CN1216600C - Levo-salbutamol hydrochloride aerosol and its prepn. - Google Patents
Levo-salbutamol hydrochloride aerosol and its prepn. Download PDFInfo
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- CN1216600C CN1216600C CN 02111473 CN02111473A CN1216600C CN 1216600 C CN1216600 C CN 1216600C CN 02111473 CN02111473 CN 02111473 CN 02111473 A CN02111473 A CN 02111473A CN 1216600 C CN1216600 C CN 1216600C
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- supplementary material
- aerosol
- levo
- qualified
- exsiccator
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Abstract
The present invention provides an L-albuterol hydrochloride aerosol and a preparing method, which belong to the technical field of medicinal preparations. When used, the aerosol of the present invention can rapidly increase the concentration in the lung, and has the characteristics of rapid effect, easy use, convenient portability because of a small volume and good clinical application prospects.
Description
Technical field
The invention belongs to technical field of medicine.Be specifically related to levo-salbutamol hydrochloride aerosol and preparation technology.
Background technology
Levalbuterol is third generation β
2Receptor stimulating agent, be in the treating asthma medicine first listing have optically active new drug, get by the resolving racemic albuterol by U.S. Sepracor company (chiral drug specialty manufacturer).A large amount of clinical trial certificates, Levalbuterol has been compared following advantage with raceme:
1. strong drug action.The drug effect of reported in literature Levalbuterol is 64 times of d-isomer.Clinical trial certificate, levo form are than the strong at least 4-10 of raceme drug effect doubly.
2. side effect is little.Slow 10 times of d-isomer internal metabolism speed than levo form, and d-isomer can increase bronchial reactivity.
In addition, the clinical data that American Lung Association and the conference of chest disease association provide shows that also this product obviously is better than raceme to the improvement of patient's pulmonary function.
Related product:
Xopenex
TM---the albuterol hydrochloride inhalant, U.S. Sepracor company produces, with the nebulizer administration.
Summary of the invention
Technical problem to be solved by this invention is to develop other dosage form of albuterol hydrochloride, makes its drug effect rapid-action, easy to use.
The invention provides levo-salbutamol hydrochloride aerosol.This aerosol is that 0.01-0.2% is that 99.99-99.8% forms with containing medicinal adjuvant by hydrochloric Levalbuterol by weight percentage.
Above-mentioned pharmaceutic adjuvant has:
Dosage of surfactant scope 0.01-0.5% (w/w), as:
The fatty acid esters of sorbitan class, as: span20, span60, span65, span80, span85;
The polyoxyethylene sorbitan fatty acid ester class, as: tween20, tween80;
The polyoxyethylene fatty acid ester class, as: Myrij;
The polyoxyethylene aliphatic alcohol ether class, as: Brij30, Brij35, Cetomacrogol, Peregol O;
Poloxalkol, as: Pluronic F-68;
The third oxygen polyethylene glycols, as: Antarox 31R1;
Polyethylene glycols, as: PEG 300;
Phospholipid, as: soybean phospholipid, lecithin etc.;
Oleic acid;
Mannitol.
Proportion regulator amount ranges 0.01-0.5% (w/w), as: Pulvis Talci, anhydrous sodium sulfate, sodium chloride etc.
Propellant amount ranges 90-98% (w/w), as: isceon (F
11), dichlorodifluoromethane (F
12), Dichlorotetrafluoromethane (F
114), tetrafluoroethane (F
134a), heptafluoro-propane (F
227) dichloro one fluoroethane (F
141b), chlorodifluoroethane (F
142b), Difluoroethane (F
152a) etc.
Another technical problem to be solved of the present invention has provided the preparation technology of levo-salbutamol hydrochloride aerosol, and this method comprises the following steps:
(1) with supplementary material respectively at vacuum drying oven inner drying a few hours, put the exsiccator internal cooling to room temperature;
(2) supplementary material is pulverized with jet mill.Supplementary material after micropowder is handled is through 400 power microscope inspections, and is standby in the qualified rearmounted exsiccator;
(3) take by weighing supplementary material by recipe quantity, place in the special sealing mixer, stir, do the intermediate of sample and measure.Measure qualified after in accordance with regulations amount pour in the hermetic container, pour into propellant again to ormal weight;
Perhaps:
(1) with supplementary material respectively at vacuum drying oven inner drying a few hours, put the exsiccator internal cooling to room temperature;
(2) supplementary material is pulverized with jet mill.Supplementary material after micropowder is handled is through 400 power microscope inspections, and is standby in the qualified rearmounted exsiccator;
(3) take by weighing supplementary material by recipe quantity, place in the special sealing mixer that pressure is arranged, stir, do the intermediate of sample and measure.Measure qualified after in accordance with regulations amount pour in the hermetic container.
Levo-salbutamol hydrochloride aerosol of the present invention and albuterol hydrochloride inhalant relatively have following advantage:
(1) target organ---the concentration of pulmonary increases rapidly because of it arrives, so to compare onset faster with traditional tablet;
(2) compare with existing atomized inhalation, easy to use;
(3) volume is little, and is easy to carry.
(albuterol, salbutamol), the trade name salbutamol is the β that is widely used in treating asthma to albuterol
2Receptor stimulating agent.Because its curative effect is safe and reliable certainly, action time is long and dosage form is complete, once enters the ranks of the world's ten big best-selling drugses, and 1998 annual sales amounts still reach 1,200,000,000 dollars.Home sale is raceme at present.Clinical trial shows that its laevoisomer (claiming the R-isomer again) will obviously be better than raceme to the improvement of patient's pulmonary function.
The specific embodiment
Embodiment 1
Levalbuterol 2.5mg
Span20 3mg
Pulvis Talci 4mg
Isceon adds to capacity
Embodiment 2
Levalbuterol 5mg
tween80 6mg
Sodium sulfate 7mg
Dichlorodifluoromethane adds to capacity
Embodiment 3
Levalbuterol 10mg
Brij?35 12mg
Sodium chloride 14mg
Tetrafluoroethane adds to capacity
Embodiment 4
Levalbuterol 20mg
Pluronic?F-68 25mg
Pulvis Talci 35mg
Heptafluoro-propane adds to capacity
Embodiment 5
Levalbuterol 2.5mg
PEG?300 3mg
Pulvis Talci 4mg
Dichloro one fluoroethane adds to capacity
Embodiment 6
Levalbuterol 5mg
Lecithin 6mg
Sodium sulfate 7mg
Chlorodifluoroethane adds to capacity
Embodiment 7
Levalbuterol 10mg
Oleic acid 12mg
Sodium chloride 14mg
Tetrafluoroethane adds to capacity
Embodiment 8
Levalbuterol 20mg
Mannitol 25mg
Sodium chloride 35mg
Difluoroethane adds to capacity
Claims (2)
1. levo-salbutamol hydrochloride aerosol is characterized in that this aerosol is made up of following component:
Levalbuterol 5mg
Lecithin 6mg
Sodium sulfate 7mg
Chlorodifluoroethane adds to capacity.
2. the preparation technology of a levo-salbutamol hydrochloride aerosol as claimed in claim 1 is characterized in that this method comprises the following steps:
(1) with supplementary material respectively at vacuum drying oven inner drying a few hours, put the exsiccator internal cooling to room temperature;
(2) supplementary material is pulverized with jet mill, the supplementary material after micropowder is handled is through 400 power microscope inspections, and is standby in the qualified rearmounted exsiccator;
(3) take by weighing supplementary material by recipe quantity, place in the special sealing mixer, stir, do the intermediate of sample and measure, measure qualified after in accordance with regulations amount pour in the hermetic container, pour into propellant again to ormal weight;
Perhaps:
(1) with supplementary material respectively at vacuum drying oven inner drying a few hours, put the exsiccator internal cooling to room temperature;
(2) supplementary material is pulverized with jet mill, the supplementary material after micropowder is handled is through 400 power microscope inspections, and is standby in the qualified rearmounted exsiccator;
(3) take by weighing supplementary material by recipe quantity, place in the special sealing mixer that pressure is arranged, stir, do the intermediate of sample and measure, measure qualified after in accordance with regulations amount pour in the hermetic container.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02111473 CN1216600C (en) | 2002-04-24 | 2002-04-24 | Levo-salbutamol hydrochloride aerosol and its prepn. |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02111473 CN1216600C (en) | 2002-04-24 | 2002-04-24 | Levo-salbutamol hydrochloride aerosol and its prepn. |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1389202A CN1389202A (en) | 2003-01-08 |
| CN1216600C true CN1216600C (en) | 2005-08-31 |
Family
ID=4741587
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 02111473 Expired - Lifetime CN1216600C (en) | 2002-04-24 | 2002-04-24 | Levo-salbutamol hydrochloride aerosol and its prepn. |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1216600C (en) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007020204A2 (en) * | 2005-08-12 | 2007-02-22 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Hfc solution formulations for inhalation containing salbutamol hydrochloride or salbutamol citrate |
| CN101849928A (en) * | 2009-03-30 | 2010-10-06 | 北京利乐生制药科技有限公司 | Inhalation preparation for treating asthma, preparation method and application thereof |
| 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 |
| GB201117621D0 (en) | 2011-10-12 | 2011-11-23 | Mexichem Amanco Holding Sa | Compositions |
| CN102871967B (en) * | 2012-09-18 | 2013-09-25 | 刘晓忠 | Preparation of salified medicinal particles of levosalbutamol and traditional Chinese medicine monomer and preparation of particle inhalable aerosol |
| GB201306984D0 (en) | 2013-04-17 | 2013-05-29 | Mexichem Amanco Holding Sa | Composition |
| ES2949975T3 (en) | 2016-09-19 | 2023-10-04 | Mexichem Fluor Sa De Cv | Pharmaceutical composition comprising indacaterol |
| UA123919C2 (en) | 2016-09-19 | 2021-06-23 | Мехікем Флуор С.А. Де С.В. | Pharmaceutical composition |
| BR112019005168A2 (en) | 2016-09-19 | 2019-06-11 | Mexichem Fluor Sa De Cv | pharmaceutical composition, sealed container, metered dose inhaler, and methods for treating a patient suffering or likely to suffer from a respiratory disorder, for improving the stability of a pharmaceutical composition and the aerosolization performance of a pharmaceutical composition global warming potential of a pharmaceutical composition |
| CN106727318A (en) * | 2016-12-22 | 2017-05-31 | 山东京卫制药有限公司 | A kind of aerosol and preparation method thereof |
-
2002
- 2002-04-24 CN CN 02111473 patent/CN1216600C/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| CN1389202A (en) | 2003-01-08 |
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| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| ASS | Succession or assignment of patent right |
Owner name: XINYI PHARMACEUTICAL FACTORY Free format text: FORMER OWNER: SHANGHAI XINYI PHARMACEUTICAL CO., LTD. Effective date: 20040917 |
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| TA01 | Transfer of patent application right |
Effective date of registration: 20040917 Address after: 201206 No. 905 Jinqiao Road, Shanghai Applicant after: Sine Pharmaceutical Factory Co., Ltd. Address before: 200085 No. 71, Shanghai, North Sichuan Road Applicant before: Xinyi Pharmaceutic Co., Ltd., Shanghai |
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Owner name: SHANGHAI SINE PHARMACEUTICAL FACTORY CO., LTD. Free format text: FORMER NAME: SINE PHARMACY FACTORY |
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| CP03 | Change of name, title or address |
Address after: No. 905 Jinqiao Road, Shanghai, Pudong New Area Patentee after: Shanghai Sine Pharmaceutical Co., Ltd. Address before: No. 905 Jinqiao Road, Shanghai Patentee before: Sine Pharmaceutical Factory Co., Ltd. |
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| C56 | Change in the name or address of the patentee | ||
| CP01 | Change in the name or title of a patent holder |
Address after: 201206 Pudong New Area new Jinqiao Road, Shanghai, No. 905 Patentee after: Shanghai Xinyi Pharmaceutical Co. Ltd.. Address before: 201206 Pudong New Area new Jinqiao Road, Shanghai, No. 905 Patentee before: Shanghai Sine Pharmaceutical Co., Ltd. |
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| CX01 | Expiry of patent term | ||
| CX01 | Expiry of patent term |
Granted publication date: 20050831 |