三七总皂苷缓释片的释放性能及体内外相关性研究

Study on Release of Panax Notoginseng Saponins Sustained-Release Tablets and Its in Vivo-in Vitro Correlation

目的评价三七总皂苷缓释片的体外释放特性、体内药物动力学及体内外相关性。方法以磷酸盐缓冲液为释放介质,考察三七总皂苷缓释片的体外释放特性。以6只Beagle犬为实验动物,测定口服给予缓释片后血药浓度的变化,计算药代动力学参数,并对体外累积释放度和体内累积吸收百分率进行回归,考察其体内外相关性。结果三七总皂苷缓释片体外药物释放具有明显的缓释特性;与普通片相比,在Beagle犬体内的达峰时间延长,峰浓度降低,平均滞留时间延长,也具有明显的缓释特性。结论制得的三七总皂苷缓释片达到了缓慢释放药物的目的,并且其体内外参数间有明显的相关性。

Objective To evaluate the in vitro release characteristics, in vivo pharmacokineties of Panax notoginseng Saponins Sustained- Release Tablets, and its in vivo- in vitro correlation. Methods The in vitro release characteristics of the sustained- release tablets were investigated by using phosphate buffer. Six Beagle dogs were chosen as the experimental animal to conduct in vivo test, the blood concentrations were detected after oral administration of the sustained-release tablets, and the pharmacokinetical parameters were calculated. Finally, the correlation between dissolution rate and percent absorption was investigated. Results The drug releasing data in vitro showed an obvious sustained-release characteristic. Compared with the common tablets, the sustained release tablets in vivo showed a prolonged tmax and MRT, and the Cmax was reduced. Conclusion The Panax notoginseng Saponins can achieve sustained release. There is a significant correlation between the dissolution in vitro and the absorption＇ in vivo of the sustained- release tablets.