Frey H, Aakvaag A, Saanum D, Falch J
Eur J Clin Pharmacol. 1979 Nov;16(5):345-9. doi: 10.1007/BF00605634.
Twenty-six male volunteers received a single oral dose of testosterone as free crystals or as the undecanoate ester. The latter was given either in crystalline form or in arachis oil. All preparations were tested three times in the same individual, whilst fasting on 2 days and on one day together with a breakfast rich in fat. Serum testosterone concentration was measured at intervals for up to 6--24 h after the dose. A significant and reproducible rise in serum testosterone level was found after ingestion of free testosterone. Testosterone esterified with undecylenic acid was only effective when administered in arachis oil. The meal increased the bioavailability of the ester, but had hardly any effect on that of the free hormone. It is concluded that bioavailability of oral testosterone can be improved by pharmaceutical means to an extent sufficient to produce adequate blood levels in substitution therapy.
26名男性志愿者接受了单次口服剂量的睾酮，形式为游离晶体或十一烷酸酯。后者以结晶形式或花生油溶液形式给药。所有制剂均在同一个体中测试三次，其中两次测试时禁食，另一次测试时搭配富含脂肪的早餐。给药后长达6至24小时内定期测量血清睾酮浓度。摄入游离睾酮后，血清睾酮水平出现了显著且可重复的升高。与十一烯酸酯化的睾酮只有在花生油溶液中给药时才有效。食物增加了酯的生物利用度，但对游离激素的生物利用度几乎没有影响。得出的结论是，口服睾酮的生物利用度可以通过药物手段提高到足以在替代治疗中产生足够血药浓度的程度。
