Factory Supply Raw Materia Indometacin Powder Analqesic Indometacin
Product Description
Product Details
| Product Name |
Indometacin |
| Apperance |
white powder |
| CAS |
53-86-1 |
| MF |
C19H16ClNO4 |
| MW |
357.79 |
Indomethacin, with the chemical name 2-methyl-1 -(4-chlorobenzyl) -5-methoxy-1H-indole-3-acetic acid, belongs to Class II drugs in the BCS classification. It has high permeability, low solubility, poor dissolution rate and low bioavailability in vivo. Indomethacin is a non-steroidal anti-inflammatory drug (NSAIDs), which has anti-inflammatory, antipyretic and analgesic effects. It exerts its anti-inflammatory effect by inhibiting cyclooxygenase and reducing the synthesis of prostaglandins, while its antipyretic effect is related to the inhibition of prostaglandin synthesis in the hypothalamus.
Application&Function
Purpose
Cyclooxygenase (COX) inhibitor, selectively inhibiting COX-1; Block the biosynthesis of prostatic cords. It has obvious anti-inflammatory and antipyretic effects in medicine and is mainly used for rheumatic arthritis, ankylosing spondylitis, osteoarthritis and other diseases that are not easily tolerated or have insignificant therapeutic effects to salicylic acid drugs.
The anti-inflammatory effect of indomethacin is stronger than that of phenylbutazone . The combined application can reduce the dosage and side effects of the latter. The antipyretic effect is ten times that of aminopyrine. However, the analgesic effect is weak, and it only has a significant analgesic effect on inflammatory pain. In monogastric animals, the gastrointestinal absorption is rapid and complete after oral administration. The peak blood drug duration is 1.5 to 2 hours, and the plasma protein binding rate reaches 90%. It combines with gluconic acid in the liver and is excreted by the kidneys. Some of it enters the intestine with bile for reabsorption, and the rest is excreted through feces. It is used for postoperative trauma, arthritis, tenosynovitis, muscle injury and other inflammatory pain.
Pharmacokinetics
Oral administration is rapid and complete in absorption. More than 90% of the dosage can be absorbed within 4 hours. Food or taking antacids containing aluminum and magnesium can slightly slow down the absorption. The plasma protein binding rate is approximately 99%. The time to reach the peak after oral administration of 25mg was 1 to 4 hours, the peak blood drug concentration (Cmax) was 1.4μg/ml, and the Cmax at 50mg was 2.8μg/ml. The average half-life (t1/2) was 4.5 hours, and it was significantly prolonged in premature infants. A small amount of indomethacin can pass through the blood-brain barrier. And it can pass through the placenta. This product is metabolized in the liver into demethylated and dechlorobenzoylated compounds, and can be hydrolyzed into indomethacin for reabsorption and recycling. Sixty percent are excreted through the kidneys, of which 10% to 20% are excreted in their original form. Some of it is excreted with feces. 33% is excreted through bile, of which 1.5% is the original form. It is also excreted in breast milk (up to 0.5-2.0mg per day). This product cannot be removed by dialysis.
Specification
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