CN102302504A - Application of high-purity baicalin or baicalein to preparation of inhaled asthma relieving medicament - Google Patents
Application of high-purity baicalin or baicalein to preparation of inhaled asthma relieving medicament Download PDFInfo
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Abstract
The invention discloses application of high-purity baicalin or baicalein to the preparation of inhaled asthma relieving medicaments. The inhaled asthma relieving medicaments comprise the formulations of inhaled solution or inhaled powder sprays, wherein the inhaled solution is prepared from the baicalin or the baicalein and pharmaceutical adjuvants A, and the pharmaceutical adjuvants may be one or more of solvents, latent solvents, surfactants or antioxidants; the inhaled powder sprays are prepared from the baicalin or the baicalein or pharmaceutical adjuvants B, and the pharmaceutical adjuvants B may be one or more of the solvents, the antioxidants or carriers; and the purity of the baicalin or the baicalein is more than 90 percent. Experiments proves that the inhaled asthma relieving medicaments prepared from the high-purity baicalin or baicalein can control the acute paroxysm of asthma effectively, relieve bronchospasm and reduce the resistance of air passages, is high in medicinal effect, small in side effect, nontoxic and low in cost.
Description
Technical field
The present invention relates to the purposes of baicalin or baicalin, particularly relate to the application of baicalin or baicalin at preparation suction-type suppressing panting calming medicine.
Background technology
Asthma is to comprise the inflammatory cell of air flue and the air flue chronic inflammation disease of structure cell (like eosinophilic granulocyte, mastocyte, T lymphocyte, neutrophilic granulocyte, smooth muscle cell, airway epithelia cell etc.) and cellular component participation by various kinds of cell.Current research shows; The pathogenesis of asthma rate is ascendant trend gradually; But asthma dependency admission rate and mortality rate all have obvious minimizing, and mainly due to along with the pathogenetic further investigation of asthma, treating asthma is that medicine also is all to have obtained very big progress and breakthrough on the non-medicine.
The American Studies personnel find that mouse pulmonary exists a kind of " Taste receptor ", effectively relieving asthma symptoms.This discovery will help research worker developing new drug thing treatment asthma.Univ Maryland-Coll Park USA's research worker utilizes mouse to do experiment, allows the mouse respiratory tissues contact bitter substance, is exposed to the asthma anaphylactogen then.Research worker is found, the respiratory tissues generation protective reaction of mouse at this moment.The research worker experiment finds that mouse pulmonary Taste receptor receives bitter substance to stimulate, and helps the respiratory tract expansion, thereby alleviates dyspnea.University of Maryland's medical college medical science and physiology professor, the special expression of cardiopulmonary genome plan director Si Di Finley lattice, they have opened trachea from the depths, open all deeply than any medicine that is used to treat asthma or chronic obstructive pulmonary disease (COPD).This discovery possibly bring brand-new Therapeutic Method, develop the new drug of treatment asthma, emphysema or chronic bronchitis, or improve present used curative effect of medication, and oral formulations can not produce this effect.(Deepak?A?Deshpandel，Wayne?C?H?Wang，Elizabeth?L?McIlmoyle，Kathryn?S?Robinett，Rachel?M?Schillinger，Steven?S?An，James?S?K?Sham?&?Stephen?B?Liggett，Bitter?taste?receptors?on?airway?smooth?muscle?bronchodilate?by?localized?calcium?signaling?and?reverse?obstruction.Nature?medicine，2010，16(11)：1299-1307)。But at present, also there is not the bitterness receptors agonist to go on the market in the world as medicine.Be not that all bitter principles all act on bitterness receptors.
Radix Scutellariae is the conventional medicament of China, and the beginning is stated from Shennong's Herbal, its bitter in the mouth, cold in nature.Heat clearing and damp drying is arranged, detoxifcation, hemostatic effect.Excessive thirst, cough due to lung-heat, dysentery pyretic stranguria, jaundice due to damp-heat, frequent fetal movement, carbuncle furuncle, conjunctival congestion and swelling pain are used to generate heat.Baicalin (Baicalin) is one of main active of Radix Scutellariae, belongs to the flavonoid glycoside composition, and molecular formula is C
21H
18O
11Baicalin is the aglycon of baicalin.Molecular formula is C
15H
10O
5
Baicalin has antiinflammatory, antiallergic action, diuresis, function of gallbladder promoting, cholesterol reducing, antithrombotic formation, relieving asthma, eliminating fire and detoxication, hemostasis, effect such as antiabortive.Baicalin is by obtaining after the baicalin hydrolysis; Have multiple pharmacologically actives such as antibiotic, antiviral, infection, removing free radical, antioxidation; The research of SRS2A and L T release and the influence of tracheal smooth muscle tensity in the sensitized guinea pig lung after having research report demonstration administered through oral baicalin to antigen challenge; Find that oral baicalin can suppress SRS2A and L T discharges, reduce the release of L TC4 and D4 simultaneously.Allergic asthma to Cavia porcellus has mitigation; Can alleviate the asthma of whole animal; And have synergism (Miyamoto K with Herba Ephedrae; Katsuragi T; Abdu P, Furukawa T.Effects of baicalein on prostanoid generation from the lung and contractile re2 sponse of the trachea in guinea pig.Am J Chi n Med, 1997; 25, (1): 37-50).At present baicalin mainly with extract part prescription form as oral be used for clinical.And do not have baicalin or baicalin to process the listing of imbedibility preparation, more do not utilize baicalin or baicalin highly purified, single dose to process the listing of imbedibility preparation.The suction-type preparation is different with oral formulations, and it directly acts on pulmonary, highly purified medicine, with reduce that impurity brings in the Chinese medicine to non-direct side effect.
Summary of the invention
The objective of the invention is to overcome deficiency of the prior art, the application at preparation suction-type suppressing panting calming medicine of high-purity baicalin or baicalin is provided.
Technical scheme of the present invention is summarized as follows:
High-purity baicalin or baicalin are in the application of preparation suction-type suppressing panting calming medicine, and the dosage form that it is characterized in that said suction-type suppressing panting calming medicine is imbedibility solution or imbedibility powder spray;
Said imbedibility solution is processed by 0.01-6 mass parts baicalin or baicalin and 94-99.99 mass parts category-A pharmaceutic adjuvant; Said category-A pharmaceutic adjuvant is any one or more of solvent, cosolvent, surfactant or antioxidant;
Said imbedibility powder spray is processed by 0.01-50 mass parts baicalin or baicalin and 50-99.99 mass parts category-B pharmaceutic adjuvant, and said category-B pharmaceutic adjuvant is any one or more of solvent, antioxidant or carrier;
Preferably the purity of baicalin or baicalin preferably is equal to or greater than 98% greater than 90%.
The particle diameter of baicalin or baicalin described in the said imbedibility powder spray is nano-particle or is the micron particle of＜10 μ m.
The particle diameter of said imbedibility powder spray is a nano-particle.
Said solvent is water or ethanol.
Said cosolvent is propylene glycol, PEG400 or Macrogol 600.
Said surfactant is tween 20, Tween-40, Tween-60, tween 80, Arlacel-20, Arlacel-40, Arlacel-60 or phospholipid.
Said antioxidant is NaHSO
3Or chlorogenic acid.
Said carrier is lactose, mannitol, polylactic acid/ethanol copolymer, Macrogol 4000, polyethylene glycol 6000, arabic gum, leucine or poloxamer.
The pH value of said imbedibility solution is 6.5-7.2.
We discover that highly purified baicalin, baicalin can directly act on the bitterness receptors of lung, help the respiratory tract expansion, thus relieving asthma effectively.
Baicalin of the present invention or baicalin are monomer component, and purity content is equal to or greater than 90%, preferably greater than 98%, have higher drug effect, lower side effect.Being prepared into the suction-type suppressing panting calming medicine with baicalin or baicalin is special-purpose new purposes, the novel formulation that baicalin or baicalin are relievingd asthma.
Experiment showed, the acute attack that can effectively control asthma with the suction-type suppressing panting calming medicine of high-purity baicalin or baicalin preparation, extenuate bronchospasm, reduce airway resistance, drug effect is high, side effect is little, nontoxic, with low cost.
Description of drawings
Fig. 1 is the paraffin section of guinea pig trachea.
α-gusducin protein expression presents strong positive reaction in the immune fluorescence grouping Faxian is shown in trachea surface (A) and lung (B) the taste bud cell of Cavia porcellus.
The specific embodiment
The following examples can make those skilled in the art more fully understand the present invention, but do not limit the present invention in any way.
The active selection principle of drug target of the present invention is to design medicine targetedly according to the disease characteristics according to asthma.
Used baicalin, Radix Scutellariae have commercially available or can reach in the document and to describe and prepare (Buddha's warrior attendant not in accordance with known methods among the present invention; Xin Shuquan, Zhang Li is beautiful. the research of baicalin purification process, Changchun Normal College's journal (natural science edition); 2008,27 (6): 63-66; Xuan Han, Chen Jun, Du Fengyu, etc. the technical study of baicalin in the macroporous adsorbent resin separation and purification Radix Scutellariae, the time precious traditional Chinese medical science traditional Chinese medicines, 2006,17 (10): 1992-1994; Li Yunxia, Suo Quanling, He Wenzhi, etc. the separation and purification of baicalin and structural characterization. spectroscopy and spectrum analysis, 2008,28 (8): 1895-1899).
The baicalin of purchasing, baicalin be behind D101 type purification with macroreticular resin, again through volumetric concentration be 80% ethanol water repeatedly recrystallization make purity reach more than 90% or equal, greater than 98%.
Embodiment 1
The suction-type powder spray of relievining asthma:
Prescription
Method for preparing: with the baicalin micronization, selecting particle diameter for use is that 0.5-5 μ m lactose and leucine are done carrier, adds an amount of 50% (v/v) ethanol water and granulates, place and revolve the sieve that shakes, and vibration 50min, oven dry promptly gets, and particle diameter is 0.5-5 μ m.Behind intermediate analysis and assay, be packed into capsule, contain principal agent 30mg with every capsules, use by capsule-type propeller type Diskus.
Embodiment 2
The suction-type powder spray of relievining asthma:
Prescription
Baicalin 15g (purity of baicalin is 91%)
Lactose 60g
Poloxamer 0.03g
Method for preparing: behind each component uniform mixing in the above-mentioned prescription, adding 95% (v/v) ethanol water is an amount of, is solution, and make it particle mean size with the spray drying method micronization and reach 1-5 μ m, 100 mesh sieves that sieve, encapsulated.Behind intermediate analysis and assay, be packed into capsule, use by capsule-type propeller type Diskus.
Embodiment 3
The suction-type powder spray of relievining asthma:
Prescription:
Baicalin 0.1g (purity of baicalin is 98%)
Mannitol 98g
Method for preparing: baicalin is spray-dried, prepares nano powder with high pressure homogenization method then, granularity 100-900nm; Mannitol is processed about 150 μ m micropowders, baicalin nano powder and mannitol are processed about 150 μ m micropowder mixings, cross 100 mesh sieves, encapsulated.Behind intermediate analysis and assay, be packed into capsule, use by capsule-type propeller type Diskus.
Mannitol in the present embodiment also can substitute with polyethylene glycol 6000 or arabic gum, preparation suction-type powder spray.
Embodiment 4
The suction-type solution of relievining asthma:
Prescription
Method for preparing: baicalin, chlorogenic acid, tween 80 are dissolved in the ethanol, treat that it dissolves fully, transfer pH to 7.1, restock surplus sterile purified water filters fill to full dose with sintered glass filter-bulb.
Tween 80 in the present embodiment also can use tween 20, Tween-40, Tween-60, Arlacel-20, Arlacel-40, Arlacel-60 or phospholipid to substitute, preparation suction-type solution.
Embodiment 5
The suction-type solution of relievining asthma:
Prescription
Method for preparing: baicalin is dissolved in the ethanol, treats that it dissolves fully, transfer pH to 6.5, add sterile purified water 30ml, add NaHSO
3, replenish the surplus sterile purified water then to full dose, filter fill with sintered glass filter-bulb.
Embodiment 6
The suction-type solution of relievining asthma:
Prescription
Baicalin 2g (purity of baicalin is 98%)
Ethanol 10ml
Sterile purified water adds to 100ml.
Method for preparing: the baicalin Borneolum Syntheticum is dissolved in the ethanol, transfers pH to 7.2, treat that it dissolves restock surplus sterile purified water fully to full dose, filter fill with sintered glass filter-bulb.
Embodiment 7
The suction-type solution of relievining asthma:
Prescription
Method for preparing: baicalin is dissolved in the ethanol, transfers pH to 7.0, treat that it dissolves fully, add tween 80, restock surplus sterile purified water filters fill to full dose with sintered glass filter-bulb.
Embodiment 8
The suction-type solution of relievining asthma:
Prescription
Method for preparing: in baicalin ethanol, transfer pH to cause 7.0, treat that it dissolves fully, add propylene glycol, Tween-60, restock surplus sterile purified water filters fill to full dose with sintered glass filter-bulb.
Can also use tween 20, Tween-40, Arlacel-20 or Arlacel-40 to substitute the Tween-60 in the present embodiment, as new embodiment.
Embodiment 9
The suction-type powder spray of relievining asthma:
Prescription
Method for preparing: with embodiment 1.
Embodiment 10
The suction-type powder spray of relievining asthma:
Prescription
Method for preparing: with embodiment 1.
Embodiment 11
The suction-type solution of relievining asthma:
Prescription
Method for preparing: with embodiment 5.
Embodiment 12
The suction-type solution of relievining asthma:
Prescription
Method for preparing: with embodiment 5.
Experimental example
1. dissolubility test:
Adopt the HPLC method to measure the equilbrium solubility of baicalin in water, different pH value phosphate buffer.Chromatographic column: SinChrom ODS-BP post (4.6mmx250mm, 5 μ m); Mobile phase: methanol one water, one glacial acetic acid (50: 50: 1); Detect wavelength: 275nm) flow velocity: 1.0mL/min; Column temperature: 25 ℃.Get reference substance and need testing solution sample introduction respectively and measure sampling volume 10 μ l.
Equilbrium solubility (n=5) in table 1 baicalin pH 3.0～pH 7.0 phosphate buffers
| PH value | Dissolubility | RSD％ |
| 3 | 3.52 | 0.36 |
| 4 | 4.95 | 0.21 |
| 5 | 61.41 | 0.35 |
| 6 | 531.86 | 0.22 |
| 6.5 | 4213.27 | 0.36 |
| 7.0 | 6172.26 | 0.28 |
| 7.2 | 6219.45 | 0.33 |
Conclusion: the baicalin dissolubility raises with pH value and increases, atomic dissolving when pH value is 6.0, and dissolubility obviously increases when pH value is 6.5 and 7.0.When pH value was too high, then the stability of baicalin reduced.
2. in vitro tests pharmaceutical research
Normal or asthmatic guinea pigs are got in the preparation of the external trachea spiral bar of Cavia porcellus, and the head of fiercelying attack causes death.Cut rapidly skin, separate trachea, from thyroid cartilage bag bone down to the trachea lower end crotch whole section trachea cut, put into the culture dish that fills the Krebs nutritional solution, reject the connective tissue around the trachea.Trachea is cut into the spiral bar of 20mm * 3mm.Respectively trachea spiral bar lower end is fixed on the logical oxygen hook of glass, specimen places and fills 37 ℃ of constant temperature Magnus' baths of 25ml K-H liquid, and the upper end links to each other with tonotransducer, and temperature is set in 37 ℃.With the tensile variation of Medlab bio signal processing system record tracheal smooth muscle.Each trachea spiral bar is carried out one group of experiment, does not reuse, and experiment finishes with its activity of Ach check, and non-activity person experimental result is given it up.Every 15min changes nutritional solution 1 time, behind the balance 1h, adds 0.2mg/mL histamine phosphate or 0.2mg/mL acecoline 0.3mL respectively.Tracheal smooth muscle tension force shrinks and 1h behind the platform to occur, with Krebs nutritional solution flushing 2 times as contrasting.Every 15min changes nutritional solution 1 time.Behind the 60min, add identical histamine phosphate or acecoline again, every after 5min appears in platform at a distance from 5min adding medicinal liquid (embodiment 1-8 is in baicalin, and wherein embodiment 1-3 adopts powder spray to add distilled water to be made into corresponding solution), repeat 3 times.Make bath baicalin concentration be respectively 0.05mg/mL.Curve fall behind each specimen administration 3min of observation comparison, and calculate the spasmolytic percentage rate.Spasmolytic percentage rate=(administration forward pull-administration backward pull)/administration forward pull * 100%.The result shows that each embodiment all can effectively suppress histamine phosphate, the acecoline guinea pig tracheal smooth muscle is shunk, and shows that purity improves increased activity.See table 2.
The pharmaceutical preparation of each embodiment of table 2 is shunk antagonism (n=5) to histamine phosphate, acecoline guinea pig tracheal smooth muscle
* P＜0.05 and matched group 1 compare
Conclusion: highly purified baicalin and baicalin activity are better than impure more matched group 1.
The animal experiment of relievining asthma
1. embodiment 4 pharmaceutical researches
(1) experiment material
Experimental subject is selected regular grade Hartley Cavia porcellus, body weight 150～200g, and dimension tonneau China laboratory animal technology company limited provides.Test sample is the embodiment 4 suction-types solution of relievining asthma.The budesonide atomized liquid, AstraZeneca pharmaceutical Co. Ltd produces, homemade YUYUE-403 type medical vaporizer.The 4L exsiccator.
(2) foundation of animal asthmatic model and screening
Adopt medicine to draw the method for breathing heavily (spraying causes the method for breathing heavily).Cavia porcellus is put into airtight glass bell jar; Spray into 2% histamine phosphate and 0.4% acecoline (2: 1) mixed liquor 25s with quantitative nebulizer; Spraying stops the back Cavia porcellus and causes rapid breathing, pants; Even suffocate; Thereby have a convulsion or fall etc., be the animality guinea pig asthmatic model and set up successfully.Begin to be called to draw and to breathe heavily incubation period from spraying to the time of twitching, falling.Test to lure the previous day and breathe heavily experiment, breathe heavily incubation period＞120s then for insensitive and unelected if draw.
(3) randomized grouping experimental
Select each 10 of qualified Cavia porcellus random packet, every treated animals.The weight of animals between each group divides balancing.Each treated animal is with quantitative nebulizer difference administration 1 time, and matched group gives the normal saline with volume, and pharmaceutical quantities is seen table 2.In the rearmounted airtight 4L glass bell jar of 10min, the similarity condition with quantitative nebulizer during by preliminary election sprays into 2% histamine phosphate and 0.4% acecoline (2: 1) mixed liquor 25s, observes also to write down and draws the number of animals of breathing heavily incubation period and falling.
(4) statistical method
All continuous datas are represented with mean ± standard deviation.
(5) result
Experimental result is seen table 3.
Table 3 baicalin induces the incubation period of Cavia porcellus asthma and the number of times of falling to influence to histamine phosphate and acecoline
* compare with the normal saline group P＜0.01
The result shows: the preparation of embodiment 4 preparation all has obvious mitigation to the Cavia porcellus asthma that acetylcholine and histamine mixed liquor bring out.
2. embodiment 5 pharmaceutical researches
Experimental technique is seen the pharmaceutical research of embodiment 4, and the suction-type solution of relievining asthma is embodiment 5 preparation; Budesonide suspension (Pumi's gram, lot number LL1875) 1mg/ml.Experimental result is seen table 4.
Table 4 baicalin induces the incubation period of Cavia porcellus asthma and the number of times of falling to influence to histamine phosphate and acecoline
* p＜0.05; Compare with the normal saline group * P＜0.01
The result shows: the preparation of embodiment 5 preparations has therapeutical effect to Cavia porcellus asthma, can breathe heavily incubation period drawing of prolonged guinea pig.
3 embodiment, 6 pharmaceutical researches
The suction-type solution of relievining asthma is seen embodiment 6 preparation, gets 60 of Cavia porcelluss, male and female half and half, and male and female divide the cage adaptability to feed for 1 week under the same conditions, routine feeding standard particle feedstuff.Then divide 6 groups at random, 10 every group, male and female half and half.Be made as blank group, model group, positive controls [dexamethasone sodium phosphate injection (Tianjin gold credit aminoacid company limited)] and high, medium and low 3 dose groups of administration (pressing embodiment 6) respectively to medicine composition.Modeling method: except that blank control group (injection and atomizing suck normal saline), every Cavia porcellus difference lumbar injection 5% ovalbumin normal saline solution 1ml, Cavia porcellus is in the sensitization state.Medication: the 15th day of experiment; High, medium and low 3 dose groups and the positive controls Cavia porcellus of administration group embodiment 6 are sprayed with propellant; Blank group, model group are all with the physiologic saline for substitute of same dose; Atomizing sucks the 1%OVA antigen liquid then; Cough until occurring choking, stridulate, stop during respiratory tract obstruction symptom such as abdomen formula spasm; Day 1 time, continuous 7 days.Get peripheral blood, execution, detect eosinophil count, result of the test is seen table 5, table 6.
The preparation of table 5 embodiment 6 preparations is to the preclinical influence of asthmatic guinea pigs
* p＜0.05; Compare with model group * P＜0.01
Model group has 2 Cavia porcellus death, and normal group can not be brought out asthma.Table 5 result is visible, and the suction-type solution (embodiment 6 preparations) of relievining asthma can prolong the incubation period of asthmatic guinea pigs.
The suction-type influence (see table 6) of solution (embodiment 6 preparation) of relievining asthma to asthmatic model Cavia porcellus eosinophil count.
The relieving asthma influence of solution (embodiment 6 preparation) asthmatic guinea pigs eosinophil count of table 6 suction-type
* compare with model group p＜0.01
Visible by table 6 result, the eosinophilic granulocyte is higher than the normal control group in the model group blood, and significant difference (P＜0.05) is arranged.The eosinophilic granulocyte has significant difference (P＜0.05) than the asthmatic model group in Dexamethasone group, administration high dose group, middle dose groups and the low dose group blood.
Immunofluorescence detects the α-gusducin of Guinea pig lung and trachea
α-gusducin protein expression presents strong positive reaction in immunofluorescence is presented at trachea surface (A) and lung (B) the taste bud cell of Cavia porcellus.We discover in trachea surface (A) and lung (B) the taste bud cell of Cavia porcellus all has stronger α-gusducin protein expression (see figure 1).
4. 4 pairs of asthma mices of embodiment influence of Pulmonary Function
The suction-type solution (embodiment 4) of relievining asthma is got 60 of mices, male and female half and half, and male and female divide the cage adaptability to feed for 1 week under the same conditions, routine feeding standard particle feedstuff.Then divide 6 groups at random, 10 every group, male and female half and half.Be made as blank group, model group, positive controls (dexamethasone injection) and high, medium and low 3 dose groups of administration (pressing embodiment 4) respectively to medicine composition.Modeling method: except that blank control group (injection and atomizing suck normal saline); 0th, 14 days every mice difference lumbar injection 0.2mL antigen liquids (aluminium hydroxide 400ug and OVA 100ug); Mice is in the sensitization state, and the blank group substitutes the antigen liquid lumbar injection with the equivalent physiological saline solution.21d begins to use the 1%OVA solution atomization, excites the mouse asthmatic outbreak, every day 1 time, and each 30min, continuous 7 days, blank control group was with equivalent physiologic saline for substitute atomisation.Administration group and positive controls be 10min atomizing inhalation before at every turn exciting respectively, and blank group, model group are all with the physiologic saline for substitute atomisation of same amount.After the atomizing of mice last sucks 24h,, lie on the back, separate the exposure trachea, medisection inverted T shape otch in the middle of the three or four annulus trachealis with pentobarbital sodium (70mg/kg) anesthesia.Insertion is connected with the tracheal intubation of three-way cock, and tracheal intubation one end is connected with animal respirator, adopts experiment toy lung function measuring equipment to measure.
Statistical procedures adopts SAS 8.2 statistical softwares to carry out statistical analysis.The result sees table 7.
Table 7 suction-type is relievingd asthma solution to asthma mice influence of Pulmonary Function (n=10)
Model group and normal group compare,
ΔP＜0.05; Compare * P＜0.05 with model group
Research shows middle and high dose groups of administration and model group relatively, and the airway resistance index has statistical significance (P＜0.05), confirms the effectively acute attack of control asthma of FORMULATION EXAMPLE 4, extenuates bronchospasm, reduces airway resistance.
Experiment showed, the powder spray of each embodiment preparation and the acute attack that solution liquid can effectively be controlled asthma, extenuate bronchospasm, reduce airway resistance.
Claims (10)
1. high-purity baicalin or baicalin are in the application of preparation suction-type suppressing panting calming medicine, and the dosage form that it is characterized in that said suction-type suppressing panting calming medicine is imbedibility solution or imbedibility powder spray;
Said imbedibility solution is processed by 0.01-6 mass parts baicalin or baicalin and 94-99.99 mass parts category-A pharmaceutic adjuvant; Said category-A pharmaceutic adjuvant is any one or more of solvent, cosolvent, surfactant or antioxidant;
Said imbedibility powder spray is processed by 0.01-50 mass parts baicalin or baicalin and 50-99.99 mass parts category-B pharmaceutic adjuvant, and said category-B pharmaceutic adjuvant is any one or more of solvent, antioxidant or carrier;
The purity of said baicalin or baicalin is greater than 90%.
2. high-purity baicalin according to claim 1 or baicalin is characterized in that in the application of preparation suction-type suppressing panting calming medicine the purity of said baicalin or baicalin is equal to or greater than 98%.
3. high-purity baicalin according to claim 1 or baicalin are in the application of preparation suction-type suppressing panting calming medicine, and the particle diameter that it is characterized in that baicalin described in the said imbedibility powder spray or baicalin is nano-particle or is the micron particle of＜10 μ m.
4. high-purity baicalin according to claim 1 or baicalin are in the application of preparation suction-type suppressing panting calming medicine, and the particle diameter that it is characterized in that said imbedibility powder spray is a nano-particle.
5. high-purity baicalin according to claim 1 or baicalin is characterized in that in the application of preparation suction-type suppressing panting calming medicine said solvent is water or ethanol.
6. high-purity baicalin according to claim 1 or baicalin is characterized in that in the application of preparation suction-type suppressing panting calming medicine said cosolvent is propylene glycol, PEG400 or Macrogol 600.
7. high-purity baicalin according to claim 1 or baicalin are in the application of preparation suction-type suppressing panting calming medicine; It is characterized in that said surfactant is tween 20, Tween-40, Tween-60, tween 80, Arlacel-20, Arlacel-40, Arlacel-60 or phospholipid.
8. high-purity baicalin according to claim 1 or baicalin is characterized in that in the application of preparation suction-type suppressing panting calming medicine said antioxidant is NaHSO
3Or chlorogenic acid.
9. high-purity baicalin according to claim 1 or baicalin is characterized in that in the application of preparation suction-type suppressing panting calming medicine said carrier is lactose, mannitol, polylactic acid/ethanol copolymer, Macrogol 4000, polyethylene glycol 6000, arabic gum, leucine or poloxamer.
10. high-purity baicalin according to claim 1 or baicalin are in the application of preparation suction-type suppressing panting calming medicine, and the pH value that it is characterized in that said imbedibility solution is 6.5-7.2.
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102579472A (en) * | 2012-01-19 | 2012-07-18 | 中国人民武装警察部队后勤学院 | Medicinal composition capable of expanding tracheal smooth muscles and application thereof |
| FR3046077A1 (en) * | 2015-12-23 | 2017-06-30 | Oreal | COMPOSITION COMPRISING HIGH CONCENTRATION BAICALIN |
| WO2018115493A1 (en) * | 2016-12-23 | 2018-06-28 | L'oreal | Composition comprising baicalin |
| CN110198714A (en) * | 2017-01-06 | 2019-09-03 | 高丽大学校世宗产学协力团 | For prevent or treat such as asthma or idiocrasy allergic disease comprising pharmaceutical composition of the baicalein as active constituent |
| CN116327743A (en) * | 2023-04-13 | 2023-06-27 | 南京芩领医药科技有限公司 | Application of baicalein inhalation preparation in preparation of acute lung injury treatment drugs |
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- 2011-09-01 CN CN201110255805A patent/CN102302504A/en active Pending
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Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102579472A (en) * | 2012-01-19 | 2012-07-18 | 中国人民武装警察部队后勤学院 | Medicinal composition capable of expanding tracheal smooth muscles and application thereof |
| FR3046077A1 (en) * | 2015-12-23 | 2017-06-30 | Oreal | COMPOSITION COMPRISING HIGH CONCENTRATION BAICALIN |
| WO2018115493A1 (en) * | 2016-12-23 | 2018-06-28 | L'oreal | Composition comprising baicalin |
| FR3060997A1 (en) * | 2016-12-23 | 2018-06-29 | L'oreal | COMPOSITION COMPRISING BAICALIN |
| US11931445B2 (en) | 2016-12-23 | 2024-03-19 | L'oreal | Composition comprising baicalin |
| CN110198714A (en) * | 2017-01-06 | 2019-09-03 | 高丽大学校世宗产学协力团 | For prevent or treat such as asthma or idiocrasy allergic disease comprising pharmaceutical composition of the baicalein as active constituent |
| CN116327743A (en) * | 2023-04-13 | 2023-06-27 | 南京芩领医药科技有限公司 | Application of baicalein inhalation preparation in preparation of acute lung injury treatment drugs |
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Application publication date: 20120104 |