新型辅料提高环孢素A眼部制剂生物利用度的研究概况  

General Situation of Novel Excipients for Improving Bioavailability of Cyclosporine A Ocular Preparations

作　　者：董星 闫梦 何朝星[1] 李素霞[2] 向柏[1] DONG Xing;YAN Meng;HE Chaoxing;LI Suxia;XIANG Bai(School of Pharmacy,Hebei Medical University,Shijiazhuang 050017;Pharmaceutical Engineering Dept.,Hebei Chemical and Pharmaceutical College,Shijiazhuang 050030)

机构地区：[1]河北医科大学药学院,河北石家庄050017 [2]河北化工医药职业技术学院,河北石家庄050030

出　　处：《中国医药工业杂志》2023年第11期1569-1577,共9页Chinese Journal of Pharmaceuticals

基　　金：国家自然科学基金资助项目(81973251)、河北省自然科学基金资助项目(H2019206445)、河北省2021年度医学科学研究课题(20211108)。

摘　　要：环孢素A免疫抑制效力强,被广泛应用于眼科治疗中,但由于相对分子质量大、疏水性强,难以突破眼部生理屏障,导致生物利用度低。有效结合新型辅料与制剂技术,可从增加药物溶解度、促进眼表黏液穿透、增强角膜组织深层渗透以及延长眼表停留时间4个方面提高环孢素A的生物利用度。该文重点围绕环孢素A眼用制剂中应用的新型辅料的特点、作用机制和相关制剂技术进行综述,以期为实现环孢素A的高效递送和今后新型制剂的开发提供参考。Cyclosporine A,a potent immunosuppressive agent,is extensively utilized in ophthalmic treatments.However,its high relative molecular mass and pronounced hydrophobicity pose challenges to its penetration through the physiological barriers of eyes,leading to low bioavailability.By strategically integrating innovative excipients and formulation technologies,the bioavailability of cyclosporine A can be enhanced from four aspects:increasing drug solubility,facilitating penetration through ocular mucus,boosting deep penetration into corneal tissues,and extending residence time on the ocular surface.This review focuses on the characteristics,action mechanisms,and associated formulation technologies of novel excipients employed in cyclosporine A ophthalmic formulations,to provide a reference for efficient delivery of cyclosporine A and the development of future novel formulations.

关 键 词：环孢素A 赋形剂 促吸收作用 眼用制剂 生物利用度 

分 类 号：R979.5[医药卫生—药品]