【作者】 张望刚； 丁宇； 叶金翠； 陈国神；

【Author】 Zhang Wang-Gang,Ding Yu,Ye Jin-Cui,et al (Institute of Materia Medica,Zhejiang Academy of Medical Science,Hangzhou,310013)

【机构】 浙江省医学科学院药物研究所； 德固萨-赫斯太平洋有限公司上海办事处；

【摘要】 以Eudragt E100为骨架材料,采用正交设计筛选与优化处方,制备了雌二醇透皮控释制剂(E2- TCDS),运用Valia—Chien双室渗透池与HPLC法测定其对人离体皮肤的雌二醇渗透率。结果表明E2-TCDS 与瑞士Estraderm TTS(Giba Geigy)相比较,两者有基本一致的皮肤渗透率,平均日渗透量达50μg左右,可持续恒速释药72h以上。更多还原

【Abstract】 Transdermal estradiol matrix diffusion controlled delivery systems (E2-TCDS)was developed using acrylic polymer Eudragit E100.The TCDS formulations of estradiol were screened and optimized by orthogonal design.Transdermal permeation of estradiol was carried out with Vali-a-Chien double-compartment permeation cells.The estradiol permeation rate and accumulative amount within 72h in vitro were detected by HPLC.The results showed that the skin permeation profiles of estradiol through human intact skin in vitro of E2-TCDS and Estraderml ITS (Ciba-Geigy)were very similar with an average permeation amount of about 50μg/d and constant drug release lasting more than 72h,no significant difference was found.更多还原