Nimesulide has superior gastrointestinal safety as compared to other NSAIDs.
Its multifactorial mode of action gives a unique and broad action on inflammatory processes.
Nimesulide is also offered in the form of gell, powder which is now available in worldwide of more than 50 countries. It also available in different trademarks like Nimesil, Nimulid, Nise e.t.c.
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Non-steroidal anti-inflammatory drug – Nimesulide
1. Non-steroidal anti-inflammatory drug – Nimesulide
Nimesuilde is a pain killer Non-steroidal medicinal drug (NSAIDs) with a complex
mode of action, characterized by a quick onset of analgesic activity.
The anti-inflammatory drug mechanism of Nimesulide should only be prescribed as
second line treatment. The decision to prescribe nimesulide should be based on
assessment of the individual patient’s overall risks.
Main purpose of using this drug is to treat acute pain, to treat degenerative joint
disease, to treat primary dysmenorrhoea in adolescents and adults above 12 years
old, it is used for treatment of all types of pains resulting from sports injury,
depression etc.
Additionally it helps in increasing energy, improve skin tone, and to cure Heart
diseases, and also helpful for dry skin and is usually recommended for the shortest
period necessary to control symptoms in patients with pain
Nimesulide has superior gastrointestinal safety as compared to other NSAIDs.
Its multifactorial mode of action gives a unique and broad action on inflammatory
processes.
Nimesulide is also offered in the form of gell, powder which is now available in
worldwide of more than 50 countries. It also available in different trademarks like
Nimesil, Nimulid, Nise e.t.c.
The solubility enhancement of 4 cox-2 inhibitors, celecoxib, rofecoxib, meloxicam,
and nimesulide, using a series of pure solvents and solvent mixtures. Water,
alcohols, glycols, glycerol, and polyethylene glycol 400 (PEG 400) were used as
solvents and water-ethanol, glycerol-ethanol, and polyethylene glycol-ethanol were
used as mixed-solvent systems. A pH-solubility profile of drugs was obtained in the
pH range 7.0 to 10.9 using 0.05M glycine-sodium hydroxide buffer solutions. Lower
alcohols, higher glycols, and PEG 400 were found to be good solvents for these
drugs. The aqueous solubility of celecoxib, rofecoxib, and nimesulide could be
enhanced significantly by using ethanol as the second solvent. Among the mixed-
solvent systems, PEG 400-ethanol system had highest solubilization potential. In the
2. case of meloxicam and nimesulide, solubility increased significantly with increase in
pH value. Physico-chemical properties of the solvent such as polarity, intermolecular
interactions, and the ability of the solvent to form a hydrogen bond with the drug
molecules were found to be the major factors involved in the dissolution of drugs by
pure solvents. The greater the difference in the polarity of the 2 solvents in a given
mixed solvent, the greater was the solubilization power. However, in a given mixed-
solvent system, the solubilization power could not be related to the polarity of the
drugs.
Assessment of nimesulide solubility: Solubility of nimesulide in phosphate buffer pH
6.8 in presence of different 323 concentrations 2-10% (v/v or w/v) of some selected
cosolvents was investigated. The selected cosolvents were: formamide, DMF, DMA,
DMSO, ethanol, propanol, isopropanol, glycerol, EG, PG, PEG 200, PEG 300, PEG
400 and PEG 600. In addition, the solubility in presence of different concentrations
2-10% (w/v) of different nonionic surfactants (tween 20, tween 40, tween 80, myrj
52, myrj 53, brij 35 and brij 58) was also studied. An excess amount of nimesulide
was added to 50-ml stoppered glass bottles containing 10 ml cosolvent solutions or
surfactant solutions. The bottles were shaken in a mechanical shaking water bath
previously equilibrated at 32°C. Aliquots were withdrawn after three hours
(equilibrium time), filtered using a 0.45 µm membrane disc filter and assayed
spectrophotometrically at max 392 nm ( max was determined practically) afterλ λ
appropriate dilution employing the same concentration of the cosolvent or surfactant
as a blank. The results are the mean values of three determinations.