Solid Dispersion

The present research work was aimed to enhance the solubility and dissolution rate of Olanzapine using Poloxamer as carrier by preparing solid dispersion. The solid dispersions and physical mixtures prepared was also evaluated  for the drug content and percentage drug yield and characterization of prepared systems is done with the help of in-vitro drug release, FTIR, XRD and DSC analysis. The results obtained showed that the percentage yield and percentage drug content was 98.32% and 99% respectively. It was clear that there was no loss of drug and polymer. The rate of dissolution of the drug in the case of solid dispersions was much enhanced as compared to the pure drug and their physical mixtures. FTIR spectra showed that there was not any interaction or hydrogen bonding between the drug and polymers in solid dispersions as well as physical mixtures. The polymorphic changes were studied with the XRD gave the idea that the solid dispersions were quite amorphous in nature as compared to the pure drug. In the diffraction pattern for solid dispersions, the number of crystalline peaks due to drug had disappeared. DSC showed that there was shifting in melting endotherm of drug in case of solid dispersion. From the XRD and DSC it was confirmed that the increase in the solubility and dissolution rate was due to polymorphic transition of drug from crystalline to amorphous form.

The main objective of the study is to enhance the dissolution rate and solubility of paliperidone by using the solid dispersion technique which were wildly used in pharmaceutical company because of its less cost. Paliperidone is antipsychotic classes of drug that can be used for the treatment of schizophrenia. Initially preformulation studies were conducted to check the incompatibilities of drug substance. Initially phase solubility studies were performed with respect to different molar ratio. Drug polymer interactions were investigated using differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier transform infrared spectroscopy (FTIR). As indicated from XRD and DSC data, paliperidone was in the amorphous form, which explains the better dissolution rate of then drug from its solid dispersion. Solid dispersion of paliperidone were prepared to check the solubility of paliperidone because of its poor solubility issue by using the different polymer and to find out the effect of various solubilizer on its solubility and dissolution rate.