单池药物溶出仿生系统考察卡马西平组合微丸的溶出特征

Dissolution of carbamazepine by single cell-DDASS

目的:动态考察卡马西平组合微丸溶出特征。方法:采用Single cell-DDASS法,连续、动态地模拟组合微丸从胃移行至肠道崩解、释放,以模拟药物在人体中的溶出过程。联合使用高效液相色谱法测定药物含量随时间的变化情况。采用动力学方程拟合药物在体外的释放行为,根据拟合优度判定拟合情况。结果:卡马西平组合微丸累积释放最优拟合方程为一级释放动力学方程。ln(1-0.01Q)=-0.022 9t+0.552 1(r=0.989 6)。释放机制为溶蚀机制。其释放度曲线拥有两个峰。峰谷波动小,释放时间延长。结论:卡马西平组合微丸具有一定的缓释效果。

Objective： To evaluate the dissolution behavior of the combined pellets of carbamazepine （CPC） on time. Methods： The formulation process from stomach to intestine was simulated by single the cell-DDASS. And the CPC was dissolved and released in the process. The high performance liquid chromatography method （HPLC） was applied to measure the content of carbamazepine to show the changes over time, And several mathematical models of drug release were used to fit the vitro release of the CPC. Therefore, the best simulations for the vitro release could be obtained by the degree of fitting. Results： The release pattern of the CPC in vitro could be described by first order kinetic equation, ln（1-0.01Q）= -0.022 9t＋0.552 1 （r=0.989 6）. The release mechanism was based on the dissolution mechanism. Furthermore, with low volatility the release curve had two peaks, and CPC release time was increased. Conclusion： The CPC has certain slow-release effect.