氟苷双层单向缓释膜的研制及质量考察  

Preparation of Bilayer Sustained_release Pellicle of Floxuridine and Its Quality in vitro and in vivo

作　　者：何文[1] 杨健[1] 张先洲[1] 詹春[2] 程强 蔡鸿生 

机构地区：[1]湖北医科大学附属第一医院药学部,湖北武汉430060 [2]湖北医科大学药学系

出　　处：《广东药学院学报》1999年第4期258-261,共4页Academic Journal of Guangdong College of Pharmacy

摘　　要：研制一种子宫颈给药的双层单向缓释膜剂并建立其质量控制方法，拟为临床防治子宫颈癌提供一种新型给药方式。以氟苷为模型药物，ＰＶＡ∶ＳＣＭＣ（１∶１） 为含药膜基质，卡波姆９４０为缓释材料，ＰＶＣ为覆盖材料制膜。紫外分光光度法测定主药含量，并进行均匀度实验、稳定性试验、用静态小室进行单向释药试验，并考察本品体内外释药特性，判断体内外释药相关性。结果表明：氟苷在ｐＨ５．０ 乙酸钠缓冲液中，在２６８．６ ｎｍ 处有吸收峰，基质几乎无紫外吸收。在０ ．５ ～２５μｇ／ｍＬ范围内线性关系良好，回收率高，均匀度合格。稳定性试验显示本品对温度和湿度较稳定，对光敏感。单向释药试验结果表明氟苷不能通过ＰＶＣ覆盖膜，只有通过含药膜单向释药。体外释药行为符合Ｈｉｇｕｃｈｉ 方程，且体内、外释药相关性好。本制剂处方合理，质控方法可靠，缓释效果理想。In order to develop a new therapeatic preparation for cervical intraepithelial neoplasia, a bilayer sustained_release pellicle of floxuridine was prepared with floxuridine as model drug,PVA∶SCMC(1∶1) as biadhesive layer, PVC as backing layer and carbopol_940 as sustained material. The content of floxuridine was determined by UV and the homogeneity, stability and its dissolution characters in vitro and in vivo and their correlation were observed. It was shown that there was a good linear relationship within the range of 0.5～25 μg/mL of floxuridine, with a standard curve of A=0.018C-0.0018(r=0.9999,n=7) and high recovery rates. The pellicle was stable under ambient conditions. The homogeneity was good and the dissolution in vitro and in vivo were ideal.

关 键 词：子宫颈给药 氟苷 双层单向 缓释膜 

分 类 号：R944.9[医药卫生—药剂学] R984[医药卫生—药学]