Schürmeyer T, Wickings E J, Freischem C W, Nieschlag E
Acta Endocrinol (Copenh). 1983 Mar;102(3):456-62. doi: 10.1530/acta.0.1020456.
Since saliva testosterone reflects the testosterone fraction available to target tissues the therapeutic effectiveness of orally administered testosterone undecanoate was assessed by measuring testosterone in serum and saliva. Matched saliva and serum samples were obtained from 12 normal men and 8 hypogonadal men before and at hourly intervals after the oral administration of 120 mg testosterone undecanoate. The test was repeated in 3 men after they had taken 40 mg testosterone undecanoate twice daily for 4 to 5 weeks. Following testosterone undecanoate administration serum and saliva testosterone always showed parallel increases. However, the absorption curves showed a high interindividual variability in the time when maximum concentrations were reached, as well as in the maximum levels themselves. The increases in serum and saliva testosterone were similar in normal and hypogonadal men. In normal men basal levels were reached 4 h after the maximum had occurred, while in hypogonadal men testosterone levels were not different from basal levels 2 h after the maximum. The study shows that testosterone undecanoate is well absorbed from the gut and releases significantly elevated amounts of testosterone which is available to target tissues. As the absorption pattern was always parallel in both fluids, hydrolysis of the circulating testosterone ester by the tissue itself seems to effect no additional increase of testosterone in the tissue.
由于唾液睾酮反映了靶组织可利用的睾酮部分，因此通过测量血清和唾液中的睾酮来评估口服十一酸睾酮的治疗效果。在12名正常男性和8名性腺功能减退男性口服120mg十一酸睾酮之前及之后，每隔一小时采集配对的唾液和血清样本。在3名男性每天两次服用40mg十一酸睾酮，持续4至5周后重复该试验。服用十一酸睾酮后，血清和唾液睾酮始终呈平行升高。然而，吸收曲线显示，达到最大浓度的时间以及最大浓度本身存在高度个体间差异。正常男性和性腺功能减退男性的血清和唾液睾酮升高情况相似。在正常男性中，最大值出现后4小时达到基础水平，而在性腺功能减退男性中，最大值出现后2小时睾酮水平与基础水平无差异。该研究表明，十一酸睾酮从肠道吸收良好，释放出显著升高的可被靶组织利用的睾酮量。由于两种体液中的吸收模式始终平行，循环中的睾酮酯被组织自身水解似乎不会导致组织中睾酮的额外增加。
