吸波面积法测定乌头二元释药颗粒的体外释放度

Determination of in Vitro Release of Wutou Binary-released Granules by Area Under Absorbance-wavelength Curve

目的:建立吸波面积法测定乌头二元释药颗粒中碱性物质的体外释放度。方法:开展乌头普通颗粒及其聚丙烯酸树脂包衣颗粒的体外释放度研究,于不同时间点获得含药释放介质,通过调节释放介质pH和三氯甲烷萃取处理获得供试液,利用Origin 8.0软件求算扫描后的吸波面积,换算供试液中不同碱性物质的混合浓度,绘制乌头二元释药颗粒的累积释放曲线,比较二者的释药趋势。结果:吸波面积法用于测定碱性物质体外释放度的方法稳定可行、结果准确,线性方程为Y=0.145 4X+3.240 4(r=0.999 3),平均加样回收率106.25%(RSD 6.2%)。体外累积释放曲线表明普通颗粒碱性物质在酸性介质中快速释放,在第10 min累积释放率达54.55%,第45 min达94.51%,而聚丙烯酸树脂包衣颗粒在酸性介质中仅少量释药,模拟肠液中释药明显,第210 min释放率达到了90.26%,具有较好的二元释药结果。结论:三氯甲烷萃取较好地呈现了不同颗粒中碱性成分的释放趋势,吸波面积法可用于乌头二元释药颗粒的体外释放度测试,为其他碱性物质中药制剂的释放度及体内外相关研究提供了良好借鉴。

Objective：To establish determination of in vitro release of alkaline substances from Wutou binary-released granules by the method of area under absorbance-wavelength curve（AUAWC）.Method：The studies on in vitro release for Wutou ordinary granules and Wutou polyacrylic acid resin coated granules were researched.Release medium containing drug was obtained at different time points,the individual sample solutions were obtained through chloroform extraction after pH adjusting.The AUAWC were calculated by Origin 8.0software,and the mixed concentration of different alkaline substances in sample solutions was obtained.Then,the cumulative release curve of Wutou binary-released granules was drawn and the drug release trends of these two granules were compared.Result：This established AUAWC was stable,feasible and accurate with the linear equation of Y=0.145 4X＋3.240 4（r=0.999 3） and the average recovery of 106.25%（RSD 6.2%）.The cumulative release curve of in vitro release showed that alkaline substances from ordinary granules in the acidic medium was rapid release,which was 54.55% at the 10th min and 94.51% at the 45th min.While the release of those from Wutou polyacrylic acid resin coated granules in acid medium was only a little release,but it released significantly in the simulated intestinal fluid with cumulative release rate of 90.26% at the 210 thmin.Conclusion：The chloroform extraction shows a good release trend of the alkaline substances in different granules.AUAWC can be used for the determination of in vitro release of Wutou binary-released granules,it will provide a good instruction for the study of release of alkaline substances in other Chinese materia medica preparations and their in vitro and in vivo researches.