Pharmaceutical compositions

• US 9,393,207 B2
• Filed: 06/24/2015
• Issued: 07/19/2016
• 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:
  US14/748,614
• Publication Number:
  US 20150328211A1
• Time in Patent Office: 391 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 comprising an antiemetic, wherein the antiemetic is promethazine or a pharmaceutically acceptable salt thereof that is present in an amount of about 12.5 mg or 25 mg; and

a layer formulated for controlled-release comprising an opioid analgesic that is present in an amount of 1 mg to about 20 mg and a non-opioid analgesic that is present in an amount of about 200-600 mg,

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 promethazine or the pharmaceutically acceptable salt thereof is present in an amount of about 12.5 mg.

3. The solid oral pharmaceutical composition of claim 1, wherein the promethazine or the pharmaceutically acceptable salt thereof is present in an amount of 25 mg.

4. The solid oral pharmaceutical composition of any one of claim 2 or 3, wherein the pharmaceutically acceptable salt of the promethazine is promethazine hydrochloride.

5. The solid oral pharmaceutical composition of claim 1, wherein the pharmaceutically acceptable salt of the promethazine is promethazine hydrochloride.

6. 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.

7. The solid oral pharmaceutical composition of claim 6, wherein the opioid analgesic is hydrocodone bitartrate.

8. The solid oral pharmaceutical composition of claim 6, wherein the opioid analgesic is oxycodone hydrochloride.

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

10. The solid oral pharmaceutical composition of claim 1, wherein the solid oral pharmaceutical composition is a bi-layer tablet.

33. 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.

11. 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 comprising a single antiemetic; and

a layer formulated for controlled-release comprising a non-opioid analgesic and an opioid analgesic, wherein the opioid analgesic is hydrocodone or a pharmaceutically acceptable salt thereof, or oxycodone or a pharmaceutically acceptable salt thereof, and the opioid analgesic is present in an amount of 1 mg to about 15 mg, and wherein the non-opioid analgesic is present in an amount of about 200-600 mg,

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.

12. The solid oral pharmaceutical composition of claim 11, wherein the opioid analgesic is hydrocodone or the pharmaceutically acceptable salt thereof, and is present in an amount of about 7.5 mg.

13. The solid oral pharmaceutical composition of claim 11, wherein the opioid analgesic is hydrocodone or the pharmaceutically acceptable salt thereof, and is present in an amount of 5 mg.

14. The solid oral pharmaceutical composition of claim 12, wherein the opioid analgesic is hydrocodone bitartrate and is present in an amount of about 7.5 mg.

15. The solid oral pharmaceutical composition of claim 11, wherein the opioid analgesic is oxycodone or the pharmaceutically acceptable salt thereof, and is present in an amount of about 7.5 mg.

16. The solid oral pharmaceutical composition of claim 11, wherein the opioid analgesic is hydrocodone bitartrate.

17. The solid oral pharmaceutical composition of claim 11, wherein the opioid analgesic is oxycodone hydrochloride.

18. The solid oral pharmaceutical composition of claim 11, wherein the antiemetic is promethazine or a pharmaceutically acceptable salt thereof.

19. The solid oral pharmaceutical composition of claim 18, wherein the antiemetic is promethazine hydrochloride.

20. The solid oral pharmaceutical composition of claim 11, wherein the non-opioid analgesic is acetaminophen or a pharmaceutically acceptable salt thereof.

21. The solid oral pharmaceutical composition of claim 11, wherein the solid oral pharmaceutical composition is a bi-layer tablet.

30. The solid oral pharmaceutical composition of claim 15, wherein the pharmaceutically acceptable salt of the oxycodone is oxycodone hydrochloride.

31. The solid oral pharmaceutical composition of claim 11, wherein the oxycodone or the pharmaceutically acceptable salt thereof is present in an amount of 5 mg.

32. The solid oral pharmaceutical composition of claim 31, wherein the pharmaceutically acceptable salt of the oxycodone is oxycodone hydrochloride.

34. The solid oral pharmaceutical composition of claim 11, wherein the solid oral pharmaceutical composition further comprises an opioid antagonist or an additional agent for reducing abuse and/or diversion.

22. 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 comprising an antiemetic that is present in an amount of 12.5 or 25 mg; and

a layer formulated for controlled-release comprising an opioid analgesic and a non-opioid analgesic, wherein the opioid analgesic is present in an amount of 1 mg to about 20 mg, and wherein the non-opioid analgesic is acetaminophen or a pharmaceutically acceptable salt thereof that is present in an amount of about 200-600 mg,

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.

23. The solid oral pharmaceutical composition of claim 22, wherein the acetaminophen or the pharmaceutically acceptable salt thereof is present in an amount of about 325 mg.

24. The solid oral pharmaceutical composition of claim 22, wherein the opioid analgesic is hydrocodone or a pharmaceutically acceptable salt, or oxycodone or a pharmaceutically acceptable salt thereof.

25. The solid oral pharmaceutical composition of claim 24, wherein the opioid analgesic is hydrocodone bitartrate.

26. The solid oral pharmaceutical composition of claim 24, wherein the opioid analgesic is oxycodone hydrochloride.

27. The solid oral pharmaceutical composition of claim 22, wherein the antiemetic is promethazine or a pharmaceutically acceptable salt thereof.

28. The solid oral pharmaceutical composition of claim 27, wherein the antiemetic is promethazine hydrochloride.

29. The solid oral pharmaceutical composition of claim 22, wherein the solid oral pharmaceutical composition is a bi-layer tablet.

35. The solid oral pharmaceutical composition of claim 22, wherein the solid oral pharmaceutical composition further comprises an opioid antagonist or an additional agent for reducing abuse and/or diversion.