2(1H)-Quinolinone, 8-hydroxy-5-[1-hydroxy-2-[(1-methylethyl)amino]butyl]-, monohydrochloride, (R*,S*)-(+-)-
procaterol hydrochloride
CAS: 62929-91-3;81262-93-3
Molecular Formula: C16H23ClN2O3
2(1H)-Quinolinone, 8-hydroxy-5-[1-hydroxy-2-[(1-methylethyl)amino]butyl]-, monohydrochloride, (R*,S*)-(+-)- - Names and Identifiers
2(1H)-Quinolinone, 8-hydroxy-5-[1-hydroxy-2-[(1-methylethyl)amino]butyl]-, monohydrochloride, (R*,S*)-(+-)- - Physico-chemical Properties
| Molecular Formula | C16H23ClN2O3 |
| Molar Mass | 326.82 |
| Boling Point | 539.5°C at 760 mmHg |
| Flash Point | 280.1°C |
| Vapor Presure | 1.79E-12mmHg at 25°C |
| Storage Condition | 2-8°C |
| Use | For the treatment of various types of bronchial asthma, asthmatic bronchitis, chronic obstructive pulmonary disease and acute bronchitis and other diseases |
2(1H)-Quinolinone, 8-hydroxy-5-[1-hydroxy-2-[(1-methylethyl)amino]butyl]-, monohydrochloride, (R*,S*)-(+-)- - Risk and Safety
| WGK Germany | 2 |
| RTECS | VC8296000 |
2(1H)-Quinolinone, 8-hydroxy-5-[1-hydroxy-2-[(1-methylethyl)amino]butyl]-, monohydrochloride, (R*,S*)-(+-)- - Nature
Open Data Verified Data
white crystalline powder. Melting point 193~197 °c (decomposition). Soluble in methanol, ethanol-soluble, almost insoluble in acetone, ethyl ether, ethyl acetate, chloroform or benzene. Colored when exposed to light.
Last Update：2024-01-02 23:10:35
2(1H)-Quinolinone, 8-hydroxy-5-[1-hydroxy-2-[(1-methylethyl)amino]butyl]-, monohydrochloride, (R*,S*)-(+-)- - Preparation Method
Open Data Verified Data
8 hydroxy quinolone in aluminum chloride catalyzed by 2 chloro butyryl chloride acylation reaction. The resulting product was partially hydrolyzed with 5% aqueous potassium hydroxide at room temperature and then aminated to give procaterol by reduction.
Last Update：2022-01-01 09:09:59
2(1H)-Quinolinone, 8-hydroxy-5-[1-hydroxy-2-[(1-methylethyl)amino]butyl]-, monohydrochloride, (R*,S*)-(+-)- - Standard
Authoritative Data Verified Data
This product is 5-(l-hydroxy-2-isopropylaminobutyl)-8-hydroxyquinolone hydrochloride hemihydrate. The content of C16H22N203 • HC1 shall not be less than 98.5% calculated as anhydrous.
Last Update：2024-01-02 23:10:35
2(1H)-Quinolinone, 8-hydroxy-5-[1-hydroxy-2-[(1-methylethyl)amino]butyl]-, monohydrochloride, (R*,S*)-(+-)- - Trait
Authoritative Data Verified Data
- This product is white or off-white crystalline powder; Odorless.
- This product is dissolved in water or methanol, slightly soluble in ethanol, almost insoluble in ether, dissolved in formic acid.
melting point
The melting point of this product (General rule 0612) is 193~198°C, and it is decomposed at the same time during melting.
Last Update：2022-01-01 14:21:03
2(1H)-Quinolinone, 8-hydroxy-5-[1-hydroxy-2-[(1-methylethyl)amino]butyl]-, monohydrochloride, (R*,S*)-(+-)- - Use
Open Data Verified Data
is a highly selective p-receptor agonist, highly selective for bronchial smooth muscle & a receptor, strong bronchodilating effect, small dose can produce obvious bronchodilating effect, it also has a strong anti-allergic effect, which can stabilize the mast cell membrane, inhibit the release of histamine and other allergic substances, and has a good effect on allergen induced bronchial asthma. For bronchial asthma, asthmatic bronchitis, emphysema, chronic bronchitis and chronic obstructive pulmonary disease caused by Dyspnea of the treatment.
Last Update：2022-01-01 09:10:00
2(1H)-Quinolinone, 8-hydroxy-5-[1-hydroxy-2-[(1-methylethyl)amino]butyl]-, monohydrochloride, (R*,S*)-(+-)- - Differential diagnosis
Authoritative Data Verified Data
- take about 2mg of this product, add 5ml of water to dissolve, add 1 drop of ferric chloride test solution, the solution is dark green.
- take this product, add water to dissolve and dilute to make a solution containing 7ug per lml, according to UV-visible spectrophotometry (General 0401), at 234nm, 259nm and 295nm wavelength has the maximum absorption.
- The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 637).
- identification reaction of aqueous solution of this product (General rule 0301).
Last Update：2022-01-01 14:21:04
2(1H)-Quinolinone, 8-hydroxy-5-[1-hydroxy-2-[(1-methylethyl)amino]butyl]-, monohydrochloride, (R*,S*)-(+-)- - Safety
Open Data Verified Data
LDso (mg]kg) in male rats: 2600 oral, 80 intravenous.
Last Update：2022-01-01 09:10:00
2(1H)-Quinolinone, 8-hydroxy-5-[1-hydroxy-2-[(1-methylethyl)amino]butyl]-, monohydrochloride, (R*,S*)-(+-)- - Exam
Authoritative Data Verified Data
acidity
take 0.10g of this product, Add 10ml of water to dissolve it, and determine it according to law (General rule 0631). The pH value should be 4.0~5.0.
clarity and color of solution
take 0.5g of this product, add water 15ml to dissolve, the solution should be clear and colorless; If the color is colored, compared with the yellow No. 2 Standard Colorimetric liquid (General rule 0901 first method), not deeper.
Related substances
take this product, add the mobile phase to dissolve and dilute to make a solution containing lmg per lml as a test solution; Take lml for precision measurement and put it in a 100ml measuring flask, dilute to the scale with the mobile phase, shake, and serve as a control solution. According to the test of high performance liquid chromatography (General rule 0512), silica gel bonded with eighteen alkyl silane was used as the filler; Phosphate buffer solution (11.04g of sodium dihydrogen phosphate was taken, 3.1±0.05 of water was added to dissolve, and phosphoric acid was used to adjust the pH value to)-Methanol (83:17) as mobile phase; Detection wavelength of 259nm. The number of theoretical plates shall not be less than 2500 based on the calculation of procaterol peak, and the separation degree between procaterol peak and adjacent impurity peaks shall meet the requirements. 20 u1 of the test solution and the control solution were respectively injected into the human liquid chromatograph, and the chromatogram was recorded to 3 times of the retention time of the main component peak. If there are impurity peaks in the chromatogram of the test solution, the sum of each impurity peak area shall not be greater than 0.5 times (0.5%) of the main peak area of the control solution.
moisture
take this product, according to the moisture determination method (General 0832 first method 1), the moisture content should be 2.5% ~ 3.3%.
ignition residue
take l.Og of this product and check it according to law (General rule 0841). The residue left shall not exceed 0.1%.
Heavy metals
The residue left under the item of taking the ignition residue shall not contain more than 10 parts per million of heavy metal when examined by law (General Principles 0821, Law II).
arsenic salt
take this product l.Og, add calcium hydroxide l. Add a small amount of water, stir well, dry, first burn with small fire to make charring, then burn to gray-white at 500~60CTC, cool, add 8ml hydrochloric acid and 20ml water to dissolve, inspection according to law (General rule 08 22 second law) shall comply with the provisions (0.0002%).
Last Update：2022-01-01 14:21:04
2(1H)-Quinolinone, 8-hydroxy-5-[1-hydroxy-2-[(1-methylethyl)amino]butyl]-, monohydrochloride, (R*,S*)-(+-)- - Content determination
Authoritative Data Verified Data
take this product about 0.25g, precision weighing, add formic acid 2ml, heat dissolution, precision and high gas acid titration solution (0.1 mol/L ) 15ml and acetic anhydride 1ml, heated on a water bath for 30 minutes, after cooling, add acetic anhydride 60ml, according to the potentiometric titration method (General rule 0701), with sodium acetate titration solution (0.1 mol/L) titration, and the results of the titration were corrected with a blank test. Each 1ml of perchloric acid titration solution (0.1 mol /L) corresponds to 32.68mg of C16H22N203. Hc1.
Last Update：2022-01-01 14:21:05
2(1H)-Quinolinone, 8-hydroxy-5-[1-hydroxy-2-[(1-methylethyl)amino]butyl]-, monohydrochloride, (R*,S*)-(+-)- - Category
Authoritative Data Verified Data
B2 adrenergic receptor agonists.
Last Update：2022-01-01 14:21:05
2(1H)-Quinolinone, 8-hydroxy-5-[1-hydroxy-2-[(1-methylethyl)amino]butyl]-, monohydrochloride, (R*,S*)-(+-)- - Storage
Authoritative Data Verified Data
light shielding, sealed storage.
Last Update：2022-01-01 14:21:06
2(1H)-Quinolinone, 8-hydroxy-5-[1-hydroxy-2-[(1-methylethyl)amino]butyl]-, monohydrochloride, (R*,S*)-(+-)- - Procaterol Hydrochloride Tablets
Authoritative Data Verified Data
This product contains procaterol hydrochloride (according to C16H22N203 • HC1) should be 93.0% ~ 107.0% of the label amount.
trait
This product is white tablet.
identification
- take an appropriate amount of fine powder of this product (approximately equivalent to procaterol hydrochloride, 0.25mg as per C16H22N203 • HC1), add 4ml of hydrochloric acid solution (1-6), shake fully, dissolve procaterol hydrochloride, filter, take filtrate, add sodium nitrite Crystal 10mg, shake and dissolve, add sodium hydroxide solution (1-5 ) lml, should appear orange yellow.
- Take appropriate amount of fine powder of this product (approximately equivalent to procaterol hydrochloride, 100ug as per C16H22N203 • HC1), add hydrochloric acid solution (9-1000)20ml, shake fully, procaterol hydrochloride was dissolved, filtered, and the filtrate had an absorption maximum at a wavelength of 0401 nm and NM as determined by UV-visible spectrophotometry (general).
- in the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the reference solution.
examination
- Content uniformity take 1 tablet of this product, put it in a 10ml measuring flask, add 5ml of mobile phase, fully shake for 10 minutes, dissolve procaterol hydrochloride, dilute it to the scale with mobile phase, shake well, filter, take the filtrate as a test solution; Take the appropriate amount of procaterol hydrochloride reference, precision weighing, and mobile phase dissolution and quantitative dilution made into each lml containing 2.5ug (25ug specification) or 5ug(50ug specification) of the solution, as a control solution. Determination of content according to the method under the content determination item, should comply with the provisions (General 0941).
- the dissolution of this product, according to the dissolution and release determination method (General rule 0931 third method), with hydrochloric acid solution (3-50000) 100ml as the dissolution medium, the rotation speed is 70 rpm, operate according to law, after 10 minutes, take 10ml of the solution, filter, take the filtrate as the test solution; Take the appropriate amount of procaterol hydrochloride reference, precision weighing, the solution containing 0.25ug(25ug specification) or 0.5ug (50ug specification) per 1 ml was prepared as a control solution by dissolution and quantitative dilution. According to the chromatographic conditions under the content determination item, 100 u1 of each of the above two solutions is accurately measured and injected into the liquid chromatograph respectively, the chromatogram is recorded, and the dissolution amount of each tablet is calculated by peak area according to external standard method. The limit is 85% of the labeled amount and shall be in accordance with the provisions.
- others shall be in accordance with the relevant provisions under the item of tablets (General rule 0101).
Content determination
- measured by high performance liquid chromatography (General 0512).
- chromatographic conditions and system suitability test using eighteen alkyl silane bonded silica gel as filler; Phosphate buffer (take sodium dihydrogen phosphate 11.04g, add water 1000ml to dissolve, adjust the pH value to 3.1±0.05 with phosphoric acid)-Methanol (83:17) as mobile phase; Detection wavelength of 259nm. The number of theoretical plates shall not be less than 2000 based on the calculation of procaterol peak.
- determination of this product 30 tablets, precision weighing, fine grinding, precision weighing take appropriate amount (about equivalent to procaterol hydrochloride, according to C16H22N203 • HCI 0.25mg), put in 50ml measuring flask, add appropriate amount of mobile phase, fully shake to dissolve procaterol hydrochloride, dilute to scale with mobile phase, shake well, filter, take continued filtrate as test solution, take 20 u1 with precision, human liquid chromatograph was used and the chromatogram was recorded. An appropriate amount of procaterol hydrochloride reference substance was added for precision weighing, and the mobile phase was added for dissolution and quantitative dilution to prepare a solution containing 5ug per lml, which was determined by the same method. According to the external standard method to calculate the peak area, that is.
category
Same as procaterol hydrochloride.
specification
by C16H22N203 • HC1 (l)25ug (2)50ug
storage
light shielding, sealed storage.
Last Update：2022-01-01 14:21:06
2(1H)-Quinolinone, 8-hydroxy-5-[1-hydroxy-2-[(1-methylethyl)amino]butyl]-, monohydrochloride, (R*,S*)-(+-)- - Procaterol hydrochloride capsules
Authoritative Data Verified Data
This product contains procaterol hydrochloride (according to C16H22N203 • HC1) should be 90.0% ~ 110.0% of the label amount.
trait
The content of this product is white or white particles or powder.
identification
- take an appropriate amount of the content of this product (approximately equivalent to procaterol hydrochloride, 0.25mg as per C16H22N203 • HCl), grind, add hydrochloric acid solution (1-6)4ml, fully grind, dissolve procaterol hydrochloride, filter, take filtrate, add sodium nitrite crystallization 10 mg, shake and dissolve, add sodium hydroxide solution (1-5) 1 ml, shake, the solution should be orange yellow.
- take an appropriate amount of the contents of this product (approximately equivalent to procaterol hydrochloride, 0.1 mg as per C16H22N203 • HCl), add 20ml of hydrochloric acid solution (9-1000), and fully shake to dissolve procaterol hydrochloride, filtering, filtrate UV-visible spectrophotometry (General 0401), at 259mn and 295mn wavelength absorption maximum.
- in the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the reference solution.
examination
- Content uniformity take 1 capsule of this product, pour the content into a 10ml measuring flask, add 5ml of mobile phase, fully shake for 10 minutes, dissolve procaterol hydrochloride, dilute to the scale with mobile phase, shake well, filter, and take the continued filtrate as the test solution; Take an appropriate amount of procaterol hydrochloride reference substance, weigh it precisely, add mobile phase to dissolve and quantitatively dilute to make a solution containing 2.5ug per 1 ml, as a control solution. Determination of content according to the method under the content determination item, should comply with the provisions (General 0941).
- the dissolution of this product, according to the dissolution and release determination method (General rule 0931 third method), with hydrochloric acid solution (3-50000) 100ml as the dissolution medium, the rotation speed is 70 rpm, operate in accordance with the law, after 20 minutes, take the solution filtration, take the filtrate as the test solution; Take the appropriate amount of procaterol hydrochloride control, precision weighing, the dissolution medium was added to dissolve and quantitatively dilute to prepare a solution containing 0.25ug per 1 ml as a control solution. According to the chromatographic conditions under the content determination item, take 100ul of each of the above two solutions with precision, inject human liquid chromatography respectively, record the chromatogram, and calculate the dissolution amount of each particle by peak area according to external standard method. The limit is 85% of the labeled amount and shall be in accordance with the provisions.
- others should comply with the relevant provisions under the capsule (General 0103).
Content determination
- measured by high performance liquid chromatography (General 0512).
- chromatographic conditions and system suitability test using eighteen alkyl silane bonded silica gel as filler; Phosphate buffer solution (take sodium dihydrogen phosphate 11.04g, add water 1000ml to dissolve, adjust pH value to 3.1±0.05 with phosphoric acid)-Methanol (83:17) as mobile phase; Detection wavelength 259mn. The number of theoretical plates shall not be less than 2000 based on the calculation of procaterol peak.
- determination Method: Take 30 capsules of this product, weigh them precisely, and calculate the average loading. Take the contents, mix well, accurately weigh an appropriate amount (equivalent to procaterol hydrochloride, 0.25mg as measured by C16H22N2O3 • HCl), put it in a 50ml measuring flask, add an appropriate amount of mobile phase, and fully shake, procaterol hydrochloride was dissolved, diluted to scale with mobile phase, shaken well, filtered, and the continuous filtrate was taken as a test solution, and 20 u1 was accurately measured and injected into the liquid chromatograph, and the chromatogram was recorded. An appropriate amount of procaterol hydrochloride reference substance was added for precision weighing, and the mobile phase was added for dissolution and quantitative dilution to prepare a solution containing 5ug per lml, which was determined by the same method. According to the external standard method to calculate the peak area, that is.
category
Same as procaterol hydrochloride.
specification
25ug (based on C16H22N203 • HC1)
storage
sealed and stored in a cool and dry place.
Last Update：2022-01-01 14:21:07
2(1H)-Quinolinone, 8-hydroxy-5-[1-hydroxy-2-[(1-methylethyl)amino]butyl]-, monohydrochloride, (R*,S*)-(+-)- - Reference Information
| biological activity | Procaterol HCl (OPC-2009) is a short-acting β2-adrenergic receptor agonist with a Kp of 8 nM, for the treatment of asthma. |
| Use | for bronchial asthma and asthmatic bronchitis. for the treatment of various types of bronchial asthma, asthmatic bronchitis, chronic obstructive pulmonary disease and acute bronchitis and other diseases |
Last Update：2024-04-10 22:29:15
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Supplier List
Multiple SpecificationsSpot supply
Product Name: Procaterol Impurity 1 Hydrochloride Visit Supplier Webpage Request for quotationCAS: 81262-93-3
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Multiple SpecificationsSpot supply
Product Name: Procaterol Impurity 1 Hydrochloride Visit Supplier Webpage Request for quotationCAS: 81262-93-3
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
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