ABSTRACT
Objective To prepare baicalin solid nanocrystal (BCN-SN) stabilized by glycyrrhizic acid (GA) and determine its in vitro release characteristics. Methods The high-speed shearing-high pressure homogenization technology was adopted in the preparation of BCN nanosuspension, and then BCN nanosuspension was solidified into BCN-SN by freeze-drying. The formula and process of BCN-SN were optimized by the single factor experiment with average particle size and polydispersity index (PDI) as indicator. BCN-SN were prepared under the optimal conditions and characterized for crystal-linity and particle size. In vitro release of BCN-SN was also determined. Results The particle size of BCN-SN stabilized by GA and protected by mannitol-GA was (478.0 ± 6.5) nm, and the polydispersity index (PDI) was 0.230 ± 0.015, respectively. The results of SEM showed that BCN-SN was irregular spherical and DSC showed that BCN-SN was amorphous after being prepared into solid nanocrystal. In the in vitro dissolution test, BCN-SN showed a significantly increased dissolution. Conclusion The method employed to prepare the BCN-SN stabilized by GA is simple and low-cost. BCN-SN can significantly improve the dissolution of BCN, which has a broad application.
ABSTRACT
Objective: To prepare the hyperoside solid nanocrystal (Hyp-SN) and to determine the in vitro release. Methods: The high pressure homogenization technology was applied to preparing Hyp nanosuspension, and then Hyp-NS was solidificated into Hyp-SN by freeze-drying. The fomulation and process of Hyp-SN were optimized by the single factor experiment. Dried powders were prepared under the optimal condition and characterized for crystallinity and particle size. In vitro dissolution of Hyp-SN was also determined. Results: The particle size of Hyp-SN protected by tert-butyl alcohol was (405.2 ± 14.6) nm, as well as the polydispersity index (PI) was 0.25 ± 0.08. The results of SEM showed that Hyp-SN powder was irregular rod and XRD showed Hyp was crystalline in both coarse powder and nanosuspensions. In the in vitro dissolution test, Hyp-SN showed an increased dissolution markedly. Conclusion: The method employed to prepare the Hyp-SN is simple and feasible. Hyp-SN could significantly improve the dissolution of Hyp. It has a broad application prospects.