Description of Diclofenac Sodium
Diclofenac Sodium is the salt form of diclofenac, an active metabolite of the NSAID aceclofenac (sc-217557). Hydrolysis of aceclofenac, an inhibitor of interleukin-1B-induced prostaglandin E2 production with no inhibitory activity against Cox (cyclooxygenase), generates diclofenac, an inhibitor of both Cox-1 and Cox-2. Oxidation of diclofenac produces the metabolite 4'-hydroxy diclofenac (sc-202423) which demonstrates specific inhibition of Cox-2. Inhibition of Cox by diclofenac and 4'-hydroxy diclofenac suppresses prostaglandin E2 synthesis, producing antiinflammatory 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.
Specification of Diclofenac Sodium
Characteristics
| White crystalline powder |
Solubility:
| Sparingly soluble in water, freely soluble in methanol, ethanol(96%);slightly soluble in acetone; practically insoluble in ether., |
Melting point | 275-277 |
Related Substances: | Single impurity max 0.2% total impurity max 0.5% |
Heavy metal:
| Max 10ppm |
Loss on drying
| Max 0.5% |
