Voglibose

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H302：Gesundheitsschädlich bei Verschlucken.

  H315：Verursacht Hautreizungen.

  H319：Verursacht schwere Augenreizung.

  H335：Kann die Atemwege reizen.

• Sicherheit

  P261：Einatmen von Staub vermeiden.

  P305+P351+P338：BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach Möglichkeit entfernen. Weiter spülen.

Voglibose Chemische Eigenschaften,Einsatz,Produktion Methoden

• R-Sätze Betriebsanweisung:

  R20/21/22:Gesundheitsschädlich beim Einatmen,Verschlucken und Berührung mit der Haut.
  R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.

• S-Sätze Betriebsanweisung:

  S36/37:Bei der Arbeit geeignete Schutzhandschuhe und Schutzkleidung tragen.
  S37/39:Bei der Arbeit geeignete Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
  S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.

• Beschreibung

  Voglibose was introduced in Japan for the treatment of postprandial hyperglycemia in diabetic patients. As an orally active α-D-glucosidase inhibitor, it is effective in decreasing the release of glucose from carbohydrate ingestion and slowing the increase of postprandial blood glucose levels, as demonstrated in animals and humans following sucrose and starch loading. In addlion, voglibose was reported to have prophylactic effect in genetically obese Wistar rats, maintaining low plasma levels of glucose, triglyceride and insulin, indicating a potential usefulness for the management of other carbohydrate-dependent metabolic disorders such as obesity. Voglibose is much more potent and has fewer side effects than acarbose, another agent in its class.

• Chemische Eigenschaften

  Colourless Crystalline Solid

• Originator

  Takeda (Japan)

• Verwenden

  For the treatment of diabetes. It is specifically used for lowering post-prandial blood glucose levels thereby reducing the risk of macrovascular complications.

• Verwenden

  An α-Glucosidase inhibitor used as an antidiabetic.

• Verwenden

  An alpha-Glucosidase inhibitor used as an antidiabetic

• Verwenden

  Voglibose is an α-glucosidase inhibitor, similar to acarbose and miglitol, used for lowering post-prandial hyperglycemia (PPHG) in people with diabetes mellitus. Voglibose is used to study it benefits as a protectant against ischemia-reperfusion injury through glucagon-like peptide 1 receptors and the phosphoinositide 3-kinase-Akt-endothelial nitric oxide synthase pathway.

• Definition

  ChEBI: Voglibose is an organic molecular entity.

• Manufacturing Process

  N-(1,3-Dihydroxy-2-propyl)valiolamine:
  To a solution of 2.0 g of valiol amine in 50 ml of N,N-dimethylformamide are added 3.4 g of dihydroxyacetone, 1.5 ml of 2 N hydrochloric acid and 2.6 g of sodium cyanoborohydride, followed by stirring at 60 to 70°C for 16 hours. The reaction solution is concentrated under reduced pressure to distill off the N,N- dimethylformamide as much as possible, and the residue is dissolved in 100 ml of water. The solution is made acid with 2 N hydrochloric acid, stirred for 30 to 40 minutes under ice-cooling, adjusted to pH 4.5 with 1 N sodium hydroxide solution and subjected to column chromatography (250 ml) on Dowex 50W x 8 (H + type) (produced by Dow Chemical of the United States of America). After the washing with water, the elution is carried out with 0.5 N aqueous ammonia. The eluate is concentrated under reduced pressure, and the concentrate is chromatographed on a column (250 ml) of Amberlite CG-50 (NH 4 + type) (produced by Rohm and Haas Co. of the United States of America), followed by the elution with water. The eluate is concentrated under reduced pressure, and the concentrate is lyophilized to give 2.0 g of white powder of N-(1,3-dihydroxy-2-propyl)valiol amine.
  Ethanol (about 60 ml) is added to the above lyophilized product (1.2 g) of N- (1,3-dihydroxy-2-propyl)valiol amine, and the mixture is warmed for 30 minutes in a hot water bath (the bath temperature: 90-95°C), followed by leaving on standing in a refiegerator. The resultant crystalline substance is recovered by filtration, washed with ethanol and then dried in a desiccator under reduced pressure. Yield of 0.95 g. MP: 162-163°C. [α] D 25 = +26.2° (c = 1, H 2 O).

• Trademarks

  Basen (Takeda); Glustat (Takeda).

• Therapeutic Function

  Antidiabetic, Antiobesity

• Weltgesundheitsorganisation (WHO)

  Acarbose and voglibose area-glucosidase inhibitors and delay digestion/absorption of carbohydrates as well as improving postprandial hyperglycaemia.

• Allgemeine Beschreibung

  The most potent -glucosidase inhibitor is the valiolamine derivative voglibose. Compared with acarbose its inhibitory potency in vitro, depending on the -glucosidase enzyme, is up to 200 times higher. In Japan, daily dosages are only 0.3 – 0.9 mg, however, therapeutic efficacy on HbA1c reduction could not be clearly demonstrated with those dosages. HbA1c, a glycated hemoglobin species, which occurs in blood, is a diagnostic measure for the non-enzymatic glycation process, and depends on the plasma glucose concentration. The process of protein glycation is discussed to be responsible for the development of diabetic complications (neuropathy, retinopathy, nephropathy). In Europe voglibose is under evaluation with distinctly higher daily dosages of 1.5 to 6 mg. In contrast to acarbose, the smaller inhibitors of the monosaccharide type (miglitol, emiglitate, voglibose) do not inhibit pancreatic -amylase.

• Biologische Aktivität

  Orally active α -glucosidase inhibitor (IC 50 values are 3.9 and 6.4 nM at sucrase and maltase respectively). Increases glucagon-like peptide 1 (GLP-1) secretion and decreases food consumption in ob/ob mice, and reduces plasma concentrations of glucose, triglycerides and insulin in Wistar fatty rats. Exhibits antidiabetic and antiobesity activity in vivo .

Voglibose Upstream-Materialien And Downstream Produkte

Voglibose Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Global(530)Suppliers

83480-29-9, Voglibose Verwandte Suche: