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    • 9. 发明申请
    • INTRAVENOUS FORMULATIONS OF COENZYME Q10 (COQ10) AND METHODS OF USE THEREOF
    • COENZYME Q10(COQ10)的内在配方及其使用方法
    • WO2011112900A2
    • 2011-09-15
    • PCT/US2011028042
    • 2011-03-11
    • CYTOTECH LABS LLCNARAIN NIVEN RAJINMCCOOK JOHN PATRICK
    • NARAIN NIVEN RAJINMCCOOK JOHN PATRICK
    • A61K9/127A61K9/107A61K31/122A61K47/30A61P35/00
    • A61K31/122A61K9/0019A61K9/10A61K47/24A61K47/34
    • Disclosed herein are formulations suitable for parenteral administration of certain hydrophobic active agents such as Coenzyme Q10. Methods of preparing the same and methods of treatment of oncological disorders using the same are also provided herein. The formulations comprise an aqueous solution; a hydrophobic active agent dispersed to form a colloidal nano-dispersion of particles; and at least one of a dispersion stabilizing agent and an opsonization reducer wherein the colloidal nano-dispersion of the active agent is dispersed into nano-dispersion particles having a mean size of less than 200-nm. Methods of preparing the parenteral formulations comprise dispersing the hydrophobic active agent by high pressure homogenization by (1) adding hydrophobic active agent to a 65°C bath of water and mixing to form a hydrophobic active agent/water mixture; (2) adding a dispersion stabilizing agent to the hydrophobic active agent/water mixture and mix at 65°C to form a hydrophobic active agent/water/stabilizer mixture; (3) adding an opsonization reducer to form a hydrophobic active agent/water/stabilizer/reducer mixture; (4) pre-heating a Microfluidizer to 65°C; and (5) processing by mixing the hydrophobic active agent/water/stabilizer/reducer mixture in the Microfluidizer at 65°C such that a hydrophobic active agent colloidal nano-dispersion having a mean particle size less than 200-nm is formed. Provided herein are also methods of treating oncological disorders by administering formulations described herein to a subject such that treatment or prevention of the oncological disorder occurs.
    • 本文公开了适用于胃肠外施用某些疏水活性剂如辅酶Q10的制剂。 本发明还提供了制备方法和使用其的肿瘤疾病治疗方法。 制剂包含水溶液; 分散以形成粒子的胶态纳米分散体的疏水性活性剂; 和分散稳定剂和调理剂还原剂中的至少一种,其中活性剂的胶体纳米分散体分散在平均粒度小于200nm的纳米分散体颗粒中。 制备肠胃外制剂的方法包括通过(1)向65℃的水浴中加入疏水活性剂并混合以形成疏水活性剂/水混合物,通过高压均质分散疏水活性剂; (2)向疏水活性剂/水混合物中加入分散稳定剂,并在65℃下混合形成疏水活性剂/水/稳定剂混合物; (3)加入调理剂还原剂以形成疏水活性剂/水/稳定剂/还原剂混合物; (4)将微流化器预热至65℃; 和(5)通过将微流化剂中的疏水性活性剂/水/稳定剂/还原剂混合物在65℃下混合进行处理,从而形成平均粒度小于200nm的疏水性活性剂胶体纳米分散体。 本文还提供了通过将本文所述的制剂施用于受试者来治疗肿瘤疾病的方法,使得发生肿瘤病症的治疗或预防。