CN101548943A - Inhalation nebulizer containing formoterol - Google Patents
Inhalation nebulizer containing formoterol Download PDFInfo
- Publication number
- CN101548943A CN101548943A CNA2008101033238A CN200810103323A CN101548943A CN 101548943 A CN101548943 A CN 101548943A CN A2008101033238 A CNA2008101033238 A CN A2008101033238A CN 200810103323 A CN200810103323 A CN 200810103323A CN 101548943 A CN101548943 A CN 101548943A
- Authority
- CN
- China
- Prior art keywords
- acid
- formoterol
- solution
- buffer
- sodium
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention relates to a solution containing formoterol. When the solution is used, the content is released out in a mist state under various pressures of a hand pump, an ultrasonic nebulizer, an air compressor, and the like, and is used for pulmonary medicament inhalation delivery.
Description
Technical field
The present invention relates to a kind of solution that contains formoterol, by manual pump, ullrasonic spraying, air compressor equal pressure content is vaporific during use and disengages, is to be used for the preparation that pulmonary sucks.
Background technology
Chronic obstructive pulmonary disease (COPD) is the stable a kind of respiratory system disease that rises of whole world sickness rate, and the most patient of suffering from copd is the lung disease of suffering from by smoking.According to the trend of smoking, it will rise to the 5th of pandemic to the year two thousand twenty in the whole world.
β
2-adrenoreceptor agonists becomes a line medicine for the treatment of asthma for many years owing to having very strong promotion bronchiectatic activity.Formoterol is by the deutero-N-anilide of epinephrine, is a selectivity β
2-3 adrenergic receptor agonists.For the patient of reversibility obstructive respiration disease, formoterol has bronchiectasic effect.Its acting duration is long, and after suction, only 1～3 minute curative effect promptly begins to manifest, and its bronchiectasic effect can obviously continue 12 hours.In addition, formoterol also has anti-allergy action and pulmonary edema inhibitory action, to chronic occlusion lung disease effectiveness height such as bronchial asthmas to respiratory tract selectivity height.
CN 1187044C discloses a kind of storable active substance concentrate that contains formoterol.Formoterol is dissolved or suspended in the liquid suitable on the pharmacology and the solution or the suspension that obtain with the high concentration conc forms.This concentrated solution is not suitable for direct administration, especially is not suitable for direct suction.Must convert this concentrated solution to pharmaceutical preparation with acceptable liquid diluting before using, this pharmaceutical preparation can change into the preparation that can suck by means of aerosol apparatus.
CN 1399540A discloses a kind of aerosol combination that comprises formoterol.This invention provides a kind of pharmaceutical composition of dry powder form, is used for sucking the treatment chronic obstructive pulmonary disease.This dry powder can use by incapsulating to be placed on to suck in the powder inhaler, also can be present in the storage storehouse of the multidose dry powder inhaler that is applicable to convey unit dosage.
CN 1638730A discloses a kind of formoterol superfine formulation.This invention provides a kind of medical aerosol pharmaceutical solutions by the pMDI administration, comprises formoterol as active component, HFA propellant and an amount of cosolvent, and wherein said active component is dissolved in propellant-cosolvent system fully.
CN 1243435A discloses a kind of new formulation for inhalation that contains formoterol that bulk density is 0.28～0.38g/ml that injects.This invention provides a kind of dry powder agent composite, wherein comprises formoterol and a kind of carrier mass, and these two kinds of materials all are fine form.This available any known Diskus administration of filling a prescription can be single dose or multi-dose inhaler, can also be a kind of respiration drive Diskus.
Because the poor stability of formoterol in solution, so many mode administrations that sucks with powder.Be the droplet shape after the aerosol inhalation solution atomizing, than dry powder inhaler formulations, absorption is fast, curative effect is rapid.Though CN 1187044C discloses a kind of storable active substance concentrate that contains formoterol, use inconvenience, need just can use after the dilution.In addition, spray does not contain propellant than aerosol, can avoid to the pollution of atmospheric environment with to the stimulation of respiratory tract.
The invention provides a kind of solution that contains formoterol, can content be vaporific by manual pump, ullrasonic spraying, air compressor equal pressure during use and disengage, be used for pulmonary's inhalation.The invention has the advantages that not contain propellant, the storage that formoterol solution can be steady in a long-term, and the direct inhalation in atomizing back, easy to use.
Summary of the invention
The applicant finds the formoterol raw material to thermally labile, poor stability in the aqueous solution.The preparation of formoterol adopts the form of powder inhalation more at present.
The objective of the invention is to, preparation does not contain the formoterol solution of propellant, and active component therein can existence steady in a long-term.During use, need not the dilution directly with atomising device with solution atomization after inhalation get final product.
The formoterol solution that does not contain propellant provided by the invention, described formoterol are acceptable salt form or hydrate forms on free alkali form and the pharmacology thereof.
Formoterol solution provided by the invention, acceptable salt form is selected from the salt form that formoterol becomes with hydrochloric acid, nitric acid, phosphoric acid, sulphuric acid, acetic acid, citric acid, fumaric acid, tartaric acid, maleic acid, succinic acid, lactic acid, malic acid, benzoic acid, formic acid or propanoic acid on the described pharmacology.
Formoterol solution provided by the invention contains the formoterol of 2.5 μ g/ml～15 μ g/ml.
Formoterol solution provided by the invention, selecting water, ethanol or the mixture of the two for use is solvent.
Formoterol solution provided by the invention, pH value are 3.0～7.0.
Formoterol solution provided by the invention adopts glycine-hydrochloride buffer, phthalic acid-hydrochloride buffer, sodium hydrogen phosphate-citrate buffer solution, citric acid-sodium hydroxide-hydrochloride buffer, citric acid-sodium citrate buffer, acetic acid-sodium acetate buffer, PBS buffer or boric acid-borate buffer solution as buffer system.
Formoterol solution provided by the invention contains osmotic pressure regulator.
Formoterol solution provided by the invention contains antioxidant, comprises ascorbic acid, sodium sulfite, sodium formaldehyde sulphoxylate, sodium pyrosulfite.
Formoterol solution provided by the invention, the preferred ascorbic acid of antioxidant.
Formoterol solution provided by the invention contains chelating agent, comprises EDTA or its salt.
Formoterol solution provided by the invention, the preferred ethylenediaminetetraacetic acid of chelating agent-calcium disodium.
Formoterol solution provided by the invention is characterized in that and can it be the vaporific administration that disengages by manual pump, air compression, ullrasonic spraying equal pressure.
The specific embodiment
Embodiment 1
Prescription is formed
Title is formed
Formoterol 5mg
Citric acid 2g
Sodium citrate 9g
Sodium chloride 4g
Add water to 2000ml
Preparation method:
Get recipe quantity citric acid, sodium citrate, sodium chloride and be dissolved in the sterilized water for injection, after the stirring and dissolving, add the recipe quantity formoterol, stir and make dissolving, add sterilized water for injection, filter, promptly get 1000 with sintered glass filter-bulb to full dose.PH value is 5.0.
Embodiment 2
Prescription is formed
Title is formed
Formoterol tartrate 22mg
Sodium acetate 19g
Sodium chloride 3g
Ascorbic acid 50mg
Add water to 2000ml
Preparation method:
Get recipe quantity sodium acetate, sodium chloride, ascorbic acid and be dissolved in the sterilized water for injection, after the stirring and dissolving, add the recipe quantity formoterol tartrate, stirring makes molten, regulates pH value to 4.0 with the 3mol/L acetic acid solution, adds water to full dose again, filter with sintered glass filter-bulb, promptly get 1000.
Embodiment 3
Prescription is formed
Title is formed
Formoterol 30mg
Sodium hydrogen phosphate 8g
Potassium dihydrogen phosphate 20g
Sodium chloride 2g
Sodium formaldehyde sulphoxylate 60mg
Ethylenediaminetetraacetic acid-calcium disodium 300mg
Add water to 2000ml
Preparation method:
Get recipe quantity sodium hydrogen phosphate, potassium dihydrogen phosphate, sodium chloride, sodium formaldehyde sulphoxylate, ethylenediaminetetraacetic acid-calcium disodium and be dissolved in the sterilized water for injection, after the stirring and dissolving, add the recipe quantity formoterol, stirring makes molten, add water to full dose again, filter, promptly get 1000 with sintered glass filter-bulb.PH value is 6.5.
Formoterol sucks the droplet measure of spread of solution
With reference to the droplet measure of spread method of 2005 editions appendix X of Chinese Pharmacopoeia H suction spray, the droplet of measuring the embodiment of the invention one distributes.The droplet medication amount is 52% of every spray drug content labelled amount as a result, meets the requirement of Chinese Pharmacopoeia.
Stability study:
Long term test
The formoterol solution of embodiment one of preparation was placed 9 months under 6 ℃ ± 2 ℃ condition,, be the results are shown in following table respectively at 0,3,6,9 month sample analysis.
Table 1 long-term test results
Stability test is the result show, formoterol solution of the present invention is long-term to be placed 9 months, and character, pH value, related substance, content all do not have significant change.Illustrate that formoterol solution of the present invention has good stable.
Claims (10)
1. a formoterol solution that does not contain propellant is characterized in that described formoterol is acceptable salt form or a hydrate forms on free alkali form and the pharmacology thereof.
2. formoterol solution as claimed in claim 1 is characterized in that acceptable salt form is selected from the salt form that formoterol becomes with hydrochloric acid, nitric acid, phosphoric acid, sulphuric acid, acetic acid, citric acid, fumaric acid, tartaric acid, maleic acid, succinic acid, lactic acid, malic acid, benzoic acid, formic acid or propanoic acid on the described pharmacology.
3. formoterol solution as claimed in claim 1 is characterized in that containing the formoterol of 2.5 μ g/ml～15 μ g/ml.
4. formoterol solution as claimed in claim 1, it is characterized in that selecting for use water, ethanol or the mixture of the two is solvent.
5. formoterol solution as claimed in claim 1 is characterized in that its pH value is 3.0～7.0.
6. formoterol solution as claimed in claim 1 is characterized in that adopting glycine-hydrochloride buffer, phthalic acid-hydrochloride buffer, sodium hydrogen phosphate-citrate buffer solution, citric acid-sodium hydroxide-hydrochloride buffer, citric acid-sodium citrate buffer, acetic acid-sodium acetate buffer, PBS buffer or boric acid-borate buffer solution as buffer system.
7. formoterol solution as claimed in claim 1 is characterized in that containing osmotic pressure regulator.
8. as each described formoterol solution of claim 1～7, it is characterized in that containing antioxidant, comprise ascorbic acid, sodium sulfite, sodium formaldehyde sulphoxylate, sodium pyrosulfite.
9. as each described formoterol solution of claim 1～8, it is characterized in that containing chelating agent, comprise EDTA or its salt.
10. as each described formoterol solution of claim 1～9, it is characterized in that and by manual pump, air compression, ullrasonic spraying equal pressure it to be the vaporific administration that disengages.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008101033238A CN101548943A (en) | 2008-04-03 | 2008-04-03 | Inhalation nebulizer containing formoterol |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008101033238A CN101548943A (en) | 2008-04-03 | 2008-04-03 | Inhalation nebulizer containing formoterol |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101548943A true CN101548943A (en) | 2009-10-07 |
Family
ID=41153586
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2008101033238A Pending CN101548943A (en) | 2008-04-03 | 2008-04-03 | Inhalation nebulizer containing formoterol |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN101548943A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107362140A (en) * | 2016-05-11 | 2017-11-21 | 广东东阳光药业有限公司 | Spray and spray assembly |
-
2008
- 2008-04-03 CN CNA2008101033238A patent/CN101548943A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107362140A (en) * | 2016-05-11 | 2017-11-21 | 广东东阳光药业有限公司 | Spray and spray assembly |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| TWI228998B (en) | Method and device for delivering an active agent to the lungs | |
| EP0786264B1 (en) | Devices for treating pulmonary vasoconstriction and asthma | |
| US5496537A (en) | Propofol hydrofluorocarbon propellant formulations | |
| KR20110120283A (en) | Pharmaceutical composition for inhalation | |
| SK4942001A3 (en) | Storable active substance concentrate with formoterol | |
| CN101606903A (en) | A kind of atomizing of ambroxol sucks with solution and preparation method thereof | |
| US11304897B2 (en) | Pharmaceutical formulation containing umeclidinium bromide and vilanterol trifenatate | |
| US20210386697A1 (en) | Peramivir solution type inhalant and preparation method therefor | |
| KR101466616B1 (en) | Dry Powder Inhaler Device | |
| CN114652704A (en) | Tryprostinil soft mist inhalant | |
| TWI488656B (en) | Tobramycin formulation | |
| JP6626890B2 (en) | Inhalation device and aqueous solution contained in the device | |
| CN101548943A (en) | Inhalation nebulizer containing formoterol | |
| CN114028364A (en) | Oldaterol inhalation solution | |
| CN115209884B (en) | Inhalable formulations containing glycopyrronium bromide and ondarite hydrochloride | |
| JP2024501372A (en) | Pharmaceutical composition for inhalation | |
| JP6908523B2 (en) | Composition for nebulizer | |
| US20210205223A1 (en) | Propellant-free formulation for inhalation | |
| WO2023206444A1 (en) | Treprostinil soft mist inhalant | |
| US20210290568A1 (en) | Inhalable formulation of a solution containing levalbuterol tartrate | |
| CN108283629A (en) | Sucking roflumilast suspension and preparation method thereof | |
| CN107510687B (en) | Inhalation suspension containing formoterol and budesonide for atomization and preparation method thereof | |
| KR20180036459A (en) | Capsule for inhalation with improved content uniformity and delivered dose of combined active ingredients and preparing method thereof | |
| CN116763763A (en) | Semiglutide inhalation spray and preparation method thereof | |
| CN117205186A (en) | Leifenacin inhalation spray and preparation method thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20091007 |