丙氨瑞林缓释微球注射剂对大鼠异位子宫内膜抑制作用  

INHIBITORY EFFECT OF ALARELIN MICROSPHERES ON EXPERIMENTAL ENDOMETRIOSIS IN RATS

作　　者：赵瑞钦[1,2] 周美华[1,2] 瞿文 陈庆华[1,2] 

机构地区：[1]上海医科大学基础医学院药理教研室 [2]上海医药工业研究院制剂室

出　　处：《药学学报》1999年第8期565-568,共4页Acta Pharmaceutica Sinica

摘　　要：目的：观察丙氨瑞林缓释微球注射剂（ＬＨＲＨＡｍｓ）对异位内膜的抑制作用。方法：用外科自体移植术建立大鼠子宫内膜异位症动物模型，随机分组给药，同时在给药后不同时间采集血样，测定血清Ｅ２水平。结果：ＬＨＲＨＡｍｓ作用相似于ＬＨＲＨＡｌｐ，剂量为１００μｇ·ｋｇ－１·ｄ－１时，对大鼠异位内膜明显抑制，可达“药物性去卵巢”作用，增加剂量，作用并未相应增加。给药后１周，血清Ｅ２可降低至间情期水平，６周后开始恢复。结论：ＬＨＲＨＡｍｓ对大鼠异位子宫内膜有明显的抑制，可达“药物性去卵巢”作用，为临床应用提供实验依据。AIM: To study the inhibitory effect of alarelin(D Ala 6, Pro 9NHEt) microspheres(LHRH Ams) on the growth of endometrial explants in rat model of endometriosis. METHODS: The model of endometriosis in rats was made by surgically autotransplanting endometrium to the peritoneum. After 4 weeks, the rats were laparotomized and randomly assigned to 4 groups: control group; alarelin lyophilized power(LHRH Alp) group (daily subcutaneous injection); LHRH Ams group(doses of 20,100,200 μg·kg -1 ·d -1 to group 1,2,3) were administered and castration group. In addition, blood samples were collected at different times to measure serum E 2 level. RESULTS: The results showed that chronic administration of LHRH Ams for 4 weeks produced obvious inhibitory effect on the growth of endometrial explants in rats in dose dependent manner. The inhibitory effect of LHRH Ams might be equal to that of ovariotomy at a dose of 100 μg·kg -1 ·d -1 . At the same time, an obvious depression in estradiol serum level occurred, the levels was equivalent to those in diestrous rats. This inhibitory effect was associated with the reduction of serum estradiol concentration. CONCLUSION: the effect of LHRH Ams on experimental endometriosis is similar to those of LHRH Alp. LHRH Ams decrease serum E 2 level and produce obvious inhibitory effect on endometrial explants in rats, which might even be equal to that of ovariotomy.

关 键 词：丙氨瑞林 缓释微球注射剂 子宫内膜异位症 

分 类 号：R711.710.5[医药卫生—妇产科学] R977.12[医药卫生—临床医学]