IP Library Granted Patent US 8,124,126
Granted Patent B2
US 8,124,126 · App. 12/351,704 · Granted Feb 28, 2012

Pharmaceutical compositions

Assignee: Charleston Laboratories, Inc.
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Quick Facts
Patent No.
US 8,124,126
App. No.
12/351,704
Granted
Feb 28, 2012
Kind
B2
Abstract

Methods and compositions are provided which comprise effective amounts of analgesic to treat a subject, including reducing or eliminating an adverse effect associated with the analgesic.

Claims (37)

1. A bi-layer tablet comprising:

(1) a controlled-release layer comprising (a) from about 6.5 mg to about 8.5 mg of hydrocodone or a pharmaceutically acceptable salt thereof, (b) from about 100 mg to about 170 mg of silicified microcrystalline cellulose, (c) from about 10 mg to about 20 mg of hydroxy propyl methyl cellulose, (d) from about 1 mg to about 4 mg of magnesium stearate, (e) from about 1 mg to about 4 mg of stearic acid, (f) about 290 mg to about 360 mg of acetaminophen or a pharmaceutically acceptable salt thereof; and

(2) an immediate release layer comprising (a) from about 11 mg to about 14 mg of promethazine or a pharmaceutically acceptable salt thereof, (b) from about 100 mg to about 140 mg of silicified microcrystalline cellulose, (c) from about 12 mg to about 18 mg of croscarmellose sodium and (d) from about 0.8 mg to about 1.5 mg of magnesium stearate,

wherein about 90% of the promethazine or a pharmaceutically acceptable salt thereof is released in about 1 minute to about 20 minutes following administration and about 100% of the promethazine or a pharmaceutically acceptable salt thereof is released in about 40 minutes following administration, wherein about 30% to about 60% of the hydrocodone or a pharmaceutically acceptable salt thereof and the acetaminophen or a pharmaceutically acceptable salt thereof are released within about 5 minutes to about 10 minutes following administration, wherein the bi-layer tablet provides an effective amount of promethazine, hydrocodone and acetaminophen or their pharmaceutically acceptable salts therof for about 4 hours to about 6 hours following administration, wherein said bi-layer tablet does not contain a NMDA receptor antagonist agent.

2. The bi-layer tablet of claim 1 , wherein the composition further comprises a stimulant.

3. The bi-layer tablet of claim 2 , wherein the stimulant is caffeine, modafinil or a pharmaceutically acceptable salt thereof.

4. The bi-layer tablet of claim 1 , further comprising an opioid antagonist agent or abuse deterrent agent.

5. The bi-layer tablet of claim 1 , wherein the opioid antagonist agent is nalmefene, naloxone, naltrexone, cyclazacine or levallorphan, or a pharmaceutically acceptable salt thereof.

6. The bi-layer tablet of claim 4 , wherein the opioid antagonist agent is naltrexone or a pharmaceutically acceptable salt thereof.

7. The bi-layer tablet of claim 1 , wherein the controlled-release layer comprises about 325 mg of acetaminophen or a pharmaceutically acceptable salt thereof.

8. The bi-layer tablet of claim 1 , wherein the controlled-release layer comprises about 7.5 mg of hydrocodone or a pharmaceutically acceptable salt thereof.

9. The bi-layer tablet of claim 1 , wherein the immediate release layer comprises about 12.5 mg of promethazine or a pharmaceutically acceptable salt thereof.

10. The bi-layer tablet of claim 1 , wherein the bi-layer tablet has a thickness of about 6.5 mm.

11. The bi-layer tablet of claim 1 , wherein the bi-layer tablet has a hardness of about 12.5 kilopond.

12. The bi-layer tablet of claim 11 , wherein the bi-layer tablet has a thickness of about 6.5 mm.

13. The bi-layer tablet of claim 1 , wherein about 90% to about 100% of the hydrocodone is released in about 40 minutes.

14. The bi-layer tablet of claim 1 , wherein about 90% to about 100% of the acetaminophen is released in about 40 minutes.

15. The bi-layer tablet of claim 1 , wherein at least about 90% of the promethazine, hydrocodone and acetaminophen dissolve in the stomach of a subject after about 45 minutes following administration.

16. The bi-layer tablet of claim 1 , wherein said bi-layer tablet does not provide an effective amount of the hydrocodone or acetaminophen after 12 hours following administration.

17. A method for treating or preventing pain, comprising administering to a subject in need thereof a bi-layer tablet comprising:

(1) a controlled-release layer comprising (a) from about 6.5 mg to about 8.5 mg of hydrocodone or a pharmaceutically acceptable salt thereof, (b) from about 100 mg to about 170 mg of silicified microcrystalline cellulose, (c) from about 10 mg to about 20 mg of hydroxy propyl methyl cellulose, (d) from about 1 mg to about 4 mg of magnesium stearate, (e) from about 1 mg to about 4 mg of stearic acid, (f) from about 290 mg to about 360 mg of acetaminophen or a pharmaceutically acceptable salt thereof; and

(2) an immediate release layer comprising (a) from about 11 mg to about 14 mg of promethazine or a pharmaceutically acceptable salt thereof, (b) from about 100 mg to about 140 mg of silicified microcrystalline cellulose, (c) from about 12 mg to about 18 mg of croscarmellose sodium and (d) from about 0.8 mg to about 1.5 mg of magnesium stearate, wherein about 90% of the promethazine or a pharmaceutically acceptable salt thereof is released in about 1 minute to about 20 minutes following administration and about 100% of the promethazine or a pharmaceutically acceptable salt thereof is released in about 40 minutes following administration, wherein about 30% to about 60% of the hydrocodone or a pharmaceutically acceptable salt thereof and the acetaminophen or a pharmaceutically acceptable salt thereof are released in about 5 minutes to about 10 minutes following administration, wherein the bi-layer tablet provides an effective amount of promethazine, hydrocodone and acetaminophen or their pharmaceutically acceptable salts thereof, for about 4 hours to about 6 hours following administration, wherein said bi-layer tablet does not contain a NMDA receptor antagonist agent.

18. A method for treating or preventing a migraine headache comprising administering to a subject in need thereof a bi-layer tablet comprising:

(1) a controlled-release layer comprising (a) from about 6.5 mg to about 8.5 mg of hydrocodone or a pharmaceutically acceptable salt thereof, (b) from about 100 mg to about 170 mg of silicified microcrystalline cellulose, (c) from about 10 mg to about 20 mg of hydroxy propyl methyl cellulose, (d) from about 1 mg to about 4 mg of magnesium stearate, (e) from about 1 mg to about 4 mg of stearic acid, (f) from about 290 mg to about 360 mg of acetaminophen or a pharmaceutically acceptable salt thereof; and

(2) an immediate release layer comprising (a) from about 11 mg to about 14 mg of promethazine or a pharmaceutically acceptable salt thereof, (b) from about 100 mg to about 140 mg of silicified microcrystalline cellulose, (c) from about 12 mg to about 18 mg of croscarmellose sodium and (d) from about 0.8 mg to about 1.5 mg of magnesium stearate, wherein about 90% of the promethazine or a pharmaceutically acceptable salt thereof is released in about 1 minute to about 20 minutes following administration and about 100% of the promethazine or a pharmaceutically acceptable salt thereof is released in about 40 minutes following administration, wherein about 30% to about 60% of the hydrocodone or a pharmaceutically acceptable salt thereof and the acetaminophen or a pharmaceutically acceptable salt thereof are released in about 5 minutes to about 10 minutes following administration, wherein the bi-layer tablet provides an effective amount of promethazine, hydrocodone and acetaminophen or their pharmaceutically acceptable salts thereof, for about 4 hours to about 6 hours following administration, wherein said bi-layer tablet does not contain a NMDA receptor antagonist agent.

19. A method for treating or preventing a headache comprising administering to a subject in need thereof a bi-layer tablet comprising:

(1) a controlled-release layer comprising (a) from about 6.5 mg to about 8.5 mg of hydrocodone or a pharmaceutically acceptable salt thereof, (b) from about 100 mg to about 170 mg of silicified microcrystalline cellulose, (c) from about 10 mg to about 20 mg of hydroxy propyl methyl cellulose, (d) from about 1 mg to about 4 mg of magnesium stearate, (e) from about 1 mg to about 4 mg of stearic acid, (f) from about 290 mg to about 360 mg of acetaminophen or a pharmaceutically acceptable salt thereof; and

(2) an immediate release layer comprising (a) from about 11 mg to about 14 mg of promethazine or a pharmaceutically acceptable salt thereof, (b) from about 100 mg to about 140 mg of silicified microcrystalline cellulose, (c) from about 12 mg to about 18 mg of croscarmellose sodium and (d) from about 0.8 mg to about 1.5 mg of magnesium stearate, wherein about 90% of the promethazine or a pharmaceutically acceptable salt thereof is released in about 1 minute to about 20 minutes following administration and about 100% of the promethazine or a pharmaceutically acceptable salt thereof is released in about 40 minutes following administration, wherein about 30% to about 60% of the hydrocodone or a pharmaceutically acceptable salt thereof and the acetaminophen or a pharmaceutically acceptable salt thereof are released in about 5 minutes to about 10 minutes following administration, wherein the bi-layer tablet provides an effective amount of promethazine, hydrocodone and acetaminophen or their pharmaceutically acceptable salts thereof, for about 4 hours to about 6 hours following administration, wherein said bi-layer tablet does not contain a NMDA receptor antagonist agent.

20. The method of claim 19 , wherein the headache is a migraine headache, cluster headache or hemicrania continua headache.

21. The method of claim 19 , wherein the headache is a chronic headache, tension headache or chronic tension headache.

22. A method for treating pain, comprising administering to a subject in need thereof a bi-layer tablet comprising:

(1) a controlled-release layer comprising (a) from about 6.5 mg to about 8.5 mg of hydrocodone or a pharmaceutically acceptable salt thereof, (b) from about 100 mg to about 170 mg of silicified microcrystalline cellulose, (c) from about 10 mg to about 20 mg of hydroxy propyl methyl cellulose, (d) from about 1 mg to about 4 mg of magnesium stearate, (e) from about 1 mg to about 4 mg of stearic acid, (f) from about 290 mg to about 360 mg of acetaminophen or a pharmaceutically acceptable salt thereof; and

(2) an immediate release layer comprising (a) from about 11 mg to about 14 mg of promethazine or a pharmaceutically acceptable salt thereof, (b) from about 100 mg to about 140 mg of silicified microcrystalline cellulose, (c) from about 12 mg to about 18 mg of croscarmellose sodium and (d) from about 0.8 mg to about 1.5 mg of magnesium stearate, wherein about 90% of the promethazine or a pharmaceutically acceptable salt thereof is released in about 1 minute to about 20 minutes following administration and about 100% of the promethazine or a pharmaceutically acceptable salt thereof is released in about 40 minutes following administration, wherein about 30% to about 60% of the hydrocodone or a pharmaceutically acceptable salt thereof and the acetaminophen or a pharmaceutically acceptable salt thereof are released in about 5 minutes to about 10 minutes following administration, wherein the bi-layer tablet provides an effective amount of promethazine, hydrocodone and acetaminophen or their pharmaceutically acceptable salts thereof, for about 4 hours to about 6 hours following administration, wherein said bi-layer tablet does not contain a NMDA receptor antagonist agent; wherein the subject is about 65 years of age or older.

23. A method for treating or preventing photophobia comprising administering to a subject in need thereof a bi-layer tablet comprising:

(1) a controlled-release layer comprising (a) from about 6.5 mg to about 8.5 mg of hydrocodone or a pharmaceutically acceptable salt thereof, (b) from about 100 mg to about 170 mg of silicified microcrystalline cellulose, (c) from about 10 mg to about 20 mg of hydroxy propyl methyl cellulose, (d) from about 1 mg to about 4 mg of magnesium stearate, (e) from about 1 mg to about 4 mg of stearic acid, (f) from about 290 mg to about 360 mg of acetaminophen or a pharmaceutically acceptable salt thereof; and

(2) an immediate release layer comprising (a) from about 11 mg to about 14 mg of promethazine or a pharmaceutically acceptable salt thereof, (b) from about 100 mg to about 140 mg of silicified microcrystalline cellulose, (c) from about 12 mg to about 18 mg of croscarmellose sodium and (d) from about 0.8 mg to about 1.5 mg of magnesium stearate, wherein about 90% of the promethazine or a pharmaceutically acceptable salt thereof is released in about 1 minute to about 20 minutes following administration and about 100% of the promethazine or a pharmaceutically acceptable salt thereof is released in about 40 minutes following administration, wherein about 30% to about 60% of the hydrocodone or a pharmaceutically acceptable salt thereof and the acetaminophen or a pharmaceutically acceptable salt thereof are released in about 5 to about 10 minutes following administration, wherein the bi-layer tablet provides an effective amount of promethazine, hydrocodone and acetaminophen or their pharmaceutically acceptable salts therof, for about 4 hours to about 6 hours following administration, wherein said bi-layer tablet does not contain a NMDA receptor antagonist agent.

24. The method of claim 23 , wherein the photophobia is associated with migraine headache.

Assignments (4)
CHANGE OF ADDRESS Recorded Dec 9, 2015
From: LOCL PHARMA, INC.
To: LOCL PHARMA, INC.
Reel/Frame 037255/0606 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 25, 2014
From: CHARLESTON LABORATORIES, INC.
To: LOCL PHARMA, INC.
Reel/Frame 033394/0394 →
CHANGE OF ADDRESS Recorded Dec 18, 2013
From: CHARLESTON LABORATORIES, INC.
To: CHARLESTON LABORATORIES, INC.
Reel/Frame 031837/0938 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 25, 2009
From: BOSSE, PAUL; SCHACHTEL, BERNARD; AMELING, JOHN; TAKIGIKU, RAY
To: CHARLESTON LABORATORIES, INC.
Reel/Frame 022306/0435 →
Continuity (4)
Provisional Application 61020139 · Jan 9, 2008
Provisional Application 61043037 · Apr 7, 2008
Provisional Application 61060758 · Jun 11, 2008
Related Publication 20090175939A1 · Jul 9, 2009