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目的:评价盐酸异丙嗪的阴道避孕(抗生育)作用及其杀精作用机理。方法:选用未经产雌性金黄地鼠,于交配前阴道内注入盐酸异丙嗪溶液,交配后第10 d剖腹检查妊娠动物数;采用精子尾低渗肿胀试验法和透射电镜观察技术探讨药物的杀精机理。结果:1%浓度的药物组抗生育率达100%,0.5%浓度药物组的抗生育率为67%,明显少于对照组,差异显著(P<0.01)。精子尾低渗肿胀实验显示,不同浓度的药物作用于人精子1min后,存活精子百分率及精子尾低渗肿胀百分率均降低,二者具正相关性(r=0.92),说明盐酸异丙嗪对精子膜功能有破坏作用。透射电镜观察结果表明,该药主要破坏精子的质膜,线粒体内膜及顶体等结构。结论:盐酸异丙嗪对金黄地鼠有明显的阴道杀精避孕作用,其杀精作用的主要靶结构在精子的生物膜系统。
Objective: To evaluate the effect of vaginal contraception (anti-fertility) of promethazine hydrochloride and its spermicidal mechanism. Methods: The non-pregnant female golden hamster was injected intravaginally with promethazine hydrochloride solution before mating, and the number of pregnant animals was examined by laparotomy on the 10th day after mating. The sperm end hypotonic swelling test and transmission electron microscope Spermicidal mechanism. Results: The anti-fertility rate was 100% in the 1% drug group and 67% in the 0.5% drug group, which was significantly lower than that in the control group (P <0.01). Sperm tail hypotonic swelling experiments showed that different concentrations of drugs on human sperm 1min, the percentage of surviving sperm and sperm tail hypoosmotic swelling rate decreased, both with a positive correlation (r = 0.92), indicating that isoprolone hydrochloride Srazine has a damaging effect on sperm membrane function. Transmission electron microscopy showed that the drug mainly destroyed the sperm plasma membrane, mitochondrial inner membrane and acrosome structures. CONCLUSION: Promethazine hydrochloride has obvious vaginal spermicidal contraceptive effect on golden hamster, and the main target structure of its spermicidal effect is in sperm biofilm system.