IP Library Granted Patent US 9,017,722
Granted Patent B2
US 9,017,722 · App. 13/662,221 · Granted Apr 28, 2015

Pharmaceutical composition containing as an active ingredient 5-methyl-1-phenyl-2-(1H)-pyridone

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Quick Facts
Patent No.
US 9,017,722
App. No.
13/662,221
Granted
Apr 28, 2015
Kind
B2
Abstract

A tablet characterized by comprising 5-methyl-1-phenyl-2-(1H)-pyridone as the main ingredient and, based on the main ingredient, 10 to 50 wt. % excipient, 5 to 40 wt. % disintegrator, 1 to 10 wt. % binder, 0.5 to 5 wt. % lubricant, 2 to 6 wt. % coating basis, and 0.05 to 3 wt. % light-shielding agent, wherein the odor or bitterness of the 5-methyl-1-phenyl-2-(1H)-pyridone is masked and the light stability is improved.

Claims (20)

1. A tablet comprising an amount of 5-methyl-1-phenyl-2-(1H)-pyridone, and further comprising 10 to 50 wt % excipient selected from lactose, corn starch, crystalline cellulose, or any mixture thereof, 5 to 40 wt % disintegrant selected from carmellose calcium, carmellose sodium, croscarmellose sodium, low substituted hydroxypropylcellulose, cross-linked polyvinylpyrrolidone, or any mixture thereof, 1 to 10 wt % binder selected from hydroxypropylcellulose and polyvinylpyrrolidone, or any mixture thereof, and 0.5 to 5 wt. % lubricant selected from magnesium stearate, talc, or any mixture thereof, the wt. % being based on the weight of the 5-methyl-1-phenyl-2-(1H)-pyridone.

2. A tablet according to claim 1 , wherein the tablet has a weight ranging from 100 to 1000 mg.

3. A tablet according to claim 1 or 2 , wherein the table comprises 10 to 85% of the 5-methyl-1-phenyl-2-(1H)-pyridone by weight based on the total weight of the tablet.

4. A tablet according to claim 1 , wherein the amount of the 5-methyl-1-phenyl-2-(1H)-pyridone ranges from 200 mg to 400 mg.

5. A tablet according to claim 1 , further comprising a light-shielding agent.

6. A tablet according to claim 5 , wherein the light-shielding agent is present in an amount ranging from 0.05 to 3 wt. %.

7. A tablet according to claim 1 , further comprising 2 to 6 wt. % coating basis, and 0.05 to 3 wt. % light-shielding agent.

8. A tablet according to claim 7 , further comprising 0.01 to 1 wt. % plasticizer.

9. A tablet according to claim 1 , further comprising a coating layer comprising 2 to 6 wt. % coating basis and 0.05 to 3 wt. % light-shielding agent.

10. A tablet as claimed in claim 9 , wherein the coating layer further comprises 0.01 to 1 wt. % plasticizer.

11. A tablet comprising:

a core comprising an amount of 5-methyl-1-phenyl-2-(1H)-pyridone, 10 to 50 wt. % excipient selected from lactose, corn starch, crystalline cellulose, or any mixture thereof; 5 to 40 wt. % disintegrator selected from carmellose calcium, carmellose sodium, croscarmellose sodium, low substituted hydroxypropylcellulose, cross-linked polyvinylpyrrolidone, or any mixture thereof; 1 to 10 wt. % binder selected from hydroxypropylcellulose and polyvinylpyrrolidone, or any mixture thereof; and 0.5 to 5 wt. % lubricant selected from magnesium stearate, talc, or any mixture thereof, and

a coating layer comprising 2 to 6 wt. % coating basis selected from hydroxypropylmethylcellulose, hydroxypropylcellulose, or any mixture thereof; 0.01 to 1 wt. % plasticizer selected from triethyl citrate, triacetin, or any mixture thereof; and 0.05 to 3 wt. % light-shielding agent selected from titanium oxide, ferric oxide, or any mixture thereof,

wherein the wt % are based on the weight of the 5-methyl-1-phenyl-2-(1H)-pyridone.

12. A tablet according to claim 11 , wherein the core comprises 10 to 50 wt. % lactose, 5 to 40 wt. % carmellose calcium, 1 to 10 wt. % hydroxypropylcellulose, and 0.5 to 5 wt. magnesium, and the coating layer comprises 2 to 6 wt. % hydroxypropylmethylcellulose, 0.01 to 1 wt. % triethyl citrate, and 0.05 to 3 wt. % titanium oxide.

13. A tablet comprising:

a core comprising an amount of 5-methyl-1-phenyl-2-(1H)-pyridone, 20 to 30 wt. % excipient selected from lactose, corn starch, crystalline cellulose, or any mixture thereof; 7.5 to 15 wt. % disintegrator selected from carmellose calcium, carmellose sodium, croscarmellose sodium, low substituted hydroxypropylcellulose, cross-linked polyvinylpyrrolidone, or any mixture thereof; 2 to 5 wt. % binder selected from hydroxypropylcellulose, polyvinylpyrrolidone, or any mixture thereof; and 0.5 to 3 wt. % lubricant selected from magnesium stearate, talc, or any mixture thereof, and

a coating layer comprising 2 to 4 wt. % coating basis selected from hydroxypropylmethylcellulose, hydroxypropylcellulose, or any mixture thereof; 0.01 to 1 wt. % plasticizer selected from triethyl citrate, triacetin, or any mixture thereof; and 0.8 to 3 wt. % titanium oxide as a light-shielding agent,

wherein the wt % are based on the weight of the 5-methyl-1-phenyl-2-(1H)-pyridone.

14. A tablet according to claim 13 , wherein the core comprises 20 to 30 wt. % lactose, 7.5 to 15 wt. % carmellose calcium, 2 to 5 wt. % hydroxypropylcellulose, and 0.5 to 3 wt. magnesium stearate, and the coating layer comprises 2 to 4 wt. % hydroxypropylmethylcellulose, 0.01 to 1 wt. % triethyl citrate and 0.8 to 3 wt. % titanium oxide.

Assignments (2)
CERTIFICATE OF CHANGE OF COMPANY'S ADDRESS Recorded Jul 27, 2018
From: INTERMUNE, INC.
To: INTERMUNE, INC.
Reel/Frame 046638/0466 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 8, 2014
From: SHIONOGI & CO., LTD.
To: INTERMUNE, INC.
Reel/Frame 032852/0963 →