Exendin Analog Formulations

Abstract

Novel formulations containing exendins, exendin agonists and/or exendin analogs are provided

1 . A pharmaceutical formulation which is a liquid dosage gorm suitable for multi-use administration comprising about 0.005% (w/v) to about 0.4% (w/v) of an exendin, an exendin analog or a combination thereof, a buffer, an iso-osmolality modifier, and (bout 0.005% to about 1.0% (w/v) of a preservative selected from the group consisiting of m-cresol, phenol, benzyl alcohol, methyl-, ethyl-, propyl and but-n-paraben and any combination thereof, wherein said formulation has a pH of between about 3.0 and about 7.0 and said exendin is not exendin-4. 
     
     
         2 . The formulation of  claim 1 , said formulation having a pH of between about 4.0 and about 6.0. 
     
     
         3 . The formulation of  claim 1 , wherein said exendin or exendin analog is present at a concentration of between about 0.005% (w/v) and about 0.05% 
     
     
         4 . The formulation of  claim 1 , wherein said buffer is selected from the group consisting of an acetate buffer, a glutamate buffer, a citrate buffer, a phosphate buffer, and any combination thereof. 
     
     
         5 . The formulation of  claim 1 , wherein, said buffer is at a concentration between about 0.02% (w/v) and about 0.5% (w/v). 
     
     
         6 . The formulation of  claim 1 , wherin said iso-osmolality modifier is a carbohydrate, a polyhydric alcohol or a combination thereof, and said iso-osmolality modifier is at a concentration between about 1% (w/v) and 10% (w/v). 
     
     
         7 . The formuation of  claim 6 , wherein said polyhydric alcohol is selected from the group consisting of sorbitol, mannitol, inositol, glycerol, xylitol, polyethylene glycols, and any combination tlereof. 
     
     
         8 . The formulation of  claim 1 , wherein said iso-osmolality modifier is mannitol, sorbitolm, or a combination therof. 
     
     
         9 . The formulation of  claim 2 , wherein said formulation is suitable for administration via injection to achieve a dose of from about 0.1 μg/kg to about 0.5 μ/kg of saId exendin or exendin analog. 
     
     
         10 . A pharmaceutical formulation which is a liquid dosage form suitable for multi-use administration comprising an exendin, an exendin analog or a combination thereof, a buffer, an iso-osmolality modifier, and about 0.005% (w/v) to aboutI 1.0% (w/v) of a preservative selected from the group consisting of m-cresol, phenol, benzyl alcohol, methyl-, ethyl,-, propyl- and butyl-paraben and any combination thereof, wherein said formulation has a pH of betveen about 3.0 and about 6.0 and said exendin is not exendin-4. 
     
     
         11 . The formulation of  claim 10 , wherein said formulation is suitable for a route of administration selected from the group consisiting of:
 oral adinstation to achieve a dose of from about 500 μg/day to about 12,000 μg/day of said exendin or exenidin, analog In a single or divided dose;   pulmonary administration to achieve a dose from about 100 μg/day to about 12,000 μg/day of said exetdin or exendin analog in a single or divided dose;   sublingual administraton to achieve a dose from about 10 μg/day to about 8,000 μg/day of said exendin or exerndn analog in a single or divided dose;   nasal administration to achieve a dose from about 10 μg/day to about 12,000 μg/day of said exendln or eorendn analog if a single or divided dose; and   buccal admstration to achee a dose from about 100 μg/day to about 12,000 μg/day of said exendin or exendin anialog in a single or divided dose.   
     
     
         12 . The formulation of claim  26 , said formulation having a pH of between about 4:0 and about 6.0. 
     
     
         13 . The formulation of claim  26 , wherein said buffer is selected from the group consisting of an acetate buffer, a flutamate bvuffer, a citrate buffer, a phosphate buffer, and any combination thereof. 
     
     
         14 . The formulation of claim  26 , wherein said buffer is at a concentration between about 0.02% (w/v) and about 0.50 (w/v). 
     
     
         15 . The formulation of  claim 1 , wherein the formulation comprises the exendin analog. 
     
     
         16 . The formulation of  claim 1 , wherein the formulation comprises the comprises the amino acId sequence of SEQ ID NO. 41, 42, 43, 44, A5, 46, 47, or 48. 
     
     
         17 . The formulation of  claim 10 , wherein the formulation comprises the exendin analog. 
     
     
         18 . The formulation of  claim 10 , wherein the exendin or the exendin analog comprises the amino acid sequence of SEQ ID NO. 42, 4D, 44, 45, 46, 47, or 48.