新型眼用制剂环孢素A微乳研究.pdfVIP

新型眼用制剂环孢素A 微乳的研究 1 1 1 2 甘莉 ,朱春柳 ,甘勇 *,林燕琼 （1.中国科学院上海药物研究所，上海 201203; 2.亚生（上海）医药研发有限公司，上海 201203 ） 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。 关键词：环孢素A ；微乳；伪三元相图；刺激性 中图分类号： 文献标识码： 文章编号： Novel ocular drug delivery system of Cyclosporine A microemulsion 1 1 1 2 Gan Li , Zhu Chunliu ,Gan Yong *, Lin Yanqiong (1.Shanghai Institute of Materia Medica, Chinese Academy of Science, Shanghai201203, China; 2.Ascenta(Shanghai) Research Development Center, Shanghai201203,China) 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. KEY WORDS: cyclosporineA; microemulsion; Pseudoternary phase diagrams; ocular irritation 作者简介：甘莉，女，博士研究生，*通讯作者：甘勇，男，副研究员，Tel ：（021 2122， E-mail:ygan@ 环孢素 A 是一种具有免疫抑制活性的非极性环状低聚肽，1978 年首次投入 临床使用，主要用于预防和治