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Non-steroidal anti-inflammatory drug NimesulideNimesuilde 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 ofNimesulide should
only be prescribed as second line treatment. The decision to
prescribe nimesulide should be based on assessment of the
individual patients 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
painNimesulide 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 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 32C. Aliquots were withdrawn after three hours (equilibrium
time), filtered using a 0.45 m membrane disc filter and assayed
spectrophotometrically at max 392 nm (max was determined
practically) after appropriate dilution employing the same
concentration of the cosolvent or surfactant as a blank. The
results are the mean values of three determinations.