可分剂量甲磺酸二氢麦角碱缓释微囊片的制备及体外释放机制的研究

Studies on Preparation and Dissolution Mechanism in Vitro of Ergoloid Mesylates Divided Dose Tablet of Extended-Release Microcapsule

关键词:  甲磺酸二氢麦角碱  壳聚糖  海藻酸钠  缓释微囊  释放机制

Key words:  ergoloid mesylates  chitosan  alginate  extended-release microcapsule  dissolution mechanism

摘要:

目的 对可分剂量甲磺酸二氢麦角碱缓释微囊片(EDDTEM)的处方进行研究，并研究其体外释放机制。方法 以海藻酸钠-壳聚糖为囊材，采用复凝聚法制备甲磺酸二氢麦角碱缓释微囊(EEM)并压制成片，采用正交设计实验优化处方。结果 EEM的最优处方为：海藻酸钠与药物比例为6∶1，海藻酸钠-壳聚糖比例为4∶1，海藻酸钠浓度为2.5%。所制缓释片释药行为符合Higuchi方程，释药机理为扩散和溶蚀并存。结论 EDDTEM具有良好的体外缓释效果，可进一步进行体内释药行为考察。

Abstract:

OBJECTIVE To study prescription of ergoloid mesylates divided dose tablet of extended-release microcapsule (EDDTEM) and inspect dissolution mechanism in vitro. METHODS Ergoloid mesylates extended-release microcapsule (EEM) were prepared with alginate-chitosan as capsule wall material. The orthogonal experiment was designed to screen prescription. RESULTS The optimization of prescription was as follows: the proportion of alginate to drug is 6∶1, the proportion of alginate to chitosan is 4∶1, the concentration of alginate is 2.5%. The release behavior of EDDTEM was coincident with Higuchi equation. The dissolution mechanism were both diffusion and corrosion. CONCLUSION EDDTEM had good effect of extended-release in vitro and the release behavior in vivo needs to be inspected.