N-[(cyclohexylamino)carbonyl]-4-{2-[4,4-dimethyl-7-(methyloxy)-1,3-dioxo-3,4-dihydroisoquinolin-2(1H)-yl]ethyl}benzenesulfonamide - Names and Identifiers
Name | Gliquidone
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Synonyms | ardf26 ardf26se Glurenorm 251-463-2 Gliquidone GLIQUIDONE Gliquidone Tablets ,4-dimethyl-1,3-dioxo-2(1h)-isoquinolinyl)ethyl)- benzenesulfonamide,n-((cyclohexylamino)carbonyl)-4-(2-(3,4-dihydro-7-methoxy-4 N-(Cyclohexylcarbamoyl)-4-[2-(7-methoxy-4,4-dimethyl-1,3-dioxo-3,4-dihydroisochinolin-2(1H)-yl)ethyl]benzolsulfonamid N-(Cyclohexylcarbamoyl)-4-[2-(7-methoxy-4,4-dimethyl-1,3-dioxo-3,4-dihydroisoquinolin-2(1H)-yl)ethyl]benzenesulfonamide N-(Cyclohexylcarbamoyl)-4-[2-(7-methoxy-4,4-dimethyl-1,3-dioxo-3,4-dihydro-2(1H)-isoquinolinyl)ethyl]benzenesulfonamide N-[(cyclohexylamino)carbonyl]-4-{2-[4,4-dimethyl-7-(methyloxy)-1,3-dioxo-3,4-dihydroisoquinolin-2(1H)-yl]ethyl}benzenesulfonamide
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CAS | 33342-05-1
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EINECS | 251-463-2 |
InChI | InChI=1/C27H33N3O6S/c1-27(2)23-14-11-20(36-3)17-22(23)24(31)30(25(27)32)16-15-18-9-12-21(13-10-18)37(34,35)29-26(33)28-19-7-5-4-6-8-19/h9-14,17,19H,4-8,15-16H2,1-3H3,(H2,28,29,33) |
N-[(cyclohexylamino)carbonyl]-4-{2-[4,4-dimethyl-7-(methyloxy)-1,3-dioxo-3,4-dihydroisoquinolin-2(1H)-yl]ethyl}benzenesulfonamide - Physico-chemical Properties
Molecular Formula | C27H33N3O6S
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Molar Mass | 527.63 |
Density | 1.34±0.1 g/cm3(Predicted) |
Melting Point | 179 °C |
Solubility | DMSO : 50 mg/mL (94.76 mM; Need ultrasonic);H2O : < 0.1 mg/mL (insoluble) |
Appearance | White powder |
Color | White to Almost white |
Merck | 14,4443 |
pKa | 5.12±0.10(Predicted) |
Storage Condition | Inert atmosphere,Room Temperature |
Refractive Index | 1.624 |
MDL | MFCD00631870 |
Use | Hypoglycemic agents for the treatment of non-insulin-dependent diabetes mellitus |
N-[(cyclohexylamino)carbonyl]-4-{2-[4,4-dimethyl-7-(methyloxy)-1,3-dioxo-3,4-dihydroisoquinolin-2(1H)-yl]ethyl}benzenesulfonamide - Risk and Safety
Safety Description | 24/25 - Avoid contact with skin and eyes.
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RTECS | DB1584250 |
HS Code | 29147000 |
N-[(cyclohexylamino)carbonyl]-4-{2-[4,4-dimethyl-7-(methyloxy)-1,3-dioxo-3,4-dihydroisoquinolin-2(1H)-yl]ethyl}benzenesulfonamide - Reference
Reference Show more | 1. Li Mengying, Zhang Rui, Yang Min, Shao Fuping, Xu Huihui, Yin Dengke. Effects of Danshen injection on pharmacokinetic parameters and intestinal absorption characteristics of gliquidone in diabetic rats [J]. Journal of Anhui University of Traditional Chinese Medicine, 2019, 38(05):67-70. |
N-[(cyclohexylamino)carbonyl]-4-{2-[4,4-dimethyl-7-(methyloxy)-1,3-dioxo-3,4-dihydroisoquinolin-2(1H)-yl]ethyl}benzenesulfonamide - Standard
Authoritative Data Verified Data
This product is 1-cyclohexyl-3-[ [p-[2-(3, 4-dihydro-7-methoxy-4, 4-dimethyl-1, 3-dioxo-2 (1H)-isoquinolyl) ethyl] phenyl] sulfonyl] urea. The content of C27H33N306S shall be 98.0% ~ 102.0% calculated as dry product.
Last Update:2024-01-02 23:10:35
N-[(cyclohexylamino)carbonyl]-4-{2-[4,4-dimethyl-7-(methyloxy)-1,3-dioxo-3,4-dihydroisoquinolin-2(1H)-yl]ethyl}benzenesulfonamide - Trait
Authoritative Data Verified Data
- This product is white crystal or crystalline powder; Odorless.
- This product is soluble in chloroform, slightly soluble in acetone, slightly soluble in ethanol or methanol, and almost insoluble in water.
melting point
The melting point of this product (General 0612) is 178~182°C.
Last Update:2022-01-01 15:36:15
N-[(cyclohexylamino)carbonyl]-4-{2-[4,4-dimethyl-7-(methyloxy)-1,3-dioxo-3,4-dihydroisoquinolin-2(1H)-yl]ethyl}benzenesulfonamide - Differential diagnosis
Authoritative Data Verified Data
- take about 10 mg of this product, add 5 drops of phenylhydrazine, heat until the solution becomes clear, and let it cool. Add 0.5ml of ammonia test solution, 10% ml of nickel sulfate solution and 1ml of chloroform, and shake vigorously, standing, the lower solution should become purple-red.
- 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.
- The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 1097).
Last Update:2022-01-01 15:36:16
N-[(cyclohexylamino)carbonyl]-4-{2-[4,4-dimethyl-7-(methyloxy)-1,3-dioxo-3,4-dihydroisoquinolin-2(1H)-yl]ethyl}benzenesulfonamide - Exam
Authoritative Data Verified Data
chloride
take 2.0g of this product, add 100ml of water, boil, to the remaining about 50ml, quickly let cool, filter, add water to the filtrate to make 50ml, take 25ml, inspection according to law (General rule 0801 ), compared with the standard sodium chloride solution 7.0ml of the control solution, not more concentrated (0.007%).
sulfate
take 25ml of the filtrate remaining under the chloride check item and check it according to law (General rule 0802). Compared with the control solution made of 0.02% of standard potassium sulfate solution, it should not be more concentrated ().
Related substances
take the right amount of this product, precision weighing, plus mobile phase ultrasound to dissolve and dilute the solution containing about 2mg per 1ml, filtering, filtrate as a test solution; take 1ml accurately, put it in a 100ml measuring flask, dilute it to the scale with mobile phase, and use it as a control solution. Take an appropriate amount of isoquinoline reference substance, and weigh it accurately, the mobile phase was added to dissolve and dilute to prepare a solution containing about lOug per 1ml as a control solution. According to the chromatographic conditions under the content determination item, 20ul of the test solution, the control solution and the reference solution are respectively injected into the liquid chromatograph, the chromatogram was recorded to 2 times of the retention time of the main component peak. If there is an impurity peak in the chromatogram of the test solution that is consistent with the retention time of the isoquinoline substance, the peak area shall be calculated according to the external standard method, and the isoquinoline substance shall not exceed 0.75%; the sum of the peak areas of other impurities shall not be greater than the main peak area of the control solution (1.0%).
loss on drying
take this product, dry to constant weight at 105°C, weight loss shall 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%.
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).
Last Update:2022-01-01 15:36:17
N-[(cyclohexylamino)carbonyl]-4-{2-[4,4-dimethyl-7-(methyloxy)-1,3-dioxo-3,4-dihydroisoquinolin-2(1H)-yl]ethyl}benzenesulfonamide - Content determination
Authoritative Data Verified Data
measured by high performance liquid chromatography (General 0512).
chromatographic conditions and system suitability test
silica gel bonded with OCTA alkyl silane as filler; Ammonium dihydrogen phosphate solution (take 1.725g of ammonium dihydrogen phosphate, add water to dissolve 3.5±0.1, adjust pH to with phosphoric acid)-acetonitrile (3:5) the detection wavelength was 310Nm. Appropriate amounts of gliquidone control and isoquinoline control were dissolved and diluted with mobile phase ultrasound to prepare 50ug solutions each in 1 ml, and 20ul was injected into the liquid chromatograph, the number of theoretical plates shall not be less than 2000 calculated by gliquidone peak, and the separation degree between gliquidone peak and isoquinoline peak shall meet the requirements.
assay
take this product, precision weighing, plus mobile phase ultrasound to dissolve, cool, and quantitative dilution made in each lml containing about 0.lmg solution was used as the test solution, and 20ul was injected into the liquid chromatograph with precision, and the chromatogram was recorded. Another gliquidone reference substance was taken and determined by the same method. According to the external standard method to calculate the peak area, that is.
Last Update:2022-01-01 15:36:17
N-[(cyclohexylamino)carbonyl]-4-{2-[4,4-dimethyl-7-(methyloxy)-1,3-dioxo-3,4-dihydroisoquinolin-2(1H)-yl]ethyl}benzenesulfonamide - Category
Authoritative Data Verified Data
Last Update:2022-01-01 15:36:18
N-[(cyclohexylamino)carbonyl]-4-{2-[4,4-dimethyl-7-(methyloxy)-1,3-dioxo-3,4-dihydroisoquinolin-2(1H)-yl]ethyl}benzenesulfonamide - Storage
Authoritative Data Verified Data
Last Update:2022-01-01 15:36:18
N-[(cyclohexylamino)carbonyl]-4-{2-[4,4-dimethyl-7-(methyloxy)-1,3-dioxo-3,4-dihydroisoquinolin-2(1H)-yl]ethyl}benzenesulfonamide - Gliquidone Tablets
Authoritative Data Verified Data
This product contains gliquidone (C27H33N306S) should be 95.0% ~ 105.0% of the label.
trait
This product is white tablet.
identification
- take an appropriate amount of fine powder of this product, add an appropriate amount of mobile phase, ultrasonic dissolve and dilute gliquidone to make about 0.1 mg of the solution was filtered, and the filtrate was used as the test solution; Another gliquidone control substance was taken, dissolved and diluted by adding mobile phase ultrasound to make about 0 per 1 ml. 1 mg solution, as a control solution. According to the chromatographic conditions under the relevant substances inspection item, 20ul of the test solution and the reference solution are respectively injected into the liquid chromatograph, and the chromatograms are recorded, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the control solution.
- take an appropriate amount of fine powder of this product (about 20mg equivalent to gliquidone), grind it finely, add 10ml of methanol, grind it and dissolve it, filter it, evaporate the filtrate to dryness, and dry the residue under reduced pressure, determination according to law (General rule 0402). The infrared absorption spectrum of this product should be consistent with the spectrum of the control (Spectrum set 1097 figure).
examination
- relevant substances: take an appropriate amount of fine powder of this product, precisely weigh it, add an appropriate amount of mobile phase, and ultrasonically dissolve and dilute gliquidone to make a solution containing about 2mg per 1ml, and filter it, the filtrate was used as the test solution; 1ml of the sample was accurately measured and placed in a 100ml measuring flask, diluted to the scale with mobile phase, and then shaken to serve as the control solution, A solution containing about 1 ug per 1ml was prepared using the mobile phase as a control solution. If there is an impurity peak in the chromatogram of the test solution with the same retention time as the isoquinoline peak, the peak area shall be calculated according to the external standard method, isoquinoline shall not exceed 1.0% of the labeled amount of gliquidone, and the sum of the peak areas of other impurities shall not be greater than 1.5 times (1.5%) of the main peak area of the control solution.
- dissolution dissolution of this product, according to the dissolution and release determination method (General rule 0931 second method), with phosphate buffer solution (take disodium hydrogen phosphate 71.2g, add water 1000ml to dissolve, adjust the pH value to 10% with 8.5 citric acid solution) as the dissolution medium, the rotation speed is 75 rpm, operate according to law, after 45 minutes, take the solution to filter, take the filtrate as the test solution; another gliquidone reference product, about 30mg, was precision weighed and dissolved by adding 10ml of N,N-dimethylformamide, and quantitatively diluted with dissolution medium to prepare a solution containing about 30ug per 1 ml as a reference solution. The absorbance of each of the above two Solutions was measured at a wavelength of 0401 NM according to ultraviolet-visible spectrophotometry (general), and the elution amount of each tablet was calculated. The limit is 75% 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
Take 10 tablets of this product, precision weighing, fine grinding, precision weighing appropriate amount (about 50mg equivalent to gliquidone), put it in a 100ml measuring flask, add about 70ml of methanol, dissolve gliquidone by ultrasound in water bath, let it cool, dilute to scale with methanol, shake well, filter, take 10ml continuous filtrate accurately and put it in 50ml measuring flask, dilute with methanol to the scale, shake, according to UV-visible spectrophotometry (General rule 0401), absorbance was measured at the wavelength of 310nm; Another gliquidone reference, precision weighing, methanol was added to dissolve and quantitatively diluted to make about 0.lmg solution, the same method for the determination, calculation, that is.
category
same glitazinone.
specification
30mg
storage
light shielding, sealed storage.
Last Update:2022-01-01 15:36:19