Thromboxane receptor antagonist formulations
The present invention provides formulations that enhances bioavailability of thromboxane receptor antagonists allowing them to bind to the thromboxane A 2 receptors in subjects suffering from disease indications in which the prostanoid thromboxane A 2 , and incidental thromboxane A 2 receptor ligands, are implicated. The formulations comprise a solid dispersion comprising a benzenesulfonyl urea and a polymer that are suitable for administration through oral or other routes of delivery.
1 . A formulation comprising:
a spray dried amorphous solid dispersion comprising:
a drug comprising a substituted benzenesulfonyl urea of formula (IV)
a vinylpyrrolidone-vinyl acetate copolymer, wherein a ratio of the substituted benzenesulfonyl urea to the vinylpyrrolidone-vinyl acetate copolymer is between 1:4 and 1:8.
2 . The formulation of claim 1 , formulated in an oral dose form.
3 . The formulation of claim 1 , wherein there is less dissolution of the formulation in environments with a pH less than 2 than in environments with a pH above 5.
4 . The formulation of claim 1 , wherein there is no dissolution of the formulation at a pH of less than 2.
5 . The formulation of claim 4 , wherein there is substantial dissolution of the formulation at a pH above 5.
6 . The formulation of claim 1 , wherein a ratio of the substituted benzenesulfonyl urea to the vinylpyrrolidone-vinyl acetate copolymer is 1:4.
7 . The formulation of claim 1 , wherein the ratio is about 1:4; wherein there is no dissolution of the formulation at a pH of less than 2; and wherein there is substantial dissolution of the formation at a pH above 5.
8 . The formulation of claim 7 , formulated in an oral dose form.
9 . A method of treating a cardiopulmonary condition, the method comprising administering to a patient a formulation of claim 8 , wherein the cardiopulmonary condition is pulmonary arterial hypertension.