Industry feasible method to improve solubility of Piroxicam withCrospovidone: Preparation, Characterization and tabletingconsideration

[摘要] Nearly 30-45 % of new seeds discovered by recent techniques suffer from poor aqueoussolubility. Various techniques, used to enhance the aqueous solubility, are reported to producemany disadvantages. Solid dispersion technique is widely used to enhance aqueous solubility.In spite of consciousness in solid dispersions technique, investigators have been able to provideonly few numbers of carriers to the industry. Moreover these carriers are reported to producemany disadvantages. Therefore, definitely there is need to explore such new carriers. Currentstudy was undertaken to explore suitability of one such carrier crospovidone as solubilityenhancer. Physical mixtures, kneading mixtures and solid dispersions were prepared by solventevaporation technique using piroxicam as model drug. Kneading mixtures at drug carrier ratioof 1:7 produced maximum solubility. The resulting systems were subjected to solubility analysisand in vitro dissolution studies, flow properties, X-ray diffraction, Infrared Fourier TransformSpectroscopy (FTIR) and differential scanning calorimetry. Kneading mixtures at 1:7 ratioproduced improved flow properties in comparison to pure piroxicam. The % drug dissolved after5 minutes for PRX: CrosPVP KM 1:7 and pure piroxicam was 26.43 % and 11.49% respectively.86.57 % of piroxicam was dissolved from PRX: CrosPVP KM 1:7 after 120 minutes. Kneadingmixtures were successfully compressed in tablets having all post compression parameters withinlimit in comparison to tablets prepared using MCC or calcium phosphate as diluent. Lowerenergy required for dissolution due to change in crystal lattice is responsible for improvement insolubility of drug.

[学科分类] 药理学