Depot formulations

Abstract

Disclosed are formulations and related methods that comprise a non-polymeric, non-water soluble high viscosity liquid carrier material having a viscosity of at least 5,000 cP at 37° C. that does not crystallize neat under ambient or physiological conditions; a specified linear polymer comprising lactide repeat units; and one or more solvents that have a solvent capacity.

1 . A formulation comprising:
 (i) a non-polymeric, non-water soluble high viscosity liquid carrier material having a viscosity of at least 5,000 cP at 37° C. that does not crystallize neat under ambient or physiological conditions;   (ii) a linear polymer comprising lactide repeat units, wherein the linear polymer possesses a ratio R of lactide repeat units to total repeat units in the linear polymer; and   (iii) one or more solvents that have a solvent capacity;   wherein the linear polymer has a weight average molecular weight less than or equal to about 15,000 Daltons, and   wherein   (a) R satisfies the following: about 0.55≦R≦about 0.95;   (b) when R satisfies the following: about 0.55≦R≦0.85, the solvent capacity of the one or more solvents is greater than or equal to about 20%; and   (c) when R satisfies the following: greater than about 0.85 to about 0.95, the solvent capacity of the one or more solvents is greater than or equal to about 10%.   
     
     
         2 . The formulation of  claim 1 , wherein when R satisfies the following: about 0.55≦R≦0.85, the solvent capacity of the one or more solvents is greater than or equal to about 25%; and when R satisfies the following: greater than about 0.85 to about 0.95, the solvent capacity of the one or more solvents is greater than or equal to about 15%. 
     
     
         3 . The formulation of  claim 2 , wherein: wherein when R satisfies the following: about 0.55≦R≦0.85, the solvent capacity of the one or more solvents is greater than or equal to  about 35%; and when R satisfies the following: greater than about 0.85 to about 0.95, the solvent capacity of the one or more solvents is greater than or equal to about 25%. 
     
     
         4 . The formulation of  claim 1 , wherein the non-polymeric, non-water soluble high viscosity liquid carrier material having a viscosity of at least 5,000 cP at 37° C. that does not crystallize neat under ambient or physiological conditions comprises sucrose acetate isobutyrate. 
     
     
         5 . The formulation of  claim 1 , further comprising a biologically active substance. 
     
     
         6 . The formulation of  claim 5 , wherein the biologically active substance comprises an atypical antipsychotic. 
     
     
         7 . The formulation of  claim 6 , wherein the atypical antipsychotic comprises risperidone or a pharmaceutically acceptable salt or polymorph thereof. 
     
     
         8 . The formulation of  claim 1 , wherein the linear polymer comprises poly (lactide-co-glycolide). 
     
     
         9 . The formulation of  claim 1 , wherein the linear polymer is present in an amount ranging from about 1 wt % to about 45 wt %, based on the total weight of the formulation. 
     
     
         10 . The formulation of  claim 9 , wherein the linear polymer is present in an amount ranging from about 15 wt % to about 45 wt %, based on the total weight of the formulation. 
     
     
         11 . A formulation comprising:
 (i) a non-polymeric, non-water soluble high viscosity liquid carrier material having a viscosity of at least 5,000 cP at 37° C. that does not crystallize neat under ambient or physiological conditions;   (ii) a linear polymer comprising lactide repeat units, wherein the linear polymer possesses a ratio R of lactide repeat units to total repeat units in the linear polymer; and   (iii) one or more solvents that have a solvent capacity;    wherein the linear polymer has a weight average molecular weight less than or equal to about 15,000 Daltons, and   wherein:   (a) R satisfies the following: about 0.55≦R≦0.85; and   (b) the solvent capacity of the one or more solvents is greater than or equal to about 20%.   
     
     
         12 . The formulation of  claim 11 , the solvent capacity of the one or more solvents is greater than or equal to about 25%. 
     
     
         13 . The formulation of  claim 12 , the solvent capacity of the one or more solvents is greater than or equal to about 35%. 
     
     
         14 . The formulation of  claim 11 , wherein the non-polymeric, non-water soluble high viscosity liquid carrier material having a viscosity of at least 5,000 cP at 37° C. that does not crystallize neat under ambient or physiological conditions comprises sucrose acetate isobutyrate. 
     
     
         15 . The formulation of  claim 11 , further comprising a biologically active substance. 
     
     
         16 . The formulation of  claim 15 , wherein the biologically active substance comprises an atypical antipsychotic. 
     
     
         17 . The formulation of  claim 16 , wherein the atypical antipsychotic comprises risperidone or a pharmaceutically acceptable salt or polymorph thereof. 
     
     
         18 . The formulation of  claim 11 , wherein the linear polymer comprises poly (lactide-co-glycolide). 
     
     
         19 . The formulation of  claim 11 , wherein the linear polymer is present in an amount ranging from about 1 wt % to about 45 wt %, based on the total weight of the formulation.  
     
     
         20 . The formulation of  claim 19 , wherein the linear polymer is present in an amount ranging from about 15 wt % to about 45 wt %, based on the total weight of the formulation. 
     
     
         21 - 40 . (canceled)