Sterile pharmaceutical compositions
The present invention provides a method for the sterilization of a labile glucocorticosteroid, which method comprises heat-treating by moist heat the labile glucocorticosteroid in the form of a suspension for a sterilizing-effective time. The methods and compositions according to the invention are useful as therapeutic tools to prevent, reverse, and/or reduce the symptoms of allergic and/or inflammatory conditions in a mammalian patient. The invention also provides methods and compositions, which may be manipulated and fine-tuned to fit the condition(s) to be treated while producing fewer side effects.
1. A heat-sterilized aqueous budesonide composition comprising budesonide at a concentration of from about 30 mg/ml to about 150 mg/ml and at least one surfactant, wherein at least 70% of the budesonide is in the form of a suspension.
2. The composition of claim 1 , wherein the surfactant comprises a pharmaceutically acceptable surfactant.
3. The composition of claim 2 , wherein the pharmaceutically acceptable surfactant is in a concentration of from about 0.2 mg/ml to about 60 mg/ml.
4. The composition of claim 1 , wherein the budesonide is suspended in a solvent and the amount of the budesonide per unit of solvent is such that at least 70% of the budesonide is suspended in the solvent.
5. The composition of claim 1 , wherein the solvent is water.
6. The composition of claim 1 , wherein the particle size of the budesonide in the composition has a Dv100 that is less than 20 μm, a Dv90 that is less than 10 μm and a Dv50 that is less than 5 μm.
7. The composition of claim 1 , comprising less than 0.2% by weight of 1,2-dihydro budesonide based on the amount of budesonide.
8. A dilute sterile aqueous suspension comprising the sterile aqueous budesonide suspension of claim 1 and at least one of a diluent and excipient, wherein the budesonide in the dilute sterile aqueous suspension is present at a pharmaceutically suitable concentration.
9. A dilute sterile aqueous suspension comprising the sterile aqueous budesonide suspension of claim 1 and at least one of a diluent and excipient, wherein the budesonide is present at a pharmaceutically suitable concentration.