PHARMACEUTICAL COMPOSITIONS

• US 20110262539A1
• Filed: 12/14/2010
• Published: 10/27/2011
• Est. Priority Date: 07/08/2009
• Status: Active Grant

• Current Assignee: LOCL Pharma, Inc. (Charleston Laboratories, Inc.)
• Original Assignee: Charleston Laboratories, Inc.
• Inventors: Schachtel, Bernard, Ameling, John, BOSSE, Paul, Takigiku, Ray
• Granted Patent: US 8,728,522 B2
• Time in Patent Office: Days
• US Class Current: 424/472
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/167 having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 31/5415 ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/209 containing drug in at least two layers or in the core and in at least one outer layer
• CPC Class Codes: A61P 25/06 Antimigraine agents
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

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

1. A pharmaceutical composition in the form of a bi-layer tablet comprising:

(1) an immediate release layer comprising;

(a) about 5 mgs to about 20 mgs of promethazine or a pharmaceutically acceptable salt thereof,

(b) about 75 mgs to about 150 mgs of silicified microcrystalline cellulose,

(c) about 5 mgs to about 20 mgs of croscarmellose sodium, and

(d) about 0.2 mgs to about 5 mgs of magnesium stearate; and

(2) a controlled release layer comprising;

(a) about 250 mgs to about 400 mgs of acetaminophen, or a pharmaceutically acceptable salt thereof,

(b) about 2 mgs to about 15 mgs of hydrocodone, or a pharmaceutically acceptable salt thereof,

(c) about 100 mgs to about 250 mgs of silicified microcrystalline cellulose,

(d) about 5 mgs to about 30 mgs of hydroxy methyl propyl cellulose,

(e) about 0.5 mgs to about 5 mgs magnesium stearate, and

(f) about 0.5 mgs to about 10 mgs stearic acid.

2. The pharmaceutical composition of claim 1, wherein:

(1) the immediate release layer comprises;

(a) about 12.5 mgs of promethazine HCL,

(b) about 121 mgs of silicified microcrystalline cellulose,

(c) about 15 mgs of croscarmellose sodium, and

(d) about 1 mg of magnesium stearate; and

(2) the controlled release layer comprises;

(a) about 361 mgs of acetaminophen,

(b) about 8 mgs of hydrocodone bitartrate,

(c) about 155 mgs of silicified microcrystalline cellulose,

(d) about 20 mgs of hydroxy methyl propyl cellulose,

(e) about 2.75 mgs magnesium stearate, and

(f) about 2.75 mgs stearic acid.

3. The pharmaceutical composition of claim 1 or 2, wherein at least about 90% of the promethazine is released within the first 10 minutes.

4. The pharmaceutical composition of claim 1, wherein at least about 90% of the promethazine is released within the first 5 minutes.

5. The pharmaceutical composition of claim 1, wherein less than about 80% of the acetaminophen is released within the first 30 minutes.

6. The pharmaceutical composition of claim 1 or 2, wherein less than about 80% of the hydrocodone is released within the first 30 minutes.

7. The pharmaceutical composition of claim 1, wherein said bilayer tablet has a hardness of between about 7 and about 15 kp.

8. The pharmaceutical composition of claim 1 or 2, wherein said bilayer tablet has a hardness of about 12 kp.

9. The pharmaceutical composition of claim 1, wherein said immediate release layer has a faster dissolution rate than said controlled release layer.

10. A method of treating or preventing pain or discomfort in a subject in need thereof by administering a pharmaceutical composition of claim 1.

11. The method of claim 10, wherein said subject experiences a reduction in a symptom associated with the administration of hydrocodone.

12. The method of claim 11, wherein said symptom associated with the administration of hydrocodone is nausea, vomiting, gastric upset, skin rash or an allergic reaction.

13. The method of claim 10, wherein the subject is 0-12 years old.

14. The method of claim 10, wherein the subject is about age 65 or older.

15. The method of claim 10, wherein said discomfort is a headache.

16. The method of claim 15, wherein the headache is a migraine headache, cluster headache, hemicrania continua headache, chronic headache, tension headache or chronic tension headache.

17. The method of claim 10, wherein said discomfort is photophobia.