Meloxicam Research Paper

5. Drug And Excipient Profile
5.1. DRUG PROFILE
Chemical Structure of Meloxicam Meloxicam, is an oxicam derivative, is a member of the enolic acid group of Nonsteroidal anti-inflammatory drugs (NSAIDs). It is chemically designated as 4hydroxy-2-methyl-N-(5-methyl-2-thiazolyl)-2H-1, 2-benzothiazine-3-carboxamide-1,1dioxide. It is pastel yellow solid, practically insoluble in water, with highest solubility observed in strong acids and bases. It is very slightly soluble in methanol.
Anti-inflammatory effects of meloxicam are believed to be due to inhibition of prostaglandin synthesis (cylooxygenase), leading to the inhibition of prostaglandin synthesis. As prostaglandins

5.2. MECHANISM OF MELOXICAM:-
This enzyme is responsible for converting arachidonic acid into prostaglandin H2. This is the first step in the synthesis of prostaglandins, which are mediators of inflammation. Meloxicam has been shown, especially at its low therapeutic dose, selectively to inhibit COX‐2 over COX‐1(9). A primary advantage of the oxicam family of drugs is their long half‐life which permits once‐day dosing (10). In gastric disease, lower dose of meloxicam is required 7.5 mg/day. Meloxicam is safer then other NSAID’s (11).
5.2.1. Pharmacokinetics
Absorption
The absolute bioavailability of meloxicam capsules was 89% following a single oral dose of 30 mg compared with 30 mg IV bolus injection. Meloxicam capsules have been shown to be bioequivalent to MOBIC tablets.Following single intravenous doses, dose-proportional pharmacokinetics were shown in the range of 5 mg to 60 mg. After multiple oral doses the pharmacokinetics of meloxicam capsules were dose-proportional over the range of 7.5 mg to 15 mg. Mean Cmax was achieved within four to five hours after a 7.5 mg

Meloxicam is ~ 99.4% bound to human plasma proteins (primarily albumin) within the therapeutic dose range. The fraction of protein binding is independent of drug concentration, over the clinically relevant concentration range, but decreases to ~ 99% in patients with renal disease. Meloxicam penetration into human red blood cells, after oral dosing, is less than 10%. Following a radiolabeled dose, over 90% of the radioactivity detected in the plasma was present as unchanged meloxicam. Meloxicam concentrations in synovial fluid, after a single oral dose, range from 40% to 50% of those in