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    • 10. 发明授权
    • Pharmaceutical formulations of corticotropin releasing factor having
improved stability in liquid form
    • 具有改善液体稳定性的促肾上腺皮质激素释放因子的药物制剂
    • US5780431A
    • 1998-07-14
    • US717306
    • 1996-09-20
    • Bert HoBehzad KhosroviPamela G. Hirtzer
    • Bert HoBehzad KhosroviPamela G. Hirtzer
    • A61K38/04A61K38/22A61K47/10A61K47/12A61K47/18A61K47/26A61P29/00A61K38/35A61K38/00C07K14/575
    • A61K47/12A61K38/2228A61K47/10A61K47/18A61K47/26A61K9/0019
    • The present invention relates to novel formulations of corticotropin releasing factor (CRF) having improved stability during storage over extended periods of time as liquids, which retain significant pharmaceutical activity during such storage and/or which are physiologically compatible. The formulations of the present invention comprise (a) a pharmaceutically effective concentration of CRF, (b) a buffer to maintain the pH of the formulation between about 2.0 to about 5.0 or about 6.0 to about 9.0 when in liquid form and (c) an alcohol such as mannitol, sorbitol, methanol, glycerol, or the like. Other aspects of the present invention involve addition of various other components to the formulations described herein for the purpose of decreasing the rate of degradation of the CRF peptide or increasing its solubility in solution. Finally, the present invention is further directed to methods for preparing such novel pharmaceutical formulations of CRF and methods of using those formulations to reduce inflammation and edema in mammals.
    • 本发明涉及促血管激素释放因子(CRF)的新制剂,其在作为液体的长时间储存​​期间具有改善的稳定性,其在这种储存期间保持显着的药物活性和/或与其生理相容。 本发明的制剂包含(a)药物有效浓度的CRF,(b)当液体形式时,将制剂的pH维持在约2.0至约5.0或约6.0至约9.0之间的缓冲剂,和(c) 醇如甘露醇,山梨糖醇,甲醇,甘油等。 本发明的其它方面涉及为了降低CRF肽的降解速率或增加其在溶液中的溶解度的目的,向本文所述的制剂中加入各种其它组分。 最后,本发明进一步涉及制备这种新型CRF药物制剂的方法以及使用这些制剂减少哺乳动物炎症和水肿的方法。