吲哚美辛宫内节育器的主要药效学研究

A Pharmacodynamic Study on Indomethacin IUD

本文应用放射免疫法测定吲哚美辛 IUD对离体大鼠子宫匀浆中前列腺素类物质(PGs)释放的影响 ,用光镜和电镜观察放置吲哚美辛 IUD后大鼠子宫内膜的形态学变化 ,并测定吲哚美辛 IUD在大鼠子宫内的动态释放规律。结果表明 :吲哚美辛组 PGs释放约为铜组的 1 / 5～ 1 / 1 0 (P<0 .0 5 ) ,而且吲哚美辛抑制 PGs释放的作用随药物浓度增加而增强。铜组和硅橡胶组 PGs释放均有随时间累积而增加趋势 ,而吲哚美辛组无此表现。 6KF和 TXB2 的比值 ,吲哚美辛组和硅橡胶组均 <1 (0 .6～ 0 .8) ,而铜组则均 >1 (1 .3～ 2 .1 )。组织学观察 ,铜 IUD组可见子宫内膜组织充血水肿 ,微血管以扩张为主 ,吲哚美辛 IUD组则无充血水肿表现 ,微血管以正常和收缩状态为主。吲哚美辛 IUD在大鼠子宫内药物释放量 3 d后稳定 ,释放速度稳定递减 ,符合均质型缓释规律。

This article reports part of the work of pharmacodynamic studies of indomethacin IUD. The effect of indomethacin IUD on prostaglandings releasing in uterine homogenous plasma of rats was studied with the method of RIA. The morphology changes of endometrium of rats after indomethacin IUD insertion were observed under microscope and transmission electron microscope. The character of indomethacin release in vivo of indomethacin IUD was also studied. The results show that the amount of PGs released in uterine homogenous plasma of rats in the groups of indomethacin IUD is only 1/5～1/10 of that in the group of copper IUD. The effect of indomethacin on inhibition of PGs releasing is dose dependence. The fact that PGs release increased by time was detected in copper IUD group and silicon rubber IUD group but not in indomethacin IUD group. The ratio of 6KF/TXB 2 was <1 (0.6～0.8) in the group of indomethacin IUD and silicon rubber IUD, and was >1 (1.3～2.07) in group of copper IUD. In histological observation, congestion and swelling of endometrium were seen in copper IUD group but not in indomethacin IUD group. The micro blood vessels appeared mostly enlarged in copper IUD group but normal or constricted in indomethacin IUD group. The amount of indomethacin released from indomethacin IUD in uterus of rats was stable 3 days later. The release rate of decreased steadily and accorded with the homogeneous system. [WT5HZ]