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    • 5. 发明申请
    • Parenteral and oral formulations of benzimidazoles
    • 苯并咪唑的肠胃外和口服制剂
    • US20080293796A1
    • 2008-11-27
    • US12220364
    • 2008-07-24
    • Diana Shu-Lian ChowPranav GuptaYulan QiJaymin ShahPeter Wisniecki
    • Diana Shu-Lian ChowPranav GuptaYulan QiJaymin ShahPeter Wisniecki
    • A61K31/4184A61P35/00
    • A61K9/0019A61K9/0095A61K9/1075A61K31/4184
    • Provided herein are drug delivery systems comprising nanosuspension formulations suitable for parenteral delivery to a subject. The nanosuspension formulations may comprise a benzimidazole derivative, e.g., mebendazole, and surface stabilizers, such as block copolymer(s), e.g., Pluronic F108, and surfactant(s), e.g., Tween 80, and, optionally, water. Provided are methods for defining nanosuspensions of a benzimidazole derivative as having maximum therapeutic efficacy for a treatment regimen by adjusting and/or selecting particles size(s) based on pharmacokinetic parameters of the derivative in the tissue. Also provided are methods for improving the bioavailability of a benzimidazole derivative during treatment of a pathophysiological condition and for treating a cancer by using formulation(s) combining particle diameters whereby the retention of the benzimidazole derivative within the particles increases as the diameter increases such that, upon administration, release of the benzimidazole derivative from the particles into tissue is continuous over a range of time as determined by the particle diameters.
    • 本文提供的药物递送系统包括适于肠胃外递送给个体的纳米悬浮制剂。 纳米悬浮液制剂可以包含苯并咪唑衍生物,例如甲苯咪唑和表面稳定剂,例如嵌段共聚物,例如Pluronic F108和表面活性剂,例如吐温80和任选的水。 提供了通过基于组织中衍生物的药代动力学参数调节和/或选择颗粒大小来定义苯并咪唑衍生物的纳米悬浮液对于治疗方案具有最大治疗功效的方法。 还提供了用于在治疗病理生理状况期间改善苯并咪唑衍生物的生物利用度和通过使用结合粒径的配方治疗癌症的方法,由此直径增加时,颗粒内苯并咪唑衍生物的保留增加, 在施用时,将苯并咪唑衍生物从颗粒中释放到组织中在由颗粒直径确定的时间范围内是连续的。