药物溶出／吸收仿生系统研究丹酚酸B缓释片释放规律

目的：应用药物溶出／吸收仿生系统（drug dissolution / absorption simulating system, DDASS）研究丹酚酸B缓释片的体外释放规律，为中药活性成分缓控释制剂的设计提供新技术。方法：分别采用DDASS法和我国药典收载的桨法对丹酚酸B固体制剂进行体外释放度试验，高效液相色谱法定量，SPSS软件对累积释放度进行释放模型拟合。改进DDASS装置使研究对象从药物固体粉末或颗粒剂扩展到片剂、胶囊剂等多种剂型，分别评价丹酚酸B缓释片DDASS改进前、后和桨法中释放规律的相关性。结果：丹酚酸B原料药及其缓释片在改进前DDASS模型中释药过程符合Weibull方程；而丹酚酸B缓释片在改进后DDASS模型中释药过程符合一级动力学方程，与桨法评价结果一致。DDASS改进前、后与桨法释药规律相关性水平r值分别为0.788 4（r_{5, 0.05}＜r_前＜r_{5, 0.001}）和0.998 2（r_后＞r_{5, 0.001}）。结论：丹酚酸B缓释片释药规律研究显示改进后DDASS法与桨法之间存在更为显著相关性。较之桨法，DDASS法模拟了一个连续动态的、更接近人体消化道环境的释药过程，表明该法评价药物固体制剂释药特性研究的合理性，为药物剂型设计研究提供了新的技术平台。

Evaluation on the release discipline of salvianolic acid B sustained-release tablets using a drug dissolution and absorption simulating system

Objective: Drug dissolution and absorption simulating system (DDASS) was used to evaluate the release discipline of salvianolic acid B sustained-release tablets. It is anticipated to establish a new technology and method for studying the sustained-release or controlled-release preparations of Chinese herbal drugs active components. Methods: DDASS method and paddle method were used to study the release feature of salvianolic acid B sustained-release tablets. High performance liquid chromatography method was used to determine the concentration of salvianolic acid B. SPSS software will be used to fit curves. The applications are expanded to tablets and capsules from powder and granules by upgrading the DDASS method. The correlations between DDASS method and paddle method and between upgraded-DDASS method and paddle method were both evaluated. Results: The releasing curves of the salvianolic acid B crude drugs and sustained-release tablets both conformed to Weibull equation in the DDASS methods, while the release equation of the sustained-release tablets was first order kinetic equations in upgraded-DDASS method and paddle method, respectively. The correlation coeffient of the release features of DDASS method and the paddle method was 0.788 4 (r _5,0.05 < r_before < r _5,0.001), while the upgraded DDASS method and the paddle method was 0.998 2 (r_after > r_5,0.001). Conclusion: For salvianolic acid B sustained-release tablets, a good linear correlation is obtained between the cumulative dissolution rate in upgraded-DDASS method and the cumulative dissolution rate in the paddle method in the same length of time. Compared with paddle method, upgraded DDASS method simulates a continuous and dynamic drug- releasing course which is closer to course of drugs being transported through the gastrointestinal tract. The result confirms the reasonableness of upgraded DDASS method to assess the releasing features of solid preparations and establish a new technology platform for the study of devising drug preparations.