ランソプラゾール 化学特性,用途語,生産方法
外観
白色～褐色, 結晶性粉末～粉末
溶解性
メタノールにやや溶けやすく、エタノール(99.5)にやや溶けにくく、ジエチルエーテルに極めて溶けにくく、水にほとんど溶けない。
用途
プロトンポンプ阻害剤です。 胃酸生成細胞である壁細胞に移行し、H+、 K+-ATPase活性を強く抑制して胃酸分泌を抑 制します。
用途
プロトンポンプ阻害剤です。
胃酸生成細胞である壁細胞に移行し、H+、
K+-ATPase 活性を強く抑制して胃酸分泌を抑
制します。
効能
消化性潰瘍薬, プロトンポンプ阻害薬
商品名
タケプロン (武田薬品工業); タケプロン (武田薬品工業); タケプロン (武田薬品工業)
説明
Lansoprazole is the second proton pump inhibitor approved as an antiulcer agent for the
short term treatment of duodenal ulcer and gastroesophageal reflux disease. Like
omeprazole, lansoprazole is reported to be more efficacious than the H
2-antagonists in treating peptic ulcer disease.Other potential uses could be in the treatment of Zollinger-Ellison syndrome.
化学的特性
White Crystalline Powder
使用
Used as a gastric proton pump inhibitor. An antiulcerative
一般的な説明
Lansoprazole, 2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl]-1H-benzimidazole(Prevacid), is a white to brownish white, odorless crystallinepowder that is practically insoluble in water.Lansoprazole is a weak base (pyridine N, pKa 3.83.) and aweak acid (benzimidazole N-H, pK 0.62). Like other PPIs,lansoprazole is essentially a prodrug that, in the acidic biophaseof the parietal cell, forms an active metabolite thatirreversibly interacts with the target ATPase of the pump.Lansoprazole must be formulated as encapsulated entericcoatedgranules for oral administration to protect the drugfrom the acidic environment of the stomach.
In the fasting state, about 80% of a dose of lansoprazole(vs. 50% of omeprazole) reaches the systemic circulation,where it is 97% bound to plasma proteins. Thedrug is metabolized in the liver (sulfone and hydroxymetabolites) and excreted in bile and urine, with a plasmahalf-life of about 1.5 hours.
生物活性
H + ,K + -ATPase inhibitor (IC 50 = 6.3 μ M) that displays antisecretory and antiulcer activity. Inhibits gastric acid secretion (IC 50 = 0.09 μ M for histamine-induced acid formation) and reduces gastric lesion formation induced by a variety of ulcerative stimuli. Antibacterial against Helicobacter pylori in vitro . Also blocks swelling-dependent chloride channel (ICIswell) in NIH3T3 fibroblasts. More potent than omeprazole (5-Methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole ).
ランソプラゾール 上流と下流の製品情報
原材料
準備製品