环孢素眼用乳剂在健康人体的耐受性及血药浓度测定  

Tolerance of cyclosporine ophthalmic emulsion and determination the concentration in Chinese healthy volunteers

作　　者：武峰[1] 赵秀丽[1] 王淑民[1] 周辉[1] 李嘉静[1] 郭韶洁[1] 邹留河[2] 金涛[2] 

机构地区：[1]首都医科大学附属北京同仁医院国家药物临床试验机构,北京100730 [2]首都医科大学附属北京同仁医院眼科,北京100730

出　　处：《中国临床药理学杂志》2010年第12期893-895,共3页The Chinese Journal of Clinical Pharmacology

摘　　要：目的观察环孢素(免疫抑制剂)眼用乳剂在健康人体内的耐受性及血药深度测定。方法健康受试者分别单次或连续给予不同浓度的环孢素眼用乳剂;观察生命体征、眼科、全身体格及实验室检查,并记录所有不良事件;用液质联用法检测环孢素的血药浓度。结果单次给药组,2例受试者出现一过性角膜荧光染色异常;连续给药后,2例受试者出现轻度一过性眼局部刺激症状;其他全身安全性指标,均未出现与研究药物有关的异常改变;在本研究定量范围内(最低定量限为0.2ng·mL-1)未测得环孢素血药浓度。结论环孢素眼用乳剂的安全性和耐受性良好。Objective To study the tolerance of cyclosporine ophthalmic emulsion and determination its concentration in Chinese healthy volunteers.Methods Cyclosporine ophthalmic emulsions were administered single or consecutive doses in healthy volunteers respectively.The safety and tolerance were assessed based on vital signs,ophthalmologic examination,physical and laboratory outcomes,and all the adverse events.Cyclosporine concentrations were determined by LC-MS/MS assay.Results Corneal fluorescein staining abnormalities occurred transiently in two subjects of single dose group.After consecutive doses,two subjects experienced mild transient topical stimulation.No subjects had any quantifiable cyclosporine in the blood（quantitation limit=0.2 ng·mL-1）.Conclusion Cyclosporine ophthalmic emulsion is tolerated well.

关 键 词：环孢素眼用乳剂 耐受性 安全性 

分 类 号：R969.3[医药卫生—药理学] R979.5[医药卫生—药学]