雌二醇是女性化激素治疗中主要的雌激素来源；针对不同用药途径，业已有了相应形态。最常见的形态包括口服片、舌下含服片剂、透皮剂以及注射剂。在许多国家（例如欧洲大部分地区），雌二醇注射剂已停产，因此无法用于女性化激素治疗 <sup>([Glintborg et al., 2021][G21])</sup>；然而，不少女性倾向跨性别者仍在使用，尤其在美国和自行用药（DIY）的群体中。常用的注射剂包括：戊酸雌二醇（EV）、环戊丙酸雌二醇（EC）和庚酸雌二醇（EEn），皆为油溶液。注射剂相较其它雌二醇形态，具有以下特点：更低的开销、更容易达到高雌二醇浓度以便压制睾酮的能力、更少的用药频率、以及理论上更小的健康风险（相对口服同等剂量而言，例如可避免肝脏首过效应）；这些特点使得其在女性化激素治疗当中广受欢迎。注射带来的高雌二醇浓度对于单服雌二醇疗法也大有裨益：这避免了抗雄制剂的使用。
不幸的是，以上数据的质量特别低：不仅样本数少，而且雌二醇水平差别明显。此外，尽管 EU 的持续时间长达数月，但上述项目仅跟踪了注射后两周内的数据。因此，无法基于这些数据为 EU 拟合一个相对准确的曲线——而是基于一种提议，即 EU 的雌二醇浓度曲线下面积约为其它非聚合物雌二醇酯的三分之一。另外还存在少量的多次注射数据，但其无法被整合<sup>([Jacobi & Altwein, 1979][JA79], [表格][TABLE_36A]; [Jacobi et al., 1980][J80], [表格][TABLE_36B]; [Derra, 1981][D81], [表格][TABLE_36C])</sup>。经处理的源数据与拟合曲线见图 6。
<sectionclass="box">
![figure][FIG_6]
**图 6**：已发表的、单次肌注 EU 油溶液之后 90 日内的雌二醇浓度—时间曲线，及源数据的拟合曲线（加粗黑/白线）。曲线已依内源性分泌量进行修正、并调整摄入量为 50mg，以与分室药代动力学模型相契合。源数据在他处亦有提供<sup>([Google 文档][WEB_36A]; [Plotly 表格][WEB_36B])</sup>。
</section>
### 聚磷酸雌二醇（PEP） {#polyestradiol-phosphate}
PEP 主要用于前列腺癌的治疗，但也见于其它需要雌激素的临床治疗当中（包括乳腺癌治疗、更年期激素疗法）。其曾被广泛使用，近来似乎已然停产。此处找到了来自 11 篇著述（表 8）的 114 人次注射的数据，均以患有前列腺癌的男性为对象。
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