caredilol
Carvedilol
CAS: 72956-09-3
Molecular Formula: C24H26N2O4
caredilol - Names and Identifiers
| Name | Carvedilol |
| Synonyms | COREG DQ-2466 DIMITONE BM-14190 caredilol Carvedilo DILATREND Carvedilol CARVEDILOL CarvedilolEp5 CarvedilolC24H26N204 1-(9h-carbazol-4-yloxy)-3-((2-(2-methoxyphenoxy)ethyl)amino)-2-propano 1-(9H-CARBAZOL-4-YLOXY)-3-[[2-(2-METHOXYPHENOXY)ETHYL]AMINO]-2-PROPANOL 1-(9h-carbozol-4-yloxy)-3-[[2-(2-methoxy phenoxy)ethyl] amino]-2-propanol 1-(9H-carbazol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol 2,3-dihydroxybutanedioate (salt) |
| CAS | 72956-09-3 |
| EINECS | 1308068-626-2 |
| InChI | InChI=1/C24H26N2O4.C4H6O6/c1-28-21-10-4-5-11-22(21)29-14-13-25-15-17(27)16-30-23-12-6-9-20-24(23)18-7-2-3-8-19(18)26-20;5-1(3(7)8)2(6)4(9)10/h2-12,17,25-27H,13-16H2,1H3;1-2,5-6H,(H,7,8)(H,9,10) |
caredilol - Physico-chemical Properties
| Molecular Formula | C24H26N2O4 |
| Molar Mass | 406.47 |
| Density | 1.250±0.06 g/cm3(Predicted) |
| Melting Point | 113-117°C |
| Boling Point | 655.2±55.0 °C(Predicted) |
| Flash Point | 482.4°C |
| Water Solubility | 449.2ug/L(22.5 ºC) |
| Solubility | DMSO: >20mg/mL |
| Vapor Presure | 1.14E-32mmHg at 25°C |
| Appearance | solid |
| Color | white to off-white |
| Merck | 14,1873 |
| pKa | 13.90±0.20(Predicted) |
| Storage Condition | 2-8°C |
| Physical and Chemical Properties | Melting Point: 113-117°C
|
| Use | Beta blockers, vasodilators |
caredilol - Risk and Safety
| Risk Codes | R51/53 - Toxic to aquatic organisms, may cause long-term adverse effects in the aquatic environment. R36/37/38 - Irritating to eyes, respiratory system and skin. R20/21/22 - Harmful by inhalation, in contact with skin and if swallowed. |
| Safety Description | S61 - Avoid release to the environment. Refer to special instructions / safety data sheets. S36 - Wear suitable protective clothing. S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
| UN IDs | UN 3077 9/PG 3 |
| WGK Germany | 3 |
| RTECS | UA8670000 |
| HS Code | 2933995300 |
| Hazard Class | IRRITANT |
| Packing Group | III |
| Toxicity | LD50 oral in dog: > 1gm/kg |
caredilol - Nature
Open Data Verified Data
colorless crystals were obtained from ethyl acetate, melting point 114-115 °c.
Last Update：2024-01-02 23:10:35
caredilol - Preparation Method
Open Data Verified Data
1, 3-cyclohexanedione was dissolved in water. Under the protection of ammonia, an aqueous solution of phenylhydrazine was slowly added dropwise and stirred. The product was filtered, washed with water, and recrystallized from ethanol to obtain phenylhydrazone. The phenylhydrazone is added to the solution of glacial acetic acid and zinc dichloride for reaction, and the carbazole derivative is treated with heat preservation, cooling, etc. This was stirred at reflux with potassium hydroxide, water, ethanol and Raney Ni under nitrogen to give a reduced product. The resulting reduced product, sodium hydroxide, water and triethylbenzylammonium salt (TEBA) were added dropwise with stirring to epichlorohydrin, followed by stirring at room temperature. Water was added and stirred. The filter cake was filtered, washed with 0.1 mol/L sodium hydroxide and water, recrystallized from ethyl acetate, and the resulting compound was refluxed with O-methoxyphenoxyethylamine and isopropanol. After cooling to room temperature, toluene was added with stirring and allowed to stand. Recrystallization from ethyl acetate yielded carvedilol.
Last Update：2022-01-01 09:10:07
caredilol - Standard
Authoritative Data Verified Data
This product is (±)-l-(9h-4-carbazolyloxy)-3-[2-(2-methoxyphenoxy) ethylamino]-2-propanediol. Calculated as dried product, containing no less than 98.5% of C24H26N204,
Last Update：2024-01-02 23:10:35
caredilol - Trait
Authoritative Data Verified Data
- This product is white or off-white crystalline powder; Odorless.
- This product is dissolved in chloroform, slightly soluble in toluene or ethyl acetate, insoluble in water; Soluble in glacial acetic acid.
melting point
The melting point of this product (General 0612) is 114~118°C.
Last Update：2022-01-01 11:37:24
caredilol - Use
Open Data Verified Data
Competitive antagonists of p-and a1-receptors and calcium channel blockers for the treatment of mild to moderate hypertension.
Last Update：2022-01-01 09:10:07
caredilol - Differential diagnosis
Authoritative Data Verified Data
- take an appropriate amount of this product, add 0.06mol/L acetic acid solution to dissolve and dilute to make a solution containing about 20ug per 1 ml, and measure it by UV-Vis spectrophotometry (General 0401), there is maximum absorption at the wavelengths of 285nm, 319nm and 331nm, and the absorbance ratio at the wavelength of 331mn and 285nm should be 0.40 to 0.44.
- The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 7U).
Last Update：2022-01-01 11:37:25
caredilol - Exam
Authoritative Data Verified Data
clarity and color of acetic acid solution
take 0.10g of this product, add 6mol/L acetic acid solution 10ml to dissolve, the solution should be clear and colorless. If the color is developed, it shall not be deeper than the yellow No. 2 Standard Colorimetric solution (General rules 0901 first method).
Related substances
take this product, add the mobile phase to dissolve and dilute to make a solution containing about 0.5mg per lml, as a test solution; Take the appropriate amount of precision, A solution containing about 1ug per 1 ml was prepared as a control solution by quantitative dilution with mobile phase. Tested according to high performance liquid chromatography (General 0512). Silica gel bonded with eighteen alkyl silane was used as filler, and 0.02mol/L potassium dihydrogen phosphate solution (adjusted to pH 3.5 with phosphoric acid)-acetonitrile (65:35) was used as mobile phase; the detection wavelength is 241rmu. The residue left under the item of taking heavy metal and taking out the residue is inspected according to law (General rule 0821, Method 2), and the heavy metal content shall not exceed 10 ppm. This product is about 12.5mg, put in an Erlenmeyer flask, add 5mol/L hydrochloric acid solution 5ml, heat in 95°C water bath for 3 hours, cool, add 5mol/L sodium hydroxide solution 5ml, mobile phase 15ml, ultrasonic wave for 10 minutes, shake well, filter, take filtrate 10 u1, inject human liquid chromatograph, and calculate the number of theoretical plates according to carvedilol peak not less than 2000, the degree of separation of the carvedilol peak from the subsequent peak of the largest degradant should be greater than 6.5. 10 u1 of the test solution and the control solution were respectively injected into the human liquid chromatograph, and the chromatogram was recorded to 3.5 times of the retention time of the main component peak. If there are impurity peaks in the chromatogram of the test solution, the area of a single impurity peak shall not be greater than the area of the main peak of the control solution (0.2% ) , the sum of each impurity peak area shall not be greater than 2.5 times (0.5%) of the main peak area of the control solution.
residual solvent
take about 0.2g of this product, precision weighing, top empty bottle, Precision Add 2M l of 20% glacial acetic acid solution to dissolve, seal, as a test solution; Another methanol, acetone, tetrahydrofuran and 1, 4-dioxane, precision weighing, quantitative dilution with 20% glacial acetic acid solution to prepare 3mg, 5mg, 0.72mg and 0.38mg Solutions per 1 ml, as a stock solution (1 ), respectively take 1, 2-dichloroethane, benzene, chloroform, toluene, ethyl ether and ethyl acetate, precision weighing, quantitative dilution with acetonitrile to prepare solutions containing about 50ug, 20ug, 0.6mg ,8.9mg, 50mg and 50mg, respectively, in 1 ml, as preparation solution (2), take stock solution (1) 10ml and stock solution (2) 1 ml, put them in a 100ml measuring flask, dilute to the mark with 20% glacial acetic acid solution, shake well, take 2ml, top empty bottle, sealed, as a control solution. Test as residual solvent assay (General 0861 second method). Polyethylene glycol (or polar similar) is used as a stationary liquid; The initial temperature is 40°C, and the temperature is maintained for 12 minutes, and the temperature is raised to 180°C at a rate of 40°C per minute for 5 minutes; the inlet temperature was 200°C; The detector temperature was 230°C; The headspace bottle equilibrium temperature was 90°C and the equilibrium time was 30 minutes. Take the reference solution into the headspace, and the separation degree between the peaks of each component shall meet the requirements. Then the sample solution and the reference solution were injected with headspace, and the chromatogram was recorded. Calculated by peak area according to external standard method, methanol, acetone, Tetrahydrofuran, 1, 4-dioxane, 1, 2-dichloroethane, benzene, trimethane, toluene, ether and ethyl acetate residual Halo should be in accordance with the provisions.
loss on drying
take this product, with phosphorus pentoxide as desiccant, under reduced pressure drying to constant weight, weight loss should not exceed 0.5% (General rule 0831).
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%.
Last Update：2022-01-01 11:37:26
caredilol - Content determination
Authoritative Data Verified Data
take this product about 0.3g, precision weighing, add glacial acetic acid 30ml dissolved, according to the potential titration method (General 0701), with perchloric acid titration solution (0.1 mol/U titration, and the results of the titration were corrected with a blank test. Each 1 ml of perchloric acid titration solution (0.1 mol/L) corresponds to 40.65mg of C24H26N204.
Last Update：2022-01-01 11:37:26
caredilol - Category
Authoritative Data Verified Data
vasodilator, B adrenergic receptor antagonist.
Last Update：2022-01-01 11:37:26
caredilol - Storage
Authoritative Data Verified Data
light shielding, sealed storage.
Last Update：2022-01-01 11:37:27
caredilol - Carvedilol Tablets
Authoritative Data Verified Data
This product contains carvedilol (C24H26N204) should be 90.0% to 110.0% of the label.
trait
This product is white or white-like tablets or film-coated tablets, white or white-like after removing the coating.
identification
- take an appropriate amount of the fine powder of this product, add 0.06mol/L acetic acid solution to dissolve carvedilol and dilute it into a solution containing about 20ug of carvedilol per lml, filter it, the filtrate was measured by UV-Vis spectrophotometry (General rule 0401), and the maximum absorption was found at 285nm, 319nm and 331nm, the absorbance ratio at the wavelength of 331nm to 285nm should be between 0.40 and 0.44.
- 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
- Related substances take an appropriate amount of fine powder of this product (about 12.5mg equivalent to carvedilol), put it in a 25ml measuring flask, add an appropriate amount of mobile phase, sonicate the carvedilol, and let it cool, dilute to the scale with mobile phase, shake, filter, and take the filtrate as the test solution; Take 1ml with precision, put it in a 100ml measuring flask, dilute to the scale with mobile phase, and shake well, as a control solution. If there are impurity peaks in the chromatogram of the test solution, the area of a single impurity peak shall not be greater than 0.5 times (0.5%) of the area of the main peak of the control solution, the sum of each impurity peak area shall not be greater than the main peak area of the control solution (1.0%).
- Content uniformity: Take 1 tablet of this product, put it in 50ml measuring flask (6.25mg specification) or 100ml measuring flask (10 mg specification, 12.5mg specification) or 200ml measuring flask (20mg specification), and add appropriate amount of mobile phase, ultrasonically dissolve carvedilol, dilute to the scale with mobile phase, shake well, filter, take the continued filtrate as the test solution, and determine the content according to the method under the content determination item, the provisions shall be met (General rule 0941).
- dissolution dissolution of this product, according to the dissolution and release determination method (General rule 0931 The first method), hydrochloric acid solution (9-100) as the dissolution medium, the speed is rpm, operate according to law, after 30 minutes, take 10ml of solution, filter, take the appropriate amount of filtrate, dilute quantitatively with dissolution medium to make a solution containing about 5ug of carvedilol per lml, as a test solution; Take about 10mg of carvedilol reference substance accurately, put it in a 100ml measuring flask, add 10ml of methanol, shake to dissolve, dilute it to scale with dissolution medium, shake well, take 5ml of precision, 100ml flask, diluted with dissolution medium to scale, shake, as a reference solution. The absorbance of the above two Solutions was measured at a wavelength of 0401 nm by ultraviolet-visible spectrophotometry (general), and the elution amount of each tablet was calculated. The limit is 80% 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; 0.02mol/L potassium dihydrogen phosphate solution (adjusted to pH 3.5 with phosphoric acid)-acetonitrile (65:35) about 12.5mg of carvedilol reference substance was taken at the detection wavelength of 241nm, placed in an Erlenmeyer flask, 5ml of 5mol/L hydrochloric acid solution was added, heated in a 95°C water bath for 3 hours, and allowed to cool, add 5mol/L sodium hydroxide solution 5mk mobile phase 15ml, sonicate for 10 minutes, shake well, filter, take 10ul of filtrate, inject into liquid chromatograph, calculate the number of theoretical plate according to carvedilol peak not less than 2000, the degree of separation of the carvedilol peak from the subsequent peak of the largest degradant should be greater than 6.5.
- determination of 20 tablets of this product, precision weighing, fine grinding, precision weighing an appropriate amount (about 10mg equivalent to carvedilol), put in a 100ml measuring flask, add an appropriate amount of mobile phase, ultrasonic dissolution of carvedilol, dilute to scale with mobile phase, shake, filter, take filtrate as test solution, take 10 u1 with precision, inject human liquid chromatograph, record chromatogram; Take appropriate amount of carvedilol reference, precision weighing, plus mobile phase dissolution and quantitative dilution made per 1 ml containing 0.lmg solution, the same method for determination. According to the external standard method to calculate the peak area, that is.
category
Same as carvedilol.
specification
(l)6.25mg (2)l0mg (3)12.5mg (4)20mg
storage
light shielding, sealed storage.
Last Update：2022-01-01 11:37:28
caredilol - Carvedilol Capsules
Authoritative Data Verified Data
This product contains carvedilol (C24H26N204) should be 90.0% to 110.0% of the label.
trait
The content of this product is white powder.
identification
- take an appropriate amount of the contents of this product, add 0.06mol/L acetic acid solution to dissolve carvedilol and make a solution containing about 20% per 1 ml, filter, take the filtrate, as determined by UV-Vis spectrophotometry (General rule 0401), there is a maximum absorption at the wavelengths of 285mn, 319nm and 331nm, and the absorbance ratio at the wavelength of 331nm and 285nm should be 0.40 to 0.44.
- 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
- relevant substances take an appropriate amount of the content of this product (about 12.5mg equivalent to carvedilol), put it in a 25ml measuring flask, add an appropriate amount of mobile phase, ultrasonic to dissolve carvedilol, cool, dilute to the scale with mobile phase, shake well, filter, and take the continued filtrate as a test solution; Take 1ml with precision, put it in a 100ml measuring flask, dilute to the scale with mobile phase, shake well, and use as a control solution. If there are impurity peaks in the chromatogram of the test solution, the area of a single impurity peak shall not be greater than 0.5 times (0.5%) of the area of the main peak of the control solution, the sum of each impurity peak area shall not be greater than the main peak area of the control solution (1.0%).
- Content uniformity take 1 capsule of this product, pour the content into a 100ml measuring flask, wash the capsule shell with mobile phase, wash it into the measuring flask, add about 80ml of mobile phase, ultrasonic dissolution of carvedilol and diluted to the scale, shake, filter, take the filtrate as a test solution, according to the content determination method under the item, should comply with the provisions (General 0941).
- dissolution of this product, according to the dissolution and release determination method (General 0931 first method) determination. Using hydrochloric acid solution (9-1000 )900ml as dissolution medium, rotating speed is 100 rpm, operating according to law, after 30 minutes, take 10ml of solution for filtration, take appropriate amount of filtrate with precision, quantitative dilution with dissolution medium to prepare a solution containing about 5ug of carvedilol per 1 ml, as a test solution; Another 10mg of carvedilol control product, precision weighing, set in a 100ml measuring flask, Add 10ml of methanol, shake to dissolve, dilute to scale with dissolution medium, shake well, take appropriate amount with precision, quantitatively dilute with dissolution medium to prepare 5ug solution per lml, shake well, as a control solution. Take the test solution and the reference solution, according to the UV-visible spectrophotometry (General rule 0401), measure the absorbance at the wavelength of 240nm, and take the empty capsule shell for blank correction, the amount of dissolution per pellet was calculated. The limit is 70% 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; Using 0.02mol/L potassium dihydrogen phosphate solution (adjusted to pH 3.5 with phosphoric acid)-acetonitrile (65:35) the detection wavelength was 241nm. Take about 12.5mg of carvedilol reference substance, put it in an Erlenmeyer flask, add 5ml of 5mol/L hydrochloric acid solution, heat it in a 95°C water bath for 3 hours, cool it, add 5ml of 5mol/L sodium hydroxide solution, the filtrate l0ul was injected into the liquid chromatograph. The number of theoretical plates was not less than 2000 according to the carvedilol peak, the degree of separation of the carvedilol peak from the subsequent peak of the largest degradant should be greater than 6.5.
- determination Method: Take 10 capsules of this product, weigh them accurately, calculate the average loading, mix the contents evenly, weigh the appropriate amount (about 10mg equivalent to carvedilol), and put them in a 100ml measuring flask, add appropriate amount of mobile phase, ultrasonic to dissolve carvedilol, dilute to scale with mobile phase, shake well, filter, take filtrate as test solution, take 10 u1 with precision, inject human liquid chromatograph, record the chromatogram; Take another carvedilol reference substance, precision weighing, plus mobile phase dissolution and quantitative dilution made per lml containing 0.lmg solution, the same method for determination. According to the external standard method to calculate the peak area, that is.
category
Same as carvedilol.
specification
lOmg
storage
sealed and stored in a dry place.
Last Update：2022-01-01 11:37:29
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Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Product Name: Carvedilol Request for quotation
CAS: 72956-09-3
Tel: 0086-551-65418684
Email: sales@tnjchem.com
info@tnjchem.com
Mobile: 0086 189 4982 3763
QQ: 2881500840
Wechat: 0086 189 4982 3763
WhatsApp: 0086 189 4982 3763
Product List: View Catalog
CAS: 72956-09-3
Tel: 0086-551-65418684
Email: sales@tnjchem.com
info@tnjchem.com
Mobile: 0086 189 4982 3763
QQ: 2881500840
Wechat: 0086 189 4982 3763
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