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Last Updated: November 26, 2020

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Claims for Patent: 9,757,406

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Summary for Patent: 9,757,406
Title:Combination formulation of two antiviral compounds
Abstract: Disclosed are pharmaceutical compositions comprising Compound I, having the formula: ##STR00001## and an effective amount of sofosbuvir wherein the sofosbuvir is substantially crystalline. Also disclosed are methods of use for the pharmaceutical composition.
Inventor(s): Gorman; Eric (Foster City, CA), Mogalian; Erik (Foster City, CA), Oliyai; Reza (Foster City, CA), Stefanidis; Dimitrios (Mountain View, CA), Wiser; Lauren (San Francisco, CA), Zia; Vahid (Palo Alto, CA)
Assignee: Gilead Pharmasset LLC (Foster City, CA)
Application Number:15/282,128
Patent Claims: 1. A pharmaceutical composition comprising: 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: ##STR00018## b) from about 35% to about 45% w/w of substantially crystalline sofosbuvir having the formula: ##STR00019## 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.

2. The pharmaceutical composition of claim 1, wherein the crystalline sofosbuvir has XRPD 2.theta.-reflections at about: 6.1 and 12.7 .degree.2.theta..+-.0.2.

3. The pharmaceutical composition of claim 1, wherein the crystalline sofosbuvir has XRPD 2.theta.-reflections at about: 6.1, 20.1, and 20.8 .degree.2.theta..+-.0.2.

4. The pharmaceutical composition of claim 1, comprising about 40% w/w of sofosbuvir.

5. The pharmaceutical composition of claim 1, comprising about 20% w/w of the solid dispersion.

6. The pharmaceutical composition of claim 1, comprising about 35.5% w/w of microcrystalline cellulose.

7. The pharmaceutical composition of claim 1, comprising about 3% w/w of croscarmellose sodium.

8. The pharmaceutical composition of claim 1, comprising about 1.5% w/w of magnesium stearate.

9. A pharmaceutical composition comprising: 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: ##STR00020## b) about 40% w/w of substantially crystalline sofosbuvir having the formula: ##STR00021## 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.

10. The pharmaceutical composition of claim 9, wherein the crystalline sofosbuvir has XRPD 2.theta.-reflections at about: 6.1 and 12.7 .degree.2.theta..+-.0.2.

11. The pharmaceutical composition of claim 9, wherein the crystalline sofosbuvir has XRPD 2.theta.-reflections at about: 6.1, 20.1, and 20.8 .degree.2.theta..+-.0.2.

12. A pharmaceutical composition comprising: 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: ##STR00022## b) about 400 mg of substantially crystalline sofosbuvir having the formula: ##STR00023## c) about 355 mg of microcrystalline cellulose; d) about 30 mg of croscarmellose sodium; and e) about 15 mg of magnesium stearate.

13. The pharmaceutical composition of claim 12 which is in the form of a tablet comprising a film coating.

14. The tablet of claim 13, wherein the film coating is a polyvinylalcohol-based coating.

15. The pharmaceutical composition of claim 12, wherein the crystalline sofosbuvir has XRPD 2.theta.-reflections at about: 6.1 and 12.7 .degree.2.theta..+-.0.2.

16. The pharmaceutical composition of claim 12, wherein the crystalline sofosbuvir has XRPD 2.theta.-reflections at about: 6.1, 20.1, and 20.8 .degree.2.theta..+-.0.2.

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Serving leading biopharmaceutical companies globally:

Medtronic
Express Scripts
Boehringer Ingelheim
McKinsey
Johnson and Johnson
Moodys

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