Formulation, Development, Evaluation and Solubility Enhancement of Lercanidipine Hydrochloride by Solid Dispersion Techniques

Background: Solid dispersions (SDs) are the dispersion of hydrophobic drugs in an inert hydrophilic carrier. SDs are prepared to improve the dissolution properties and bioavailability of slightly water-soluble drug molecules by dispersing them into an inert hydrophilic carrier.

Aims and Objective: Evaluate the dissolution and solubility of Solid Dispersion of Lercanidipine Hydrochloride (LER).

Materials and Methods: To study the effect of polymer, dissolution and solubility studies were carried out. Solid state characterizations of prepared solid dispersions were performed by differential scanning calorimetry (DSC).Drug- carrier interactions were studied by FT-IR spectroscopy, whereas X-ray diffraction of powder was done to demonstrate the crystal structure of the dispersions.

Results: The prepared solid dispersion exhibited 94% drug release at 30 minutes which is higher than both LER pure and LER MKT. Better dissolution characteristic of solid dispersion was confirmed by 9.86 min MDT and 63.12% DE30 which is higher than that of LER MKT (13.64 MDT, 46.92 % DE30) Solid state characterization revealed that enhancement of dissolution is the result of conversion of crystalline form of LER to less crystalline and/or amorphous form.

Conclusion: Solid dispersion of LER can successfully be prepared with the PEG6000 in the ratio of 1:6 using solvent evaporation technique. It is a successful and easy approach for the increase in onset of action of drug after administration and facilitates treatment of cardiovascular diseases.