Enhancement of dissolution and the anti-inflammatory effect of nimesulide, using liquisolid compact for oral application

ABSTRACT

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 201, 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 anti-inflammatory 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 anti-inflammatory effect of nimesulide