CN103169653A - Biphenylacetic acid and novel use of biphenylacetate - Google Patents
Biphenylacetic acid and novel use of biphenylacetate Download PDFInfo
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- CN103169653A CN103169653A CN2013100815760A CN201310081576A CN103169653A CN 103169653 A CN103169653 A CN 103169653A CN 2013100815760 A CN2013100815760 A CN 2013100815760A CN 201310081576 A CN201310081576 A CN 201310081576A CN 103169653 A CN103169653 A CN 103169653A
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- gargarism
- biphenylacetate
- butantriol salt
- biphenylacetic acid
- carbomer
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Abstract
The invention discloses biphenylacetic acid and a novel use of biphenylacetate. The invention discloses gargle with a bio-adhesion effect. The gargle includes biphenylacetic acid and/or ammonium biphenylacetate butantriol salt, polyvinylpyrrolidone and carbomer. According to the test, the gargle has better tolerance and is capable of forming a biological membrane containing biphenylacetic acid and/or ammonium biphenylacetate butantriol salt on the surface of oral mucosa, so that the local acting time of the medicine is prolonged and the oral inflammation can be restrained.
Description
Technical field:
The present invention relates to new purposes of a kind of felbinac and salt thereof and preparation method thereof.
Background technology:
My company applied for a patent a kind of biphenyl ammonia acetate butantriol salt and preparation method thereof in 2007, disclosed the preparation method of biphenyl ammonia acetate butantriol salt and the preparation method of injection, and disclosed the application of injection for ease pain.
Gingivitis refer to occur in gingiva tissue Acute and chronic inflammation.Gingiva (gingiva) refer to be covered in alveolar process surface and neck section on every side oral mucous epithelia and the connective tissue of below
[1]Dental plaque is the initiation factor of gingivitis, and the gingivitis common manifestation is gingival hemorrhage, redness, and distending pain might cause periodontitis to Deep Development.
Present Therapeutic Method: (1) antibiotic: the general disease causer, should be take the treatment general disease as main.Acute inflammation stage can be selected spiramycin 0.2 gram, every day 3～4 times, metronidazole 0.4 gram, every day 3 times: cefazolin 0.25 gram, every day 3～4 times: the intramuscular injection of penicillin 800,000 units, every day 2 times.(2) remove bacterial plaque, the tartar that is attached to Tooth surface, the smooth minimizing of facing is stimulated, rescue food impaction.(3) suitably use vitamin c, vitamin A and D, to improve human body resistance and repair ability, help the reparation of periodontal tissue.(4) the various chronic diseases of active treatment.(5) local application: can use after removing tartar, bacterial plaque and food debris.Coating 1% iodine glycerol after hydrogenperoxide steam generator with 3% or normal saline flushing, also available 1: 5000 potassium permanganate solution or Dobell's solution are gargled, the alternative rinsing the mouth medicine that uses also, gargarism as safe in mouth, refined scholar's collutorium etc.
If can there be a kind of anti-inflammatory agent can play a role in the part, the side effect that just can avoid the whole body administration and bring, yet can bring into play drug effect in the part, and has a toleration preferably, the one, depend on medicine itself, at first medicine itself can just can be brought into play antiphlogistic effects without internal metabolism, and the 2nd, depend on concentration and the action time of medicine, the 3rd, the technical study situation of medicine and prescription.
Summary of the invention:
the invention discloses a kind of gargarism that contains felbinac or biphenyl ammonia acetate butantriol salt, can act on oral cavity partial, has toleration preferably, it is that solution mucosal sites in the oral cavity by certain viscosity forms one deck biomembrane, contain a certain amount of biphenyl ammonia acetate butantriol salt in biomembrane, this layer biomembrane can extend solution and rest on the intraoral time, this is for inner performance drug effect is very important in the oral cavity, I have selected polyvinylpyrrolidone at company's research worker in repeatedly groping, carbomer, glycerol equal solvent and adjuvant have formed the prescription in the invention, has toleration preferably through the test table name, there is no the mucous membrane irritation reaction in oral cavity, and can suppress the oral inflammation reaction.
As everyone knows, gargarism generally needs to satisfy following feature: 1, the stability in medicine and adjuvant, solvent contact process.2, the local irritation of solution, the namely problem of resistance of gargarism.3, medicine is in the time of staying of part, and this has determined whether can effectively bring into play its drug action.
The present invention solves above key issue through a large amount of test, and by verification experimental verification drug effect and irritating safety issue.
We observe simultaneously felbinac and or the concentration range of biphenyl ammonia acetate butantriol salt can be set to the scope of 0.01-2% (w/w).The prescription of this gargarism contains aromatic, sweeting agent and antiseptic.
Sweeting agent can be: sucrose, xylitol, fructose, sorbitol, mannitol, aspartame, sucralose
Antiseptic can be: ethyl benzoate, benzoic acid, sorbic acid, hibitane, benzalkonium chloride.
The bioadhesive polymer of pivotal role can be selected polycarbophil and carbomer.
Specific embodiment:
Gargarism prescription and the preparation of embodiment 1:100ml
| Composition | Quantity |
| Biphenyl ammonia acetate butantriol salt | 0.08g |
| Natrium carbonicum calcinatum 0.1mol/L% | Regulate pH to 7.0-7.5 |
| Carbomer | 0.225g |
| PVP K90 | 1.500g |
| Xylitol | 15.000g |
| Sucralose | 0.150g |
| Sodium ethylene diamine tetracetate | 0.025g |
| Sodium benzoate | 0.500g |
| Glycerol | 5.000g |
| Propylene glycol | 5.000g |
[0015]?
| Mint Essence | 0.150g |
| Pure water | Add to to100ml |
Preparation method: xylitol, glycerol, propylene glycol, sucralose, tetrasodium ethylenediamine tetraacetate, sodium benzoate, carbomer are dissolved in 2/3 pure water.Mint Essence and biphenyl ammonia acetate butantriol salt join in the 20ml pure water, regulate PH to 7-8 with the natrium carbonicum calcinatum of 0.1mol, and stir to clarify.Mix above-mentioned two kinds of solution, add pure water to 100ml, and stir.
Embodiment 2: write out a prescription as follows, preparation method is with embodiment 1.
| Composition | Quantity |
| Biphenyl ammonia acetate butantriol salt | 0.1g |
| Natrium carbonicum calcinatum 0.1mol/L% | Regulate pH to 7.0-7.5 |
| Carbomer | 0.225g |
| PVP K90 | 1.500g |
| Xylitol | 15.000g |
| Sucralose | 0.150g |
| Sodium ethylene diamine tetracetate | 0.025g |
| Sodium benzoate | 0.500g |
| Glycerol | 5.000g |
| Propylene glycol | 5.000g |
| Mint Essence | 0.050g |
| Pure water | Add to to100ml |
Embodiment 3: write out a prescription as follows, preparation method is with embodiment 1.
| Composition | Quantity |
| Biphenyl ammonia acetate butantriol salt | 0.3g |
| Natrium carbonicum calcinatum 0.1mol/L% | Regulate pH to 7.0-7.5 |
| Carbomer | 0.225g |
| PVP K90 | 1.500g |
| Aspartame | 0.500g |
| Sodium ethylene diamine tetracetate | 0.025g |
| Sodium benzoate | 0.500g |
| Glycerol | 5.000g |
| Propylene glycol | 5.000g |
| Mint Essence | 0.050g |
| Pure water | Add to to100ml |
Embodiment 4: write out a prescription as follows, preparation method is with embodiment 1.
| Composition | Quantity |
| Biphenyl ammonia acetate butantriol salt | 0.05g |
| Natrium carbonicum calcinatum 0.1mol/L% | Regulate pH to 7.0-7.5 |
| Polycarbophil | 0.225g |
| PVP K90 | 1.500g |
| Aspartame | 0.500g |
| Sodium ethylene diamine tetracetate | 0.025g |
| Sodium benzoate | 0.500g |
| Glycerol | 5.000g |
| Propylene glycol | 5.000g |
[0023]?
| Radix Glycyrrhizae extract | 0.10g |
| Pure water | Add to to100ml |
Embodiment 5 prescriptions are as follows, and preparation method is with embodiment 1.
| Composition | Quantity |
| Felbinac | 0.1g |
| Trometamol | 0.06g |
| Carbomer | 0.225g |
| PVP K90 | 1.500g |
| Xylitol | 15.000g |
| Sucralose | 0.150g |
| Sodium ethylene diamine tetracetate | 0.025g |
| Sodium benzoate | 0.500g |
| Glycerol | 5.000g |
| Propylene glycol | 5.000g |
| Mint Essence | 0.050g |
| Natrium carbonicum calcinatum 0.1mol/L% | Regulate pH to 7.0-7.5 |
| Pure water | Add to to100ml |
The oral stimulation test of embodiment 6 biphenyl ammonia acetate butantriol salt gargarism
Tested medicine: the gargarism of A embodiment 1
B: blank sample (solution that does not contain biphenyl ammonia acetate butantriol salt)
C: positive control sample (PH is 2 acetum)
Animal: select the healthy Golden Hamster of 60-70 days
Test method and result:
Golden Hamster oral mucosa irritant test:
Get 10 of healthy Golden Hamster, be divided at random 2 groups, wherein on the left of a treated animal, mucosa is placed the A medicine, and another group is inserted the C medicine, and B contrast liquid is all placed on the right side of two treated animals.
Method is for the pentobarbital sodium anesthetized animal of 50g/L, upset left side cheek pouch and with after normal saline flushing, and the cotton balls that diameter 5mm is soaked with medicinal liquid is put into its central buccal mucosa utmost point lower.
As a child observed animal respectively at 1,4,6,8 and have or not systemic adverse reactions, and the local oral mucosa that contacts with tested medicinal liquid has or not color and luster abnormal, congested, rotten to the corn and the abnormal phenomena such as ooze out.
Put to death animal after 8 hours, get with medicinal liquid contact site buccal mucosa and around connective tissue, do histopathologic examination after conventional fixing, section, HE dyeing, observe the histiocytic reaction of mucosa part.
Result: after 1 hour and 4 hours, cotton balls is in place all right, and all animal subjects are without systemic adverse reactions, after 6 hours, only 1 A liquid sample, 1 C liquid sample and 1 B liquid sample come off (came off 8 hours around, and do not affect experimental result), and all the other are in place all right.The mucosa that contacts with the positive control material after 8 hours shows slightly coarse, and redness is arranged, and that the buccal mucosa that contacts with the embodiment of the present invention has no is coarse, redness and ulcer reaction.The buccal mucosa that contacts with B liquid is no abnormality seen also.
Histological observation as seen, pathological change, the visible edema of lamina propria, vasodilation, hyperemia and the kitchen range chronic inflammation cellular infiltrations such as the visible edema of mucous epithelium, abscess, erosion and chronic inflammation cellular infiltration that contact with C liquid (positive control solution).The all animals mucous epithelium that contacts with A liquid of the present invention is complete, and the slight dilatation and congestion of blood vessel in 1 mucous membrane of animal lamina propria is only arranged.The all animals mucosa no abnormality seen that contacts with B liquid.
The gargarism of other embodiment preparations has similar result with above-mentioned experiment.
Result: the gargarism that contains biphenyl ammonia acetate butantriol salt of the present invention, the Golden Hamster oral mucosa is all had no stimulation, show that reform the sanction side's gargarism has outstanding characteristics and progressive.
The application of embodiment 6 in the reaction for the treatment of oral inflammation
Patient's 50 examples, male's 30 examples, women's 20 examples, year makes 18-48 year, and on inspection, patient's symptom is that simple red swelling of gingiva, kermesinus, gingival sulcus are deepened, gingival sulcus pyorrhea, the rotten to the corn and gingiva severe haemorrhage of gum edge, gingiva congestion and edema.All cases is without the odontoseisis person.Medical front all without taking any antibiotic medicine.
Therapeutic scheme: use the gargarism of embodiment 1 preparation to treat, use 20ml to gargle at every turn, be no less than 45 seconds every day 3 times at every turn, used continuously for 1 week.
Criterion of therapeutical effect:
Produce effects: after medication 1-3 days, gingival hemorrhage stops, and the gingiva congestion and edema disappears substantially, and halitosis disappears.
Effectively: after medication 3-7 days, gingival hemorrhage stops, and redness disappears substantially, and halitosis obviously alleviates or disappears.
Invalid: medication after 7 days symptom without obvious improvement.
Therapeutic outcome: after using continuously for 1 week, 50 routine patients, produce effects 48 examples 100%.
Untoward reaction: do not find untoward reaction in therapeutic process.
Claims (6)
1. one kind contains oral cavity gargle, it is characterized in that containing felbinac and/or biphenyl ammonia acetate butantriol salt.
2. gargarism as claimed in claim 1, except containing felbinac and/or biphenyl ammonia acetate butantriol salt, also contain the polyvinylpyrrolidone and carbomer and the polycarbophil that play the bioadhesion effect.
3. gargarism as claimed in claim 1 contains felbinac and/or the biphenyl ammonia acetate butantriol salt of 0.01%-3%.
4. gargarism as described in claim 1-3, the concentration of polyvinylpyrrolidone is 1%-10%.
5. gargarism as described in claim 1-4, the concentration of polycarbophil or carbomer is 0.1-2%.
6. the application of gargarism as claimed in claim 1 in preparation treatment oral inflammation reaction medicine.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013100815760A CN103169653A (en) | 2013-03-13 | 2013-03-13 | Biphenylacetic acid and novel use of biphenylacetate |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013100815760A CN103169653A (en) | 2013-03-13 | 2013-03-13 | Biphenylacetic acid and novel use of biphenylacetate |
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| CN103169653A true CN103169653A (en) | 2013-06-26 |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1944378A (en) * | 2006-10-23 | 2007-04-11 | 广东中科药物研究有限公司 | Biphenyl ammonia acetate butantriol salt and its preparing method |
| CN101396370A (en) * | 2007-09-27 | 2009-04-01 | 北京天川军威医药技术开发有限公司 | Medicine composition for treating mouth, throat disease and preparation method thereof |
-
2013
- 2013-03-13 CN CN2013100815760A patent/CN103169653A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1944378A (en) * | 2006-10-23 | 2007-04-11 | 广东中科药物研究有限公司 | Biphenyl ammonia acetate butantriol salt and its preparing method |
| CN101396370A (en) * | 2007-09-27 | 2009-04-01 | 北京天川军威医药技术开发有限公司 | Medicine composition for treating mouth, throat disease and preparation method thereof |
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Application publication date: 20130626 |