アカルボース 化学特性,用途語,生産方法
外観
白色～わずかにうすい黄色、結晶～粉末
溶解性
水に溶ける。
解説
C25H43NO18(645.61)．アカルボースは，放線菌Actinoplanes sp. SE 50の培養液から精製された無定形粉末．擬似オリゴ糖で強力なα-グルコシダーゼ阻害物質．1995年にアメリカで糖尿病や肥満の治療薬として認可された．[α]D＋147.2°(水)．森北出版「化学辞典（第2版）
用途
α- グルコシダーゼ阻害剤です。
二糖から単糖に分解するα- グルコシダーゼ
を阻害し、糖質の消化・吸収を遅延させる作
用があります。
用途
α-グルコシダーゼ阻害剤です。 二糖から単糖に分解するα-グルコシダーゼ を阻害し、糖質の消化・吸収を遅延させる作 用があります。
効能
糖尿病治療薬, α-グルコシダーゼ阻害薬
商品名
グルコバイ (バイエル薬品); グルコバイ (バイエル薬品)
使用上の注意
不活性ガス封入
説明
Acarbose, a complex oligosaccharide isolated from Actinoplanes, is reportedly
useful as an adjuvant therapy in diabetes. By inhibiting alpha-glucosidase,
acarbose delays carbohydrate metabolism in the gastrointestinal tract and modulates
changes in food induced blood sugar levels.
化学的特性
Off-White Solid
使用
Acarbose is pseudo-oligosaccharide with a terminal C7-cyclitol patented in 1975 by Bayer. Acarbose is a component of the amylostatin complex produced by a species of Actinoplanes and Streptomyces. Acarbose acts as a potent inhibitor of alpha-glucosidases and saccharases. Since 1990, acarbose has been used therapeutically for the treatment of type 2 diabetes.
定義
ChEBI: A tetrasaccharide derivative consisting of a dideoxy-4-{[4,5,6-trihydroxy-3-(hydroxymethyl)cyclohex-2-en-1-yl C7 cyclitol moiety [called valienol (or valienamine)] linked via nitrogen to isomaltotriose.
世界保健機関（WHO）
Acarbose, ana-glucosidase inhibitor, is used as an adjunctive
therapy in the control of postprandial hyperglycaemia in non-insulin-dependent
diabetes mellitus. Use of two or more hypoglycaemic drugs is not recommended.
一般的な説明
Acarbose is a naturally occurring oligosaccharide,which is obtained from the microorganism Actinoplanes utahensis. It is a white to off-white powder that is soluble in water and has a pKa of 5.1. As one mightexpect, its affinity for α-glucosidase is based on it being apolysaccharide that the enzyme attempts to hydrolyze. Thisallows acarbose to act as a competitive inhibitor, which inturn reduces the intestinal absorption of starch, dextrin, anddissacharides.
It is sold as 25-, 50-, and 100-mg tablets (Precose,generics) dosed with the first bite of each meal, up to t.i.d. Acarbose potently inhibits the glucoamylase activity of MGAM α-glucosidases and the sucrase activity of α-glucosidases, where as isomaltase activity is at most moderately inhibited at concentrations in the range of those in theintestinal lumen upon oral dosing, and trehalase and lactaseare not significantly inhibited. Some inhibition of pancreaticα-amylases may also contribute to the clinical effects.
https://www.sciencedirect.com
臨床応用
Based on the structure of acarbose, it should come as nosurprise that little intact acarbose reaches the systemic circulation;instead, acarbose is extensively biotransformed by the actionof microbes and digestive enzymes in the gut. Only about35% of the radioactivity in a dose of
14C-labeled acarbose administeredorally to men was excreted in the urine, appearingas several metabolites, some of which are phase II conversionproducts of 4-methylpyrogallol (O-methyl, O-sulfate, orO-glucuronide conjugates); the methylpyrogallol fragmentarises from the terminal valienamine pseudosugar. That thesebiotransformation products are mostly formed in the gut isshown by the fact that nearly 90% of an intravenously administereddose of acarbose is excreted intact in urine.
安全性プロファイル
Low toxicity by ingestion,subcutaneous, and intravenous routes. Human systemiceffects: liver function impaired. When heated todecomposition it emits toxic vapors of NOx.
アカルボース 上流と下流の製品情報
原材料
準備製品