复方丹参黏附脉冲微丸的制备工艺研究

Study on Preparation Technology of Compound Danshen Pulsatile Release Pellets

目的制备复方丹参黏附脉冲微丸。方法使用不同的包衣材料,于载药微丸由内至外依次包溶胀层、控释层和黏附层,考察包衣后对溶出效果的影响并优化包衣处方,评价脉冲微丸的黏附性。结果溶胀层、控释层和黏附层材料类型、包衣增重、增塑剂种类及用量等对黏附脉冲微丸的释药时滞和释药速率均有显著性影响。结论优选的最佳包衣处方,在模拟人体内胃肠道pH值变化条件下时滞达到4.5 h,时滞后1.5 h累积释药80%以上的脉冲释药效果。

OBJECTIVE To prepare compound Danshen adhesion pulsatile release pellets. METHODS Different coating materials were used. Swelling layer, controlled-release layer and adhesive layer were packed on drug-containing pellets from inside to out- side. The coating effect on the dissolution was studied. The coating formulation was optimized. The adhesiveness of the pellets was evaluated. RESULTS The release delay and rate were affected by the materials of swelling layer, controlled-release layer and adhesive layer, the weight of coating layer, and the type and quantity of plasticizer. CONCLUSION With the best coating prescription, a delay of 4. 5 h in drug release was reached in simulated changing human gastrointestinal pH environment. The cumulative release reached more than 80% 1.5 h post the release lag, indicating a pulsatile release effect.