IP Library Granted Patent US 9,498,444
Granted Patent B2
US 9,498,444 · App. 14/789,886 · Granted Nov 22, 2016

Pharmaceutical compositions

Inventors: Paul Bosse (Jupiter, FL); John Ameling (Jupiter, FL); Bernard Schachtel (Jupiter, FL); Ray Takigiku (Loveland, OH)
Assignee: LOCL PHARMA, INC.
A61K9/209A61K9/2027A61K9/2054A61K9/4808A61K31/165A61K31/167A61K31/24A61K31/403A61K31/404A61K31/4196A61K31/422A61K31/437A61K31/454A61K31/485A61K31/515A61K31/522A61K31/5415A61K45/06A61K9/0024A61K9/1694A61K47/36
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Quick Facts
Patent No.
US 9,498,444
App. No.
14/789,886
Granted
Nov 22, 2016
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 (36)

1. A method for treating pain, and reducing or preventing opioid-induced nausea or vomiting, the method comprising administering a solid oral pharmaceutical composition to a subject in need thereof, wherein the solid oral pharmaceutical composition comprises:

an immediate-release matrix comprising an antiemetic; and

a controlled-release matrix comprising an opioid analgesic and a non-opioid analgesic, wherein the solid oral pharmaceutical composition demonstrates the following dissolution profile: wherein about 90% of the antiemetic is released in about 1 minute to about 20 minutes following contact of the solid oral pharmaceutical composition with a dissolution fluid as measured by a USP Apparatus 2 (Paddle Apparatus), wherein about 30% to about 60% of the opioid analgesic is released in about 5 to 10 minutes following contact of the solid oral pharmaceutical composition with a dissolution fluid as measured by a USP Apparatus 2 (Paddle Apparatus), and wherein about 100% of the opioid analgesic is released in about 60 minutes following contact of the solid oral pharmaceutical composition with a dissolution fluid as measured by a USP Apparatus 2 (Paddle Apparatus), and

wherein the solid oral pharmaceutical composition provides an effective amount of the opioid analgesic and the non-opioid analgesic to treat pain, 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.

2. The method of claim 1 , wherein the opioid analgesic is hydrocodone, oxycodone, acetyldihydrocodeinone, diamorphine, codeine, pethidine, alfentanil, buprenorphine, butorphanol, codeine, dezocine, fentanyl, hydromorphone, levomethadyl acetate, levorphanol, meperidine, methadone, morphine sulfate, nalbuphine, oxymorphone, pentazocine, propoxyphene, remifentanil, sufentanil, tramadol, or a pharmaceutically acceptable salt thereof.

3. The method of claim 1 , wherein the opioid analgesic is present in an amount of about 5 mg, about 7.5 mg, about 10 mg, about 15 mg, about 20 mg, or about 30 mg.

4. The method of claim 2 , wherein the opioid analgesic is hydrocodone bitartrate.

5. The method 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 method of claim 5 , wherein the pharmaceutically acceptable salt of the hydrocodone is hydrocodone bitartrate, and is present in an amount of about 7.5 mg.

7. The method of claim 1 , wherein the opioid analgesic is hydrocodone or a pharmaceutically acceptable salt thereof, and is present in an amount of about 5 mg or about 10 mg.

8. The method of claim 3 , wherein the opioid analgesic is hydrocodone or a pharmaceutically acceptable salt thereof, or oxycodone or a pharmaceutically acceptable salt thereof.

9. The method of claim 8 , wherein the opioid analgesic is oxycodone or the pharmaceutically acceptable salt thereof, and is present in an amount of about 7.5 mg.

10. The method of claim 8 , wherein the opioid analgesic is oxycodone or the pharmaceutically acceptable salt thereof, and is present in an amount of about 5 mg.

11. The method of claim 2 , wherein the opioid analgesic is a pharmaceutically acceptable salt of oxycodone that is oxycodone hydrochloride.

12. The method of claim 1 , wherein the antiemetic is promethazine or a pharmaceutically acceptable salt thereof.

13. The method of claim 12 , wherein the promethazine or the pharmaceutically acceptable salt thereof is present in an amount of about 11-14 mg.

14. The method of claim 13 , wherein the promethazine or the pharmaceutically acceptable salt thereof is present in an amount of about 12.5 mg.

15. The method of claim 14 , wherein the pharmaceutically acceptable salt of the promethazine is promethazine hydrochloride, and is present in an amount of about 12.5 mg.

16. The method of claim 13 , wherein the promethazine or the pharmaceutically acceptable salt thereof is present in an amount of about 11 mg.

17. The method of claim 12 , wherein the antiemetic is the pharmaceutically acceptable salt of the promethazine that is promethazine hydrochloride.

18. The method of claim 1 , wherein the non-opioid analgesic is acetaminophen or a pharmaceutically acceptable salt thereof.

19. The method of claim 18 , wherein the acetaminophen or the pharmaceutically acceptable salt thereof is present in an amount of about 290-360 mg.

20. The method of claim 19 , wherein the acetaminophen or the pharmaceutically acceptable salt thereof is present in an amount of about 325 mg.

21. The method of claim 1 , wherein the antiemetic is present in an amount of about 0.5 mg to about 60 mg.

22. The method of claim 1 or 21 , wherein the antiemetic is aprepitant, dronabinol, perphenazine, palonosetron, trimethyobenzamide, metoclopromide, domperidone, prochlorperazine, promethazine, chlorpromazine, trimethobenzamide, ondansetron, granisetron, hydroxyzine, acetylleucine monoethanolamine, alizapride, azasetron, benzquinamide, bietanautine, bromopride, buclizine, clebopride, cyclizine, dimenhydrinate, diphenidol, dolasetron, meclizine, methallatal, metopimazine, nabilone, oxyperndyl, pipamazine, scopolamine, sulpiride, tetrahydrocannabinol, thiethylperazine, thioproperazine, tropisetron, droperidol, haloperidol, prochloperazine, metoclopramide, diphenhydramine, cannabis, midazolam, lorazepam, hyoscine, dexamethasone, emetrol, propofol, or a pharmaceutically acceptable salt thereof.

23. The method of claim 21 , wherein the antiemetic is promethazine or a pharmaceutically acceptable salt thereof, and is present in an amount of about 12.5 mg, about 25 mg, or about 50 mg.

24. The method of claim 1 , wherein the non-opioid analgesic is present in an amount of about 200 mg to about 1000 mg.

25. The method of claim 24 , wherein the non-opioid analgesic is acetaminophen, ibuprofen, ketaprofen, naproxen, aspirin, or a pharmaceutically acceptable salt thereof.

26. The method of claim 1 , wherein the immediate-release matrix is a first layer and the controlled-release matrix is a second layer.

27. The method of any one of claim 1 - 17 , 18 - 20 , 21 , or 23 - 26 , wherein the solid oral pharmaceutical composition is a tablet.

28. The method of claim 27 , wherein the tablet has a thickness of about 6.5 mm or a hardness of about 15 kp.

29. The method of claim 27 , wherein the tablet is a bi-layer tablet.

30. The method of claim 1 , 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 for about 4 to about 6 hours, and an effective amount of the opioid analgesic and the non-opioid analgesic to treat pain for about 4 to about 6 hours.

31. The method of claim 1 , wherein the opioid analgesic is hydrocodone or a pharmaceutically acceptable salt thereof, wherein the non-opioid analgesic is acetaminophen or a pharmaceutically acceptable salt thereof, and wherein the antiemetic is promethazine or a pharmaceutically acceptable salt thereof.

32. The method of claim 7 , wherein the pharmaceutically acceptable salt of the hydrocodone is hydrocodone bitartrate, and is present in an amount of about 5 mg or about 10 mg.

33. The method of claim 1 , wherein the solid oral pharmaceutical composition further comprises an opioid antagonist or an abuse deterrent agent.

Assignments (3)
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 1, 2015
From: CHARLESTON LABORATORIES, INC.
To: LOCL PHARMA, INC.
Reel/Frame 035989/0708 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 1, 2015
From: BOSSE, PAUL; AMELING, JOHN; SCHACHTEL, BERNARD; TAKIGIKU, RAY
To: CHARLESTON LABORATORIES, INC
Reel/Frame 035990/0743 →
Continuity (7)
Continuation 14036946 · Sep 25, 2013
Continuation 13347552 · Jan 10, 2012
Continuation 12351704 · Jan 9, 2009
Provisional Application 61020139 · Jan 9, 2008
Provisional Application 61043037 · Apr 7, 2008
Provisional Application 61060758 · Jun 11, 2008
Related Publication 20150297525A1 · Oct 22, 2015