Combination formulation of two antiviral compounds
AssigneeGilead Pharmasset LLC
InventorsEric Gorman, Erik Mogalian, Reza Oliyai, Dimitrios Stefanidis, Lauren Wiser, Vahid Zia
Life of this patent
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Abstract
Disclosed are pharmaceutical compositions comprising Compound I, having the formula: and an effective amount of sofosbuvir wherein the sofosbuvir is substantially crystalline. Also disclosed are methods of use for the pharmaceutical composition.
Claims20
-59. (canceled)
A method of treating hepatitis C in a human patient in need thereof comprising administering to the patient a therapeutically effective amount of a pharmaceutical composition, wherein the pharmaceutical composition comprises:
- a) from about 1% to about 25% w/w of a solid dispersion comprising Compound I dispersed within a polymer matrix formed by copovidone, wherein the weight ratio of Compound I to copovidone in the solid dispersion is about 1:1 and wherein Compound I is substantially amorphous having the formula:
- b) from about 35% to about 45% w/w of substantially crystalline sofosbuvir having the formula:
- c) from about 30% to about 40% w/w of microcrystalline cellulose;
- d) from about 1% to about 5% w/w of croscarmellose sodium;
- and
- e) from about 0.5% to about 2.5% w/w of magnesium stearate.
A method of treating hepatitis C in a human patient in need thereof comprising administering to the patient a therapeutically effective amount of a pharmaceutical composition, wherein the pharmaceutical composition comprises:
- a) about 20% w/w of a solid dispersion comprising Compound I dispersed within a polymer matrix formed by copovidone, wherein the weight ratio of Compound I to copovidone in the solid dispersion is about 1:1 and wherein Compound I is substantially amorphous having the formula:
- b) about 40% w/w of substantially crystalline sofosbuvir having the formula:
- c) about 35.5% w/w of microcrystalline cellulose;
- d) about 3% w/w of croscarmellose sodium;
- and
- e) about 1.5% w/w of magnesium stearate.
A method of treating hepatitis C in a human patient in need thereof comprising administering to the patient a pharmaceutical composition, wherein the pharmaceutical composition comprises:
- a) about 200 mg of a solid dispersion comprising Compound I dispersed within a polymer matrix formed by copovidone, wherein the weight ratio of Compound I to copovidone in the solid dispersion is about 1:1 and wherein Compound I is substantially amorphous having the formula:
- b) about 400 mg of substantially crystalline sofosbuvir having the formula:
- c) about 355 mg of microcrystalline cellulose;
- d) about 30 mg of croscarmellose sodium;
- and
- e) about 15 mg of magnesium stearate.
Dependencies are inferred from the claim text.