Pharmaceutical compositions

• US 9,402,813 B2
• Filed: 06/24/2015
• Issued: 08/02/2016
• Est. Priority Date: 10/09/2006
• Status: Active Grant

• Current Assignee: LOCL Pharma, Inc. (Charleston Laboratories, Inc.)
• Original Assignee: LOCL Pharma, Inc. (Charleston Laboratories, Inc.)
• Inventors: Bosse, Paul
• Primary Examiner(s): JEAN-LOUIS, SAMIRA JM
• Application Number:
  US14/748,605
• Publication Number:
  US 20150328161A1
• Time in Patent Office: 405 Days
• US Class Current: 1/1
• 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 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 9/20 Pills, tablets, discs, rods A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095
• CPC Class Codes: A61K 9/2086 Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat active cores with a complete drug-free outer coat A61K9/28
• 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 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 1/08 for nausea, cinetosis or vertigo; Antiemetics
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 37/08 Antiallergic agents antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 7/04 Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents

Abstract

Pharmaceutical compositions are provided which comprise effective amounts of analgesic to treat a subject, including to reduce or eliminate an adverse effect associated with the analgesic.

Claims

1. A solid oral pharmaceutical composition for treatment of pain, and reduction or prevention of nausea or vomiting associated with an opioid analgesic, comprising:

a layer formulated for immediate-release that comprises an antiemetic; and

a layer formulated for controlled-release that comprises an opioid analgesic and a non-opioid analgesic,

wherein the opioid analgesic, the non-opioid analgesic, and the antiemetic are present in a ratio by weight of (1 to

     2);

(40 to

     45);

(1 to

     2), respectively, and

wherein the solid oral pharmaceutical composition provides an effective amount of the antiemetic to reduce or prevent nausea associated with the opioid analgesic or vomiting associated with the opioid analgesic in a subject in need thereof, and an effective amount of the opioid analgesic and the non-opioid analgesic to treat pain in the subject in need thereof.

2. The solid oral pharmaceutical composition of claim 1, wherein the opioid analgesic is hydrocodone or a pharmaceutically acceptable salt thereof, or oxycodone or a pharmaceutically acceptable salt thereof.

3. The solid oral pharmaceutical composition of claim 2, wherein the hydrocodone or the pharmaceutically acceptable salt thereof, or the oxycodone or the pharmaceutically acceptable salt thereof is present in an amount of 1-20 mg.

4. The solid oral pharmaceutical composition of claim 2, wherein the opioid analgesic is hydrocodone or the pharmaceutically acceptable salt thereof, and is present in an amount of about 1-15 mg.

5. The solid oral pharmaceutical composition of claim 1, wherein the opioid analgesic is hydrocodone or a pharmaceutically acceptable salt thereof, and is present in an amount of about 7.5 mg.

6. The solid oral pharmaceutical composition of claim 1, wherein the opioid analgesic is hydrocodone or the pharmaceutically acceptable salt thereof, and is present in an amount of 5 mg.

7. The solid oral pharmaceutical composition of claim 1, wherein the opioid analgesic is hydrocodone bitartrate and is present in an amount of about 7.5 mg.

8. The solid oral pharmaceutical composition of claim 1, wherein the opioid analgesic is oxycodone or a pharmaceutically acceptable salt thereof, and is present in an amount of about 7.5 mg.

9. The solid oral pharmaceutical composition of claim 1, wherein the opioid analgesic is oxycodone or a pharmaceutically acceptable salt thereof, and is present in an amount of 10 mg.

10. The solid oral pharmaceutical composition of any one of claims 1, 2, 3, 4, or 6, wherein the opioid analgesic is hydrocodone bitartrate.

11. The solid oral pharmaceutical composition of any one of claims 1, 2, 3, 8 or 9, wherein the opioid analgesic is oxycodone hydrochloride.

12. The solid oral pharmaceutical composition of any one of claims 1 or 3-9, wherein the antiemetic is promethazine or a pharmaceutically acceptable salt thereof.

13. The solid oral pharmaceutical composition of any one of claims 1, or 3-9, wherein the antiemetic is promethazine hydrochloride.

14. The solid oral pharmaceutical composition of any one of claims 1 or 2, wherein the antiemetic is promethazine or a pharmaceutically acceptable salt thereof, and is present in an amount of about 0.5-60 mg.

15. The solid oral pharmaceutical composition of any one of claims 1-5, 7 or 8, wherein the antiemetic is promethazine or a pharmaceutically acceptable salt thereof, and is present in an amount of about 12.5 mg.

16. The solid oral pharmaceutical composition of claim 1, wherein the antiemetic is promethazine and is present in an amount of 11 mg.

17. The solid oral pharmaceutical composition of claim 15, wherein the antiemetic is promethazine hydrochloride and is present in an amount of about 12.5 mg.

18. The solid oral pharmaceutical composition of any one of claims 1-9, wherein the non-opioid analgesic is acetaminophen or a pharmaceutically acceptable salt thereof.

19. The solid oral pharmaceutical composition of any one of claims 1-9, wherein the non-opioid analgesic is acetaminophen or a pharmaceutically acceptable salt thereof and is present in an amount of about 200-600 mg.

20. The solid oral pharmaceutical composition of any one of claims 1-5, 7 or 8, wherein the non-opioid analgesic is acetaminophen or a pharmaceutically acceptable salt thereof, and is present in an amount of about 325 mg.

21. The solid oral pharmaceutical composition of claim 1, wherein the opioid analgesic is hydrocodone or a pharmaceutically acceptable salt thereof, the non-opioid analgesic is acetaminophen or a pharmaceutically acceptable salt thereof, and the antiemetic is promethazine or a pharmaceutically acceptable salt thereof, which are present in a ratio by weight of about 1:

43;

1.7, respectively.

22. The solid oral pharmaceutical composition of claim 1, wherein the opioid analgesic is hydrocodone or a pharmaceutically acceptable salt thereof, the non-opioid analgesic is acetaminophen or a pharmaceutically acceptable salt thereof, and the antiemetic is promethazine or a pharmaceutically acceptable salt thereof, which are present in a ratio by weight of 1:

43.33;

1.67, respectively.

23. The solid oral pharmaceutical composition of claim 1, wherein the opioid analgesic is hydrocodone or a pharmaceutically acceptable salt thereof, the non-opioid analgesic is acetaminophen or a pharmaceutically acceptable salt thereof, and the antiemetic is promethazine or a pharmaceutically acceptable salt thereof, which are present in an amount of 6-8 mg, 200-350 mg, and 5-13 mg, respectively.

24. The solid oral pharmaceutical composition of claim 1, wherein the opioid analgesic is hydrocodone or a pharmaceutically acceptable salt thereof, the non-opioid analgesic is acetaminophen or a pharmaceutically acceptable salt thereof, and the antiemetic is promethazine or a pharmaceutically acceptable salt thereof, which are present in an amount of about 7.5 mg, about 325 mg, and about 12.5 mg, respectively.

25. The solid oral pharmaceutical composition of claim 1, wherein the opioid analgesic oxycodone or a pharmaceutically acceptable salt thereof, the non-opioid analgesic is acetaminophen or a pharmaceutically acceptable salt thereof, and the antiemetic is promethazine or a pharmaceutically acceptable salt thereof, which are present in an amount of about 7.5 mg, about 325 mg, and about 12.5 mg, respectively.

26. The solid oral pharmaceutical composition of any one of claims 1-9, 21-24 or 25, wherein the solid oral pharmaceutical composition is a tablet.

27. The solid oral pharmaceutical composition of claim 26, wherein the tablet is a bi-layer tablet.

28. The solid oral pharmaceutical composition of claim 1, wherein the solid oral pharmaceutical composition further comprises an opioid antagonist or an additional agent for reducing abuse and/or diversion.