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Product details
Diclofenac sodium is a white crystalline powder, with trade names such as fu-tarine, to be kefenac, suitarine, etc. It is a non-steroidal anti-inflammatory drug (NSAID) derived from phenylacetic acid, and is mainly used in the treatment of osteoarthritis, rheumatoid arthritis, polymyositis, dermatomyositis, spondyloarthropathies, ankylosing spondylitis, etc., where acute pain relief is required.
Uses and functions of Diclofenac sodium.
Diclofenac sodium is used as an anti-inflammatory and analgesic, mainly for the treatment of osteoarthritis,rheumatoid arthritis, polymyositis, dermatomyositis, spondyloarthropathies, ankylosing spondylitis, gout, as well as migraines, toothaches, gallstones, and kidney stones that require acute pain relief.
Diclofenac sodium is a potent antipyretic, analgesic and anti-inflammatory drug. Its anti-inflammatory effect is 2-2.5 times stronger than that of indomethacin and 26-50 times stronger than that of acetylsalicylic acid. It is suitable for rheumatoid arthritis, osteoarthritis, post-surgical pain relief and fever caused by various reasons.
Pharmacological Effect of Diclofenac sodium.
Diclofenac Sodium exerts antipyretic and anti-inflammatory effects by inhibiting the enzyme cyclooxygenase,thereby reducing the synthesis of prostaglandins, as well as inhibiting the enzyme lipoxygenase to a certain extent,thereby reducing the production of leukotrienes, bradykinin and other products.
The antipyretic effect of this product has been confirmed in animal tests and human clinical practice. Acute toxicity test results: rat oral LD50 is 150mg/kg; mouse oral LD50 is 390mg/kg. Oral absorption is rapid and complete. Taking with food reduces the absorption rate. Blood concentration peaks at 1~2 hours on average when taken on an empty stomach, peaks at 6 hours when taken with food, and plasma concentration decreases. Drug half-life is about 2 hours.
Plasma protein binding rate is 99%. Concentrations in breast milk are negligibly low, and in synovial fluid, levels are higher than prevailing serum levels by 4 hours after dosing and can be maintained for 12 hours. About 50% of the drug is metabolised in the liver, 40%~65% is excreted from the kidney, 35% is excreted from the bile, and 1.2~2 hours from the faeces. There is no accumulation effect in long-term application.
Product Method of Bulk Diclofenac sodium.
Synthesis of 2,6-dichlorodiphenylamine: 2,6-dichlorophenol and aniline were used as raw materials for 2,6-dichlorodiphenylamine, which was obtained by acylation, condensation, Chapman rearrangement and hydrolysis.The three-step reactions of acylation, condensation and rearrangement, except for the recovery of solvents (toluenefor acylation, and DMF for condensation and rearrangement), were carried out in a "one-pot" manner, i.e., they were completed in the same reactor without the need to separate the step-by-step process.
The reaction was reproducible. Synthesis of diclofenac sodium: 2,6-dichlorodiphenylamine and chloroacetyl chloride were used as the main raw materials, and 1-(2,6 dichlorophenyl)dihydroindol-2-one was obtained by acylation and intramolecular Foucault alkylation, and finally the product, diclofenac sodium, was obtained by alkaline hydrolysis of ring-opening.
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