AQUEOUS ORAL SOLUTIONS OF STEROID HORMONES AND HYDROXYPROPYL-BETA-CYCLODEXTRIN WITH OPTIMISED BIOAVAILABILITY
    2.
    发明申请
    AQUEOUS ORAL SOLUTIONS OF STEROID HORMONES AND HYDROXYPROPYL-BETA-CYCLODEXTRIN WITH OPTIMISED BIOAVAILABILITY 审中-公开
    具有优化生物利用度的甾体激素和羟丙基-β-环糊精的水溶性口服溶液

    公开(公告)号:WO2014082724A1

    公开(公告)日:2014-06-05

    申请号:PCT/EP2013/003538

    申请日:2013-11-22

    Applicant: ALTERGON S.A.

    Abstract: The present invention concerns the preparation and the therapeutic use of aqueous solutions of Progesterone or Testosterone, complexed with hydroxypropyl-3-cyclodextrin (HPβCD) that are suitable for oral administration. The solutions are characterised by a specific molar ratio between HPβCD and the hormones such as to ensure high hormone plasma levels, following oral administration, thanks to the optimisation of their solubility, permeability, metabolic stability and ultimately, bio availability. The formulation object of the present patent makes it possible to achieve effective plasma concentrations following oral administration of lower doses of hormone with respect to oral formulations currently on the market (e.g. Prometrium, Andriol) to the advantage of greater safety and compliance of the patients.

    Abstract translation: 本发明涉及与适用于口服给药的羟丙基-3-环糊精(HP&bgr; CD)络合的孕酮或睾酮水溶液的制备和治疗用途。 通过优化其溶解性,渗透性,代谢稳定性以及最终的生物可利用性,这些溶液的特征在于HP和bgr.CD与激素之间的特定摩尔比,例如口服给药后确保高激素血浆水平。 本发明的制剂目的使得有可能在目前市售的口服制剂(例如,Prometrium,Andriol)口服给予较低剂量的激素之后实现有效的血浆浓度,从而具有更好的患者安全性和顺应性的优点。

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