A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.
一种用于给药的制剂,通过与
甾醇和/或
甾醇酯配制,可增强对亲脂性治疗剂的溶解度、稳定性、吸收、代谢和/或药代动力学特征的调节,从而提高给需要此类治疗剂的受试者施用的治疗剂的
生物利用度。制剂中含有一种治疗剂和一种
甾醇或
甾醇酯,还可选择进一步含有
增溶剂和/或增强剂。此外,还描述了含有这些制剂的药物组合物以及制剂和药物组合物的制造方法和使用方法。当治疗剂包括
睾酮或
睾酮酯时,本公开的制剂可用于最大限度地减少双氢
睾酮的合成。