CN106667974A - Preparation method of terbutaline sulfate solution for inhalation - Google Patents
Preparation method of terbutaline sulfate solution for inhalation Download PDFInfo
- Publication number
- CN106667974A CN106667974A CN201710079596.2A CN201710079596A CN106667974A CN 106667974 A CN106667974 A CN 106667974A CN 201710079596 A CN201710079596 A CN 201710079596A CN 106667974 A CN106667974 A CN 106667974A
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- China
- Prior art keywords
- solution preparation
- inhalation solution
- preparation
- alleviating
- inhalation
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
- A61K47/183—Amino acids, e.g. glycine, EDTA or aspartame
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/007—Pulmonary tract; Aromatherapy
- A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
- A61K9/008—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
Abstract
The invention relates to a preparation method of a terbutaline sulfate solution for inhalation. The terbutaline sulfate solution contains a main ingredient, a stabilizer, an iso-osmolar agent, a pH regulator and injection water, and pH value of the terbutaline sulfate solution is 3.0-5.0. The terbutaline sulfate solution has good effect on improving lung functions.
Description
Technical field
The present invention is belonging to pharmaceutical technology field, and in particular to a kind of suction sulphur for preventing and alleviating breathing problem
The preparation method of sour Terbutaline solution.
Background technology
Asthma is a kind of common multiple breathing problem.China's asthma number of patients is more, and children fall ill also more
It is common, it is a kind of physically and mentally healthy serious harm human body, reduce a kind of disease of quality of life.This kind of disease is difficult to be effected a radical cure,
It is clinically many based on expectant treatment.In recent years, the exacerbation with air pollution quality and the decrease of people's locomitivity so that
Asthma prevalence is in the trend that is gradually increasing, therefore treatment asthma is very urgent.
Bricalin is that one kind is mainly used in treatment bronchial astehma, asthmatic bronchitis and chronic obstructive pulmonary
The medicine of bronchial spasm during portion's illness, also known as Terbutaline, terbutaline, entitled (+) α-[(the tertiary fourth amino) first of chemistry
Base] -3,5- dihydroxybenzyl alcohol sulfate（2:1）, molecular formula is (C12H19NO3)2﹒ H2SO4, molecular weight is 548.66, structural formula
It is as follows：
。
The product are a kind of 2-adrenergic agonist components, alternative excitement β2 Acceptor, and diastole bronchial smooth muscle, suppression
Endogenous causes the oedema that the release of spasm material and endogenous mediator cause, and improves tunica mucosa bronchiorum cilliated epithelium and cleans up ability,
Also can diastole uterine smooth muscle, oral administration biaavailability be 15% ± 6%, there is antiasthmatic effect in about 30min, and effective blood drug concentration is
3mg/ml, plasma protein binding rate is 25%, and effect in 2 ~ 4 hours peaks, and lasts about 4 ~ 7 hours, clinically for treating branch
San bronchial asthma, chronic bronchitis, pulmonary emphysema and other PUD Ds are merged the bronchial spasm medicine, at the same the medicine due to
It is to β2Acceptor has high selectivity, and cardiac side effects are small, and the patient to angiocardiopathies such as accompanied with hypertension, coronary heart disease also may be used
Use.
The formulation of bricalin includes oral and spraying two kinds of formulations of suction, peroral dosage form on current domestic and international market
Including tablet, dripping pill, by tablet producing technology technology is had the special feature that so that this kind of oral formulations disintegration time is long, rise
Effect is slow, and bioavilability is relatively low, so as to influence giving full play to for drug effect；Dripping pill for tablet, its disintegration time and life
Thing availability increases, and equally has the shortcomings that peroral dosage form.
Inhalation solution preparation of the invention, it can be by nebulizer administration；Liquid preparation of the invention must be accorded with
Close high quality standards, with absorbing that fast, curative effect is high, bioavilability it is high without stomach and intestine toxic and side effect and irritating feature, can be by
Medicine directly acts on diseased region, compared with other oral and injections, aerosol inhalation solution agent be more suitable for underage child and
Postoperative patient and the elderly.
The content of the invention
The invention provides the preparation method of bricalin inhalation solution.
Solution for inhalation of the invention includes main ingredient, stabilizer, isotonic agent, pH conditioning agents and solvent.Main ingredient is preferably sulphur
Sour Terbutaline, the preferred water for injection of solvent.
Preparation pH values of the invention between 3.0-5.0, and between preferably 3.0-4.0.
PH value is adjusted by adding pharmaceutically acceptable acid or alkali, and such as inorganic acid includes：Hydrochloric acid, phosphoric acid, organic acid
Such as：Citric acid, tartaric acid, acetic acid etc.；The alkali that may be adapted to is for example：NaOH etc..
According to the present invention, used as the stabilizer in this preparation, amount ranges are 0.01 ~ 1mg/ to addition sodium ethylene diamine tetracetate
Ml, preferably 0.01 ~ 0.05mg/ml.
According to the present invention, used as the isotonic agent in this preparation, amount ranges are 5 ~ 9mg/ml for addition sodium chloride or glucose,
Preferably 8 ~ 9mg/ml.
The single dose bricalin inhalation solution that the present invention is provided uses single dose of drug composition and its packaging, institute
The single dose stated refers to the dosage of the medicinal active ingredient that A Single Intake by Inhalation is used.
Currently preferred device includes：Portable spray device, can allow patient to carry with, and this atomizer is without injection
Agent, is disengaged content with mist by the pressure of manual pump.
Specific embodiment
Embodiment 1：
Technique：Under heating state, add during above-mentioned all the components are dissolved in pure water in addition to NaOH and hydrochloric acid, use hydroxide
The pH of sodium and hydrochloric acid conditioning solution to 3.5, resulting solution is filtered by sterilizing filter, is then loaded on medicine liquid irrigation after filtering
In 2~5ml ampoule bottles, 121 degree of 15min of high pressure steam sterilization obtain final product bricalin inhalation solution preparation.
Embodiment 2：
Technique：Under heating state, add during above-mentioned all the components are dissolved in pure water in addition to NaOH and hydrochloric acid, use hydroxide
The pH of sodium and hydrochloric acid conditioning solution to 3.5, resulting solution is filtered by sterilizing filter, is then loaded on medicine liquid irrigation after filtering
In water white transparency 2~5ml ampoule bottles, 121 degree of 15min of high pressure steam sterilization obtain final product bricalin inhalation solution preparation.
Embodiment 3：
Technique：Under heating state, add during above-mentioned all the components are dissolved in pure water in addition to NaOH and hydrochloric acid, use hydroxide
The pH of sodium and hydrochloric acid conditioning solution to 3.5, resulting solution is filtered by sterilizing filter, is then loaded on medicine liquid irrigation after filtering
In water white transparency 2~5ml ampoule bottles, 121 degree of 15min of high pressure steam sterilization obtain final product bricalin inhalation solution preparation.
Embodiment 4：
Technique：Under heating state, add during above-mentioned all the components are dissolved in pure water in addition to NaOH and hydrochloric acid, use hydroxide
The pH of sodium and hydrochloric acid conditioning solution to 3.5, resulting solution is filtered by sterilizing filter, is then loaded on medicine liquid irrigation after filtering
In water white transparency 2~5ml ampoule bottles, 121 degree of 15min of high pressure steam sterilization obtain final product bricalin inhalation solution preparation.
Claims (7)
1. a kind of for alleviating the bronchus that bronchial astehma, chronic bronchitis, pulmonary emphysema and other PUD Ds are merged
The inhalation solution preparation of spasm, is placed in atomising device by liquid and obtained, it is characterised in that described liquid includes pharmaceutical activity
The concentration of composition bricalin, solvent and pharmaceutically acceptable carrier, wherein bricalin is 2~10mg/
Ml, pharmaceutically acceptable carrier is 5~10mg/ml.
2. inhalation solution preparation according to claim 1, it is characterised in that its preparation loaded in ampoule, loading amount be 1ml ~
20ml。
3. inhalation solution preparation according to claim 1, it is characterised in that the consumption that sulfuric acid is special to walk his woods is every spray for 1 ~
5mg/ml。
4. the inhalation solution preparation for alleviating bronchial astehma according to claim 1, it is characterised in that described medicine
Acceptable carrier includes stabilizer, isotonic agent, pH adjusting agent on.
5. the mist inhalation solution preparation for alleviating bronchial astehma according to claim 4, it is characterised in that described
Stabilizer is one or more mixing in natrium adetate and sodium pyrosulfite, and the concentration of stabilizer is 0.01 ~ 1mg/ml.
6. the mist inhalation solution preparation for alleviating bronchial astehma according to claim 4, it is characterised in that described
Isotonic agent is one or more mixing in sodium chloride, glucose, and isotonic agent concentration is 5~9mg/ml.
7. the inhalation solution preparation for alleviating bronchial astehma according to claim 4, it is characterised in that described pH
Conditioning agent is one or more mixing in hydrochloric acid, citric acid, disodium hydrogen phosphate, NaOH, pH value regulation to 3.0 ~ 5.0.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710079596.2A CN106667974A (en) | 2017-02-15 | 2017-02-15 | Preparation method of terbutaline sulfate solution for inhalation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710079596.2A CN106667974A (en) | 2017-02-15 | 2017-02-15 | Preparation method of terbutaline sulfate solution for inhalation |
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| Publication Number | Publication Date |
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| CN106667974A true CN106667974A (en) | 2017-05-17 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
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| CN201710079596.2A Pending CN106667974A (en) | 2017-02-15 | 2017-02-15 | Preparation method of terbutaline sulfate solution for inhalation |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110693861A (en) * | 2018-07-09 | 2020-01-17 | 北京盈科瑞创新药物研究有限公司 | Terbutaline sulfate solution preparation for aerosol inhalation and preparation method thereof |
| CN112274484A (en) * | 2020-09-02 | 2021-01-29 | 南京华盖制药有限公司 | Process treatment method for improving stability of terbutaline sulfate atomized liquid |
| CN112826793A (en) * | 2021-01-25 | 2021-05-25 | 石家庄四药有限公司 | Terbutaline sulfate injection and preparation method thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1992016173A1 (en) * | 1991-03-19 | 1992-10-01 | Sepracor, Inc. | Methods and compositions for treating pulmonary disorders using optically pure terbutaline |
| CN102416167A (en) * | 2011-12-08 | 2012-04-18 | 北京三元基因工程有限公司 | Aerosol inhalant containing interferon alpha and terbutaline sulfate |
-
2017
- 2017-02-15 CN CN201710079596.2A patent/CN106667974A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1992016173A1 (en) * | 1991-03-19 | 1992-10-01 | Sepracor, Inc. | Methods and compositions for treating pulmonary disorders using optically pure terbutaline |
| CN102416167A (en) * | 2011-12-08 | 2012-04-18 | 北京三元基因工程有限公司 | Aerosol inhalant containing interferon alpha and terbutaline sulfate |
Non-Patent Citations (2)
| Title |
|---|
| 刘翠琴: "小儿重症肺炎合并心衰临床分析和小儿哮喘临床治疗效果观察", 《中国社区医师》 * |
| 无: "Bricanyl Respules 2.5 mg/ml Nebuliser Solution", 《网页HTTPS://WWW.MEDICINES.ORG.UK/EMC/PRODUCT/868/SMPC》 * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110693861A (en) * | 2018-07-09 | 2020-01-17 | 北京盈科瑞创新药物研究有限公司 | Terbutaline sulfate solution preparation for aerosol inhalation and preparation method thereof |
| CN112274484A (en) * | 2020-09-02 | 2021-01-29 | 南京华盖制药有限公司 | Process treatment method for improving stability of terbutaline sulfate atomized liquid |
| CN112826793A (en) * | 2021-01-25 | 2021-05-25 | 石家庄四药有限公司 | Terbutaline sulfate injection and preparation method thereof |
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Application publication date: 20170517 |