CN1353980A - Quick-acting aerosol for relieving asthma and its preparation method - Google Patents
Quick-acting aerosol for relieving asthma and its preparation method Download PDFInfo
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- CN1353980A CN1353980A CN 01130404 CN01130404A CN1353980A CN 1353980 A CN1353980 A CN 1353980A CN 01130404 CN01130404 CN 01130404 CN 01130404 A CN01130404 A CN 01130404A CN 1353980 A CN1353980 A CN 1353980A
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Abstract
The present invention is characterized by that at the same time of diverting the propellant to HFC from CFCs, i.e, eliminating the possibility of damaging earth's ozonosphere, it provides a quick-acting asthma-relieving aerosol and its preparation process. The medicinal penetration accelerating agent selected by said invention can favourably make the drug approach to and penetrate into the target cell wall so as to make the drug attain the goal of quickly-acting. The invented medicine penetration accelerating agent also possesses suspension-supporting action capable of making drug more stable and corrective flavour action capable of producing nice and cool comfortable feeling in the patient's respiratory tract after the aerosol is sprayed by patient.
Description
The invention belongs to suppressing panting calming medicine preparation 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, ipratropium bromide aerosol, sodium cromoglicate aerosol, bufrolin aerosol, propionic acid beclometasone aerosol, budesonide aerosol, breathes heavily safe aerosol and Combivent aerosol or the like.A shortcoming of conventional aerosol is that its propellant contains the dichlorodifluoromethan hydro carbons, the destruction of its participation earth's ozone layer under a cloud.
When the objective of the invention is to turn to HFC promptly to eliminate from CFCs the propellant to earth depletion of the ozone layer probability, a kind of quick-acting aerosol for relieving asthma and preparation method thereof is proposed, so that on the basis of original HFC aerosol, further shorten responding time, make it more quick-acting.
Quick-acting aerosol for relieving asthma of the present invention, it is matched and is prepared from biphase aerosol, three-phase suspension aerosol carrier by medicine, pharmaceutical penetration enhancer, it is characterized in that medicine can select sodium cromoglicate, bufrolin, beclometasone, budesonide, albuterol, salmaterol, clenbuterol, fenoterol for use, adjoin Boot sieve, hexoprenaline, terbutaline, Flutropium Bromide, sodium nedocromil, ipratropium bromide or its compound, its consumption is 0.00001～10% of an aerosol content gross weight; Pharmaceutical penetration enhancer can be selected Oleum menthae, Mentholum, capric acid, lauric acid, laurocapram, lecithin, cineole 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 glycerol, Polyethylene Glycol, propylene glycol etc. for use, and its consumption is aerosol content gross weight 0-5%; Solvent can be selected ethanol, propanol, isopropyl alcohol, ethyl acetate etc. for use, and its consumption is aerosol content gross weight 5-50%; Propellant can select 1,1,1 for use, 2-tetrafluoroethane [hereinafter claiming HFC-134a] and 1,1,1,2,3,3, and 3-heptafluoro-propane [hereinafter claiming HFC-227], its consumption is the 50-95% of aerosol content gross weight; Three-phase suspension aerosol carrier is respectively: dispersant can be selected oleic acid, oleyl alcohol, Arlacel-85, Oleum menthae, Mentholum, capric acid, lauric acid, laurocapram, lecithin, cineole and Borneolum Syntheticum etc. for use, especially pharmaceutical penetration enhancer as: the whiles such as Oleum menthae, Mentholum, capric acid, lauric acid, laurocapram, lecithin, cineole and Borneolum Syntheticum should stress to select for use in the time of can doing dispersant, and its consumption is aerosol content gross weight 0.001-5%.The latent solvent matchmaker---HFC-134a solvability regulator can be selected ethanol, propanol, isopropyl alcohol, ethyl acetate, glycerol, Polyethylene Glycol, propylene glycol, Radix Oenotherae erythrosepalae oil, Semen Maydis oil, Oleum helianthi, soybean oil for use, and its consumption is the 0-5% of aerosol content gross weight; Propellant can select 1,1,1 for use, 2-tetrafluoroethane [hereinafter claiming HFC-134a] and 1,1,1,2,3,3,3-heptafluoro-propane [hereinafter claiming HFC-227], its consumption is the 95-99.99% 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 at low temperatures or in pressure vessel, be suspended in the mixed solution that contains dispersant, pharmaceutical penetration enhancer, solvent, latent solvent matchmaker and propellant with the solid drugs micropowder, to be mixed evenly after the assay was approved, 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%, solvent, 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: when turning to HFC promptly to eliminate from CFCs propellant, propose a kind of quick-acting aerosol for relieving asthma and preparation method thereof earth depletion of the ozone layer probability.The selected pharmaceutical penetration enhancer of the present invention helps the approaching and infiltration of medicine to the target cell wall, thereby make it the purpose that reaches quick-acting, also have suspending effect and taste-calibrating effect in the selected pharmaceutical penetration enhancer of this present invention simultaneously, but the suspending medicine is more stable, the school flavor produces a kind of nice and cool comfort immediately at respiratory tract after can making patient's spray delivery.
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 3300g
1,1,1, the 2-tetrafluoroethane adds to 14000g
Preparation technology:
Albuterol, Mentholum, propylene glycol are added respectively after ethanol makes it dissolving, stir, after the assay was approved, be sub-packed in 1000 bottles, the lid that has quantitative valve on the gland, and by every bottle of injection 1,1 of the valve on the lid, 1, the 2-tetrafluoroethane to 14g promptly.
Annotate: salmaterol aerosol, clenbuterol aerosol, sodium cromoglicate aerosol, bufrolin aerosol, propionic acid beclometasone aerosol, budesonide aerosol, terbutaline inhales, fenoterol aerosol, the embodiment that adjoins Boot sieve aerosol, hexoprenaline aerosol, Flutropium Bromide aerosol, sodium nedocromil aerosol, ipratropium bromide 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 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 3300g 1,1,1, the 2-tetrafluoroethane adds to 14000g
Preparation technology:
Albuterol, beclometasone, Mentholum, propylene glycol are added respectively after ethanol makes it dissolving, stir, after the assay was approved, be sub-packed in 1000 bottles, the lid that has quantitative valve on the gland, and by every bottle of injection 1,1 of the valve on the lid, 1, the 2-tetrafluoroethane 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 terbutaline three-phase suspension aerosols
Composition of raw materials:
Terbutaline 50g Mentholum 50g
Anhydrous sodium sulfate 40g ethanol 260g
1,1,1,2-tetrafluoroethane 13700g
Preparation technology:
To be crushed to terbutaline 50g below the 5 μ m via jet mill or oscillatory type pulverizer, anhydrous sodium sulfate 40g, add at low temperatures or under the high pressure 1 of the 50g Mentholum of mix homogeneously, 260g ethanol and 13700g, 1,1, in the 2-tetrafluoroethane mixed liquor, fully stir, make it even, after the assay was approved, be sub-packed in by the valve on the lid in the aluminum Room bottle of 1000 sealings, every bottle is injected admixing medical solutions 14g.
Annotate: salmaterol aerosol, clenbuterol aerosol, sodium cromoglicate aerosol, bufrolin aerosol, propionic acid beclometasone aerosol, budesonide aerosol, albuterol aerosol, fenoterol aerosol, the embodiment that adjoins Boot sieve aerosol, hexoprenaline aerosol, Flutropium Bromide aerosol, sodium nedocromil aerosol, ipratropium bromide aerosol and the foregoing description are identical, just on the basis of former aerosol, add appropriate amount of drug penetration enhancer and ethanol, so be omitted.
Embodiment 4: quick-acting salbutamols (albuterol) three-phase suspension aerosol
Composition of raw materials:
Albuterol 20g Mentholum 50g
Anhydrous sodium sulfate 20g 1,1,1,2-tetrafluoroethane 14000g
Preparation technology:
To be crushed to albuterol 20g below the 5 μ m via jet mill or oscillatory type pulverizer, anhydrous sodium sulfate 20g, add at low temperatures or under the high pressure 1 of the 50g Mentholum of mix homogeneously and 14000g, 1,1, in the 2-tetrafluoroethane mixed liquor, fully stir, make it even, after the assay was approved, be sub-packed in by the valve on the lid in the aluminum Room bottle of 1000 sealings, every bottle is injected admixing medical solutions 14g.
Embodiment 5: compound recipe albuterol (Combivent) three-phase suspension aerosol
Composition of raw materials:
Albuterol 20g ipratropium bromide 4g
Mentholum 50g anhydrous sodium sulfate 20g
Ethanol 150g 1,1,1,2-tetrafluoroethane 13800g
Preparation technology:
To be crushed to albuterol 20g, ipratropium bromide 4g below the 5 μ m via jet mill or oscillatory type pulverizer, anhydrous sodium sulfate 20g, add at low temperatures or under the high pressure 1 of the 50g Mentholum of mix homogeneously, 150g ethanol and 13800g, 1,1, in the 2-tetrafluoroethane mixed liquor, fully stir, make it even, after the assay was approved, be sub-packed in by the valve on the lid in the aluminum Room bottle of 1000 sealings, every bottle is injected admixing medical solutions 14g.
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 medicine, pharmaceutical penetration enhancer and aerosol carrier and forms, it is characterized in that medicine can select sodium cromoglicate, bufrolin, beclometasone, budesonide, albuterol, salmaterol, clenbuterol, fenoterol for use, adjoin Boot sieve, hexoprenaline, terbutaline, Flutropium Bromide, sodium nedocromil, ipratropium bromide or its compound, its consumption is 0.00001～10% of an aerosol content gross weight; Pharmaceutical penetration enhancer can be selected Oleum menthae, Mentholum, capric acid, lauric acid, laurocapram, lecithin, cineole and Borneolum Syntheticum for use, and its consumption is 0.001～5% of an aerosol content gross weight; The carrier of biphase aerosol is respectively: the latent solvent matchmaker can select glycerol, Polyethylene Glycol, propylene glycol etc. for use, and its consumption is aerosol content gross weight 0-5%; Solvent can be selected ethanol, propanol, isopropyl alcohol, ethyl acetate etc. for use, and its consumption is aerosol content gross weight 5-50%; Propellant can select 1,1,1 for use, 2-tetrafluoroethane and 1,1,1,2,3,3, and 3-heptafluoro-propane, its consumption are the 50-95% of aerosol content gross weight; Three-phase suspension aerosol carrier is respectively: dispersant can be selected oleic acid, oleyl alcohol, Arlacel-85, Oleum menthae, Mentholum, capric acid, lauric acid, laurocapram, lecithin, cineole and Borneolum Syntheticum etc. for use, especially pharmaceutical penetration enhancer as: the whiles such as Oleum menthae, Mentholum, capric acid, lauric acid, laurocapram, lecithin, cineole and Borneolum Syntheticum should stress to select for use in the time of can doing dispersant, and its consumption is aerosol content gross weight 0.001-5%; The latent solvent matchmaker---HFC-134a solvability regulator can be selected ethanol, propanol, isopropyl alcohol, ethyl acetate, glycerol, Polyethylene Glycol, propylene glycol, Radix Oenotherae erythrosepalae oil, Semen Maydis oil, Oleum helianthi, soybean oil for use, and its consumption is the 0-5% of aerosol content gross weight; Propellant can select 1,1,1 for use, 2-tetrafluoroethane and 1,1,1,2,3,3, and 3-heptafluoro-propane, its consumption are the 95-99.99% 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 at low temperatures or in pressure vessel, directly be suspended in and contain dispersant with the solid drugs micropowder behind the micronization, pharmaceutical penetration enhancer, solvent, in the mixing material of latent solvent matchmaker and propellant, to be mixed evenly after the assay was approved, directly inject the empty aluminum Room bottle that is stamped quantitative valve by the valve on the lid and get final product.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 01130404 CN1353980A (en) | 2001-11-14 | 2001-11-14 | Quick-acting aerosol for relieving asthma and its preparation method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 01130404 CN1353980A (en) | 2001-11-14 | 2001-11-14 | Quick-acting aerosol for relieving asthma and its preparation method |
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| Publication Number | Publication Date |
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| CN1353980A true CN1353980A (en) | 2002-06-19 |
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| CN 01130404 Pending CN1353980A (en) | 2001-11-14 | 2001-11-14 | Quick-acting aerosol for relieving asthma and its preparation method |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100551988C (en) * | 2007-02-27 | 2009-10-21 | 江苏阳生生物工程有限公司 | Not the aerosol safety in fluorine-containing Lyons, efficient complex spreading system |
| 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 |
| CN101889993B (en) * | 2009-05-19 | 2013-03-27 | 扬州市三药制药有限公司 | Surface-modified salbutamol suspension type non-Freon inhalation aerosol and preparation method thereof |
| CN109646400A (en) * | 2018-12-25 | 2019-04-19 | 上海信谊百路达药业有限公司 | A kind of budesonide inhalation aerosol and preparation method thereof |
-
2001
- 2001-11-14 CN CN 01130404 patent/CN1353980A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100551988C (en) * | 2007-02-27 | 2009-10-21 | 江苏阳生生物工程有限公司 | Not the aerosol safety in fluorine-containing Lyons, efficient complex spreading system |
| CN101889993B (en) * | 2009-05-19 | 2013-03-27 | 扬州市三药制药有限公司 | Surface-modified salbutamol suspension type non-Freon inhalation aerosol and preparation method thereof |
| 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 |
| CN109646400A (en) * | 2018-12-25 | 2019-04-19 | 上海信谊百路达药业有限公司 | A kind of budesonide inhalation aerosol and preparation method thereof |
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