Behre H M, Abshagen K, Oettel M, Hübler D, Nieschlag E
Institute of Reproductive Medicine of the University, Domagkstrasse 11, D-48129 Münster, Germany.
Eur J Endocrinol. 1999 May;140(5):414-9. doi: 10.1530/eje.0.1400414.
In the search for long-acting testosterone preparations suited for substitution therapy of hypogonadal men, testosterone undecanoate (TU) dissolved in either tea seed oil or castor oil was investigated.
In study I, 1000 mg TU in tea seed oil (125 mg/ml) were injected in equal parts into the gluteal muscles of seven hypogonadal men. In study II, 1000 mg TU in castor oil (250 mg/ml) were injected into one gluteal muscle of 14 patients.
In comparison with published data on testosterone enanthate, most widely used for i.m. injections, the kinetic profiles of both TU preparations showed extended half-lives and serum levels not exceeding the upper limit of normal. The castor oil preparation had a longer half-life than TU in tea seed oil (33.9+/-4.9 vs 20.9+/-6.0 days (mean pm S.E.M.)).
The longer half-life and the smaller injection volume make TU in castor oil a strong candidate for further applications in substitution therapy and in trials for male contraception.
为寻找适合性腺功能减退男性替代治疗的长效睾酮制剂，对溶解于茶籽油或蓖麻油中的十一酸睾酮（TU）进行了研究。
在研究I中，将1000毫克溶解于茶籽油（125毫克/毫升）中的TU等份注射到7名性腺功能减退男性的臀肌中。在研究II中，将1000毫克溶解于蓖麻油（250毫克/毫升）中的TU注射到14名患者的一侧臀肌中。
与最广泛用于肌内注射的庚酸睾酮的已发表数据相比，两种TU制剂的动力学曲线均显示半衰期延长且血清水平未超过正常上限。蓖麻油制剂的半衰期比茶籽油中的TU更长（33.9±4.9天对20.9±6.0天（平均值±标准误））。
更长的半衰期和更小的注射体积使蓖麻油中的TU成为替代治疗和男性避孕试验中进一步应用的有力候选者。
