Subsyde-CR Mechanism of Action



Raptakos Brett


Raptakos Brett
Full Prescribing Info
Pharmacology: Diclofenac Sodium (Subsyde-CR) is a controlled-release formulation which employs the new Diffusion Rate Controlling Membrane (DRCM). Diclofenac Sodium (Subsyde-CR) is a multiple unit formulation containing many pellets. Each pellet is comprised of a core with alternative layers of drug and special dialyzing membrane, which controls the diffusion rate of the drug contents. After release of pellets into the stomach, entry of gastric fluid takes place via osmosis, starting from the fluid initial layer itself. This water dissolves Diclofenac until a saturated solution is formed internally. The drug then diffuses through the dialyzing membrane into the surrounding lumen for absorption into the blood stream. Dialyzing membrane ensures slow and steady release of the drug for absorption throughout its passage in the intestinal tract. This process continues layer by layer in a slow and steady manner ensuring that plasma Diclofenac concentrations are maintained for 24 hours after a single dose. When all the drug has been diffused out the pellets then it collapsed and are excreted out.
Properties/Effects: Diclofenac Sodium (Subsyde-CR) contains the sodium salts of diclofenac, a non-steroidal anti-inflammatory drug. In pharmacologic studies, diclofenac has shown anti-inflammatory, analgesic & antipyretic effects. Inhibition of prostaglandin biosynthesis which has been demonstrated in experiments are considered to be fundamental to the mechanism of action of diclofenac. Prostaglandins play a major role in the pathogenesis of inflammation, pain & fever. In rheumatic diseases, diclofenac produces marked relief from signs & symptoms such as pain at rest, pain on movement, morning stiffness & swelling of joints as well as by an improvement in function. Diclofenac Sodium (Subsyde-CR) is punctually suitable for patients requiring a daily dosage of 100 mg.
Pharmacokinetics: Absorption: Diclofenac in Subsyde-CR is completely absorbed from the gastrointestinal tract. After administration of 100 mg Diclofenac Sodium (Subsyde-CR), mean peak plasma concentrations of about 1.39 mcg/ml were reached at the mean of 4.83 hours. Pharmacokinetic behavior does not change after repeated administration of  drug. The area under plasma concentration curve (AUC) is 18.87 mcg/mL.
Distribution: More than 99 percent of Diclofenac is reversibly bound to human plasma-2 albumin. As with other NSAIDs, diclofenac diffuses into & out into synovial fluid. Diffusion into the joint occurs when plasma levels of diclofenac are higher than those of synovial fluid.
Metabolism & Excretion: Diclofenac is excreted through metabolism & subsequent urinary & biliary excretions of glucuronide & the sulphate conjugates of the metabolites. Approximately of the 65% of the dose is excreted in the urine & approximately 36% in the bile.
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