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目的:制备盐酸索他洛尔生物粘附微球,考察其体外释药特性并评价其粘附性能。方法:应用正交试验筛选盐酸索他洛尔生物粘附微球的最佳处方,采用高效液相色谱法测定盐酸索他洛尔生物粘附微球的含量与释放度,选用滞留率为指标考察微球的粘附特性。结果:盐酸索他洛尔生物粘附微球的最佳处方为盐酸索他洛尔投药量占处方组成的30%,分散相与连续相比为70%,司盘80用量为9.0g;体外释药试验结果表明盐酸索他洛尔生物粘附微球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(87.6±2.8)%与(60.2±9.8)%。结论:盐酸索他洛尔生物粘附微球处方设计合理,制备工艺简单,与盐酸索他洛尔普通片相比,盐酸索他洛尔生物粘附微球具有一定缓释特性,且其在离体与在体模型中粘附性能良好。
OBJECTIVE: To prepare sotalol hydrochloride bioadhesive microspheres and study its in vitro release characteristics and evaluate its adhesive properties. Methods: The orthogonal test was used to screen sotalol bioadhesive microspheres. The content and release of sotalol hydrochloride bioadhesive microspheres were determined by high performance liquid chromatography (HPLC) Investigate the adhesion properties of microspheres. Results: The best prescription of sotalol hydrochloride bioadhesive microspheres was 30% of the prescription of sotalol hydrochloride, 70% of the disperse phase and the dosage of Span 80 was 9.0g. In vitro The results of drug release test showed that the cumulative release rate of sotalol bioadhesive microspheres was 30% in 30 min and 90% in 4 h, and the retention rates of microspheres’ gastric mucosa measured by in vitro and in vivo methods were (87.6 ± 2.8)% and (60.2 ± 9.8)%, respectively. CONCLUSIONS: Sotalol hydrochloride bioadhesive microspheres have reasonable formulation design and simple preparation process. Sotalol hydrochloride bioadhesive microspheres have some sustained-release properties compared with ordinary tablets of sotalol hydrochloride, Good adhesion between in vitro and in vivo models.