CN106727320A - A kind of composition for repairing schneiderian membrane, reducing allergic reaction, antiinflammatory action - Google Patents
A kind of composition for repairing schneiderian membrane, reducing allergic reaction, antiinflammatory action Download PDFInfo
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Abstract
Prepared for treating the application in repairing schneiderian membrane and reducing anaphylactoid medicine or medical product the invention provides the composition containing α ketone acids.The present invention can effectively remove pollutant in nasal cavity, alien bacteria, virus, anaphylactogen, pollen, various dust and deleterious particle, it is to avoid or reduce accumulation of the virulence factor on people's upper respiratory tract.And security that the present invention has is very high, long-term use does not exist risk yet, and extensively using being conducive to improving, nasal cavity is disease-resistant and antiallergy ability, while the incidence of disease of the various infectious respiratory diseases such as flu, rhinitis, nasosinusitis and nasopharyngitis can be reduced.
Description
Technical field
The present invention relates to a kind of composition for repairing schneiderian membrane, reducing allergic reaction, antiinflammatory action, belong to medical use
Product technical field.
Background technology
Breathing is sustain life basic, and breathing is completed jointly by the upper respiratory tract and lower respiratory tract, nasal cavity, nasal sinus and nasopharynx
The chief component of the upper respiratory tract, be human body with the Nature carry out mass exchange must be through part.Sodium Pyruvate be people and
All of normal composition in animal body, is biological analytic metabolism, and Sodium Pyruvate has significant to many cells and multiple organ work(
Energy protective effect, particularly to vitals：The ischemia/reperfusion injury reparation of heart, liver, brain and kidney, and nontoxic pair
Effect, while Sodium Pyruvate is antioxidant, has preferably effect for suppressing inflammation.
People have a selection to the drinking water needed for daily, but air to needing is difficult selection, the particularly powder in air
Pathogenic pollution sources of dirt, virus, bacterium and mould etc., without selection, are frequently accompanied by breathing and propagate and infected, considerably increase urgency
Rhinitis chronic, allergic rhinitis, flu, the incidence of breathing problem cause very big injury to nasal membrane.To some
Be susceptible to suffer from rhinitis and nasosinusitis, easily catch a cold or with flu patient often in contact with crowd and work under poor environment it is special
Work post professional population progressively mitigates or finally diminishes inflammation, it is necessary to often carry out nursing reparation to nasal cavity.
The principle of all of nasal mist nursing nasal cavity is to remove nasal foreign body by cleaning nasal cavity in the market,
It is damaged for schneiderian membrane and does not play repair.
The content of the invention
The purpose of the present invention is to overcome the deficiencies in the prior art part, there is provided one kind is for repairing schneiderian membrane, reducing allergy
Reaction, the composition of antiinflammatory action.
Technical scheme is as follows：
A kind of composition for repairing schneiderian membrane, reducing allergic reaction, antiinflammatory action, the activity in described composition
Composition is 2-ketoacid molecule pair, and described composition also includes osmotic pressure regulator, and described 2-ketoacid molecule is to selected from acetone
Two or more in acid and its salt or ester.
Described 2-ketoacid molecule is to being acetonate-ethyl pyruvate；Described acetonate and ethyl pyruvate
Mass ratio is 3-20:1.
Described acetonate is 10-15 with the mass ratio of ethyl pyruvate:1.
Described acetonate is 12 with the mass ratio of ethyl pyruvate:1.
Described composition also includes one or more in freshener, pH adjusting agent and bacteriostatic agent.
Described osmotic pressure regulator is from sodium chloride, glucose, mannitol, potassium chloride or phosphate；
Described freshener is selected from Novamint Peppermint, menthol, eucalyptus oil, camphor, WS-23, WS-3
One or more.
Described pH adjusting agent is selected from citric acid, sodium citrate, hydrochloric acid, NaOH, potassium hydroxide or phosphate, and pH is adjusted
Section agent adjusts pH value to pH=4-8；
Described bacteriostatic agent is selected from benzalkonium chloride, benzalkonium bromide, poly hexamethylene biguanide or ethylparaben.
Described composition includes following component according to parts by weight：2-ketoacid molecule is adjusted to 5.5-50 parts, osmotic pressure
Agent 10-100 parts, bacteriostatic agent 1-50 parts, pH adjusting agent adjusts pH value to pH=4-7.
Described composition includes following component according to parts by weight：2-ketoacid molecule is adjusted to 5.5-22 parts, osmotic pressure
Agent 15-45 parts, bacteriostatic agent 1-50 parts, pH adjusting agent adjusts pH value to pH=4-7, and described osmotic pressure regulator is from sodium chloride；
Described bacteriostatic agent is selected from benzalkonium chloride or poly hexamethylene biguanide.
Described composition includes following component according to parts by weight：2-ketoacid molecule is pricked to 22 parts, 45 parts of sodium chloride, benzene
1 part or 3 parts of oronain, pH adjusting agent adjusts pH value to pH=4-7.
Described composition includes following component according to parts by weight：2-ketoacid molecule to 22 parts, 45 parts of sodium chloride, poly- six
50 parts of methylene biguanides, pH adjusting agent adjusts pH value to pH=4-7, water surplus.
Described composition includes according to percetage by weight：2-ketoacid molecule is adjusted to 0.055%-0.5%w/w, osmotic pressure
Section agent 0.1%-1%w/w, bacteriostatic agent 0.01%-0.5%w/w, pH adjusting agent adjusts pH value to pH=4-7, water surplus.
Described composition includes according to percetage by weight：2-ketoacid molecule is adjusted to 0.055%-0.22%w/w, osmotic pressure
Section agent 0.15%-0.45%w/w, bacteriostatic agent 0.01%-0.5%w/w, pH adjusting agent adjusts pH value to pH=4-7, water surplus.
Described composition includes according to percetage by weight：2-ketoacid molecule to 0.22%w/w, sodium chloride 0.45%w/w,
Benzalkonium chloride 0.01% or 0.03%w/w, pH adjusting agent adjust pH value to pH=4-7.
Described composition includes according to percetage by weight：2-ketoacid molecule to 0.22%w/w, sodium chloride 0.45%w/w,
Poly hexamethylene biguanide 0.5%w/w, pH adjusting agent adjusts pH value to pH=4-7, water surplus.
In the present invention, 2-ketoacid molecule represents acetonate with ethyl pyruvate to " acetonate-ethyl pyruvate "
Mixture.
The present invention is different with CN201210052155.0, and the present invention is to use osmotic pressure regulator and 2-ketoacid molecule pair
System based on cushioning liquid, its concentration and acid-base value are close with human body fluid, have biocompatibility with nasal cavity tissue.Infiltration
To after schneiderian membrane, while schneiderian membrane SPA nourishings are given, can rapid-digestion mycteroxerosis situation, the life of holding nasal cavity moistening
Reason environment, recovers and promotes the normal swing of nose cilium, safeguards the normal physiological function of nasal cavity.Oxygen radical (ROS) is considered as
It is a kind of Second messenger in cell, participates in posttranslational modification, and adjustable oxidation-sensitive transcription factor NF-KB, and oxidant can shadow
Ring the activity of various kinases in NF-KB paths.Therefore, the present invention using antioxidant 2-ketoacid molecule to suppressing NF-KB's
Produce or its BA is beneficial to diseases such as limitation inflammation.The bacteriostatic agent that the other present invention contains, effectively suppresses bacterium pair
The attachment of respiratory epithelium cell, keeps the activity of the lysozyme of mucous secretion, suppresses and dissolve pathogenic microorganism, and promote white
The phagocytosis function of cell, plays a part of to clear up inflammation, mitigates interstitial edema, reduces infection.
We use and are with 2-ketoacid molecule pair and osmotic pressure regulator in the research to 2-ketoacid molecule to nasal spray
Main solution system, its technique effect following points：
1st, 2-ketoacid molecule can suppress the inflammation of the signal transduction pathway with NF-KB as core to being a kind of antioxidant
Disease, so as to play antiinflammatory action.
2nd, 2-ketoacid molecule is compared to nasal spray solution (pH6) with other buffer solutions (such as phosphate), to the thorn of nasal cavity
Sharp effect is smaller, therefore in all buffer solutions, it is preferably selection.
3rd, acetonate is intrinsic benefit materials in human body, safe, do not have any side-effects；It is existing multiple dynamic
Thing experiment demonstrates the security of acetonate；Acetonate be widely used in fitness and weight losing dietary supplements, cosmetics,
Biological medium, the detection of children's mitochondria, cell culture, stem cell and internal organ are preserved, and are also used to do skin and eye in America and Europe
The buffer solution of eyeball nursing product.
4th, the research in terms of consciousness also shows that acetonate can strengthen the smooth sense of nasal cavity, when reducing flushing liquor nasal irrigation
The tingling sensation of generation.
5th, the effect of pH adjusting agent is extremely important, pH6 closer to the isoelectric point of glycoprotein in mucus pH value, this pH's
Solution can preferably help decompose mucus, moreover it is possible to reduce mucosa edema, alleviate nasal obstruction.
6th, the pH (acid-base value) of snotter can influence solution bacterium enzyme effect and ciliary movement, and normal nasal secretion pH value is inclined
In acidity, and various nasal diseases such as acute rhinitis, allergic rhinitis, atrophic rhinitis and nasal polyp etc., intranasal acid-base value is equal
Relatively alkalescence, nasal cavity is appeared again existing bacterium.The pollutant of some such as pathogenic bacteria enters nasal cavity and changes pH so that nasal cavity becomes not to be good for
Health, so that bacterial growth.PH is that 4~7 buffer solution can help the restorative pH environment of nasal cavity, nasal cavity is kept normal
Acid or alkali environment, more effectively suppresses harmful bacteria breeding.
The present invention treats liquid and makes pollutant, alien bacteria, virus, allergy that nasal spray can be removed effectively in nasal cavity
Original, pollen, various dust and deleterious particle, it is to avoid or reduce accumulation of the virulence factor on people's upper respiratory tract.And institute of the present invention
The security having is very high, and long-term use does not exist risk yet, and extensive use is conducive to raising nasal cavity disease-resistant and antiallergy energy
Power, while the incidence of disease of the various infectious respiratory diseases such as flu, rhinitis, nasosinusitis and nasopharyngitis can be reduced.
Brief description of the drawings
Fig. 1 is that nasal mist group is reduced to 2.4 in treatment effectively scoring in three weeks from 8.5, and nasal cavity sem observation is down to from 1.7
0.3, it is obvious to schneiderian membrane repairing effect.
Fig. 2 is that physiological saline group is reduced to 4.6 in treatment effectively scoring in three weeks from 7.8, and nasal cavity sem observation is down to from 1.7
1.2, it is general to schneiderian membrane repairing effect.
Fig. 3 is that nasal mist and physiology seawater compare in treatment effectively scoring in three weeks.
Fig. 4 is the comparing that nasal mist and physiology seawater use weekly rear symptom and conchoscope variable quantity, is shown in figure
Sodium Pyruvate nasal mist is repaired on schneiderian membrane than physiology seawater in treatment obvious superiority.
Specific embodiment
Embodiment 1
In the present embodiment, composition and content are as follows in composition：
| Name of material | Consumption (gram) |
| 2-ketoacid molecule pair | 22 |
| Sodium chloride | 45 |
| Benzalkonium chloride | 1 |
| The NaOH of 0.1mol/l | Adjust pH value to pH=6 |
| Purified water | It is settled to 10000 grams of full dose |
Preparation technology：
The 2-ketoacid molecule of the present embodiment to be Sodium Pyruvate and ethyl pyruvate mixture, Sodium Pyruvate and pyruvic acid
The mass ratio of ethyl ester is 3：1；
The 2-ketoacid molecule of recipe quantity is respectively added slowly in 9500 grams of purified waters to, sodium chloride, 40-50 DEG C is heated to
Dissolving is sufficiently stirred for, the 25-35 DEG C of benzalkonium chloride of addition recipe quantity is cooled to, stirred, with the NaOH of 0.1mol/l
Regulation pH value of solution=6, then 10000 grams of full dose is settled to remaining water, filter, it is filling to obtain final product.Said preparation Sodium Pyruvate contains
Amount 0.22%, is mainly used in schneiderian membrane reparation and nasal cavity anti-inflammatory.
Embodiment 2
In the present embodiment, composition and content are as follows in composition：
| Name of material | Consumption (gram) |
| 2-ketoacid molecule pair | 22 |
| Sodium chloride | 45 |
| Poly hexamethylene biguanide | 50 |
| The sodium citrate of 0.1mol/l | Adjust pH value to pH=6 |
| Purified water | It is settled to 10000 grams of full dose |
Preparation technology：
The 2-ketoacid molecule of the present embodiment to be Potassium pyruvate and ethyl pyruvate mixture, Sodium Pyruvate and pyruvic acid
The mass ratio of ethyl ester is 10：1；
The 2-ketoacid molecule of recipe quantity is respectively added slowly in 9500 grams of purified waters to, sodium chloride, 40-50 DEG C is heated to
Dissolving is sufficiently stirred for, the 25-35 DEG C of poly hexamethylene biguanide of addition recipe quantity is cooled to, stirred, with the Chinese holly of 0.1mol/l
Rafter acid sodium regulation pH value of solution=6, then 10000 grams of full dose is settled to remaining water, filter, it is filling to obtain final product.Said preparation pyruvic acid
The content 0.22% of sodium, is mainly used in schneiderian membrane reparation and nasal cavity anti-inflammatory.
Embodiment 3
In the present embodiment, composition and content are as follows in composition：
| Name of material | Consumption (gram) |
| 2-ketoacid molecule pair | 11 |
| Glucose | 30 |
| Benzalkonium chloride | 25 |
| The hydrochloric acid of 0.1mol/l | Adjust pH value to pH=4.5 |
| Purified water | It is settled to 10000 grams of full dose |
The 2-ketoacid molecule of the present embodiment to be Sodium Pyruvate and ethyl pyruvate mixture, Sodium Pyruvate and pyruvic acid
The mass ratio of ethyl ester is 12：1；
The 2-ketoacid molecule of recipe quantity is respectively added slowly in 9500 grams of purified waters to, glucose, 40-50 DEG C is heated to
Dissolving is sufficiently stirred for, 25-35 DEG C of addition benzalkonium chloride is cooled to, stirred, with the hydrochloric acid conditioning solution pH=of 0.1mol/l
4.5, then 10000 grams of full dose is settled to remaining water, filter, it is filling to obtain final product.The content 0.11% of said preparation Sodium Pyruvate, it is main
It is used for schneiderian membrane reparation and nasal cavity anti-inflammatory.
Embodiment 4
In the present embodiment, composition and content are as follows in composition：
| Name of material | Consumption (gram) |
| 2-ketoacid molecule pair | 5.5 |
| Sodium chloride | 15 |
| Benzalkonium chloride | 1 |
| The NaOH of 0.1mol/l | Adjust pH value to pH=6.5 |
| Purified water | It is settled to 10000 grams of full dose |
The 2-ketoacid molecule of the present embodiment to be Potassium pyruvate and ethyl pyruvate mixture, Sodium Pyruvate and pyruvic acid
The mass ratio of ethyl ester is 15：1；
The 2-ketoacid molecule of recipe quantity is respectively added slowly in 9500 grams of purified waters to, sodium chloride, 40-50 DEG C is heated to
Dissolving is sufficiently stirred for, 25-35 DEG C of addition benzalkonium chloride is cooled to, stirred, with the sodium hydrate regulator solution of 0.1mol/l
PH=6.5, then 10000 grams of full dose is settled to remaining water, filter, it is filling to obtain final product.The content of said preparation Sodium Pyruvate
0.055%, it is mainly used in schneiderian membrane reparation and nasal cavity anti-inflammatory.
Embodiment 5
In the present embodiment, composition and content are as follows in composition：
The 2-ketoacid molecule of the present embodiment to be Sodium Pyruvate and ethyl pyruvate mixture, Sodium Pyruvate and pyruvic acid
The mass ratio of ethyl ester is 20：1；
The 2-ketoacid molecule of recipe quantity is respectively added slowly in 9500 grams of purified waters to, sodium chloride, 40-50 DEG C is heated to
Dissolving is sufficiently stirred for, the 25-35 DEG C of benzalkonium chloride of addition recipe quantity is cooled to, stirred, with the NaOH of 0.1mol/l
Regulation pH value of solution=7.0, then 10000 grams of full dose is settled to remaining water, filter, it is filling to obtain final product.Said preparation 2-ketoacid molecule
To content 0.11%, be mainly used in schneiderian membrane reparation and nasal cavity anti-inflammatory.
Embodiment 6
In the present embodiment, composition and content are as follows in composition：
| Name of material | Consumption (gram) |
| 2-ketoacid molecule pair | 32 |
| Sodium chloride | 60 |
| Ethylparaben | 10 |
| The hydrochloric acid of 0.1mol/l | Adjust pH value to pH=4 |
| Purified water | It is settled to 10000 grams of full dose |
The 2-ketoacid molecule of the present embodiment to be Sodium Pyruvate and ethyl pyruvate mixture, Sodium Pyruvate and pyruvic acid
The mass ratio of ethyl ester is 8：1；
The 2-ketoacid molecule of recipe quantity is respectively added slowly in 9500 grams of purified waters to, sodium chloride, 40-50 DEG C is heated to
Dissolving is sufficiently stirred for, the 25-35 DEG C of ethylparaben of addition recipe quantity is cooled to, stirred, adjusted with the hydrochloric acid of 0.1mol/l
Section pH value of solution=4.0, then 10000 grams of full dose is settled to remaining water, filter, it is filling to obtain final product.Said preparation 2-ketoacid molecule pair
Content 0.32%, be mainly used in schneiderian membrane reparation and nasal cavity anti-inflammatory.
Embodiment 7
In the present embodiment, composition and content are as follows in composition：
Preparation technology：
The 2-ketoacid molecule of the present embodiment to be Potassium pyruvate and ethyl pyruvate mixture, Sodium Pyruvate and pyruvic acid
The mass ratio of ethyl ester is 6：1；
The 2-ketoacid molecule of recipe quantity is respectively added slowly in 9500 grams of purified waters to, sodium chloride, 40-50 DEG C is heated to
Dissolving is sufficiently stirred for, the 25-35 DEG C of benzalkonium chloride of addition recipe quantity is cooled to, stirred, adjusted with the citric acid of 0.1mol/l
Section pH value of solution=5.0, then 10000 grams of full dose is settled to remaining water, filter, it is filling to obtain final product.Said preparation 2-ketoacid molecule pair
Content 0.41%, be mainly used in schneiderian membrane reparation and nasal cavity anti-inflammatory.
Embodiment 8
In the present embodiment, composition and content are as follows in composition：
| Name of material | Consumption (gram) |
| 2-ketoacid molecule pair | 50 |
| Sodium chloride | 100 |
| Benzalkonium bromide | 50 |
| The hydrochloric acid of 0.1mol/l | Adjust pH value to pH=4.5 |
| Purified water | It is settled to 10000 grams of full dose |
Preparation technology：
The 2-ketoacid molecule of the present embodiment to be Sodium Pyruvate and ethyl pyruvate mixture, Sodium Pyruvate and pyruvic acid
The mass ratio of ethyl ester is 16：1；
The 2-ketoacid molecule of recipe quantity is respectively added slowly in 9500 grams of purified waters to, sodium chloride, 40-50 DEG C is heated to
Dissolving is sufficiently stirred for, the 25-35 DEG C of benzalkonium bromide of addition recipe quantity is cooled to, stirred, adjusted with the hydrochloric acid of 0.1mol/l
PH value of solution=4.5, then 10000 grams of full dose is settled to remaining water, filter, it is filling to obtain final product.Said preparation 2-ketoacid molecule pair
Content 0.5%, is mainly used in schneiderian membrane reparation and nasal cavity anti-inflammatory.
Embodiment 9
In the present embodiment, composition and content are as follows in composition：
| Name of material | Consumption (gram) |
| 2-ketoacid molecule pair | 22 |
| Potassium chloride | 45 |
| Benzalkonium chloride | 3 |
| The potassium hydroxide of 0.1mol/l | Adjust pH value to pH=5.5 |
| Purified water | It is settled to 10000 grams of full dose |
Preparation technology：
The 2-ketoacid molecule of the present embodiment to be Sodium Pyruvate and ethyl pyruvate mixture, Sodium Pyruvate and pyruvic acid
The mass ratio of ethyl ester is 18：1；
The 2-ketoacid molecule of recipe quantity is respectively added slowly in 9500 grams of purified waters to, potassium chloride, 40-50 DEG C is heated to
Dissolving is sufficiently stirred for, the 25-35 DEG C of benzalkonium chloride of addition recipe quantity is cooled to, stirred, with the potassium hydroxide of 0.1mol/l
Regulation pH value of solution=5.5, then 10000 grams of full dose is settled to remaining water, filter, it is filling to obtain final product.Said preparation Sodium Pyruvate
Content 0.22%, is mainly used in schneiderian membrane reparation and nasal cavity anti-inflammatory.
By preparing embodiment 1~9, it has been found that：(5.5~50 weight portion), osmotic pressure are adjusted using 2-ketoacid molecule
Section agent (10-100 weight portions), bacteriostatic agent (1-50 weight portions), wherein osmotic pressure regulator are from sodium chloride, potassium chloride or grape
Sugar；Bacteriostatic agent is selected from benzalkonium chloride, benzalkonium bromide, ethylparaben or poly hexamethylene biguanide, and pH value is controlled between 4~7,
Can well prepare suitable nasal spray.
Further preferably we have found that：Embodiment 1~4,9, bacteriostatic agent its consumption when effective fungistatic effect is reached
Smaller, toxicity is smaller, and bacteriostatic agent is controlled in 1-50 weight portions；Osmotic pressure regulator is controlled at (15-45 weight portions) with sodium chloride,
Mucosal tissue can not only be effectively protected, and liquid can be made to soak well and mucous membrane is infiltrated into；Sodium Pyruvate control exists
5.5-22 weight portions, stability and, modest viscosity smaller to the excitant of nasal cavity to liquid, not only effectively increase treatment liquid
Holdup time in nasal cavity, and be adapted to be used in the nasal cavity of people.PH value is controlled between 4~7, can be prepared well
Go out the nasal spray for meeting.
Still more preferably we have found that：Embodiment 1 and 9, sodium chloride is controlled in 45 weight portions, can be produced isotonic well
Effect, in 22 weight portions, stability and curative effect all reach best, and pH value is controlled between 4~7 for Sodium Pyruvate control.
Embodiment 10
Here is that the present invention investigates result to nasal membrane reparation and antiphlogistic effects.Specific method is：
Experiment packet：
1) model：Set up the animal model of allergic rhinitis.Experimental group rat uses ovalbumin 3ml/ of 0.1%,
Adding aluminum hydroxide adjuvant 30mg carries out basic sensitization, the next day 1 row intraperitoneal injection, totally 7 times, then one time a day, totally 7 times.With
2%OVA collunariums, 50 μ l/ sides, once a day, totally 7 times.
2) control group：
After the success of A models, physiological saline nasal spray water is used 3 times daily, each 1ml, totally 10 days.
After the success of B models, azelastine hydrochloride nasal spray is used 2 times daily, each 1ml, totally 10 days.
After C model success, fluticasone propionate nasal spray is used 2 times daily, each 1ml, totally 10 days.
3) experimental group：After model success, daily using molecule containing 2-ketoacid to nasal mist 3 times, each 1ml, totally 10
My god.Preparation method is as follows：
One group of preparation method of Sodium Pyruvate spray：
The 2-ketoacid molecule of recipe quantity is respectively added slowly in 9500 grams of purified waters to, sodium chloride, 40-50 DEG C is heated to
Dissolving is sufficiently stirred for, the 25-35 DEG C of poly hexamethylene biguanide of addition recipe quantity is cooled to, stirred, with the hydrogen of 0.1mol/l
Sodium oxide molybdena adjusts pH value of solution=6, then is settled to 10000 grams of full dose with remaining water, filters, filling to obtain final product.Said preparation 2-ketoacid
The content 0.5% of molecule pair, is mainly used in schneiderian membrane reparation and nasal cavity anti-inflammatory.
2-ketoacid molecule is to two groups and three groups same group of preparation methods of spray.
(1) observation index and scoring
Method, in reaction of animals is observed in after OVA collunariums 30 minutes, scored animal in experiment the 23rd day, scored
Method carries out scoring with reference to the method for Zhao Changqing etc. according to nose, sneeze, runny nose degree is grabbed
Total score is considered as more than 4 points and models successfully.
(2) nasal mucosal tissue is obtained
Skin before rat nasal bone is separated, is stung except nasal bone, take out bilateral nose breathing area mucous membrane, it is fixed in 4% paraformaldehyde,
FFPE, conventional section.
(3) schneiderian membrane HE dyeing Microscopic observation:
Rat Nasal Mucosa swelling degree, lumen of gland and thin vessels tube chamber, goblet cell change.It is small in mucous membrane and submucosa
Around blood vessel and body of gland, whether there is the infiltration of inflammatory cell.
(4) extraction of cell total rna
Histocyte is homogenized, and the PBS washings of 1ml precoolings are added in every hole, is repeated 3 times.In exhausting per hole after PBS, respectively
1ml Trizol are added, is placed on 4 DEG C of shaking tables, 5min is vibrated at a slow speed.Then by Trizol and the cell of cracking, Rnase- is transferred to
In the 1.5ml centrifuge tubes of free, and to addition 0.2ml chloroforms in every pipe.Lid is covered tightly, is fully mixed, be stored at room temperature 5min.Turn
Enter low temperature (4 DEG C) centrifuge, 13000rmp is centrifuged 15min.Draw 500 μ l upper phase solution and be transferred to new 1.5ml centrifuge tubes
In, isometric isopropanol is added, fully mix, after being placed in -20 DEG C of refrigerator 5min, low temperature 13000rmp is centrifuged 10min.Go
Supernatant, leaves and takes precipitation.Plus the ethanol (precooling) of the 75% of 1ml DEPC water preparation, vibration washing precipitate, low temperature 13000rmp,
Centrifugation 10min.Supernatant is removed, precipitation is left and taken, drying (about 5min) in superclean bench is placed in, RNA precipitate bleach (is noted
RNA precipitate can not be completely dried, and solubility can be greatly reduced after drying).30 μ l DEPC water dissolves are added in most backward often pipe
Precipitation, and the hydrotropy at 60-65 DEG C, collect sample after 7min, be placed on ice.The RNA of extraction uses NanoDrop detectable concentrations
Afterwards, it is immediately available for reverse transcription experiment.Design inflammatory factor IL and TNF, expression of the observation each group in rna level.
(5) extraction of total protein of cell
Histocyte is homogenized, and the PBS washings of 1ml precoolings are added in every hole, is repeated 3 times.It is then used by the PBS of 1ml precoolings
Cell is scraped, low temperature (4 DEG C) centrifuge is transferred to, 9000rpm is centrifuged 20sec.Supernatant is removed, albumen is contained to being added in cell precipitation
RIPA lysates (150mM NaCl, the 10mM Tris-HCl, 0.1%SDS, 1% of enzyme inhibitor Cocktail and PMSF
TritonX-100,1%Deoxycholate, 5mM EDTA), often pipe adds 150 μ l, and the suspension of precipitation group is got up, multigelation
3 times, refrigerated centrifuge is transferred to, 13000rpm is centrifuged 15min, collects supernatant in new centrifuge tube, determine dense with NanoDrop
Degree, then adds sample-loading buffer (6 × Sample buffer) in 100 DEG C of dry heating pot denaturation 7min.Be stored in -70 DEG C it is ultralow
In temperature refrigerator, or Western Blot detections are carried out immediately.Detection inflammatory factor TNF and inflammatory signals molecule NF-KB.
As a result：Inflammatory factor of the nasal mist group containing Sodium Pyruvate on rna level is significantly less than physiology seawater group.
Different groups to inflammatory factor IL-1 β and TNFαConcentration influence result
The different groups of influences to intervening NF-KB albumen
Result shown in different experiments group shows：Each group can detect NF-KB albumen, and wherein 2-ketoacid molecule sprays to nasal cavity
Mist agent group is slightly above azelastine hydrochloride nasal spray and fluticasone propionate spray, but there was no significant difference；Physiology seawater
Group is apparently higher than azelastine hydrochloride nasal spray and fluticasone propionate spray group, therefore 2-ketoacid molecule is to nasal spray
Agent as fluticasone propionate spray, has inhibitory action with azelastine hydrochloride nasal spray to NF-KB albumen, with anti-
Inflammatory effects.One of which is slightly above two groups and three groups, it can be seen that 2-ketoacid molecule is to the anti-inflammatory that is used alone compared with 2-ketoacid
Effect is better.
Claims (14)
1. it is a kind of for repair schneiderian membrane, reduce allergic reaction, antiinflammatory action composition, it is characterised in that described combination
Active component in thing is 2-ketoacid molecule pair, and described composition also includes osmotic pressure regulator, described 2-ketoacid molecule
To selected from two or more in pyruvic acid and its salt or ester.
2. composition according to claim 1, it is characterised in that described 2-ketoacid molecule is to being acetonate-acetone
Acetoacetic ester；Described acetonate is 3-20 with the mass ratio of ethyl pyruvate:1.
3. composition according to claim 2, it is characterised in that the mass ratio of described acetonate and ethyl pyruvate
It is 10-15:1.
4. composition according to claim 3, it is characterised in that the mass ratio of described acetonate and ethyl pyruvate
It is 12:1.
5. composition according to claim 1, it is characterised in that described composition also includes freshener, pH adjusting agent
With one or more in bacteriostatic agent.
6. composition according to claim 1 or 5, it is characterised in that
Described osmotic pressure regulator is from sodium chloride, glucose, mannitol, potassium chloride or phosphate；
Described freshener is selected from the one kind in Novamint Peppermint, menthol, eucalyptus oil, camphor, WS-23, WS-3
Or more than one.
Described pH adjusting agent is selected from citric acid, sodium citrate, hydrochloric acid, NaOH, potassium hydroxide or phosphate, pH adjusting agent
Adjust pH value to pH=4-8；
Described bacteriostatic agent is selected from benzalkonium chloride, benzalkonium bromide, poly hexamethylene biguanide or ethylparaben.
7. composition according to claim 1, it is characterised in that described composition includes such as the following group according to parts by weight
Point：2-ketoacid molecule to 5.5-50 parts, osmotic pressure regulator 10-100 parts, bacteriostatic agent 1-50 parts, pH adjusting agent adjust pH value to
PH=4-7.
8. composition according to claim 7, it is characterised in that described composition includes such as the following group according to parts by weight
Point：To 5.5-22 parts, osmotic pressure regulator 15-45 parts, bacteriostatic agent 1-50 parts, pH adjusting agent adjusts pH value to pH to 2-ketoacid molecule
=4-7, described osmotic pressure regulator is from sodium chloride；Described bacteriostatic agent is selected from benzalkonium chloride or poly hexamethylene biguanide.
9. composition according to claim 7, it is characterised in that described composition includes such as the following group according to parts by weight
Point：2-ketoacid molecule to 22 parts, 45 parts of sodium chloride, 1 part or 3 parts of benzalkonium chloride, pH adjusting agent adjusts pH value to pH=4-7.
10. composition according to claim 7, it is characterised in that described composition includes as follows according to parts by weight
Component：2-ketoacid molecule to 22 parts, 45 parts of sodium chloride, 50 parts of poly hexamethylene biguanide, pH adjusting agent adjusts pH value to pH=4-
7。
11. compositions according to claim 1, it is characterised in that described composition includes according to percetage by weight：α-
Ketone acid molecule is to 0.055%-0.5%w/w, osmotic pressure regulator 0.1%-1%w/w, bacteriostatic agent 0.01%-0.5%w/w, pH
Conditioning agent adjusts pH value to pH=4-7, water surplus.
12. compositions according to claim 11, it is characterised in that described composition includes according to percetage by weight：
2-ketoacid molecule is to 0.055%-0.22%w/w, osmotic pressure regulator 0.15%-0.45%w/w, bacteriostatic agent 0.01%-0.5%
W/w, pH adjusting agent adjusts pH value to pH=4-7, water surplus.
13. compositions according to claim 11, it is characterised in that described composition includes according to percetage by weight：
2-ketoacid molecule is to 0.22%w/w, sodium chloride 0.45%w/w, benzalkonium chloride 0.01% or 0.03%w/w, pH adjusting agent regulation
PH value is to pH=4-7, water surplus.
14. compositions according to claim 11, it is characterised in that described composition includes according to percetage by weight：
2-ketoacid molecule is to 0.22%w/w, sodium chloride 0.45%w/w, poly hexamethylene biguanide 0.5%w/w, pH adjusting agent regulation pH value
To pH=4-7, water surplus.
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| CN109806224A (en) * | 2019-03-15 | 2019-05-28 | 江苏长泰药业有限公司 | A kind of olopatadine composition and preparation method thereof |
| CN111803468A (en) * | 2020-06-23 | 2020-10-23 | 黑龙江天龙药业有限公司 | Nasal cavity film spraying agent for targeting, slow-release, film-forming and virus and bacteria inhibiting and preparation method thereof |
| WO2022228651A1 (en) * | 2021-04-26 | 2022-11-03 | Gerd Birkenmeier | Pyruvate esters for the treatment of viral diseases |
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| CN102657611A (en) * | 2012-03-02 | 2012-09-12 | 江苏长泰药业有限公司 | Sodium pyruvate nasal spray and preparation method thereof |
| CN103720682A (en) * | 2013-08-02 | 2014-04-16 | 江苏长泰药业有限公司 | Pyruvic acid medicinal composition and application thereof in preparation of medicament for treating chronic obstructive pulmonary diseases |
| CN104116706A (en) * | 2014-06-13 | 2014-10-29 | 温州医科大学附属眼视光医院 | Ethyl pyruvate eye drop and preparation method thereof |
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| WO2003088955A1 (en) * | 2002-04-17 | 2003-10-30 | Critical Therapeutics, Inc. | Pharmaceutical composition comprising an alpha-ketoalkanoic acid ester or -amine and lactic acid or a lactic acid salt |
| CN102657611A (en) * | 2012-03-02 | 2012-09-12 | 江苏长泰药业有限公司 | Sodium pyruvate nasal spray and preparation method thereof |
| CN103720682A (en) * | 2013-08-02 | 2014-04-16 | 江苏长泰药业有限公司 | Pyruvic acid medicinal composition and application thereof in preparation of medicament for treating chronic obstructive pulmonary diseases |
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| CN109806224A (en) * | 2019-03-15 | 2019-05-28 | 江苏长泰药业有限公司 | A kind of olopatadine composition and preparation method thereof |
| CN111803468A (en) * | 2020-06-23 | 2020-10-23 | 黑龙江天龙药业有限公司 | Nasal cavity film spraying agent for targeting, slow-release, film-forming and virus and bacteria inhibiting and preparation method thereof |
| CN111803468B (en) * | 2020-06-23 | 2022-12-23 | 黑龙江天龙药业有限公司 | Nasal cavity film spraying agent for targeting, slow-release, film-forming and virus and bacteria inhibiting and preparation method thereof |
| WO2022228651A1 (en) * | 2021-04-26 | 2022-11-03 | Gerd Birkenmeier | Pyruvate esters for the treatment of viral diseases |
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