|Title:||Formulation for lipophilic agents|
|Abstract:||The invention relates to pharmaceutical formulations of lipophilic therapeutic agents in which such agents are solubilized in largely aqueous vehicles, and processes for preparing and using the same.|
|Inventor(s):||Mazess; Richard B. (Madison, WI), Driscoll; Jeffrey W. (Middleton, WI), Goldensoph; Creighton Reed (DeForest, WI), LeVan; Leon W. (Oregon, WI)|
|Assignee:||Genzyme Corporation (Cambridge, MA)|
1. A parenteral formulation, comprising a lipophilic drug which is doxercalciferol, a non-ionic solubilizer which is polysorbate 20 present at a concentration of about
0.05% to about 5% w/w, a lipophilic antioxidant which is butylated hydroxytoluene (BHT) present at a concentration of about 20 to about 2000 ppm, an optional agent which is ethanol present at a concentration of 0 to 30% w/w, and an aqueous vehicle.
2. A formulation as set forth in claim 1, wherein the optional agent is present in a concentration of 0% to about 10% w/w.
3. A formulalion as set forth in claim 1, wherein the optional agent is present in a concentration of about 1% to about 3% w/w.
4. A formulation as set forth in claim 1, wherein the non-ionic solubilizer includes 0.5% 2.5% w/w polysorbate 20, the lipophilic antioxidant includes 20 ppm BHT and the optional agent includes 2.5% w/w ethanol.
5. A formulation as set forth in claim 1, wherein the doxercalciferol is present at a concentration of 2 10 .mu.g/mL.
6. A parenteral formulation suitable for treatment of secondary hyperparathyroidism comprising 2 10 .mu.g/mL of doxercalciferol 0.5% 2.5% w/w polysorbate 20, 20 ppm BHT and 2.5% w/w ethanol.