薄膜包衣对西罗莫司滴丸溶出度及稳定性的影响研究

Effect of Membrane-coating on Dissolution and Stability of Sirolimus Dropping Pills

目的:探讨薄膜包衣对西罗莫司(SRL)滴丸溶出度及稳定性的影响,以证实薄膜包衣的作用及合理性。方法:选用欧巴代为SRL滴丸的包衣材料进行包衣;对其体外释药及稳定性进行考察,并与未包衣的SRL滴丸进行比较。结果:与未包衣滴丸相比,在相同时间内,薄膜包衣SRL滴丸的体外释药量明显降低(P<0.05),而稳态释药速率并无显著影响(P>0.05);高湿条件下(75%±5%)包衣SRL滴丸的吸湿性显著下降,在强光环境中(4 500 lx±500 lx),包衣SRL滴丸的稳定性也较好,而在高温条件下(40℃±2℃),稳定性无显著提高。结论:欧巴代薄膜包衣可明显提高SRL滴丸的稳定性,而对其药物溶出无显著性影响。

Objective：To study the effect of membrane-coating on dissolution and stability of sirolimus （ SRL） dropping pills to prove the effect and rationality of the coating process. Methods：Opadry was used as the coating material for SRL dropping pills. Compared with those of uncoated SRL dropping pills, the dissolution and stability of membrane-coating SRL dropping pills were studied in vitro. Results：Compared with that of uncoated SRL dropping pills, the drug release amount of membrane-coating SRL dropping pills was lower （P〈0. 05）, however, the stable release rate showed no significant difference （P〉0. 05）. After the membrane-coating, the stability of SRL dropping pills was notable enhanced under high humidity （75% ± 5%） and strong light （4500lx ± 500lx） conditions, however, the stability showed no improved under high temperature（40℃ ± 2℃） condition. Conclusion： The membrane-coating can enhance the stability of SRL dropping pills without significant effect on drug release in vitro.