含铜宫内节育器中吲哚美辛体外释放规律的研究

Study on in vitro release behavior of indomethacin used for CuIUD

目的：测定含铜宫内节育器（CuIUD）中吲哚美辛（IMC）在体外模拟宫腔液中的释放规律。方法：以体外模拟宫腔液作为提取介质,在37±0.5℃条件下静态释放IMC,然后通过高效液相色谱（HPLC）检测IMC的释放量。结果：IMC释放试验的前期释放量有较大（2.2~2.5 mg）的药物突释现象,释放率占载药量的10%,中期IMC的日均释放量逐渐变得缓慢,后期IMC的日均释放量趋于稳定。整个周期的释放量为7~12 mg,释放率占载药量的36%~49%。结论：建立了HPLC测定IMC在模拟宫腔液释放量的方法,且IMC体外累积释放率呈幂函数释放规律,每日释放量呈逐日下降趋势。

Objective： To evaluate the release behavior of indomethacin（IMC） in vitro used for CuIUD.Methods： Four kinds of CuIUDs soaked in simulated uterine fluid, the concentration of IMC was analyzed by high performance liquid chromatography（HPLC）. Results： IMC was released profusely from indomethacin rubber in initial term（2.2-2.5 mg）, the releasing degree was 10%, then the daily release degree of IMC was slowly in medium term. In the following days, the trend of release level was even and steady. Releasing amount of IMC was 7-12 mg during the whole experiment, the releasing degree was 36%-49%. Conclusion： The HPLC method was established for the determination of IMC releasing content in simulated uterine fluid, and the accumulating release behavior of IMC follows the power function rule and the daily releasing trend is decreasing gradually.