CN102266560A - Drug composition for treating asthma - Google Patents
Drug composition for treating asthma Download PDFInfo
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- CN102266560A CN102266560A CN2010101919496A CN201010191949A CN102266560A CN 102266560 A CN102266560 A CN 102266560A CN 2010101919496 A CN2010101919496 A CN 2010101919496A CN 201010191949 A CN201010191949 A CN 201010191949A CN 102266560 A CN102266560 A CN 102266560A
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- spray
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- asthma
- afromoterol
- momestasone furoate
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Abstract
The invention provides a drug composition for treating asthma. The drug composition comprises components of momestasone furoate and a beta2 adrenergic receptor agonist. The composition is an inhalant formulation, including but not limited to inhalant powder, inhalant aerosol, inhalant spray. The drug composition can be applicable for treating the asthma caused by various causes, and COPD.
Description
Technical field
The present invention is a kind of pharmaceutical composition that is used for the treatment of asthma, belongs to medical technical field.
Background technology
Momestasone furoate is one of the strongest suction 17-hydroxy-11-dehydrocorticosterone of present anti-inflammatory activity.Its anti-inflammatory activity surpasses momestasone furoate, with fluticasone about equally or strong slightly.Can be used as 12 years old and the prophylactic treatment of above asthmatic patient, a line that can be used for asthma is kept treatment.For the asthmatic patient of accepting bronchodilator list medicine or inhaled glucocorticoid class Drug therapy in the past, be that getting permission with 1 medication on the one at present is initial induction type asthma control medicine.Clinical trial shows that the momestasone furoate inhalant can make patient's pulmonary function substantive the improvement occur, reduces the use of first aid medicine, reduces wake up night number of times and significantly improve symptom in the daytime such as cough, wheezing of patient.
The beta-2 adrenoceptor agonist also is one of medicine of treatment asthma.After the beta-2 adrenoceptor agonist enters human body, combine with the beta receptor of the affine state of height, activated adenyl cyclase, make cell interior 3,5-cyclic adenosine monophosphate (cAMP) content increases, protein kinase A activation, thereby the phosphorylation of inhibition myosin, cause Ca2+ lowering of concentration in the cell, make airway smooth muscle lax; In addition, the beta receptor agonist can also suppress mastocyte, basophilic granulocyte takes off granule, and inflammatory mediator is discharged reduce, and the beta 2 receptor by existing on the parasympathetic nervous presynaptic membrane, suppress the release of cholinergic neurotransmitter, cause airway smooth muscle lax.Epinephrine, isoproterenol, ephedrine are the main medicines of in the past treating asthma, are now replaced by selectivity beta 2 receptor agonist gradually.
Inhalant through the oral cavity administration has a bit a lot: but the toxic and side effects to other positions can be avoided or reduce to medicine through sucking rapid subsidence in pulmonary; Pulmonary's sorbent surface is long-pending big, the membrane permeability height, and blood flow is abundant, and drug absorption is rapid; Pulmonary's enzymatic activity is lower, and does not have liver first-pass effect, and these help improving bioavailability of medicament.And pulmonary administration can be used for local disease's treatment of pulmonary.A lot of successful examples have been arranged at present, and as hormones, treatment asthma class medicine, the kind of exploitation is a lot.The technology of pulmonary's inhalation mainly contains 3 kinds at present: Foradil Aerolizer formoterol fumarate, aerosol (also becoming metered dose inhalation aerosol) and spray.
Summary of the invention
The present invention is a kind of pharmaceutical composition that is used for the treatment of asthma, and its active component is momestasone furoate and a kind of beta 2 adrenoreceptor agonists.Beta 2 adrenoreceptor agonists wherein, comprise salmaterol, procaterol, Afromoterol, fenoterol, clenbuterol, reproterol, tulobuterol, bambuterol, xamoterol, Mabuterol, pirbuterol, bitolterol, ring Lun Teluo and their optical isomer, pharmaceutical salts etc., pharmaceutical salts comprises hydroxynaphthoate, tartrate, fumarate, hydrochlorate, sulfate, benzene sulfonate, succinate etc.
Compositions of the present invention is to exist with inhalant dosage form, includes but are not limited to suck powder spray, inhalation aerosol, suction spray.The unit administration amount of its active component is as follows
Momestasone furoate: whenever press or spray and be 40-2000mcg, be preferably 200-400mcg.
Salmaterol: whenever press or spray and be 5-250mcg, be preferably 25-50mcg.
Procaterol: whenever press or spray and be 2-100mcg, be preferably 10-20mcg.
Afromoterol: every suction or spray are 3-150mcg.Be preferably 15-30mcg.
Fenoterol: whenever press or spray and be 40-2000mcg, be preferably 200-400mcg.
Clenbuterol: whenever press or spray and be 2-100mcg, be preferably 10-20mcg.
Reproterol: whenever press or spray and be 100-5000mcg, be preferably 500-1000mcg.
What the pharmaceutically acceptable pharmaceutic adjuvant of described suction powder spray was commonly used is glycine or lactose, is preferably lactose.They need to carry out micronization processes, and particle size distribution range is preferably between the 1-100 micron between the 0.02-200 micron.
The pharmaceutically acceptable pharmaceutic adjuvant of described inhalation aerosol is commonly used comprises dispersion and propellant.Wherein dispersion can exist with the form of Emulsion, suspension.Propellant is freon, Hydrocarbon and Compressed Gas etc.
Described suction spray can be the dispersion of emulsion-type and suspension type.
Compositions of the present invention can be used for the asthma that a variety of causes causes, the treatment of COPD.
The specific embodiment
Embodiment 1: suck powder spray
Method for making:
Two flavor principal agents are carried out micronization respectively, make its particle diameter about 7um.Under aseptic condition, lactose equivalent incremental method, mix homogeneously.Be respectively charged in No. 3 capsules.Put into specific suction device, get final product.
Embodiment 2: suck spray
Method for making:
Afromoterol is carried out micronization, make its particle diameter about 7um.Momestasone furoate is dissolved in the dehydrated alcohol of recipe quantity,, adds the Afromoterol stirring and make evenly, pour the momestasone furoate alcoholic solution into, make evenly tween and 80ml water mix homogeneously.Transfer pH value 4-6 with citric acid and sodium salt, add purified water, divide to be filled in the particular spray bottle every bottle of 10ml, every spray 100ul to 100ml.
Embodiment 3: inhalation aerosol
Method for making:
Afromoterol is carried out micronization, make its particle diameter about 7um.Momestasone furoate is dissolved in the dehydrated alcohol of recipe quantity, adds the tween mix homogeneously, add the Afromoterol stirring and make evenly.Quantitatively divide to be filled in the aluminium pot compression set metered valve, quantitative pressurising propellant 134a, every bottle of 10ml, every spray 100ul.
The present invention is representative with compound recipe momestasone furoate Afromoterol, by following pharmaceutical test method the curative effect of its compound recipe is verified.
Embodiment 4: compound recipe momestasone furoate Afromoterol is to the anti-effect of picking up of asthma attack
Experimental technique: 40 Cavia porcelluss that primary dcreening operation is qualified are divided into 4 groups, 10 every group at random.Be respectively normal saline matched group (A group), compound recipe momestasone furoate+Afromoterol treatment group (B group), momestasone furoate treatment group (C group), Afromoterol treatment group (D group).Put Cavia porcellus in the airtight vial of 4L volume,, inhale human therapy with the jet atomization of 5L/rain flow by Central oxygen-supply.Human physiology saline, momestasone furoate+Afromoterol, momestasone furoate, Afromoterol 120s are inhaled in jet atomization respectively.Pressed the experimental program administration in continuous 4 days, behind administration 0.5h (the 1st day), 1h (the 2nd day), 2h (the 3rd day), 3h (the 4th day), Cavia porcellus is placed in the airtight vial of 4L volume, sucking the 0.8% solution 10S of histamine phosphate with the jet atomization of 5L/rain flow lures and breathes heavily, the incubation period of III degree asthma (tic is fallen) appears in the record Cavia porcellus, if do not occur III degree asthma in the 360s, then calculate with 360S incubation period.
Experimental result: the result shows, with matched group relatively, each treatment group all significantly prolongs asthma attack incubation period, but momestasone furoate+Afromoterol treatment group effect is more remarkable, and effect is continual and steady.
Each treatment group of table 1 is drawn Cavia porcellus and is breathed heavily preclinical influence
Embodiment 5: compound recipe momestasone furoate Afromoterol is to the influence of COPD airway inflammation
Experimental technique: 40 rats are divided into four groups at random, 10 every group.Be respectively model control group (A group), compound recipe momestasone furoate+Afromoterol treatment group (B group), momestasone furoate treatment group (C group), Afromoterol treatment group (D group).Each group is all injected lipopolysaccharide 1mg/kg in the 1st, 20 day trachea of experiment, the 2nd～19,21～40 days put passive smoking in people 80cm * 60cm * 58cm lucite case with rat, every day 2 times (4h at interval), continue 1h (10 medicated cigarette) at every turn.Each treatment group was all given corresponding treatment medicine+normal saline 5ml in the 2nd～19,21～40 days respectively in modeling, sucked (placing in 30cm * 30cm * 20cm glass box), 1 time/d, 25min/ time, successive administration 40 days with the 5L/rain atomizing.Model control group only gives the normal saline atomizing and sucks.Other gets 10 healthy rats as blank (O group), and experimental session only gives the normal saline atomizing on time and sucks, and does not do other any processing.Detect bronchoalveolar lavage fluid (BALF) numeration of leukocyte and classification after 40 days.The result: each administration group all has certain antiinflammatory protective effect to COPD induced lung function, so the antiinflammatory action of people's compound recipe momestasone furoate+Afromoterol is fit to COPD significantly better than momestasone furoate or Afromoterol folk prescription administering effect long-term treatment is inhaled in atomizing.
Total white blood cells and classification among the table 2BALF
The pharmacologically active of arbitrary prescription of the present invention all verifies that by above method of pharmacy experimental result shows: the treatment benefit of the compound preparation of momestasone furoate and any 17-hydroxy-11-dehydrocorticosterone all is better than the momestasone furoate or the 17-hydroxy-11-dehydrocorticosterone of folk prescription.
Claims (9)
1. a pharmaceutical composition that is used for the treatment of asthma is characterized in that, contains following active component:
First kind of composition: momestasone furoate;
Second kind of composition: a kind of beta 2 adrenoreceptor agonists comprises salmaterol, procaterol, Afromoterol, fenoterol, clenbuterol, reproterol, tulobuterol, bambuterol, xamoterol, Mabuterol, pirbuterol, bitolterol, ring Lun Teluo and their optical isomer, pharmaceutical salts etc.
2. the described compositions of claim 1 is characterized in that, pharmaceutical salts comprises hydroxynaphthoate, tartrate, fumarate, hydrochlorate, sulfate, benzene sulfonate, succinate etc.
3. the described compositions of claim 1 is characterized in that, is to exist with inhalant dosage form, includes but are not limited to suck powder spray, inhalation aerosol, suction spray.
4. the described compositions of claim 1 is characterized in that, the consumption of described momestasone furoate is 40-2000mcg for whenever pressing or spraying, and is preferably 200-400mcg.
5. the described compositions of claim 1 is characterized in that, the consumption of beta 2 adrenoreceptor agonists is as follows:
Salmaterol: whenever press or spray and be 5-250mcg, be preferably 25-50mcg;
Procaterol: whenever press or spray and be 2-100mcg, be preferably 10-20mcg;
Afromoterol: every suction or spray are 3-150mcg.Be preferably 15-30mcg;
Fenoterol: whenever press or spray and be 40-2000mcg, be preferably 200-400mcg;
Clenbuterol: whenever press or spray and be 2-100mcg, be preferably 10-20mcg;
Reproterol: whenever press or spray and be 100-5000mcg, be preferably 500-1000mcg.
6. the described compositions of claim 3, it is characterized in that, what its pharmaceutically acceptable pharmaceutic adjuvant that sucks powder spray was used always is glycine or lactose, be preferably lactose, they need to carry out micronization processes, particle size distribution range is preferably between the 1-100 micron between the 0.02-200 micron.
7. the described compositions of claim 3, it is characterized in that, the pharmaceutically acceptable pharmaceutic adjuvant of its inhalation aerosol is commonly used comprises dispersion and propellant, wherein dispersion can exist with the form of Emulsion, suspension, and propellant is freon, Hydrocarbon and Compressed Gas etc.
8. the described compositions of claim 3 is characterized in that, it sucks spray can be the dispersion of emulsion-type and suspension type.
9. the described compositions of claim 1 can be used for the asthma that a variety of causes causes, the treatment of COPD.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2010101919496A CN102266560A (en) | 2010-06-04 | 2010-06-04 | Drug composition for treating asthma |
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| Application Number | Priority Date | Filing Date | Title |
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| CN2010101919496A CN102266560A (en) | 2010-06-04 | 2010-06-04 | Drug composition for treating asthma |
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| CN102266560A true CN102266560A (en) | 2011-12-07 |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101155590A (en) * | 2005-02-10 | 2008-04-02 | 葛兰素集团有限公司 | Processes for making lactose utilizing pre-classification techniques and pharmaceutical formulations formed therefrom |
| CN101389341A (en) * | 2006-04-21 | 2009-03-18 | 奇斯药制品公司 | Pharmaceutical solution formulations for pressurised metereddose inhalers |
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2010
- 2010-06-04 CN CN2010101919496A patent/CN102266560A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101155590A (en) * | 2005-02-10 | 2008-04-02 | 葛兰素集团有限公司 | Processes for making lactose utilizing pre-classification techniques and pharmaceutical formulations formed therefrom |
| CN101389341A (en) * | 2006-04-21 | 2009-03-18 | 奇斯药制品公司 | Pharmaceutical solution formulations for pressurised metereddose inhalers |
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Application publication date: 20111207 |