CN102247380A - Compound preparation with budesonide and indacaterol as the active components - Google Patents
Compound preparation with budesonide and indacaterol as the active components Download PDFInfo
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- CN102247380A CN102247380A CN2011102403588A CN201110240358A CN102247380A CN 102247380 A CN102247380 A CN 102247380A CN 2011102403588 A CN2011102403588 A CN 2011102403588A CN 201110240358 A CN201110240358 A CN 201110240358A CN 102247380 A CN102247380 A CN 102247380A
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- budesonide
- compound preparation
- indenes
- teluo
- 75mcg
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Abstract
The invention relates to a compound preparation with budesonide and indacaterol as the active components and usage thereof. The compound preparation is prepared by mixing the active medicinal components, namely, budesonide and indacaterol, with pharmaceutically acceptable accessories and is prepared into aerosol dosed through oral cavities through technical means specified in the invention. The compound preparation has the advantages of fast action, rapid effects, convenient usage, etc., and can be used for treating various types of asthma, COPD (chronic obstructive pulmonary disease) and other diseases.
Description
Technical field
The present invention for a kind of be the compound preparation of active component with budesonide and indenes Da Teluo, belong to medical technical field.
Background technology
Chronic obstructive pulmonary disease (COPD) is a kind of disease that can prevent and treat with flow limitation feature, and flow limitation is not exclusively reversible, be and carry out sexual development, and is relevant to the abnormal inflammatory reaction of harmful gas such as smoke from cigarette or deleterious particle with pulmonary.COPD is to be the respiratory system disease of feature with stingy road chronic nonspecific inflammation and the respiratory tract obstruction of carrying out property, and essence is air flue, pulmonary parenchyma and pulmonary vascular chronic inflammatory disease.COPD mainly involves lungs, but also can the cause whole body ill effect of (or claim lung outer).COPD comprises chronic bronchitis and emphysema.
Indenes Da Teluo is that overlength of new generation is imitated the beta 2 receptor agonist. a large amount of preclinical tests and clinical trial confirm that indenes Da Teluo onset is rapid, 5min can produce the bronchodilatation effect in vivo, acting duration reaches 24h, only need every day medication once can well control pant symptom and improve pulmonary function of chronic obstructive pulmonary disease and bronchial asthma patient. in addition, the whole body system untoward reaction that indenes Da Teluo causes is few, degree is slight, is the ideal medicament of treatment chronic obstructive pulmonary disease and bronchial asthma.
Budesonide is one to have the glucocorticoid of efficient local anti-inflammatory effect.It can strengthen the stability of endotheliocyte, smooth muscle cell and lysosome membrane, suppress immunoreation and reduce antibody synthetic, thereby the release that makes irritated active mediums such as histamine reduces and active the reduction, and can alleviate antigen-antibody in conjunction with the time enzymatic processes that excites, suppress the synthetic of bronchoconstriction material and discharge and alleviate the contractile response of smooth muscle.Be applied topically to bronchus, its antiinflammatory action is strong approximately 1000 times than cortisone.Be applicable to local non-special inflammation of antagonism and antiallergic, as bronchial asthma and airway hyperreactivity state.
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
Having the purpose of this invention is to provide a kind of is the compound recipe suction preparation of active component with budesonide and indenes Da Teluo, through pulmonary's inhalation.These pulmonary's inhalation preparations mainly exist with following three kinds of forms: Foradil Aerolizer formoterol fumarate, aerosol, spray.
In the middle of above three kinds of dosage forms, preferably Foradil Aerolizer formoterol fumarate and aerosol, from the compliance of administration and the complexity of preparation, the present inventor more is inclined to and Foradil Aerolizer formoterol fumarate.In this inhalant, its active component is budesonide and indenes Da Teluo, and the consumption of described budesonide is that every suction or spray are 50-2400mcg, is preferably 100-800mcg., the consumption of described indenes Da Teluo is that every suction or spray are 18.75-300mcg, is preferably 75mcg.
In described dosage and the combination thereof, indenes Da Teluo is in active component.Can be its pharmaceutical salts during use, exist as salifiable form such as maleate, tartrate, fumarate, hydrochlorate, sulfate, benzene sulfonate, succinate.Be preferably maleate.The form of expression of budesonide can for, the budesonide of raceme, the budesonide of d-isomer and their pharmaceutical salts thereof.
The dosage combination of described budesonide and indenes Da Teluo is preferably every suction or sprays 100mcg/75mcg, 200mcg/75mcg, 400mcg/75mcg, 800mcg/75mcg.
When this inhalant is that form with Foradil Aerolizer formoterol fumarate is when existing, also must add some other adjuvant, these adjuvants include but are not limited to wherein one or more such as microcrystalline Cellulose, lactose, glucose, fructose, sucrose, mannitol, xylitol, maltose alcohol, glycine, Aspartic Acid, alanine, tryptophan, threonine.If necessary, also to add an amount of surface active ingredient, as dipalmitoyl phosphatidyl choline, two Laurel phosphatidyl cholines, cholesterol, poloxamer etc.Also might add suitable polymer substance, as in starch, polylactic acid, polylactic acid-glycolic guanidine-acetic acid, the Polyethylene Glycol one or more.
When medicinal active ingredient mixed with these adjuvants, its weight ratio was 1: 50-1: 1000.And these adjuvants and medicine all need through micronization processes, and their particle size distribution range is preferably between the 1-100 micron between the 0.02-200 micron.
If inhalant described in the invention is the form of aerosol when existing, normally with two kinds of active component dissolvings or be dispersed in certain solvent, these dispersions can be Emulsion or suspensoid.Simultaneously, also must add some propellant, propellant is freon, Hydrocarbon and Compressed Gas etc.
When if inhalant of the present invention is spray, the dispersion that is adopted can be emulsion-type and suspension type liquid.
No matter how institute adopts dispersible carrier, active constituents of medicine all needs to pass through micronization processes, absorbs preferably and utilizes effect thereby reach.
Compound preparation 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: compound recipe budesonide indenes Da Teluo sucks 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: compound recipe budesonide indenes Da Teluo sucks spray
Method for making:
Indenes Da Teluo is carried out micronization, make its particle diameter about 7um.Budesonide is dissolved in the dehydrated alcohol of recipe quantity,, adds indenes Da Teluo stirring and make evenly, pour the budesonide 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 bottle every bottle of 10ml, every spray 100ul to 100ml.
Embodiment 3: compound recipe budesonide indenes Da Teluo inhalation aerosol
Method for making:
Indenes Da Teluo is carried out micronization, make its particle diameter about 7um.Budesonide is dissolved in the dehydrated alcohol of recipe quantity, adds the tween mix homogeneously, add indenes Da Teluo 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.
Embodiment 4: compound recipe budesonide indenes Da Teluo is to the antagonism 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 budesonide+indenes Da Teluo treatment group (B group), budesonide treatment group (C group), indenes Da Teluo 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.Jet atomization suction human physiology saline, budesonide+indenes Da Teluo, budesonide, indenes reach special sieve 120s 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 budesonide+indenes Da Teluo 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 budesonide indenes Da Teluo 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 budesonide+indenes Da Teluo treatment group (B group), budesonide treatment group (C group), indenes Da Teluo 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 x20cm 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 budesonide+indenes Da Teluo is fit to COPD significantly better than budesonide or indenes Da Teluo folk prescription administering effect long-term treatment is inhaled in atomizing.
Total white blood cells and classification among the table 2BALF
Claims (10)
- The present invention for a kind of be the compound preparation of active component with budesonide and indenes Da Teluo, it is characterized in that it is a budesonide and the active component of indenes Da Teluo formation, with the Pharmaceutical composition of mixing acceptable accessories formation.
- 2. compound preparation as claimed in claim 1 is characterized in that the form of expression of indenes Da Teluo is maleate, tartrate, fumarate, hydrochlorate, sulfate, benzene sulfonate, succinate, is preferably maleate.
- 3. compound preparation as claimed in claim 1 is characterized in that, the form of expression of budesonide is racemization budesonide, dextrorotation budesonide and their pharmaceutical salts thereof.
- 4. compound preparation as claimed in claim 1 is to exist with inhalant dosage form, includes but are not limited to suck powder spray, inhalation aerosol, suction spray.
- 5. compound preparation as claimed in claim 3 is characterized in that, the consumption of described budesonide is 50-2400mcg for whenever pressing or spraying, and is preferably 100-800mcg.
- 6. compound preparation as claimed in claim 3 is characterized in that, the consumption of described indenes Da Teluo is that every suction or spray are 18.75-300mcg, is preferably 75mcg.
- 7. compound preparation as claimed in claim 3 is characterized in that, the dosage combination of described budesonide and indenes Da Teluo is preferably every suction or sprays 100mcg/75mcg, 200mcg/75mcg, 400mcg/75mcg, 800mcg/75mcg.
- 8. compound preparation as claimed in claim 3 is characterized in that, what its pharmaceutically acceptable pharmaceutic adjuvant that sucks powder spray was used always 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.
- 9. compound preparation as claimed in claim 3 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.Propellant is freon, Hydrocarbon and Compressed Gas etc.
- 10. compound preparation as claimed in claim 3 is characterized in that, it sucks spray can be the dispersion of emulsion-type and suspension type.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2011102403588A CN102247380A (en) | 2011-08-19 | 2011-08-19 | Compound preparation with budesonide and indacaterol as the active components |
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| Application Number | Priority Date | Filing Date | Title |
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| CN2011102403588A CN102247380A (en) | 2011-08-19 | 2011-08-19 | Compound preparation with budesonide and indacaterol as the active components |
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| CN102247380A true CN102247380A (en) | 2011-11-23 |
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| CN2011102403588A Pending CN102247380A (en) | 2011-08-19 | 2011-08-19 | Compound preparation with budesonide and indacaterol as the active components |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103784420A (en) * | 2014-02-18 | 2014-05-14 | 青岛市城阳区人民医院 | Indacaterol maleate liquid preparation and preparation method thereof |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1477963A (en) * | 2000-12-04 | 2004-02-25 | ��˹��ŵ�� | Organic compounds |
| WO2004028545A1 (en) * | 2002-09-25 | 2004-04-08 | Astrazeneca Ab | A COMBINATION OF A LONG-ACTING β2-AGONIST AND A GLUCOCORTICOSTEROID IN THE TREATMENT OF FIBROTIC DISEASES |
| WO2008102128A2 (en) * | 2007-02-19 | 2008-08-28 | Cipla Limited | Pharmaceutical combinations of at least two bronchodilators or of a bronchodilator with a corticosteroid |
| CN101321539A (en) * | 2005-12-21 | 2008-12-10 | Meda制药有限及两合公司 | Novel combination of anticholinergics, ss2-adrenoceptor agonists, antileukotrienes (leukotriene receptor antagonists), glucocorticoids and/or PDE 4 inhibitors for the treatment of inflammatory disease |
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2011
- 2011-08-19 CN CN2011102403588A patent/CN102247380A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1477963A (en) * | 2000-12-04 | 2004-02-25 | ��˹��ŵ�� | Organic compounds |
| WO2004028545A1 (en) * | 2002-09-25 | 2004-04-08 | Astrazeneca Ab | A COMBINATION OF A LONG-ACTING β2-AGONIST AND A GLUCOCORTICOSTEROID IN THE TREATMENT OF FIBROTIC DISEASES |
| CN101321539A (en) * | 2005-12-21 | 2008-12-10 | Meda制药有限及两合公司 | Novel combination of anticholinergics, ss2-adrenoceptor agonists, antileukotrienes (leukotriene receptor antagonists), glucocorticoids and/or PDE 4 inhibitors for the treatment of inflammatory disease |
| WO2008102128A2 (en) * | 2007-02-19 | 2008-08-28 | Cipla Limited | Pharmaceutical combinations of at least two bronchodilators or of a bronchodilator with a corticosteroid |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103784420A (en) * | 2014-02-18 | 2014-05-14 | 青岛市城阳区人民医院 | Indacaterol maleate liquid preparation and preparation method thereof |
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Application publication date: 20111123 |