血塞通包衣脉冲控释片体外释药特性的研究

Drug release of Xuesaitong pulsatile-coated tablets in vitro

目的建立血塞通包衣脉冲片体外释放度测定方法,考察其体外释药特性。方法 RP-HPLC梯度洗脱法测定血塞通包衣脉冲控释片中的人参皂苷Rb1、人参皂苷Rg1、三七皂苷R1的含量;在模拟人胃肠溶出介质环境下,比较血塞通包衣脉冲控释片与普通片剂体外释药时滞和累积释药的脉冲效果。结果人参皂苷Rb1、人参皂苷Rg1在3.0-60μg,三七皂苷R1在0.8-16μg内与峰面积具有良好的线性关系,r值分别为0.999 8、0.999 4、0.999 6,低、中、高浓度平均回收率分别在99.0%-99.4%、99.1%-99.3%、98.7%-99.6%,RSD均〈3.0%（n=3）;体外释放度试验表明与血塞通普通片剂相比,血塞通包衣脉冲控释片释药时滞为5 h,体外累积释药〉80%。结论血塞通包衣脉冲控释片在体外具有明显的脉冲释药特性,从而指导及优化处方作进一步研究。

Objective To develop a method to determine the drug release of Xuesaitong pulsatile-coated tablets in vitro, and investigate its drug release behavior. Methods Contents of panaxsaponin Rb1, panaxsaponin Rg1 and notoginsenoside R1 in Xuesaitong pulsatile-coated tablets were determined by RP-HPLC with gradient elution. In the environment of simulating people＇s gastrointestinal tract dissolution medium, we compared the lag time of the in vitro drug release and the effect of cumulative drug release between Xuesaitong pulsatile-release tablets and common tablets. Results A good linearity was shown when the contents of panaxsaponin Rb1 and Rg1 were at 3.0- 60 μg, and notoginsenoside R1 at 0.8- 16 μg, and r value was 0.999 8, 0.999 4 and 0.999 6, respectively. The average recoveries were at 99.0%- 99.4%, 99.1%- 99.3%, 98.7%- 99.6%. RSDs were less than 3.0%, respectively（n= 6）. The release of pulsatile tablets lasted 5 h in vitro, and the cumulative drug release was above 80%. ConclusionXuesaitong pulsatile-release tablets has obvious characteristics of pulsed drug release in vitro, which can be used for guiding and optimizating prescription in further research.