雷帕霉素眼用缓释膜的制备及体外释放分析  

Preparation and Properties of Rapamycin Sustained-release Film

作　　者：颜志超 游秀华[2] 邓彩彬 YAN Zhi-chao;YOU Xiu-hua;DENG Cai-bin(Department of Ophthalmology,The Second Affiliated Hospital of Guangzhou Medical University,Guangzhou 510260,China;School of Pharmaceutical Sciences,Sun Yat-Sen University,Guangzhou 510006,China;State Key Laboratory of Ophthalmology,Zhongshan Ophthalmic Center,Sun Yat-sen University,Guangzhou 510060,China)

机构地区：[1]广州医科大学附属第二医院眼科,广东广州510260 [2]中山大学药学院,广东广州510006 [3]中山大学中山眼科中心眼科学国家重点实验室,广东广州510060

出　　处：《中山大学学报（医学版）》2020年第1期143-148,共6页Journal of Sun Yat-Sen University:Medical Sciences

基　　金：国家自然科学基金(81900858);广东省自然科学基金(2018A030310185);广州医科大学科研项目(2016C21)

摘　　要：[目的]制备雷帕霉素(RAPA)眼用缓释膜,并评价其体外释放性能。[方法]利用聚乳酸(PLA)和聚糖酸(PGA)的共聚物聚乳糖酸(PLGA)为载体与RAPA制成眼用缓释膜,并对该缓释膜的药物含量进行测定(包括缓释膜的专属性考察、回收率、精密度及稳定性的测定),以及缓释膜的体外释放分析研究。[结果]通过RAPA标准曲线可知,RAPA浓度在0.408~40.8μg/mL范围内,与峰面积呈良好的线性关系;专属性考察发现缓释膜中辅料及0.3%SDS溶液对RAPA含量测定没有干扰,含量测定专属性好;对空白缓释膜加入高中低3组不同药物含量并检测其回收率和精密度结果均良好;通过RAPA缓释膜的药物含量测定分析,缓释膜平均RAPA含量为(112.6±10.1)μg/片(R SD8.99%);而RAPA稳定性测定也发现,以0.3%SDS溶液为释放介质的RAPA在15d内稳定性好。同时通过缓释膜体外释放研究发现,药物释放量在第5天达到峰值浓度,并持续维持至15d。[结论]一定行为学参数的RAPA眼用缓释膜具有良好的缓释性能,具有青光眼术后抗瘢痕化的应用潜力。[Objective]To prepare rapamycin(RAPA)sustained-release film and to evaluate its dissolution.[Methods]RAPA sustained-release film was created by using polymer polyactioglyconic acid(PLGA),copolymer of polyactic acid(PLA)and polyglycolic acid(PGA).Drug content of the sustained-release film was determined using specificity test,recov ery,relative standard deviation(R SD)and stability test.Then,the dissolution of the sustained-release film was analyzed.[Results]The concentration of RAPA had a linear relationship with peak area,which ranged between 0.408μg/mL and 40.8μg/mL through the standard curve.The specificity test of the drug content determination indicated the excipient of the film and the solution with 0.3%sodium dodecyl sulfate(SDS)did not affect in determining the RAPA content.The recovery and RSD were excellent through drug content determination in blank films,which had three different levels of RAPA concentrations.The mean RAPA content of the sustained-release films was(112.6±10.1)μg(RSD 8.99%)through the drug content determi nation of the films,and the stability of RAPA with 0.3%SDS was good within 15 days.In addition,dissolution test of the sus tained-release film indicated that the amount of drug release reached a high level and sustained up to 15 days.[Conclusion]The RAPA sustained-release film with certain behavioral characteristic parameters had a stable drug content and favorable sus tained-release property,and it may have certain application potential in anti-proliferation after glaucoma filtering surgery.

关 键 词：雷帕霉素 缓释膜 体外释放 青光眼 抗瘢痕化 

分 类 号：R917[医药卫生—药物分析学]