Der Pharmacia Lettre
Abstract
Author(s): Dinesh Kumar Sharma, Vipin Bihari Gupta, Suresh Purohit
Nearly 30-45 % of new seeds discovered by recent techniques suffer from poor aqueous
solubility. Various techniques, used to enhance the aqueous solubility, are reported to produce
many disadvantages. Solid dispersion technique is widely used to enhance aqueous solubility.
In spite of consciousness in solid dispersions technique, investigators have been able to provide
only few numbers of carriers to the industry. Moreover these carriers are reported to produce
many disadvantages. Therefore, definitely there is need to explore such new carriers. Current
study was undertaken to explore suitability of one such carrier crospovidone as solubility
enhancer. Physical mixtures, kneading mixtures and solid dispersions were prepared by solvent
evaporation technique using piroxicam as model drug. Kneading mixtures at drug carrier ratio
of 1:7 produced maximum solubility. The resulting systems were subjected to solubility analysis
and in vitro dissolution studies, flow properties, X-ray diffraction, Infrared Fourier Transform
Spectroscopy (FTIR) and differential scanning calorimetry. Kneading mixtures at 1:7 ratio
produced improved flow properties in comparison to pure piroxicam. The % drug dissolved after
5 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. Kneading
mixtures were successfully compressed in tablets having all post compression parameters within
limit in comparison to tablets prepared using MCC or calcium phosphate as diluent. Lower
energy required for dissolution due to change in crystal lattice is responsible for improvement in
solubility of drug.
