Etodolac Raw material Etodolac Powder

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Etodolac Powder Usage and Synthesis.

Etodolac, also known as etodolac, indole pyranoacetic acid, rodin, etc., under the trade name Lodine, is a new generation of COX-2 highly selective non-steroidal anti-inflammatory drug. It is a weakly acidic drug, which is in molecular form at lower pH, which is favourable for drug absorption.

It is widely used in the treatment of post-surgical pain, has analgesic and anti-inflammatory effects can relieve the symptoms of rheumatoid arthritis and osteoarthritis, delay arthritis-induced bone pathological changes, can selectively inhibit the synthesis of prostaglandins at the site of inflammation and anti-inflammatory.

It is especially suitable for elderly patients. It is white crystalline powder, melting point:145-148℃.

Etodolac was first developed by a subsidiary of AHP in the United States and was successfully marketed in the United Kingdom in 1985, and then in France, the United States, Germany, Japan and other countries.

Uses of Etodolac.

Used as anti-inflammatory and analgesic

Indoleacetic acid non-steroidal anti-inflammatory drug with analgesic and anti-inflammatory effects. It can inhibit prostaglandin synthesis selectively at the site of inflammation and anti-inflammatory.

It is rapidly absorbed and shows no signs of accidental accumulation of the drug. It is used in the treatment of rheumatoid arthritis, rheumatoid arthritis, osteoarthritis and postoperative pain relief. It is a suitable drug for the treatment of elderly patients.

Mechanism of action Etodolac.

Etodolac is a non-steroidal anti-inflammatory drug. Its effect is similar to aspirin in that it selectively inhibits prostaglandin biosynthesis by blocking cyclooxygenase activity at the site of inflammation. The inhibition of gastric PGE2 is mild and transient, resulting in fewer gastrointestinal adverse effects.

Oral absorption is rapid, a single dose of 200mg tonic, Tmax is 1h, Cmax is about 18.6μg/ml. T1/2 is 7.4h. PPB is 95%. The drug does not accumulate in the body, after tissue cell metabolism, 60% of the dose is excreted within 24h. 74% of the dose is excreted in the urine via the kidney.

74% is excreted in urine via the kidneys and 19% in faeces. It reduces the incidence and severity of bone and joint damage and reverses the progression of the disease.

Current studies have shown no teratogenic effects in animal studies, and low effects on fertility and general reproductive function.

Product Method of Bulk Etodolac Powder.

Reaction of o-ethyl aniline with trichloroacetaldehyde hydrate and hydroxylamine results in the formation of an oxime along with acylation, followed by sulfuric acid-catalyzed cyclisation and reduction with lithium aluminium hydride to form an indole derivative, reaction with oxaloyl chloride and ethanol introduces a 1,2-dicarbonyl side-chain at the 3-position, which is reduced to a hydroxyethyl group by lithium aluminium hydride, and the condensation of the cyclisation with propionyl acetate, which is hydrolysed to form etodolac.

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