他克莫司阳离子微乳凝胶的兔眼刺激性研究及房水药动学研究  

The eye irritation test and pharmacokinetic study of tacrolimus-loaded cationic nanoemulsion-based in-situ gel in rabbits

作　　者：林昕 张佳良 周欣 宋洪涛 LIN Xin;ZHANG Jialiang;ZHOU Xin;SONG Hongtao(Department of Pharmacy,No.900 Hospital of Joint Logistic Support Force of the PLA,Fuzhou 350025,China)

机构地区：[1]中国人民解放军联勤保障部队第九〇〇医院药学科,福建福州350025

出　　处：《药学实践与服务》2023年第3期177-181,共5页Journal of Pharmaceutical Practice and Service

摘　　要：目的研究他克莫司阳离子微乳凝胶对兔眼的刺激性及房水药动学。方法通过HE染色处理的兔眼组织病理切片观察该制剂的眼部刺激性。采用角膜穿刺术抽取兔眼房水,通过液相色谱-质谱联用仪进行房水药动学研究。结果他克莫司阳离子微乳凝胶对兔眼无明显刺激性,其房水药动学参数AUC为(128.34±13.09)ng·h/ml,是他克莫司阳离子纳米乳AUC(113.61±12.36)ng·h/ml的1.13倍,是市售他克莫司滴眼液Talymus®AUC(68.25±10.82)ng·h/ml的1.88倍。结论他克莫司阳离子微乳凝胶眼部刺激性小、滞留时间长且生物利用度高,具有较好的临床应用前景。Objective To study the eye irritation and the pharmacokinetics of tacrolimus-loaded cationic nanoemulsion-based in-situ gel in rabbits.Methods The eye irritation of tacrolimus-loaded cationic nanoemulsion-based in-situ gel in rabbits was observed by histological cross-sections of external ocular tissues stained with HE.The aqueous humor of rabbit eyes was extracted by corneal puncture and analyzed by HPLC-MS for pharmacokinetic study.Results Tacrolimus-loaded cationic nanoemulsion-based in-situ gel had no significant irritation on rabbit eyes.The pharmacokinetic parameter showed that the AUC of tacrolimus-loaded cationic nanoemulsion-based in-situ gel was(128.34±13.09)ng·h/ml,which was 1.13 times of tacrolimus-loaded cationic nanoemulsion(113.61±12.36)ng·h/ml and 1.88 times of Talymus®(68.25±10.82)ng·h/ml.Conclusion Tacrolimus-loaded cationic nanoemulsion-based in-situ gel had the advantages of low irritation,long retention time and high bioavailability in rabbit eyes.It has a good potential for clinical application.

关 键 词：他克莫司 阳离子微乳凝胶 眼部刺激性 药动学 

分 类 号：R943[医药卫生—药剂学]