ENHANCEMENT OF DISSOLUTION AND THE ANTIINFLAMMATORY EFFECT OF NIMESULIDE, USING LIQUISOLID COMPACT FOR ORAL APPLICATION

Nimesulide is a poorly soluble drug, the rate of its oral absorption is often controlled by
the dissolution rate in the gastrointestinal tract. There are several techniques to enhance the
dissolution of poorly soluble drugs. Among them the technique of liquisolid compacts which is a
promising one. The liquisolid compacts were prepared using 20 mg nimesulide, Avicel PH102
as a carrier, and Aerosil 200 as a coating material in a ratio of 20:1, as well as AC-DI-SOL as
a disintegrant in a concentration of 5% from the total weight of the compact. The liquids used
include PEG400, PG, and a mixture of these solvents with Tween 80. From the results obtained
it is concluded that the suitable loading factor (Lf) is 0.2 which gave good flowability and
compressibility. Friability, hardness, disintegration time and the dissolution rate were carried
out. All the liquisolid compacts showed higher dissolution rate than the conventional tablets.
The liquisolid compacts containing the PEG400 showed the highest dissolution rate than the
other preparations. The effect of different concentrations of drug on the dissolution rate was
studied, and it was observed that 20% of drug gave the maximum dissolution rate, and no
significant increase of the dissolution rate with increasing the drug concentration. Conventional
tablets and liquisolid compacts containing PG and PEG400 were tested for their antiinflammatory
effects using paw oedema test. liquisolid compacts exhibited a pronounced
inhibition of swelling than that of conventional tablets. In conclusion liquisolid compact of
nimesulide can be used as a technique to improve the dissolution rate and the antiinflammatory
effect of nimesulide.