活性元宫型药铜宫内节育器铜离子及药物体外释放的研究  

Release of cupric ion and drugs of Yuan Gong medicated Cu-IUDs in simulated uterine solution

作　　者：侯丽 周越 辛玲 高娜娜 杜江[1,2] 邵海浩[3] 吴尚纯 王慧萍 

机构地区：[1]国家卫生计生委科学技术研究所,北京100081 [2]北京协和医学院研究生院,北京100730 [3]上海市计划生育科学研究所,上海200032

出　　处：《生殖医学杂志》2015年第8期650-660,共11页Journal of Reproductive Medicine

基　　金：十二五国家科技支撑计划项目(2012BAI31B03)

摘　　要：目的比较含吲哚美辛（IMC）和含双氯芬酸钠（DFS）的两种含铜宫内节育器（IUD）在模拟宫腔液中的铜离子和药物的释放规律，以及铜丝浸泡后的表面形貌改变差异。方法将含IMC或含DFS的元宫药铜288型宫内节育器分别浸泡在37℃的50m1的模拟宫腔液中，定期换液。采用电感耦合等离子体发射光谱法及紫外可见分光光度仪分别测试了不同浸泡时间后模拟宫腔液中的铜离子（Cu^2＋）浓度，及吲哚美辛、双氯芬酸钠浓度，并用扫描电子显微镜观测了元宫药铜宫内节育器在模拟宫腔液中浸泡10d、30d及60d后的铜丝表面形貌。结果IMC-IUD和DFS-IUD的铜离子释放均是前期快，后期慢，两组的Cu^2＋的累计释放量在前、后期差别不大，差值变化较小（P〉0．05），但在5～33d有显著差别（P〈0．05）；DFS在释放介质中呈现双相释放，20d后基本达到稳态，每24h平均释放量约为（0．134±0．025）mg，而IMC的早期释放则呈不规则状态，前7d内的释放量显著少于DFS（P〈0．05），8d后每天释放量又显著大于DFS（P〈0．05），20d后IMC的24h平均释放量约为（0．675±0．175）mg；两组浸泡后的铜丝表面形貌均呈现明显的不均匀腐蚀现象。结论DFS-IUD中的DFS体外释放较IMC-IUD释放IMC更为恒定。Objective： To investigate the release pattern of cupric ion and indometacin（IMC）or diclofenac（DFC）of medicated Cu-IUDs,and the corrosion of the wire of Cu-IUDs in the simulated uterine solution. Methods： Yuan Gong Cu-IUDs were dipped in the simulated uterine solution which was changed in regularity. The concentrations of copper ion and drugs in simulated uterine solution with different immersed time were determined by using inductively coupled plasma atomic emission spectrometry and UV analyzer respectively. The surface morphology of samples was observed under scanning electron microscope before and 10,30, and 60 days after dipped. Results： The releasing rate of cupric ion were very high at the early stage,and then decreased rapidly, afterwards tended to be stable gradually both in IMC-IUD and DFS-IUD. The cumulative release amountof Cu^2＋ at the early stage or later stage was not significantly changed（P〉0.05） ,but there was a significant change from day 5 to day 33 （P〈0.05）. The releasing rate of diclofenac sodium presented a hi-phase pattern. The releasing rate became stable after 20 days. The average releasing amount of diclofenac sodium for 24 hours was（0. 134±0. 025）mg. The releasing rate of indometacin presented irregular pattern. The releasing amount of indometacin was significantly less than diclofenac sodium in the first seven days （P〈0. 05）. The releasing amount of indometacin was significantly more than diclofenac sodium after 8 days（P〈0.05）. The average releasing amount of indometacin for 24 hours was（0. 675±0. 175）mg. The pits were observed on the copper wire surface of the medicated Cu-IUDs after immersed in simulated uterine solution. Conclusions： The release of diclofenac sodium is more stable than indometacin in Yuan Gong medicated Cu-IUDs.

关 键 词：药铜宫内节育器 吲哚美辛 双氯芬酸钠 模拟宫腔液 铜离子释放 

分 类 号：R[医药卫生]