Amlodipine besylate is a sparingly soluble orally administered drug and the rate of absorption is often controlled by the rate of dissolution. Reports suggest that the drug has poor water solubility which may be challenging for developing liquid dosage forms of Amlodipine besylate. Hence in the present study, we sought to develop orodispersible nanoparticles to enhance the solubility by anti-solvent evaporation using stabilizers such as PVPK-30, Poloxamer-188, PVA, and L-Arginine. We found that the particle size was ranging between 225.7nm-942.7nm and % DEE was 78% - 98% respectively. Among all the formulations, F8 stabilized with Poloxamer-188 and PVA has been found to show 99.2% drug release at the end of 10 minutes in both 0.1N HCL and phosphate buffer (pH 6.8). Through SEM studies we found that the particles were small with no aggregation. Further, the particles (F8) were compressed into tablets F8(f) through the direct compression method and characterized based on some selected parameters in comparison with the marketed tablet. We have also observed satisfactory amlodipine excipient compatibility through FTIR investigation. DSC and XRD results have illustrated that the crystallinity of the drug was lost in lyophilized powder and tablet converted to an amorphous form. Hence, we concluded that an optimized formulation of amlodipine could improve the rate of absorption controlled by the rate of dissolution.

The present invention relates to an Amlodipine besylate orodispersible nanoparticulate tablet dosage form and its preparation method anti-solvent evaporation method and lyophilization. The process for the preparation of amlodipine nanoparticles with significant improvement of solubility and dissolution characteristics. The Nanoparticulate orodispersible tablet form of amlodipine besylate is prepared by direct compression method with enhanced bioavailability and improved rate of absorption