Preparation and dissolusion performance of total triterpenes from Paliurus ramosissimus solid dispersion / 中草药

Objective To prepare total triterpene of Paliurus ramosissimus solid dispersions (TTPR-SD) and study their dissolution properties in vitro. Methods The dissolution of paliurusene and betulinic acid were used as indicators to examine the effect of different carrier materials and different preparation methods on drug dissolution in total triterpenoid solid dispersions by single factor. The preparation technology parameters of total triterpenes of P. ramosissimus solid dispersion were optimized by orthogonal design. Existential state of drugs in this solid dispersion was analyzed by FT-IR and X-ray. Results The solid dispersion was prepared by solvent method with PVPK30 as carrier, the ratio of drug to carrier was 1∶5, ultrasonic for 10 min, and the magnetic stirring temperature was 80 ℃. The cumulative dissolution of paliurusene and betulinic acid within 60 min was achieved 89.19% and 80.49%, respectively. The drug dispersed in the PVPK30 in an amorphous state, and combined with the carrier in the form of hydrogen bonds. Conclusion The prepared solid dispersion can significantly improve the dissolution properties of total triterpene of P. ramosissimus.

Chemical constituents from Paliurus ramosissimus / 中草药

Objective: To study the chemical constituents in the ethanol extract from Paliurus ramosissimus. Methods: The compounds were isolated and purified by repeated silica gel column chromatographies and HPLC. The structures of the compounds were identified on the basis of chemical and spectral methods of NMR, MS, etc. Combined with the MTT method, the inhibitory effect of compound 2 in vitro against the HepG-2 and HeLa cells was assayed. Results: Two new compounds were isolated from P. ramosissimus and identified as betulinic acid (1) and 2α,27-di (E-p-hydroxy cinnamoyloxy)-betulinic acid (2) for the first time. The IC50 values of compound 2 are 20.34 and 14.83 μmol/L against the HepG-2 and HeLa cells. Conclusion: Compound 2 is a new compound named as paliurusene, which belongs to triterpenoids and shows the obvious cytotoxicity in vitro against the cancer cell lines.