Compositions and methods for treating severe pain

Patent metadata

Field	Value
Publication number	US-9795577-B2
Application number	US-201615295933-A
Country	US
Kind code	B2
Filing date	Oct 17, 2016
Priority date	Oct 29, 2010
Publication date	Oct 24, 2017
Grant date	Oct 24, 2017

Abstract

The present specification discloses pharmaceutical compositions, methods of preparing such pharmaceutical compositions, and methods and uses of treating a chronic inflammation and/or an inflammatory disease in an individual using such pharmaceutical compositions.

First claim

The invention claimed is:

1. A method of treating an individual with an inflammatory pain, the method comprising the step of: administering to the individual in need thereof a pharmaceutical composition, wherein the pharmaceutical composition comprises:
a) a naproxen, or a pharmaceutically acceptable salt, solvate, or solvate of a salt thereof, in an amount of about 15% to about 30% of the total weight of the composition;
b) a pharmaceutically-acceptable lipid in an amount of at least 60% of the total weight of the composition, the pharmaceutically-acceptable lipid comprising a pharmaceutically-acceptable fat in an amount of at least 30% of the total weight of the composition, the pharmaceutically-acceptable fat comprising a triglyceride, an acetylated triglyceride and/or a triester of glycerol and a pharmaceutically-acceptable monoglyceride in an amount of at least 30% of the total weight of the composition,
wherein the pharmaceutical composition does not comprise a surfactant, and
wherein the pharmaceutical composition is formulated to be a solid at a temperature of about 15° C. or lower and have a melting point temperature of about 25° C. or higher.

2. The method according to claim 1 , wherein the inflammatory pain is an acute pain, a subacute pain, a chronic pain, or any combination thereof.

3. The method according to claim 1 , wherein the inflammatory pain is a nociceptive pain, a pathological pain, a referred pain, a headache, or any combination thereof.

4. The method according to claim 3 , wherein the nociceptive pain is a visceral pain, a deep somatic pain, a superficial somatic pain, or any combination thereof.

5. The method according to claim 3 , wherein the pathological pain is a neuropathic pain, a dysfunctional pain, or any combination thereof.

6. The method according to claim 5 , wherein the neuropathic pain is a central neuropathic pain, a peripheral neuropathic pain, a deafferentation pain, or any combination thereof.

7. The method according to claim 6 , wherein the peripheral neuropathic pain is a mononeuropathy, a mononeuropathic multiplex, a polyneuropathy, or an autonomic neuropathy.

8. The method according to claim 7 , wherein the polyneuropathy is a distal axonopathy, a myelinopathy, or a neuronopathy.

9. The method according to claim 6 , wherein the peripheral neuropathic pain is a neuralgia or a complex regional pain syndrome.

10. The method according to claim 3 , wherein the headache is a muscular/myogenic headache, a vascular headache, a migraine, a traction headache, inflammatory headache, a chronic sinusitis headache, a hormone headache, a rebound headache, an organic headache, or an ictal headache.

11. The method according to claim 1 , wherein upon administration to an individual, there is an increase in bio-distribution of the naproxen, or a pharmaceutically acceptable salt, solvate, or solvate of a salt thereof into macrophages by at least 5% when compared to bio-distribution of the naproxen, or a pharmaceutically acceptable salt, solvate, or solvate of a salt thereof comprises in the same pharmaceutical composition, except without the pharmaceutically-acceptable lipid.

12. The method according to claim 1 , wherein upon administration to an individual, the amount of the naproxen, or a pharmaceutically acceptable salt, solvate, or solvate of a salt thereof of the pharmaceutical composition delivered to a macrophage is at least 10% of the total amount of the naproxen, or a pharmaceutically acceptable salt, solvate, or solvate of a salt thereof contained in the administered pharmaceutical composition.

13. The method according to claim 1 , wherein upon administration to an individual, the pharmaceutical composition reduces intestinal and/or gastric irritation by at least 10% when compared to the same pharmaceutical composition, except without the pharmaceutically-acceptable lipid.

14. The method according to claim 1 , wherein the naproxen, or a pharmaceutically acceptable salt, solvate, or solvate of a salt thereof, is in an amount of about 20% to about 30% of the total weight of the composition.

15. The method according to claim 1 , wherein the triglyceride comprises a mixtures of saturated C 10 -C 18 triglycerides having a melting point around 43° C.

16. The method according to claim 1 , wherein the pharmaceutically-acceptable lipid is in an amount of at least 70% of the total weight of the composition.

17. The method according to claim 16 , wherein the pharmaceutically-acceptable fat is in an amount of at least 35% of the total weight of the composition.

18. The method according to claim 16 , wherein the pharmaceutically-acceptable monoglyceride is in an amount of at least 35% of the total weight of the composition.

19. The method according to claim 1 , wherein the pharmaceutically-acceptable lipid is in an amount of at least 75% of the total weight of the composition.

20. The method according to claim 19 , wherein the pharmaceutically-acceptable fat is in an amount of at least 35% of the total weight of the composition.

21. The method according to claim 19 , wherein the pharmaceutically-acceptable monoglyceride is in an amount of at least 35% of the total weight of the composition.

22. The method according to claim 1 , wherein the pharmaceutically-acceptable monoglyceride is a glyceryl monolinoleate.

23. The method according to claim 1 , further comprising a pharmaceutically-acceptable liquid polyethylene glycol (PEG) polymer in an amount less than about 15% of the total weight of the composition.

24. The method according to claim 23 , wherein the pharmaceutically-acceptable liquid PEG polymer is in an amount of about 1% to about 10% of the total weight of the composition.

Assignees

• Infirst Healthcare Ltd

Inventors

• Bannister Robin M
• Brew John

Classifications

• A61K31/4035

  Isoindoles, e.g. phthalimide · CPC title

• A61K31/381

  having five-membered rings · CPC title

• A61K9/06

  Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)} · CPC title

• A61K31/421

  1,3-Oxazoles, e.g. pemoline, trimethadione · CPC title

• A61K31/194

  having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid · CPC title