盐酸索他洛尔生物黏附微球的体外释药及黏附性能研究

目的考察盐酸索他洛尔生物黏附微球的体外释药特性并评价其黏附性能。方法采用高效液相色谱法测定释放介质与微球中盐酸索他洛尔含量，并以滞留率为指标考察微球的黏附特性。结果盐酸索他洛尔生物黏附微球30min累积释药百分率达30％，4h释药达90％；离体法与在体法测得微球胃黏膜上的滞留率分别为87．60±2．8％与60．2％±9．8％。结论盐酸索他洛尔高效液相色谱测定方法简便、可靠，与盐酸索他洛尔普通片相比，盐酸索他洛尔生物黏附微球具有一定缓释特性，且其在离体与在体模型中黏附性能良好。

In vitro drug release profiles and mucoadhesive property of sotalol hydrochloride bioadhesive microspheres

Objective To investigate the in vitro drug release profiles and mucoadhesive characteristics of sotalol hydrochloride bioadhesive mierospheres. Methods Content of sotalol hydrochloride in the release medium and bioadhesive microspheres was analyzed by HPLC and its mucoadhesive property was studied using stagnation percentage as the content index. Results The release profiles of sotalol hydrochloride demonstrated that the accumulated drug release at 30 min and 4 h was 30% and 90%, respectively. Mucoadhesive property test showed that stagnation percentage of sotalol hydrochloride bioadhesive microspheres in vitro and in vivo was 87.6%± 2. 8% and 60. 2%± 9.8%, respectively. Conclusion The HPLC method for sotatol hydrochloride is simple reliable. The release of sotalol hydrochloride bioadhesive mierospheres is sustained with in vitro and in vivo adhesiveness.