Preparation and bioavailability of magnolol solid dispersions / 中草药

ABSTRACT

Objective: Hot-melt extrusion technique was applied to prepare magnolol solid dispersions, which can improve the in vitro solubility of magnolol and the in vivo bioavailability in rats. Methods: Four kinds of excipients, such as PS-630, HPC, EPO, and Soluplus, which were compatible with magnolol were used to prepare solid dispersions of different drug loadings by solubility parameter calculation. The prepared solid dispersion was characterized by differential scanning calorimetry (DSC), X-ray diffraction analysis (XRPD) and infrared spectroscopy (IR) using in vitro dissolution as an indicator; UPLC-MS/MS was used to evaluate the pharmacokinetic behavior of rats after oral administration of magnolol solid dispersion. Results: The in vitro dissolution test showed that the solid dispersion prepared by the 16 drug loading of PS-630, HPC, and EPO can significantly improve the dissolution of magnolol, and the drug was dispersed in the carrier in an amorphous state. The in vivo bioavailability test showed that the Cmax of magnolol in the solid dispersion prepared by PS-630 and HPC was about five times and 2.3 times that of the monomer, respectively, and the AUC0-t was increased about 37.22% and 70.88%, respectively. There was no increase in the EPO system. Conclusion: Hot melt extrusion technology can be successfully applied to improve the in vitro dissolution and in vivo bioavailability of the poorly soluble drug magnolol.