In vitro characteristic evaluation of ursolic acid co-crystal solid dispersions / 中草药

ABSTRACT

Objective: To use co-crystal and solid dispersion technology, screen a suitable carrier material to prepare ursolic acid (UA) co-crystal solid dispersion in order to improve the solubility and dissolution of UA. Methods: UA and UA piperazine co-crystal (UA-PP) solid dispersions were prepared with solvent method by using four carriers, respectively. The solubility and in vitro dissolution of free drug, co-crystal, and solid dispersions were determined. Results: The solubility of UA and UA-PP solid dispersions was significantly higher than free drug and its physical mixtures. Solid dispersion technology could further increase the solubility of UA-PP and accelerate its in vitro dissolution rate. The result layed the foundation for the development of a novel oral formulation of ursolic acid. Conclusion: The co-crystal and solid dispersion technology could improve the solubility and dissolution of UA. The UA-PP solid dispersions show the best improvement in the solubility and dissolution of UA.