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    • 10. 发明申请
    • Cyanocobalamin low viscosity aqueous formulations for intranasal delivery
    • 用于鼻内给药的氰钴胺素低粘度含水制剂
    • US20080182817A1
    • 2008-07-31
    • US12079875
    • 2008-03-27
    • Steven C. QuayPeter C. AprileZenaida O. GoAnthony P. Sileno
    • Steven C. QuayPeter C. AprileZenaida O. GoAnthony P. Sileno
    • A61K31/7056A61P43/00
    • A61K9/0043A61K9/08A61K31/7056A61K31/714A61K47/10A61K47/12A61K47/186
    • A stable pharmaceutical mercury-free aqueous solution of cyanocobalamin comprised of cyanocobalamin and water wherein said solution of cyanocobalamin is suitable for intranasal administration, has a viscosity less than about 1000 cPs, and wherein said solution of cyanocobalamin has a bioavailability of cyanocobalamin when administered intranasally of at least about 7% relative to an intramuscular injection of cyanocobalamin with the proviso that the solution is essentially free of mercury and mercury-containing compounds. The present invention is also directed towards a method for elevating the vitamin B12 levels in the cerebral spinal fluid (CSF) comprising administering intranasally a sufficient amount of a mercury-free cyanocobalamin solution so as to increase the average ratio of vitamin B12 in the CSF to that in the blood serum (B12 CSF/B12 Serum×100) to at least about 1.1 comprising intranasally administering an aqueous solution of a cyanocobalamin, wherein said solution of cyanocobalamin has a bioavailability of at least 7% relative to an intramuscular injection of a cyanocobalamin.
    • 一种由氰钴胺素和水组成的稳定的药用无汞水溶液,其中所述氰钴胺溶液适合于鼻内给药,其粘度小于约1000cPs,其中所述氰钴胺溶液在鼻内给药时具有氰钴胺素的生物利用度 相对于肌内注射氰钴胺素至少约7%,条件是溶液基本上不含汞和含汞化合物。 本发明还涉及提高脑脊髓液(CSF)中维生素B12水平的方法,其包括向鼻内施用足够量的无汞氰钴胺溶液,以增加CSF中维生素B12的平均比例 在血清中(B12 CSF / B12 Serumx100)至少约1.1,包括鼻内施用氰钴胺水溶液,其中所述氰钴胺溶液相对于肌内注射氰钴胺素具有至少7%的生物利用度。