【作者】 甘莉； 朱春柳； 甘勇； 林燕琼；

【Author】 Gan Li1, Zhu Chunliu1,Gan Yong1*, Lin Yanqiong2 (1.Shanghai Institute of Materia Medica, Chinese Academy of Science, Shanghai201203, China; 2.Ascenta(Shanghai) Research &Development Center, Shanghai201203,China)

【机构】 中国科学院上海药物研究所； 亚生(上海)医药研发有限公司；

【摘要】 目的制备安全舒适的环孢素A眼用微乳制剂。方法采用伪三元相图法研究了合适的乳化剂-辅助乳化剂-油相形成的微乳区域,并进一步优化剪切速率和乳化温度等工艺参数;通过长期稳定性试验评价了微乳的稳定性,并通过家兔眼刺激性试验评价了环孢素A眼用微乳制剂的安全性。结果理想的环孢素A眼用微乳制剂平均粒径小于100nm,包封率约85%,长期放置稳定,且对家兔眼组织无刺激性。结论首次研制的环孢素A眼用微乳稳定性及安全性良好,适合于眼部给药。更多还原

【Abstract】 OBJECTIVE To prepare cyclosporine A ophthalmic emulsion with high safety and compatibility. METHOD Pseudoternary phase diagrams were drawn to evaluate the microemulsion area, then process parameters such as high-shear rotation speed and temperature were optimized; the stability studies was conducted under long term storage conditions; the safety study was processed with ocular irritation test on rabbit. RESULTS The optimized cyclosporine A ophthalmic emulsion is stable under both storage conditions and non-irritating to rabbit ocular, with average diameter to be less than 100nm and encapsulation efficiency more than 85%. CONCLUSION The cyclosporine A emulsion was developed to be of good stability and safety, which is suitable for ocular drug delivery.更多还原