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Glibenclamide

$64

  • Brand : BIOFRON

  • Catalogue Number : BN-O1284

  • Specification : 98%(HPLC)

  • CAS number : 10238-21-8

  • Formula : C23H28ClN3O5S

  • Molecular Weight : 494

  • PUBCHEM ID : 3488

  • Volume : 20mg

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Catalogue Number

BN-O1284

Analysis Method

Specification

98%(HPLC)

Storage

2-8°C

Molecular Weight

494

Appearance

Botanical Source

Structure Type

Category

SMILES

COC1=C(C=C(C=C1)Cl)C(=O)NCCC2=CC=C(C=C2)S(=O)(=O)NC(=O)NC3CCCCC3

Synonyms

glybenzcyclamide/Glybenclamide/Daonil/5-Chloro-N-(2-{4-[(cyclohexylcarbamoyl)sulfamoyl]phenyl}ethyl)-2-methoxybenzamide/Benzamide, 5-chloro-N-[2-[4-[[[(cyclohexylamino)carbonyl]amino]sulfonyl]phenyl]ethyl]-2-methoxy-/Benzenecarboximidic acid, 5-chloro-N-[2-[4-[[[(E)-(cyclohexylimino)hydroxymethyl]amino]sulfonyl]phenyl]ethyl]-2-methoxy-/Glyburide/5-Chloro-N-[2-(4-{[(E)-(cyclohexylimino)(hydroxy)methyl]sulfamoyl}phenyl)ethyl]-2-methoxybenzenecarboximidic acid/Diabeta/Euglucon/Micronase/5-Chloro-N-[4-(3-cyclohexylureidosulfonyl)phenethyl]-2-methoxybenzamide/Glynase/Glibenclamide/5-chloro-N-[2-[4-(cyclohexylcarbamoylsulfamoyl)phenyl]ethyl]-2-methoxybenzamide/5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide

IUPAC Name

5-chloro-N-[2-[4-(cyclohexylcarbamoylsulfamoyl)phenyl]ethyl]-2-methoxybenzamide

Density

1.4±0.1 g/cm3

Solubility

Flash Point

380.6±35.7 °C

Boiling Point

705.7±70.0 °C at 760 mmHg

Melting Point

173-175°C

InChl

InChl Key

ZNNLBTZKUZBEKO-UHFFFAOYSA-N

WGK Germany

RID/ADR

HS Code Reference

Personal Projective Equipment

Correct Usage

For Reference Standard and R&D, Not for Human Use Directly.

Meta Tag

provides coniferyl ferulate(CAS#:10238-21-8) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of coniferyl ferulate are included as well.>> amp version: coniferyl ferulate

No Technical Documents Available For This Product.

PMID

28665392

Abstract

The article presents a review of the literature on the use of a fundamentally new technique for prevention and treatment of cerebral edema. A drug glibenclamide, which is used to treat type 2 diabetes mellitus, is able to reduce cerebral edema and neuronal damage as evidenced by the results of preclinical trials in rodents and the first results of drug application in patients. The article describes the mechanism of glibenclamide action and discusses the potential for its application.

KEYWORDS

glibenclamide; malignant cerebral edema; neuroprotection; sulfonylurea receptor 1 (SUR-1)

Title

[Glibenclamide as a promising agent for prevention and treatment of cerebral edema].

Author

Tsarenko SV1, Dzyadz'ko AM2, Rybalko SS3.

Publish date

2017

PMID

30027418

Abstract

In an attempt to decrease the dose, anticipated side effects, and the cost of production of glibenclamide, GLC, a potent oral hypoglycemic drug, the enhancement of the dissolution and hence the oral bioavailability were investigated. Adsorption and co-adsorption techniques using carriers having a very large surface area and surface active agents were utilized to enhance the drug dissolution. Moreover, the Langmuir adsorption isotherms were constructed to identify the type and mechanism of adsorption. The optimized formulation showing the highest in vitro release was compressed into mini-tablet to facilitate drug administration to elderly patients and those having swallowing difficulties. The produced mini-tablets were tested for their mechanical strength and in vitro release pattern. In addition, the pharmacodynamic and pharmacokinetic studies in New Zealand rabbits were performed using the optimized mini-tablet formulation. Mini-tablets containing GLC co-adsorbate with Pluronic F-68 and Laponite RD showed 100 ± 1.88% of GLC released after 20 min. Pharmacodynamic studies in rabbits revealed significantly higher (p ≤ 0.05) hypoglycemic effect with the optimized mini-tablets at a lower GLC dose compared to mini-tablets containing the commercial GLC dose. Moreover, pharmacokinetic analysis showed significantly higher (p ≤ 0.05) AUC, Cmax, and shorter Tmax. The optimized mini-tablet formulation showed 1.5-fold enhancement of the oral bioavailability compared to mini-tablets containing untreated GLC. It could be concluded that the co-adsorption technique successfully enhanced the oral bioavailability of GLC. Furthermore, the produced mini-tablets have a higher oral bioavailability with a lower GLC dose, which could offer economic benefit for industry as well as acceptability for patients.

KEYWORDS

co-adsorbates; glibenclamide; mini-tablets; oral bioavailability; pharmacodynamics

Title

Glibenclamide Mini-tablets with an Enhanced Pharmacokinetic and Pharmacodynamic Performance.

Author

Tawfeek HM1,2, Roberts M3, El Hamd MA4,5, Abdellatif AAH6,7, Younis MA8.

Publish date

2018 Oct

PMID

32127822

Abstract

BACKGROUND:
Oral hypoglycemic agents use during pregnancy was assumed to cause fetal macrosomia and skeletal deformities, and maternal complications due to significant transfer across placenta or ineffective control of blood glucose.

OBJECTIVE:
This study investigated effects of insulin, metformin and glibenclamide on maternal blood glucose; and fetal crown-rump length, gross malformation and pancreatic histology in pregnant streptozotocin-induced diabetic rats.

METHODS:
Twenty-five pregnant rats of groups 1 to 5 as normal and diabetic controls; and diabetic treated with insulin, metformin and glibenclamide were used. Experimental GDM was induced using 45 and 35mg/Kgbw of intraperitoneal streptozotocin.

RESULTS:
Metformin, Insulin and Glibenclamide significantly reduced maternal glucose by 140.6mg/dL, 103.2mg/dL and 98.54mg/dl; respectively and showed islets with regular interlobular ducts, islets with some irregular interlobular ducts, and islets with many irregular interlobular ducts in histological fetal pancreatic photomicrographs respectively. This depicts metformin having highest ameliorative effect. There were no significant differences in maternal and fetal body weights, maternal blood glucose between diabetic groups, and fetal gross examination.

CONCLUSION:
At the doses used in this research, metformin and glibenclamide showed no adverse effects on maternal and fetal features in the treatment of GDM. Thus, they can be used as safe and inexpensive alternatives to insulin.

© 2019 Lawal et al.

KEYWORDS

Gestational diabetes mellitus; blood glucose; fetal malformation and fetal pancreatic histology; oral hypoglycemic agents

Title

Comparative effects of glibenclamide, metformin and insulin on fetal pancreatic histology and maternal blood glucose in pregnant streptozotocin-induced diabetic rats.

Author

Lawal SK1,2, Adeniji AA3, Sulaiman SO4, Akajewole MM5, Buhari MO6, Osinubi AA3.

Publish date

2019 Sep


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