CN1298699A - Quick acting aerosol for treating asthma and preparing process thereof - Google Patents
Quick acting aerosol for treating asthma and preparing process thereof Download PDFInfo
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- CN1298699A CN1298699A CN 00131828 CN00131828A CN1298699A CN 1298699 A CN1298699 A CN 1298699A CN 00131828 CN00131828 CN 00131828 CN 00131828 A CN00131828 A CN 00131828A CN 1298699 A CN1298699 A CN 1298699A
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Abstract
A quick-effect asthma relieving aerosol preparation is characterized by that on the basis of original aerosol preparation, a medicine penetration promoting agent is added which can achieve the aim of quickly taking effect.
Description
The invention belongs to suppressing panting calming medicine and preparation technology thereof.
The class aerosol of relievining asthma commonly used both at home and abroad at present has albuterol aerosol, salmaterol aerosol, clenbuterol aerosol, the second third holder bromine ammonium aerosol, sodium cromoglicate aerosol, bufrolin aerosol, propionic acid beclometasone aerosol, budesonide aerosol and breathes heavily safe aerosol, Combivent aerosol etc.These aerosols all took effect at 3～10 minutes after sucking, and effect in 30～60 minutes reaches the peak, acts on sustainable 4,6,12 hours, and its curative effect is very sure.But for asthmatic patient, particularly those asthma patient with severe symptoms these 3,10,30 minutes also was the very long time that makes the patient very hard to bear.
The objective of the invention is to propose a kind of quick-acting aerosol for relieving asthma and preparation method thereof,, make it more quick-acting so that on the basis of original aerosol, further shorten responding time.
Quick-acting aerosol for relieving asthma of the present invention, main is that raw material matches and is prepared from biphase aerosol, three-phase suspension aerosol carrier with medicine, pharmaceutical penetration enhancer, it is characterized in that medicine is sodium cromoglicate, bufrolin, beclometasone, budesonide, albuterol, salmaterol, clenbuterol, ipratropium bromide or its compound, its consumption is 0.0001～10% of an aerosol content gross weight; Pharmaceutical penetration enhancer can be selected Oleum menthae, Mentholum, eucalyptus oil and Borneolum Syntheticum for use, and its consumption is 0.001～5% of an aerosol content gross weight; Aerosol carrier: the carrier of biphase aerosol is respectively: the latent solvent matchmaker can select propylene glycol etc. for use, and its consumption is aerosol content gross weight 0-5%; Solvent can be selected ethanol etc. for use, and its consumption is aerosol content gross weight 10-50%; Propellant can be selected dichlorodifluoromethane, tetrafluoroethane and heptafluoro-propane for use, its consumption is the 50-90% of aerosol content gross weight, three-phase suspension aerosol carrier is respectively: dispersant can be selected oleic acid, oleyl alcohol, Arlacel-85 and lecithin etc. for use, and its consumption is aerosol content gross weight 0-5%.The latent solvent matchmaker can select isceon and dichlorotetra-fluoroethane for use, and its consumption is the 10-50% of aerosol content gross weight; Propellant can be selected dichlorodifluoromethane, tetrafluoroethane and heptafluoro-propane for use, its consumption is the 40-90% of aerosol content gross weight, preparation method: the preparation method of biphase aerosol by batching, adjustment, packing, gland, charge into several procedures such as propellant and finish, it is characterized in that pharmaceutical penetration enhancer can directly add also can be by adding in the propellant in the solvent; The preparation method of three-phase aerosol by micronization, batching, adjustment, packing, gland, charge into several procedures such as propellant and finish.Or the solid drugs micropowder is suspended in pressure vessel among the latent solvent matchmaker and propellant of containing dispersant, pharmaceutical penetration enhancer, directly inject the empty aluminum Room bottle that is stamped quantitative valve and get final product.Wherein the micronization operation can be selected spray drying method, crystallization control method, air-flowing type comminuting method for use, or oscillatory type micronizing method, the granularity of solid material is crushed to below the 5 μ m, otherwise medicine does not reach alveolar, production overall process before the gland all should be controlled temperature, humidity and moisture content, temperature is below 20 ℃, humidity is at relative humidity below 40%, latent solvent matchmaker, propellant should be done before use except that water treatment, finished product moisture content should be controlled at below the 300PPM, the homogeneity of temperature high product is poor, and the stability of humidity, moisture content high product will be affected.
The invention has the advantages that: thus the selected pharmaceutical penetration enhancer of quick-acting aerosol for relieving asthma of the present invention help medicine to the target cell wall near and the infiltration make it to reach quick-acting, after also having taste-calibrating effect, can make patient's spray delivery, the selected pharmaceutical penetration enhancer of this present invention simultaneously produces a kind of nice and cool comfort immediately at respiratory tract.
Embodiments of the invention:
Embodiment 1: the biphase aerosol of quick-acting salbutamols (albuterol)
Composition of raw materials:
Albuterol 28g Mentholum 50g
Propylene glycol 350g ethanol 3322g
Dichlorodifluoromethane adds to 14000g
Preparation technology:
With albuterol, Mentholum, propylene glycol add respectively ethanol make it the dissolving after, stir, after the assay was approved, be sub-packed in 1000 bottles, have the lid of quantitative valve on the gland, and by every bottle on the valve on the lid inject dichlorodifluoromethane to 14g promptly.
Annotate: embodiment and the foregoing description of biphase salmaterol aerosol, clenbuterol aerosol, the second third holder bromine ammonium aerosol, propionic acid beclometasone aerosol are identical, just add the appropriate amount of drug penetration enhancer on the basis of former aerosol, so be omitted.
Embodiment 2: the biphase aerosol of compound quick-acting albuterol (breathing heavily Thailand)
Composition of raw materials:
Albuterol 28g beclometasone 14g
Mentholum 50g propylene glycol 350g
Ethanol 3308g dichlorodifluoromethane adds to 14000g
Preparation technology:
With albuterol, beclometasone, Mentholum, propylene glycol add respectively ethanol make it the dissolving after, stir, after the assay was approved, be sub-packed in 1000 bottles, have the lid of quantitative valve on the gland, and by every bottle on the valve on the lid inject dichlorodifluoromethane to 14g promptly.
Annotate: the embodiment of compound recipe aerosol, albuterol and the ipratropium bromide of biphase albuterol and two kinds of medicines of ipratropium bromide and the compound recipe aerosol of three kinds of medicines of beclometasone and the foregoing description are identical, just on the basis of former aerosol, add the appropriate amount of drug penetration enhancer, so be omitted.
Embodiment 3: quick-acting salbutamols (albuterol) three-phase suspension aerosol
Composition of raw materials:
Albuterol 20g Mentholum 50g
Anhydrous sodium sulfate 20g Arlacel-85,25g
Isceon 5000g dichlorodifluoromethane 9000g
Preparation technology:
To be crushed to albuterol 20g below the 5 μ m via jet mill or oscillatory type pulverizer, anhydrous sodium sulfate 20g, after placing the 2000g isceon that contains the 25g Arlacel-85 to stir under 9 ℃, move in the adjustment jar, with the 50g Mentholum add make it in the remaining 3000g isceon dissolving after, move in the above-mentioned adjustment jar, stir, after the assay was approved, be sub-packed in 1000 aluminum Room bottles, the lid that has quantitative valve on the gland, and by every bottle of injection of the valve on lid 9g dichlorodifluoromethane promptly.
Annotate: the embodiment of salmaterol aerosol, clenbuterol aerosol, sodium cromoglicate aerosol, bufrolin aerosol, propionic acid beclometasone aerosol, budesonide aerosol and the foregoing description are identical, just on the basis of former aerosol, add the appropriate amount of drug penetration enhancer, so be omitted.
Embodiment 4: compound recipe albuterol (Combivent) three-phase suspension aerosol
Composition of raw materials:
Albuterol 20g ipratropium bromide 4g
Mentholum 50g anhydrous sodium sulfate 20g
Arlacel-85,25g isceon 5000g
Dichlorodifluoromethane 9000g
Preparation technology:
To be crushed to albuterol 20g, ipratropium bromide 4g, anhydrous sodium sulfate 20g below the 5 μ m via jet mill or oscillatory type pulverizer, after placing the 2000g isceon that contains the 25g Arlacel-85 to stir under 9 ℃, move in the adjustment jar, with the 50g Mentholum add make it in the remaining 3000g isceon dissolving after, move in the above-mentioned adjustment jar, stir, after the assay was approved, be sub-packed in 1000 aluminum Room bottles, the lid that has quantitative valve on the gland, and by every bottle of injection of the valve on lid 9g dichlorodifluoromethane promptly.
Annotate: the embodiment of the compound recipe three-phase aerosol of compound recipe three-phase aerosol, albuterol and the beclometasone of albuterol and beclometasone and three kinds of medicines of ipratropium bromide and the foregoing description are identical, just on the basis of former aerosol, add the appropriate amount of drug penetration enhancer, so be omitted.
Claims (3)
1, a kind of quick-acting aerosol for relieving asthma, it is prepared by principal agent part, pharmaceutical penetration enhancer and aerosol carrier and forms, it is characterized in that medicine is sodium cromoglicate, bufrolin, beclometasone, budesonide, albuterol, salmaterol, clenbuterol, ipratropium bromide or its compound, its consumption is the 0.0001-10% of aerosol content gross weight: pharmaceutical penetration enhancer can be selected Oleum menthae, Mentholum, eucalyptus oil and Borneolum Syntheticum for use, and its consumption is the 0.001-5% of aerosol content gross weight; The carrier of biphase aerosol is respectively: the latent solvent matchmaker can select propylene glycol etc. for use, and its consumption is aerosol content gross weight 0-5%; Solvent can be selected ethanol etc. for use, and its consumption is aerosol content gross weight 10-50%; Propellant can be selected dichlorodifluoromethane, tetrafluoroethane and heptafluoro-propane for use, its consumption is the 50-90% of aerosol content gross weight, suspension type three-phase aerosol carrier is respectively: dispersant can be selected oleic acid, oleyl alcohol, Arlacel-85, lecithin for use, its consumption is the 0-5% of aerosol content gross weight, and it is the 10-50% of aerosol content gross weight that the latent solvent matchmaker can select isceon and dichlorotetra-fluoroethane, its consumption for use; Propellant can be selected dichlorodifluoromethane, tetrafluoroethane and heptafluoro-propane for use, and its consumption is the 40-90% of aerosol content gross weight.
2, the preparation method of the biphase aerosol of a kind of quick-acting asthma-relieving: it is by the described medicine of claim 1, pharmaceutical penetration enhancer, aerosol carrier and proportioning thereof, by batching, adjustment, packing, gland, charge into that several procedures such as propellant finish, it is characterized in that pharmaceutical penetration enhancer can directly add also can be by adding in the propellant in the solvent.
3, a kind of preparation method of quick-acting asthma-relieving three-phase suspension aerosol: it is by the described medicine of claim 1, pharmaceutical penetration enhancer, aerosol carrier and proportioning thereof, pass through micronization, batching, adjust, packing, gland, charge into that several procedures such as propellant finish, no matter the micronization that it is characterized in that solid drugs is via spray drying, crystallization control or pulverize its particle diameter and all should be controlled at below the 5 μ m, batching, adjust, packing, the temperature of several procedures such as gland should be controlled at below 20 ℃, relative humidity should be controlled at below 40%, or the solid drugs micropowder behind the micronization directly is suspended in pressure vessel contains dispersant, among the latent solvent matchmaker and propellant of pharmaceutical penetration enhancer, and the empty aluminum Room bottle that is stamped quantitative valve by the direct injection of the valve on the lid gets final product.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 00131828 CN1298699A (en) | 2000-02-15 | 2000-11-05 | Quick acting aerosol for treating asthma and preparing process thereof |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 00101292 CN1265887A (en) | 2000-02-15 | 2000-02-15 | Quick-acting asthma-relieving aerosol and its preparation method |
| CN00101292.4 | 2000-02-15 | ||
| CN 00131828 CN1298699A (en) | 2000-02-15 | 2000-11-05 | Quick acting aerosol for treating asthma and preparing process thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1298699A true CN1298699A (en) | 2001-06-13 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 00131828 Pending CN1298699A (en) | 2000-02-15 | 2000-11-05 | Quick acting aerosol for treating asthma and preparing process thereof |
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| Country | Link |
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| CN (1) | CN1298699A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102416179A (en) * | 2010-09-28 | 2012-04-18 | 健乔信元医药生技股份有限公司 | Inhaled compound composition for asthma |
| CN105476961A (en) * | 2015-12-16 | 2016-04-13 | 武汉同济现代医药科技股份有限公司 | Beclomethasone aerosol and preparation method thereof |
-
2000
- 2000-11-05 CN CN 00131828 patent/CN1298699A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102416179A (en) * | 2010-09-28 | 2012-04-18 | 健乔信元医药生技股份有限公司 | Inhaled compound composition for asthma |
| CN102416179B (en) * | 2010-09-28 | 2014-05-07 | 益得生物科技股份有限公司 | Inhaled compound composition for asthma |
| CN105476961A (en) * | 2015-12-16 | 2016-04-13 | 武汉同济现代医药科技股份有限公司 | Beclomethasone aerosol and preparation method thereof |
| CN105476961B (en) * | 2015-12-16 | 2019-01-04 | 武汉同济现代医药科技股份有限公司 | A kind of beclometasone dipropionate aerosol and preparation method thereof |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |