PHARMACEUTICAL FORMULATION FOR DELIVERY OF RECEPTOR TYROSINE KINASE INHIBITING (RTKi) COMPOUNDS TO THE EYE
    1.
    发明申请
    PHARMACEUTICAL FORMULATION FOR DELIVERY OF RECEPTOR TYROSINE KINASE INHIBITING (RTKi) COMPOUNDS TO THE EYE 审中-公开
    用于将受体酪氨酸激酶抑制(RTKi)化合物递送至眼睛的药物制剂

    公开(公告)号:US20070173538A1

    公开(公告)日:2007-07-26

    申请号:US11613257

    申请日:2006-12-20

    IPC分类号: A61K31/416 A61K31/08

    摘要: The present invention relates to development of efficacious pharmaceutical compositions comprising a poorly water soluble active compound in a therapeutically effective amount and a co-solvent in a suitable amount to treat or prevent diseases due to ocular neovascularization and enhanced vascular permeability. In preferred aspects the composition is in the form of a gel.

    摘要翻译: 本发明涉及有效药物组合物的开发,其包含治疗有效量的难溶于水的活性化合物和适量的助溶剂,以治疗或预防由于眼新生血管形成和增强的血管通透性引起的疾病。 在优选的方面,组合物是凝胶的形式。

    PHARMACEUTICAL FORMULATION FOR DELIVERY OF RECEPTOR TYROSINE KINASE INHIBITING (RTKi) COMPOUNDS TO THE EYE
    6.
    发明申请
    PHARMACEUTICAL FORMULATION FOR DELIVERY OF RECEPTOR TYROSINE KINASE INHIBITING (RTKi) COMPOUNDS TO THE EYE 审中-公开
    用于将受体酪氨酸激酶抑制(RTKi)化合物递送至眼睛的药物制剂

    公开(公告)号:US20070149593A1

    公开(公告)日:2007-06-28

    申请号:US11612744

    申请日:2006-12-19

    IPC分类号: A61K31/416 A61K31/08

    摘要: The present invention relates to development of efficacious intravitreal pharmaceutical compositions comprising a poorly water soluble agent with anti-angiogenic and/or anti vascular leakage properties in a therapeutically effective amount and a co-solvent in a suitable amount to treat or prevent diseases due to ocular neovascularization and enhanced vascular permeability. Other aspects of the invention details the development of efficacious compositions for the treatment of the said diseases via periocular, topical and oral administration.

    摘要翻译: 本发明涉及有效的玻璃体内药物组合物的开发,其包含治疗有效量的具有抗血管生成和/或抗血管渗透性能的水溶性差的药剂,以及适当量的用于治疗或预防由于眼睛引起的疾病的共溶剂 新血管形成和血管通透性增强。 本发明的其它方面详细描述了通过眼周,局部和口服给药治疗所述疾病的有效组合物的发展。

    SELF PRESERVED AQUEOUS PHARMACEUTICAL COMPOSITIONS
    8.
    发明申请
    SELF PRESERVED AQUEOUS PHARMACEUTICAL COMPOSITIONS 有权
    自我保留的水性药物组合物

    公开(公告)号:US20080075790A1

    公开(公告)日:2008-03-27

    申请号:US11858781

    申请日:2007-09-20

    IPC分类号: A61K33/30 A61P27/02

    摘要: The present invention is directed to the provision of multi-dose, self-preserved ophthalmic compositions. The compositions possess sufficient antimicrobial activity to satisfy USP preservative efficacy requirements, as well as similar preservative standards (e.g., EP and JP), without requiring the presence of conventional anti-microbial preservative agents, such as benzalkonium chloride. The compositions are effectively preserved by a balanced ionic buffer system containing zinc ions at a concentration of 0.04 to 0.9 mM, preferably 0.04 to 0.4 mM. One aspect of the balanced buffer system is limitation of the amount of buffering anions present to a concentration of 15 mM or less, preferably 5 mM or less. In a preferred embodiment, the compositions also contain borate or, most preferably, one or more borate/polyol complexes. The use of propylene glycol as the polyol in such complexes is strongly preferred. Limiting the amount of divalent metals other than zinc and the amount of ionized salts present has also been determined to be important to maximize the antimicrobial activity of the balanced buffer systems.

    摘要翻译: 本发明涉及提供多剂量,自我保存的眼用组合物。 组合物具有足够的抗微生物活性以满足USP防腐功效要求,以及类似的防腐标准品(例如EP和JP),而不需要存在常规的抗微生物防腐剂,例如苯扎氯铵。 通过含有浓度为0.04至0.9mM,优选0.04至0.4mM的锌离子的平衡离子缓冲系统有效地保护了组合物。 平衡缓冲系统的一个方面是存在的缓冲剂阴离子的量的限制为15mM或更低,优选5mM或更低的浓度。 在优选的实施方案中,组合物还含有硼酸盐或最优选一种或多种硼酸盐/多元醇络合物。 在这种络合物中使用丙二醇作为多元醇是非常优选的。 限制锌以外的二价金属的量和存在的离子盐的量也被确定为使平衡缓冲体系的抗菌活性最大化是重要的。