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    • 17. 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。
    • 20. 发明授权
    • Long-acting oxytocin analogues for the treatment and prevention of breast cancer and psychiatric disorders
    • 长效催产素类似物用于治疗和预防乳腺癌和精神疾病
    • US06894026B1
    • 2005-05-17
    • US09678591
    • 2000-10-03
    • Steven C. Quay
    • Steven C. Quay
    • A61K31/395A61K38/00
    • A61K31/395
    • Methods and compositions are provided for prophylaxis and treatment of breast cancer involving administration of a therapeutically effective amount of carbetocin and/or other long-acting oxytocin analogues. 1-Butanoic acid-2-(O-methyl-L-tyrosine)-1-carbaoxytocin (carbetocin) and/or other long-acting oxytocin analogues are formulated with a pharmaceutically acceptable carrier and administered in an amount sufficient to inhibit initiation or growth of breast cancer in the patient. The carbetocin and/or other long-acting oxytocin analogues may also be formulated with a pharmaceutically acceptable carrier and administered in an amount sufficient to treat, prevent or alleviate the symptoms of a psychiatric disorder in the patient. Carbetocin may be administered prophylactically or to treat existing conditions in patients by a variety of administration modes, including intramuscular, intravenous, intranasal, intrapulmonary, subcutaneous, parenteral, oral, or transdermal delivery methods and formulations. Preferably, the carbetocin is administered to a mucosal surface of the patient via intranasal delivery. For this purpose, pharmaceutical compositions are provided for intranasal delivery that incorporate carbetocin in a powder or aqueous formulation for intranasal delivery.
    • 提供了用于预防和治疗乳腺癌的方法和组合物,其涉及施用治疗有效量的卡贝缩丁和/或其它长效催产素类似物。 使用药学上可接受的载体配制1-丁酸-2-(O-甲基-L-酪氨酸)-1-氨基羰基(卡贝肝素)和/或其它长效催产素类似物,并以足以抑制起始或生长的量施用 的乳腺癌患者。 还可以用药学上可接受的载体配制卡贝缩丁酯和/或其它长效催产素类似物,并以足以治疗,预防或减轻患者精神障碍症状的量施用。 卡培西可以预防性施用或通过各种施用方式治疗患者的现有病症,包括肌肉内,静脉内,鼻内,肺内,皮下,胃肠外,口服或透皮递送方法和制剂。 优选地,通过鼻内递送将卡贝缩is物施用于患者的粘膜表面。 为此目的,提供药物组合物用于鼻内递送,其中将卡贝缩胆胺掺入粉末或水性制剂用于鼻内递送。