ST-246 liquid formulations and methods
The present invention provides for a novel liquid formulation for solubilizing poorly soluble ST-246 in cyclodextrins and a novel process of making the formulation.
1. A process of making a liquid formulation comprising a therapeutically effective amount of ST-246 and cyclodextrin, and further comprising one or more pharmaceutically acceptable ingredients comprising the steps of:
a) mixing ST-246 with cyclodextrin in a pharmaceutically acceptable liquid carrier; and
b) optionally filtering the mixture of step a).
2. The process of claim 1 , wherein said ST-246 is selected from a group consisting of ST-246 polymorph Form I, ST-246 polymorph Form II, ST-246 polymorph Form III, ST-246 polymorph Form IV, ST-246 polymorph Form V and ST-246 polymorph Form VI.
3. The process of claim 1 , wherein said cyclodextrin is hydroxypropyl-β-cyclodextrin.
4. The process of claim 1 , wherein said hydroxypropyl-β-cyclodextrin is present in amounts from about 20% to about 40% by weight.
5. The process of claim 1 , wherein said liquid formulation is adjusted to a pH between about 3 and 10.
6. The process of claim 3 , wherein said hydroxypropyl-β-cyclodextrin has a degree of substitution between about 4.0 to about 8.0.
7. The process of claim 1 , wherein the mixture of step (a) is brought to solubility equilibrium at a temperature of about 25° C.
8. The process of claim 1 , wherein the mixture of step (a) is brought to solubility equilibrium at a temperature of about 37° C.
9. The process of claim 1 , wherein said ST-246 is mixed with pharmaceutically acceptable carrier for about 72 hours.