LONG-ACTING COLLOIDAL FORMULATION OF INSULIN AND PREPARATION THEREOF,申请号WO2007EP00335-传众专利搜索

LONG-ACTING COLLOIDAL FORMULATION OF INSULIN AND PREPARATION THEREOF

申请公布号：WO2007082712(A1)

申请号：WO2007EP00335

申请日期：2007.01.16

申请公布日期：2007.07.26

申请人：

FLAMEL TECHNOLOGIES;CONSTANCIS, ALAIN;DURACHER, DAVID;SOULA, OLIVIER;BRYSON, NATHAN

发明人：CONSTANCIS, ALAIN;DURACHER, DAVID;SOULA, OLIVIER;BRYSON, NATHAN

分类号：A61K9/51;A61K38/28;A61K47/02;A61K47/34;A61P3/10

主分类号：A61K9/51

摘要：<p>The invention relates to injectable long-acting insulin formulations for the treatment of type I and II diabetes in humans and animals. The essential objective of the invention is to provide a long-acting insulin formulation in the form of a colloidal suspension: which makes it possible to readily fill a syringe through a small-diameter needle (for example, of 29G, 30G or 31G gauge) and/or which is readily injectable through a small-diameter needle (for example, of 29G, 30G or 31G gauge), without harming the therapeutic efficacy of the insulin. To achieve this objective, the invention relates to an aqueous and stable colloidal formulation of nanoparticles of at least one poly(Leu-bloc-Glu), loaded with insulin, in which the pH is such that: 6.0 = pH = 7.0, characterized in that it comprises at least one magnesium salt in an amount such that: the osmolarity Osm (in mOsmol) is such that: 270 = Osm = 600, the viscosity v (in mPa.s), measured according to a procedure Mv, is such that: v = 15, preferably v = 10, and even more preferably v = 5; the concentration (in mg/ml) of poly(Leu-bloc-Glu) is between 30 and 70, preferably between 38 and 65.</p>