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Product details
Keto Ibuprofen (mainly through the reversible inhibition of cyclooxygenases (COXs) pro-inflammatory peptides and/or lipoxygenases (LOXs) activity, thereby inhibiting the biosynthesis of inflammatory substances prostaglandins (PGs), leukotrienes (LTs) and thromboxanes (TXs), so that bradykinin release is reduced, and then exert its good antipyretic and anti-inflammatory effect, and also has a certain inhibition effect on the adherence and aggregation of platelets. It has a certain inhibitory effect on platelet adhesion and aggregation, and is widely used in the treatment of rheumatoid arthritis, rheumatoid arthritis, ankylosing spondylitis, osteoarthritis, rheumatoid arthritis, as well as dysmenorrhoea, dental pain, postoperative pain, cancer pain and acute renal colic and other pain.
Uses and functions of Ketoprofen.
Anti-inflammatory and analgesic drugs for the treatment of rheumatoid arthritis, ankylosing spondylitis and gout, etc.
Rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, acute joint and periarticular disorders, cervical spondylitis, lower back pain (sprains, lumbago, sciatica, fibrositis), pain in the skeletal muscles and dysmenorrhoea.
Keto Ibuprofen belongs to the arylpropionic acid class of new non-steroidal anti-inflammatory drugs, used in the treatment of all kinds of arthritis, ankylosing spondylitis caused by joint pain, as well as menstrual cramps, dental pain, postoperative pain and cancer pain, etc., and is therefore well received by experts and scholars at home and abroad, as well as the pharmaceutical industry and the patient's respect.
Pharmacological Effect of Ketoprofen.
It has anti-inflammatory, analgesic and antipyretic effects. It has strong anti-inflammatory effect, low side effects and low toxicity. In the same dose, the anti-inflammatory and analgesic effect is 150 times stronger than aspirin, the antipyretic effect is 4 times that of indomethacin, 100 times that of aspirin, and the toxicity is only 1/20 of indomethacin.
It is easily absorbed orally and reaches the peak plasma concentration in 0.5~2 hours after a single administration. Plasma protein binding rate is very strong. 24 hours from the urinary excretion rate of 30% ~ 90%, in the form of glucuronide conjugate excretion. t1/2 for 1.6 ~ 1.9 hours.
1. Aspirin or probenecid can reduce the plasma protein binding rate of this product and increase the blood concentration of this product.
2. The concomitant use of this product with heparin, bicoumarin, warfarin and other anticoagulants can lead to prolongation of the prothrombin time and increase the tendency to bleeding.
4. This product can reduce the antihypertensive effect of antihypertensive drugs. 5. This product can increase the blood concentration of digoxin, methotrexate and oral hypoglycemic drugs, so it is not suitable for co-administration.4. This product can reduce the antihypertensive effect of antihypertensive drugs.
5. This product can increase the blood concentration of digoxin, methotrexate and oral hypoglycemic drugs, so it is not suitable for coadministration.
Preparation of Bulk Ketoprofen Powder.
Route 1: 3-cyanomethylbenzoic acid as starting material, Friedel-Crafts reaction, monomethylation with dimethyl carbonate reagent, then hydrolysis to keto ibuprofen
Route 2: Using 2-aminobenzophenone and its aminoprotectant as starting materials, the keto Ibuprofen is synthesised by α-halogenation, propionylation (or propionylation and then halogenation), keton reduction, rearrangement, hydrolysis, diazotisation and deamidation.
Route 3: 5-benzoyl-3-methyl-2-dihydroindolone (13) was produced by the Friedel-Crafts benzoylation of 3-methyl-2-dihydroindolone with benzoyl halide, and then the amide bond of the five-membered ring structure was cleaved to form a basic compound (13a) under alkaline conditions, and the keto ibuprofen was produced by diazotisation.
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