三七总皂苷控释制剂的制备及其释药特性研究

Study on Preparation and Release Characteristics of Panax Notoginseng Saponins Controlled-Release Preparations

目的制备三七总皂苷(PNS)脉冲控释片与胃漂浮控释片,并对其体外释药特性进行研究。方法以人参皂苷Rg1为指标性成分,采用HPLC法测定PNS控释制剂体外释放度,考察释药特性并进行释放机制的研究。结果PNS胃漂浮片具有良好的漂浮性能,片剂的平均累积释放百分率F(t)与时间t呈现良好的的线性关系(r=0.9846),其体外释药符合零级释放过程,并按Higuichi方程能很好地描述漂浮片的体外释放曲线,符合骨架型制剂的释药特点;PNS脉冲控释片在4h内其释放率小于10%,5h释放约50%,6.5h释放量可达90%,基本达到了脉冲定时释药的目的。结论 PNS胃漂浮片无明显突释现象,释药速率平稳,控释效果较好。PNS脉冲控释片能实现定时脉冲释药,并可通过调整制剂处方实现不同时滞的控释效果,达到了设计要求。

Objective To prepare pulsatile controlled-release tablets PNS and gastric floating controlled-release tables,study the release characteristics in vitro.Methods Use ginsenoside Rg1 as index components,investigated the release characteristics and study the release mechanism through PNS controlled-release preparations in vitro determined by HPLC.Results PNS gastric floating tablets have good floating performance,the tablets average cumulative release percentage F（t）showed a good linear relationship（r = 0.9846）with time t,and its release profile be in line with zero order release process;The floating tablets in vitro release profile can be well described by Higuichi equation,in line with the release of the skeleton preparations characteristics.The release rate of PNS pulsatile controlled-release tablets is less than 10% in 4 hours,release of about 50% in 5 hours,release up to 90% in 6.5 hours,basically reached the purpose of the pulse timed release.Conclusion Conclusion PNS gastric floating tablets have no significant burst release,the release rate is relatively stable with better controlled release,PNS pulsatile controlled-release tablets can achieve timing pulse release,the different delay controlled-release effect can be achieved by adjusting the formulation,as to reach the design requirements.