摘要
醋酸亮丙瑞林是视丘下部所产生的黄体生成激素释放激素(LHRH)的高活性衍生物,为合成的两端封闭的水溶性九肽。它可以刺激垂体分泌促性腺激素,诱发生殖器官生成类固醇,长期大量使用会使LHRH受体脱敏,抑制促性腺激素的分泌以及睾丸或卵巢甾类的生成,临床上用来治疗或缓解多种性激素依赖性疾病如前列腺癌、子宫内膜异位症、子宫肌瘤、中枢性性早熟等。但是醋酸亮丙瑞林不易透过生物膜,在胃肠道中不稳定,易被消化酶降解,口服、鼻腔、直肠、阴道途径给药生物利用度极低,所以目前人们针对醋酸亮丙瑞林的非胃肠道给药途径的制剂进行了广泛的研究,有些已经成功开发为上市药品。本文主要就醋酸亮丙瑞林的临床应用及其制剂的研究情况进行综述。
Leuprorelin acetate, an analogue of the luteinizing hormone-releasing hormone （LHRH） with high bioactivities, is a synthesized nona-pcptide which can stimulate the pituitary releasing gonadotropin and induce reproductive organs producing steroids. Long-term use of lueprolide acetate can bring on LHRH-receptor desensitization and decrease the gonadal hormone level. Thus, it is used to cure or relief the symptoms of prostate cancer, endometriosis and so on. Because of poor biomembrane permeation ability, the parenteral delivery syestem of this drug is concerned and has been studied widely. The current research of the clinical application and the drug delivery system of leuprolide acetate is reviewed.
出处
《药学与临床研究》
2009年第4期309-315,共7页
Pharmaceutical and Clinical Research
基金
国家科技支撑计划(2008BA155B03)
关键词
醋酸亮丙瑞林
缓释
微球
原位成形
前列腺癌
Leuprolide acetate
Sustained release
Microspheres
In situ forming
Prostate cancer
