hydrobromate, mesylate, citrate, it can form arbitrary form, comprise pharmaceutically acceptable forms such as crystal form (comprise and have a water of crystallization and do not have water of crystallization), hydrate forms, preferred glucosamine hydrochloride and sulfate.These salt and different forms can be according to method preparations well known in the art.
Effective dose of the present invention is that glucosamine is in the amount ranges that is used for oral cavity something lost infections experiment.The inventor is through repeatedly discovering, the effective dose that is suitable for glucosamine treatment oral ulcer is 0.01g～5g, preferred 0.1-1g, more preferably 0.1-0.5g.
Therefore the invention provides the application of glucosamine in the medicine of preparation treatment oral ulcer.
Medicine of the present invention is to be the pharmaceutical preparations composition that active constituents of medicine is prepared into the glucosamine.
Pharmaceutical composition of the present invention can contain the medicine acceptable carrier as required, and medicine acceptable carrier shared percentage by weight in preparation can be 0.1-99.9%.Pharmaceutical composition of the present invention exists with unit dosage form, and described unit dosage form is meant the unit of preparation, as every of tablet, and capsular every capsules, every bottle of oral liquid, every bag of granule, every of injection, every card of patch etc.
Pharmaceutical composition of the present invention can be any pharmaceutically useful dosage form, these dosage forms comprise: tablet, sugar coated tablet, film coated tablet, enteric coated tablet, capsule, hard capsule, soft capsule, oral liquid, suck agent, granule, electuary, pill, powder, unguentum, sublimed preparation, suspensoid, powder, solution, injection, suppository, ointment, plaster, cream, spray, drop, drop pill, patch, eye drop, buccal bioadhesive tablet, pigmenta pro cavo qris, oral cavity powder, paste etc.
Pharmaceutical composition of the present invention, the preparation of its oral administration can contain excipient commonly used, such as binding agent, filler, diluent, tablet agent, lubricant, disintegrating agent, coloring agent, flavoring agent and wetting agent, can carry out coating to tablet in case of necessity.
The filler that is suitable for comprises cellulose, mannitol, lactose and other similar filler.Suitable disintegrating agent comprises starch, polyvinylpyrrolidone and starch derivatives, for example sodium starch glycollate.Suitable lubricant comprises, for example magnesium stearate.The acceptable wetting agent of appropriate drug comprises sodium lauryl sulphate.
Can fill by mixing, the method that tabletting etc. are commonly used prepares solid oral composition.Mix repeatedly active substance is distributed in those compositionss of a large amount of filleies of whole use.
The form of oral liquid for example can be aqueous or oily suspensions, solution, Emulsion, syrup or elixir, perhaps can be a kind of available water before use or other suitable composite dry products of carrier.This liquid preparation can contain conventional additive, such as suspending agent, for example sorbitol, syrup, methylcellulose, gelatin, hydroxyethyl-cellulose, carboxymethyl cellulose, aluminium stearate gel or hydrogenation edible fat, emulsifying agent, for example lecithin, anhydro sorbitol monooleate or arabic gum; Non-aqueous carrier (they can comprise edible oil), for example almond oil, fractionated coconut oil, such as oily ester, propylene glycol or the ethanol of the ester of glycerol; Antiseptic, for example para hydroxybenzene methyl ester or propyl p-hydroxybenzoate or sorbic acid, and if desired, can contain conventional flavouring agent or coloring agent.
For liquid preparation, the liquid unit dosage forms of preparation contains active substance of the present invention and sterile carrier.According to carrier and concentration, this chemical compound can be suspended or dissolving.The preparation of solution is normally by being dissolved in active substance in a kind of carrier filter-sterilized before it is packed into a kind of suitable bottle or ampoule, sealing then.For example a kind of local anesthetic of adjuvant, antiseptic and buffer agent also can be dissolved in this carrier.In order to improve its stability, can be after the bottle of packing into that this compositions is freezing, and under vacuum, water is removed.
Pharmaceutical composition of the present invention, when being prepared into medicament, optionally add suitable medicine acceptable carrier, described medicine acceptable carrier includes but not limited to following material, be selected from: mannitol, sorbitol, sodium pyrosulfite, sodium sulfite, sodium thiosulfate, cysteine hydrochloride, TGA, methionine, vitamin C, the EDTA disodium, EDTA calcium sodium, the alkali-metal carbonate of monovalence, acetate, phosphate or its aqueous solution, hydrochloric acid, acetic acid, sulphuric acid, phosphoric acid, aminoacid, sodium chloride, potassium chloride, sodium lactate, xylitol, maltose, glucose, fructose, dextran, glycine, starch, sucrose, lactose, mannitol, silicon derivative, cellulose and derivant thereof, alginate, gelatin, polyvinylpyrrolidone, glycerol, soil temperature 80, agar, calcium carbonate, calcium bicarbonate, surfactant, Polyethylene Glycol, cyclodextrin, beta-schardinger dextrin-, the phospholipid material, Kaolin, Pulvis Talci, calcium stearate, magnesium stearate etc.
Preferred pharmaceutical composition of the present invention is a pharmaceutical dosage forms, and the dosage form of oral local administration most preferably is as buccal bioadhesive tablet, buccal tablet, collutory, paste, spray, contain agent, aerosol etc., oral preparation of the present invention can be liquid, suspendible, the form that the grade of dry powder is commonly used, buccal bioadhesive tablet most preferably, buccal tablet.Its preparation is according to galenic pharmacy routine techniques preparation, preferred manufacturing procedure as:.
The preparation of mouth ulcer lozenge:
Buccal tablet of the present invention is formed by following composition and medicine acceptable carrier processing and preparing:
Glucosamine, binding agent, correctives, fluidizer, lubricant,, above supplementary material, mixing granulation tabletting are made 1000 tablets of tablets.
The preparation of collutory
Prescription is formed with preparation and 1. formed: glucosamine, distilled water is an amount of.2. preparation: get glucosamine and be dissolved in surely in an amount of hot distilled water, cooled and filtered, adding distil water gets final product to 1000ml on filter.
The preparation of patch:
Preparation method 1: the PVA adding distil water is macerated, and heating for dissolving in water-bath makes its expansion, and placement is spent the night, and makes rubber cement.Get glucosamine and pulverize, cross 180 mesh sieves, in the liquid, mix well gently in the adding.Leave standstill and remove bubble, incline to and sterilize in advance and scribble on the glass plate of liquid paraffin, paint the uniform membrane of thickness, put (70-80 ℃) dry, skinning in the baking box, be cut into suitable big or small diaphragm, packing.
Preparation method 2 with more than the 85% soak with ethanol 24h, is filtered the PVA of commercially available commercial size, press dry, and soaks 1 time again, and filter is done.Get the PVA that handled and add an amount of distilled water, place and make its abundant swelling a night, put in 100 ℃ the water-bath heated and stirred and filter standby to fully dissolving; Be equipped with PVA rubber cement liquid with legal system, glycerol adding 1ml stirs, and adds water to capacity, puts in the water-bath about 50 ℃ and is incubated 10～20min, and it is standby to remove bubble.In addition glucosamine is dissolved in an amount of distilled water, cleum jecoris piscis concentratum is dissolved in the glycerol, merge behind two liquid slowly in the impouring PVA rubber cement liquid, the limit edged stirs and add water to capacity and blank PVA rubber cement liquid is removed bubble with method.This rubber cement liquid is applied on the glass plate of sterilizing equably, and the about 0.3mm of rete puts in the drying baker below 60 ℃ after the drying, be coated with on film with pastille PVA rubber cement liquid not, thick about 0.2mm is with the dry rear demoulding of method again, with the ultra violet lamp 1h that sterilizes, draw the lattice area as required, packing is promptly.
The preparation of paste:
(1) earlier ethyl hydroxybenzoate is dissolved in an amount of hot distilled water, (2) PVA-124 adds in an amount of hot distilled water, stirs evenly, and puts and heats peptization in the water-bath.(3) MC expands with an amount of cold distilled water and dissolves.(4) glucosamine stirs evenly in the adding glycerol with a small amount of 95% dissolve with ethanol.(5) starch adds in an amount of distilled water, and the heating in water bath gelatinizing stirs evenly (2) adding while hot, and cold slightly back adds (3), (4) stir evenly, and adding distil water stirs evenly to full dose, and packing promptly.
Compositions of the present invention, its prescription obtains through screening, the present invention has adopted different prescriptions to compare screening, having found out most preferred prescription is prescription of the present invention, the prescription of the existing preparation of this recipe ratio have many advantages good as: mouthfeel, do not stimulate, rapid-action, consumption is few, safety non-toxic easy to use.
Pharmaceutical composition of the present invention is determined usage and dosage according to patient's situation in use.
Below by test data beneficial effect of the present invention is described:
The experimentation of glucosamine being carried out the anti-experimental character oral ulcer is as follows.
Materials and methods
The material animal: 40 of SD rats, female, body weight 180～220g.Medicine and reagent: the suspension that glucosamine is made into, BINGPENG SAN,
Experimental technique
Set up experimental oral ulcer model, get 40 of SD rats, with bottom diameter is the glass tubing of 2mm, built-in cotton pellet, make cotton pellet bottom and glass end opening flat, then in pipe, splash into 90% carbolic acid solution to just soaking into till the cotton pellet, be placed on then on the inboard cheek mucosa of rat oral cavity lower lip and burn 45s, the local oral ulcer that forms behind the 24h.
Treatment to experimental oral ulcer rat is divided into suspension basic, normal, high dosage group, the positive and the model control group that glucosamine is made into observation at random with the modeling rat.To basic, normal, high dosage, be respectively 1g, 5g, 10g.The medicinal BINGPENG SAN of positive control, dosage are 0.25g/.Each is administration after organizing modeling, and observe the recovery situation of rat ulcer face every day after the administration, gets blood behind the eyeball behind the administration 3d, splashes into the anticoagulant heparin pipe of oven dry, is used for numeration of leukocyte.Behind the successive administration 12 days, put to death rat, take by weighing its body weight, spleen and heavily reach thymus heavily, calculate spleen and thymus index.
The result: the suspension that glucosamine is made into to oral cavity ulcer rat ordinary circumstance and oral ulcer healing natural law influence the modeling success after, each organizes the activity of rat and food-intake all than before reducing to some extent.Observed 5 days continuously after the administration, compared tangible recovery before the activity of the suspension administration group that glucosamine is made into and food-intake and the administration, and the recovery situation of model group rat is obviously not as good as the administration group.After administration the 8th day, all have the ulcer healing animal to occur in each administration group, and the model group rat there was the healing animal to occur in the 11st day beginning.
Glucosamine hydrochloride is to the therapeutic effect of 9 subject oral cavity ulcer:
Subjects: the experimenter is totally 9 people, male 4 people wherein, and women 5 people all suffer from a place and above oral ulcer.
Test medication: glucosamine hydrochloride powder
Test method: after the patient gargled, 0.2g was applied to ulcer surface, every day 3-5 time with the glucosamine hydrochloride powder.3 days observation periods.
Evaluation criterion:
Effectively: ulcer heals fully
Produce effects: treatment back congestion and swelling pain alleviates, and ulcer surface dwindles
Invalid: treatment back congestion and swelling pain alleviates, and ulcer surface does not dwindle
Result of the test:
All ulcer all effectively (9 people, 13 place's ulcer) in 3 days belong to healing fully, and healing rate reaches 100%.
The present invention aims at oral ulcer patient design according to modern pharmaceutical technology.According to following advantage is arranged: mouthfeel is good, do not stimulate, rapid-action, consumption is few, safety non-toxic easy to use, the drug-induced drug resistance of antibiotic-free class, do not contain hormone, no hormonelike side effect, use pad pasting of the present invention, can not only make the ulcer surface healing, reduce recurrence, and can effectively prevent gingival swelling and pain, angular cheilitis, pharyngitis, toothache etc.In a single day above-mentioned disease is produced, use effectively mitigation symptoms of product of the present invention.
Compositions of the present invention is effective to oral diseases such as various oral ulcer such as red aphtha, whitish aphthae and laryngopharynx swelling and pain, with a little sprinkling of this medicine or be coated on the affected part, can fully recover in 1-3 days, thereby solve the difficult problem that oral ulcer disease for a long time is difficult to cure.
The specific embodiment:
The invention will be further described by following specific embodiment, but not as limitation of the present invention.
Embodiment 1, buccal tablet
Glucosamine hydrochloride 100g, carboxymethyl cellulose 20g, steviol glycosides 50g, micropowder silica gel 10g.Get above supplementary material, mix, granulate, tabletting is made 1000 tablets of tablets.
Embodiment 2, paste
(1) earlier ethyl hydroxybenzoate is dissolved in an amount of hot distilled water, (2) PVA-124 adds in an amount of hot distilled water, stirs evenly, and puts and heats peptization in the water-bath.(3) MC expands with an amount of cold distilled water and dissolves.(4) glucosamine sulfate stirs evenly in the adding glycerol with a small amount of 95% dissolve with ethanol.(5) starch adds in an amount of distilled water, and the heating in water bath gelatinizing stirs evenly (2) adding while hot, and cold slightly back adds (3), (4) stir evenly, and adding distil water stirs evenly to full dose, and packing promptly.
Claims (10)
1. the application of glucosamine in the medicine of preparation treatment oral ulcer.
2. according to the application of claim 1, it is characterized in that wherein said glucosamine comprises pharmaceutically acceptable salt forms such as its hydrochlorate, nitrate, sulfate, phosphate, hydrobromate, mesylate, citrate.
3. according to the application of claim 1, it is characterized in that wherein said glucosamine is glucosamine hydrochloride and glucosamine sulphate.
4. according to the application of claim 1, it is characterized in that the effective dose of wherein said glucosamine treatment oral ulcer is 0.01g～5g.
5. according to the application of claim 1, it is characterized in that wherein said medicine is to be the pharmaceutical composition of active constituents of medicine with the glucosamine, said composition can contain the medicine acceptable carrier as required.
6. according to the application of claim 1, it is characterized in that wherein said pharmaceutical composition can be any pharmaceutically useful dosage form.
7. according to the application of claim 1, it is characterized in that wherein said compositions is a buccal bioadhesive tablet, buccal tablet, collutory, paste, spray.
8. according to the application of claim 1, it is characterized in that wherein said compositions can be a liquid, suspendible, the form that the grade of dry powder is commonly used.
9. according to the application of claim 1, it is characterized in that, wherein said compositions mouthfeel is good, do not stimulate, rapid-action, consumption is few, safety non-toxic easy to use, the drug-induced drug resistance of antibiotic-free class, do not contain hormone, no hormonelike side effect.
10. according to the application of claim 1, it is characterized in that, wherein said compositions is effective to oral diseases such as various oral ulcer such as red aphtha, whitish aphthae and laryngopharynx swelling and pain, it can not only be the ulcer surface healing, reduce recurrence, and can effectively prevent gingival swelling and pain, angular cheilitis, pharyngitis, toothache etc.
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| CN201010601958.8A CN102058608B (en) | 2010-12-17 | 2010-12-17 | New application of glucosamine in treating dental ulcer |
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| CN201010601958.8A CN102058608B (en) | 2010-12-17 | 2010-12-17 | New application of glucosamine in treating dental ulcer |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102600110A (en) * | 2012-03-09 | 2012-07-25 | 阮克锋 | Glucosamine cataplasm, preparation method thereof and application |
| RU2542469C1 (en) * | 2014-02-25 | 2015-02-20 | Сергей Владимирович Сирак | Agent for local therapy of recurrent oral aphthae accompanying dental stomatitis and periodontitis |
| CN112385838A (en) * | 2019-10-16 | 2021-02-23 | 富诺健康股份有限公司 | Food containing anthocyanin and preparation method thereof |
| CN114191405A (en) * | 2021-11-06 | 2022-03-18 | 山东润德生物科技有限公司 | Preparation method and application of gel type glucosamine preparation |
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| CN1470244A (en) * | 2002-07-22 | 2004-01-28 | 中国人民解放军第三军医大学 | Use of N-acetyl-D-aminoglucose in preparation of skin membrane mucosa microecologica balance regulator medicines |
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| CN1470244A (en) * | 2002-07-22 | 2004-01-28 | 中国人民解放军第三军医大学 | Use of N-acetyl-D-aminoglucose in preparation of skin membrane mucosa microecologica balance regulator medicines |
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| 杨艳等: "氨基葡萄糖抗炎功能的研究", 《华东六省一市生物化学与分子生物学会2008年学术交流会议论文摘要汇编》 * |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102600110A (en) * | 2012-03-09 | 2012-07-25 | 阮克锋 | Glucosamine cataplasm, preparation method thereof and application |
| RU2542469C1 (en) * | 2014-02-25 | 2015-02-20 | Сергей Владимирович Сирак | Agent for local therapy of recurrent oral aphthae accompanying dental stomatitis and periodontitis |
| CN112385838A (en) * | 2019-10-16 | 2021-02-23 | 富诺健康股份有限公司 | Food containing anthocyanin and preparation method thereof |
| CN112385838B (en) * | 2019-10-16 | 2022-11-08 | 富诺健康股份有限公司 | Food containing anthocyanin and preparation method thereof |
| CN114191405A (en) * | 2021-11-06 | 2022-03-18 | 山东润德生物科技有限公司 | Preparation method and application of gel type glucosamine preparation |
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| CN102058608B (en) | 2014-12-17 |
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