Granted Patent B2

US 10,300,046 · App. 15/260,424 · Granted May 28, 2019

Abstract

Claims (57)

1. A pharmaceutical composition comprising prior to mixing:

(a) radezolid or a pharmaceutically acceptable salt, ester, or prodrug thereof;

(b) a hydroxypropylmethyl cellulose polymer;

(c) croscarmellose sodium;

(d) a lubricant selected from colloidal silicon dioxide, magnesium stearate, and mixtures thereof;

(e) microcrystalline cellulose; and

(f) a filler selected from lactose monohydrate, dicalciumphosphate, and mixtures thereof;

wherein the pharmaceutical composition comprises a physical mixture.

2. A pharmaceutical composition comprising:

(a) radezolid or a pharmaceutically acceptable salt, ester, or prodrug thereof;

(b) a hydroxypropylmethyl cellulose polymer;

(c) croscarmellose sodium;

(d) a lubricant selected from colloidal silicon dioxide, magnesium stearate, and mixtures thereof; and

(e) a filler selected from lactose monohydrate, dicalciumphosphate, and mixtures thereof;

wherein the pharmaceutical composition comprises a physical mixture.

3. A pharmaceutical composition according to claim 2 wherein said radezolid or a pharmaceutically acceptable salt, ester, or prodrug thereof comprises a pharmaceutically acceptable amount.

4. A pharmaceutical composition according to claim 2 wherein said radezolid or a pharmaceutically acceptable salt, ester, or prodrug thereof comprises a prophylactically effective amount.

5. A pharmaceutical composition according to claim 2 wherein said pharmaceutically acceptable salt is a hydrochloride salt.

6. A pharmaceutical composition according to claim 5 wherein said pharmaceutically acceptable salt is a monohydrochloride salt.

7. A pharmaceutical composition according to claim 2 wherein said hydroxypropylmethylcellulose polymer is a hydroxypropylmethylcellulose acetate succinate (“HPMCAS”).

8. A pharmaceutical composition according to claim 7 wherein said HPMCAS is selected from HPMCAS-M, HPMCAS-H, and mixtures thereof.

9. A pharmaceutical composition comprising:

Percent by

Ingredients

Weight

Intra Granular

Radezolid hydrochloride

20.31%

(amount as hydrochloride salt)

HPMCAS-M Spray Dried

13.28%

HPMCAS-H Spray Dried

13.28%

Croscarmellose Sodium

4.00%

Microcrystalline cellulose

11.60%

Lactose monohydrate

11.60%

Colloidal silicon dioxide

0.75%

Magnesium Stearate

0.19%

Extra Granular

Croscarmellose Sodium

1.50%

Di-Cal Phosphate (DC Grade)

23.38%

Colloidal silicon dioxide

0.06%

Magnesium Stearate

0.06%

wherein the pharmaceutical composition comprises a physical mixture.

10. A method of treating a microbial infection in a patient comprising administering a pharmaceutically effective amount of a pharmaceutical composition according to claim 1 .

11. A method of reducing the risk of a microbial infection in a patient comprising administering a prophylactically effective amount of a pharmaceutical composition according to claim 1 .

12. The method according to claim 10 wherein said patient is a human or an animal.

13. The method according to claim 10 wherein said patient is a human.

Assignments (6)