银杏内酯缓释微丸的制备及释放度研究

Preparation and evaluation on sustained-release pellets containing total lactones of Ginkgo biloba

目的制备可4种成分同步释放的银杏总内酯缓释微丸,并对其体外释放进行评价。方法以Eudragit RS 30D/RL 30D为包衣材料,制备银杏内酯缓释微丸,以银杏内酯A、B、C和白果内酯为指标进行体外释放度评价,高效液相色谱法进行含量测定,筛选优化包衣处方及工艺参数。结果当EudragitRS 30D和RL 30D的比例为8∶2,增塑剂和抗黏剂的用量分别为20%和50%、包衣增重为10%时,制备得到的微丸可实现4种成分同步12 h缓释释放。结论本研究微丸制备工艺快速、简便、高效,适合工业化生产。

AIM To obtain simultaneous controlled release of four active ingredients in ginkgolide pellets. METHODS Sustained-release pellets coated with Eudragit RS 30D/RL 30D were prepared. HPLC was used to determine the content of total lactones of Ginkgo biloba. The composition of coating film was optimized by using in vitro release percentage of ginkgolide A, B, C and bilobalide as indexes. RESULTS When the ratio of RS 30D and RL 30D was 8 to 2, the content of plasticizer and antisticking agent was 20% and 50% of the dry weight of film polymer, the increased amount of the coating materials was 10% of the pellets, sustained release of active ingredients in 12 h was achieved and described by first-order equations. CONCLUSION The preparation of the pellets is rapid, simple, efficient and suitable for industrial production.