The effect of Pluronic F127 on the physicochemical properties and dissolution profile of lovastatin solid dispersions

• DOI: 10.1007/s10973-015-4935-z
• Publication Date: 2015-07-25T01:22:47Z
• Authors: Bożena Karolewicz; Maciej Gajda; Janusz Pluta; Agata Górniak
• Keywords: Powder Diffraction

Lovastatin (LOV) is a BCS class II drug and hence has poor water solubility, due to which its rate of solubilization is low. The objective of this study was to improve the dissolution rate of LOV by preparing, using the kneading method, solid dispersions with Pluronic F127 (PLU) as a carrier. LOV/PLU solid dispersions were characterized by means of differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), X-ray powder diffractometry (XRPD), and in vitro dissolution tests. The DSC investigation revealed that LOV and PLU form a simple eutectic system containing 6.0 % w/w of LOV at the eutectic point. FTIR spectroscopy and XRPD studies indicated no interaction between LOV and PLU in the solid state. The intrinsic dissolution rate and in vitro release into a hard gelatin capsule of LOV from solid dispersions was compared to pure LOV. The dissolution rate of LOV reached within 24 h was improved among all solid dispersions with PLU. The intrinsic dissolution rate in pH 7.0 phosphate buffer with 0.5 % sodium lauryl sulfate of LOV in solid dispersion containing the substance by mass percentage of 60, 70 and 80 % w/w increased more than 30-fold. While within 24 h 16.53 % of the pure drug was dissolved, 100 % of the drug was dissolved with the formulations containing 50–80 % w/w of LOV within 240 min. The dissolution rate of LOV from solid dispersions 50/50 LOV/PLU, 60/40 LOV/PLU, 70/30 LOV/PLU and 80/20 LOV/PLU percent, respectively, into a hard gelatin capsule was higher (100.0, 83.37, 98.95 and 87.50 %, respectively) than that of pure LOV (71.15 %) within 30 min.