Preparation and in vitro evaluation of curcumol solid dispersion / 中草药

ABSTRACT

Objective Curcumol solid dispersions (Cur-SDs) were explored and the optimal formulation was selected for improving the in vitro dissolution of curcumol. Methods In this study, Cur-SDs were prepared by solvent method, fusion method and solvent-fusion method using F68, PVP K30, PEG4000, and PEG6000 as matrix, and in vitro dissolution rate was evaluated. Fourier transform infrared spectroscopy (IR), differential scanning calorimetry (DSC), and X-ray diffractometry (XRD) were employed to characterize the molecular arrangement of curcumol in SDs. And a brief investigation of its stability in the long-term storage process was also performed. Results The Cur-SD prepared with F68 as matrix and by solvent-fusion method was better in improving the in vitro dissolution than those with other matrix or those prepared by other methods. Furthermore, the optimal drug-matrix ratio was 1:5. DSC, IR and XRD indicated that the drug could be dispersed molecularly or amorphously in matrix, and no chemical reaction occurred. There was no decrease in its dissolution, and no significant change in molecular arrangement in a six-month stability study under room temperature. Conclusion The preparation of insoluble drug curcumol into solid dispersion can significantly improve its dissolution rate in vitro. Moreover, the preparation method is simple and feasible, and has good stability.