| 摘要 |
<p>The present invention provides oligomers of phosphorylated insulin and formulations thereof. The oligomeric derivatives of the invention exhibit pharmacodynamic properties that are significantly improved over native insulin or other intermediate-acting or basal insulins, for example NPH, Lantus or Detemir, in that they demonstrate a 4-fold higher therapeutic index and a 4-fold lower risk of hypoglycemia. The invention provides the advantage of protracted glycemic lowering and combines it with the advantage of reduced hypoglycaemic risk. The above is not a property of any presently-known or available basal or intermediate-acting insulin. In a further embodiment of the invention, formulations of oligomeric phosphorylated insulin are suitable for all routes of administration including inhalation, buccal absorption, subcutaneous injection, infusion or other technically proven routes for insulin administration. The invention additionally provides the advantage of a longer-acting formulation for inhalation between meals and at bedtime. Such longer-acting inhalable formulations are not presently available.</p> |
