Name | Glybenzcyclamide |
Synonyms | GLYBURIDE Glyburide GIBENCLAMIDE GLYBENCLAMIDE GLYBURIDE USP GLIBENCLAMIDE glybenclamide Glibenclamide glyburide usp Glybenzcyclamide GLYBENZCYCLAMIDE LABOTEST-BB LT00244861 GlibenclamideGlibenclamideBp 5-chloro-2-methoxy-N-[2-[4-(phenylcarbamoylsulfamoyl)phenyl]ethyl]benzamide 5-chloro-N-(2-{4-[(cyclohexylcarbamoyl)sulfamoyl]phenyl}ethyl)-2-methoxybenzamide 5-Chloro-N-[2-[4-[[[(cyclohexylamino)carbonyl]-amino]sulfonyl]phenyl]-ethyl]-2-methoxybenzamide 5-chloro-n-(2-(4-((((cyclohexylamino)carbonyl)-amino)sulfonyl)phenyl)-ethyl)-2-methoxybenzamide |
CAS | 10238-21-8 |
EINECS | 233-570-6 |
InChI | InChI=1/C23H22ClN3O5S/c1-32-21-12-9-17(24)15-20(21)22(28)25-14-13-16-7-10-19(11-8-16)33(30,31)27-23(29)26-18-5-3-2-4-6-18/h2-12,15H,13-14H2,1H3,(H,25,28)(H2,26,27,29) |
InChIKey | ZNNLBTZKUZBEKO-UHFFFAOYSA-N |
Molecular Formula | C23H28ClN3O5S |
Molar Mass | 494 |
Density | 1.1805 (rough estimate) |
Melting Point | 173-175°C |
Boling Point | 705.7±70.0 °C at 760 mmHg |
Water Solubility | Soluble in ethanol (5 mg/mL), DMSO (25 mg/mL), chloroform (1:36), methanol (1:250), and DMF. Insoluble in water. |
Solubility | Soluble in ethanol (5 mg/ml),DMSO(25 mg/ml), chloroform (1:36), methanol (abstract),DMF. Insoluble in water. |
Appearance | Powder |
Color | White |
Merck | 14,4478 |
pKa | 5.3(at 25℃) |
Storage Condition | 2-8°C |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months. |
Refractive Index | 1.6100 (estimate) |
MDL | MFCD00056625 |
Physical and Chemical Properties | White crystalline powder. Melting point 168-173 ℃. Insoluble in water, slightly soluble in ethanol, acetone, chloroform. |
Use | Hypoglycemic agents for the treatment of moderate to mild non-insulin dependent diabetes mellitus |
Hazard Symbols | Xn - Harmful |
Risk Codes | 20/21/22 - Harmful by inhalation, in contact with skin and if swallowed. |
Safety Description | S22 - Do not breathe dust. S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. S36 - Wear suitable protective clothing. S24/25 - Avoid contact with skin and eyes. |
WGK Germany | 2 |
RTECS | YS4725200 |
HS Code | 29350090 |
Toxicity | LD50 in rats and mice (g/kg): >20 orally; >12.5 i.p.; >20 s.c. (Mizukami) |
Reference Show more | 1. Liang Haimei Yu Hua Peng Xia Hu Yi Li Fang Zekui Li Zhongli. Expression of NLRP3 and IL-33 in LPS-induced macrophages and the effect of glibenclamide on their expression [J]. Journal of Tropical Medicine 2013 13(05):570-572 594 669. 2. Xu Chao, Zhang Hua, Chen Jianli et al. Effect of NLRP3 on Pulmonary Inflammation Induced by Respiratory Syncytial Virus [J]. Chinese Journal of Endemic Diseases 2016 031(012):1383-1384. 3. Sheng Chenming, Shi Xiaoyan, Ding Zexian, etc. Effects of Mulberry Leaf Extract on Cytochrome P450 Enzyme Activity in Rats [J]. Journal of Anhui College of Traditional Chinese Medicine, 2019, 038(002):55-60. 4. Ge Tao, Peng Hui, Zhang Xiang, et al. Effects of Polyoxyethylene Sorbitol Monooleate on Cytochrome P450 Enzyme Activity in Rats [J]. Zhongnan Pharmacy, 2017, 015(012):1699-1703. 5. Song Xiang, chen Weidong, Wang Lei, et al. Ultra performance liquid chromatography-tandem mass spectrometry determination of blood-cutting saponin a in rat plasma [J]. Zhongnan pharmacy, 2020, v.18;No.171(04):54-58. 6. Sun, Jing, et al. "Effect of gambogenic acid on cytochrome P450 1A2, 2B1 and 2E1, and constitutive androstane receptor in rats." European journal of drug metabolism and pharmacokinetics 43.6 (2018): 655-664.https://doi.org/10.1007/s13318-018-0477-7 7. Jayachandran, Muthukumaran, et al. "Isoquercetin upregulates antioxidant genes, suppresses inflammatory cytokines and regulates AMPK pathway in streptozotocin-induced diabetic rats." Chemico-biological interactions 303 (2019): 62-69.https:// doi.org/10.1016 8. [IF = 1.913] Sun Jing et al. "Effect of Gambogenic Acid on Cytochrome P450 1A2, 2B1 and 2E1, and Constitutive Androstane Receptor in Rats." Eur J Drug Metab Ph. 2018 Dec;43(6): 655-664 9. [IF = 3.411] Hong Li-li et al. "Evaluation of Zhenwu Decoction Effects on CYP450 Enzymes in Rats Using a Cocktail Method by UPLC-MS/MS." Biomed Res Int. 2020;2020:4816209 |
This product is N-[2-[4-[[(cyclohexylamino)) YL] amino] sulfonyl] phenyl] ethyl]-2-methoxy-5-chlorobenzamide. Calculated as dry product, containing no less than 99.0% of C23H28C1N305S.
The melting point of this product (General 0612) is 170~174°C.
take this product l. Add 50ml of water, boil, quickly cool, filtered, filtrate to 50ml, take 25ml, check according to law (General rule 0801), and standard sodium chloride solution 7.0ml of the control solution should not be more concentrated (0.014%).
take 25ml of the filtrate remaining under the above chloride item and check it according to law (General rule 0802). Compared with the control solution made of 0.040% of standard potassium sulfate solution, it should not be more concentrated ().
take about 25mg of this product, accurately weigh, put it in 50ml measuring flask, add methanol 25ml, ultrasonic to dissolve, dilute to scale with mobile phase, shake, as a test solution; take another 4-[2-(5-chloro-2-methoxybenzoylamino) ethyl] benzenesulfonamide (impurity I) 15mg for each of the reference and N-[4-[2-(5-chloro-2-methoxybenzoylamino) ethyl] benzenesulfonyl] carbamic acid ethyl ester (impurity II), in the same 50ml measuring flask, add methanol 10ml, ultrasonic to dissolve, dilute to scale with mobile phase, shake well, as a stock solution of mixed impurity reference substance; 1ml of each sample solution and 1ml of the stock solution of the mixed impurity reference substance were respectively accurately weighed, placed in the same 100ml measuring flask, diluted to the scale with the mobile phase, and shaken well to serve as a control solution. According to the chromatographic conditions under the content determination item, 20ul of each of the test solution and the control solution are accurately measured and injected into the liquid chromatograph respectively, and the chromatogram is recorded to 2 times of the retention time of the main component peak. If there are chromatographic peaks in the chromatogram of the test solution that are consistent with the retention time of impurity I or impurity II in the chromatogram of the control solution, the peak area shall be calculated according to the external standard method, and shall not exceed 0.6%, the sum of the peak areas of other impurities shall not be greater than 0.5 times (0.5%) of the main peak area of the control solution.
take this product, dry to constant weight at 105°C, weight loss shall not exceed 0.5% (General rule 0831).
take l.Og of this product and check it according to law (General rule 0841). The residue left shall not exceed 0.1%.
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).
measured by high performance liquid chromatography (General 0512).
silica gel bonded with OCTA alkyl silane as filler; Ammonium dihydrogen phosphate solution (1.725g of ammonium dihydrogen phosphate, 300ml of water, pH adjusted to 3.5±0.05 with phosphoric acid)-methanol (3:5) mobile phase; The detection wavelength was 300nm. The reference solution 20u1 under the item of related substances is injected into the liquid chromatograph, and the chromatogram is recorded. The order of the separated peaks in each group is impurity I, impurity II and glibenclamide. The number of theoretical plates shall not be less than 5000 calculated by glibenclamide peak, and the separation degree of impurity I peak and impurity II peak shall meet the requirements.
take about 10mg of this product, weigh it accurately, put it in a 50ml measuring flask, add 12ml of methanol, ultrasonic dissolve glibenclamide, dilute it to the scale with mobile phase, shake it well, as a test solution, 20ul was injected into the liquid chromatograph with precise quantity, and the chromatogram was recorded. Another reference substance of glibenclamide was taken and determined by the same method. According to the external standard method to calculate the peak area, that is.
hypoglycemic drugs.
sealed storage.
This product contains glibenclamide (C23H28CIN305S) should be labeled amount of 90.0% ~ 110.0%.
This product is white tablet.
Take 20 tablets of this product, precision weighing, fine grinding, precision weighing an appropriate amount (about 10mg equivalent to Glibenclamide), put it in a 50ml measuring flask, add 12ml methanol, ultrasound to dissolve glibenclamide, dilute to the scale with mobile phase, shake, filter, take the continued filtrate as a test solution, take 20 u1 with precision, and measure according to the method under the content determination of glibenclamide.
Same as glibenclamide.
2.5mg
sealed storage.