Use of the liquisolid compact technique for improvement of the dissolution rate of valsartan

The aim of this study was to improve the dissolution rate of the poorly soluble drug valsartan by delivering the drug as a liquisolid compact. Liquisolid compacts were prepared using propylene glycol as solvent, Avicel PH102 as carrier, and Aerosil 200 as the coating material. The crystallinity of the newly formulated drug and the interaction between excipients was examined by X-ray powder diffraction and Fourier-transform infrared spectroscopy, respectively. The dissolution studies for the liquisolid formulation and the marketed product were carried out at different pH values. The results showed no change in the crystallinity of the drug and no interaction between excipients. The dissolution efficiency of valsartan at 15 min was increased from 4.02% for plain drug and 13.58% for marketed product to 29.47% for the liquisolid formulation. The increase in the dissolution rate was also found to be significant compared to the marketed product at lower pH values, simulating the gastric environment where valsartan is largely absorbed. The liquisolid technique appears to be a promising approach for improving the dissolution of poorly soluble drugs like valsartan.

Graphical abstractThe dissolution rate of the poorly soluble drug valsartan was improved by formulation as a liquisolid compact using propylene glycol as solvent, Avicel PH102 as carrier, and Aerosil 200 as the coating material. The increase in the dissolution rate was significant compared to the marketed product at lower pH values which simulate the site of absorption in the upper gastrointestinal tract.Figure optionsDownload full-size imageDownload as PowerPoint slide