盐酸异丙嗪的阴道杀精避孕作用及其作用机理的研究

EXPERIMENTAL STUDY OF INTRAVAGINAL CONTRACEPTIVE EFFECT OF PROMETHAZINI HYDROCHLORIDUM AND ITS SPERMATICIDAL MECHANISM

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。

To evaluate the intravaginal contraceptive effect of promethazini hydrochloridum and its spermaticidal mechanism. Methods: Promethazini hydrochloridum solutions were injected intravaginally to nonpregnant hamsters before copulation. All animals were killed ten days after postinsemination and the number of the pregnant hamsters was examined. The spermaticidal mechanism of promethazini hydrochloridum was explored by sperm-tail hypo-osmotic swelling test method and transmission electron microscopy. Results: The anti fertility was 100% with 1 % promethazini hydrochloridum and 67% with 0. 5% promethazini hydrochloridum, showing a significant decrease (P<0. 01 ). The sperm-tail hypo-osmotic swelling test suggested that the percentage of the live spermatozoa and the sperm-tail hypo-osmotic swelling was decreased after the treatment with promethazini hydrochloridum for 1 min, indicating a good correlation(r=0. 92). The death of the spermatozoa caused by promethazini hydrochloridum is probably due to the injury of the sperm membrane function. \ observation demonstrated that the plasma membrane, mitochondria and the acrosome of sperm were damaged. Conclusion: Promethazini hydrochloridum has a significant intravaginal contraceptive effect and its main target structures of spermacidal effect existed in the biological membrane system of sperm.