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目的研究睾酮经皮吸收制剂的有效性、安全性及稳定性,即新药临床前试验。方法将睾酮制成软膏剂,对睾酮软膏进行动物药效学、毒理试验(局部刺激试验、皮肤过敏试验、急性毒性试验)。结果睾酮经皮吸收制剂可显著增加去势未成年雄性大鼠的前列腺和精囊重量,显著提高去势大鼠血浆睾酮水平;动物毒理试验表明该制剂对家兔脱毛后完整皮肤,破损皮肤无刺激性,对豚鼠皮肤无致敏作用,给大鼠皮肤涂抹该制剂达人用量300倍时无皮肤急性毒性反应,给小鼠灌喂该制剂最大耐受量达人用量4300倍以上,表明该制剂安全无毒。结论所研制的睾酮经皮吸收制剂能有效提高大鼠血浆睾酮水平,在靶器官表达出雄激素效应,并且具有良好的安全性。
Objective To study the efficacy, safety and stability of testosterone percutaneous absorption preparations, ie, the preclinical test of new drugs. Methods Testosterone was made into an ointment, and the testosterone ointment was subjected to animal pharmacodynamics and toxicological tests (local irritation test, skin allergy test and acute toxicity test). Results Testosterone percutaneous absorption preparations can significantly increase the prostate and seminal vesicle weight in ovariectomized male rats and significantly increase the level of plasma testosterone in ovariectomized rats. The animal toxicological tests show that the preparations have no effect on intact skin, damaged skin, Irritating to guinea pig skin no sensitizing effect to the rat skin smear the preparation up to 300 times the dosage of no acute skin reaction, the mice were fed with the maximum tolerated dose of 4300 times the dosage of more than that, The preparation is safe and non-toxic. Conclusion The testosterone transdermal absorption preparation developed can effectively improve the level of plasma testosterone in rats and express the androgen effect in the target organs with good safety.