ジクロフェナクナトリウム 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
メタノール,エタノールに易溶、水,酢酸にやや可溶、アセトンに難溶、エーテル,クロロホルムにほとんど不溶。
用途
フェニル酢酸系化合物です。シクロオキシゲナーゼ(COX)を阻害し、プロスタグランジン生合成抑制作用を示します。
用途
薬理・生理作用研究用。
効能
鎮痛薬, 抗炎症薬, 解熱薬, シクロオキシゲナーゼ阻害薬
商品名
ジクロード (わかもと製薬); ナボール (久光製薬); ナボール (久光製薬); ナボール (久光製薬); ナボール (久光製薬); ナボール (久光製薬); ボルタレン (ノバルティスファーマ); ボルタレン (ノバルティスファーマ); ボルタレン (同仁医薬化工); ボルタレン (同仁医薬化工); ボルタレン (同仁医薬化工); ボルタレン (同仁医薬化工)
説明
Diclofenac is a non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor (IC
50s = 0.9-2.7 and 1.5-20 μM, for human COX-1 and COX-2, respectively). It is also an active metabolite of diclofenac methyl ester and diclofenac amide . Diclofenac inhibits release of arachidonic acid (Item Nos.
90010 |
90010.1 |
10006607) induced by A23187 in isolated rat peritoneal neutrophils and macrophages (IC
50s = 60 and 10 μM, respectively). Transdermal administration of diclofenac inhibits carrageenan-induced paw edema in rats. Formulations containing diclofenac have been used in the treatment of pain associated with osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis.
化学的特性
Off-White Crystalline Solid
来歴
Diclofenac sodium is a classic nonsteroidal anti-inflammatory drug (NSAID), known for its potent antipyretic, analgesic, and anti-inflammatory effects, and is marketed under brand names such as Voltaren. Its discovery and widespread use have had a profound impact on the treatment of pain and inflammation.
Discovery and Patent (1965): Diclofenac sodium was synthesized by a team of researchers Rudolf Pfister and Alfred Sallmann at the Swiss pharmaceutical company Ciba-Geigy AG (now part of Novartis) while searching for a highly active and well-tolerated NSAID. The compound was patented in 1965.
First Market Launch (1973): After extensive preclinical and clinical trials, diclofenac sodium was first marketed globally in 1973 under the brand name Voltaren. Its design philosophy is based on clear principles and aims to be an effective cyclooxygenase (COX) inhibitor.
使用
Diclofenac sodium is a nonsteroidal anti-inflammatory compound and cyclooxygenase (COX) inhibitor. Oxidation of diclofenac sodium produces the metabolite 4'-hydroxy diclofenac) which demonstrates specific inhibition of Cox-2. Inhibition of Cox by diclofenac and 4'-hydroxy diclofenac suppresses prostaglandin E2 synthesis, producing anti-inflammatory and analgesic effects. Diclofenac is also shown to stabilize the native tetrameric conformation of transthyretin (TTR) fibrils, preventing the formation of insoluble amyloidogenic TTR deposits. Diclofenac Sodium is a substrate of CYP2C9. It is also used as an inhibitor of Cox-1 and Cox-2.
定義
ChEBI: Diclofenac sodium is the sodium salt of diclofenac. It contains a diclofenac(1-).
世界保健機関（WHO）
The World Health Organization currently has no information to
suggest that diclofenac is less safe than other widely available non-steroidal
antiinflammatory substances of this type, or that children are particularly liable to
react adversely. It is registered in many countries in several dosage forms,
including a 12.5 mg suppository indicated for juvenile arthritis.
一般的な説明
Pharmaceutical secondary standards for application in quality control, provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards.
Diclofenac is a derivative of benzeneacetic acid. It is categorized under the class of non-steroidal anti-inflammatory drugs (NSAIDs). It shows inflammatory, analgesic and antipyretic activities.
臨床応用
Diclofenac sodium is indicated for the treatment of rheumatoid arthritis, osteoarthritis, and ankylosing spondylitis.
合成
Synthesis: Acylation of N-phenyl-2,6- dichloroaniline with chloroacetyl chloride gives the corresponding chloroacetanilide, which is fused with aluminum chloride to give 1-(2,6- dichlorophenyl)-2-indolinone. Hydrolysis of the indolinone with dilute aqueous-alcoholic sodium hydroxide affords the desired sodium salt directly.
ジクロフェナクナトリウム 上流と下流の製品情報
原材料
準備製品