IP Library Granted Patent US 9,283,220
Granted Patent B2
US 9,283,220 · App. 13/076,564 · Granted Mar 15, 2016

Compositions of opioid antagonists and methods for treating conditions caused by the varicella-zoster virus therewith

Inventors: Ibrahim Mustafa Iskender Pisak (Istanbul, TR); Semra Bingol (Istanbul, TR); Mehmet Levent Selamoglu (Istanbul, TR); Mehmet Pisak (Istanbul, TR)
Assignee: IMUNEKS FARMA ILAC SANAYI VE TICARET ANONIM SIRKETI PAK IS MERKEZI
A61K31/485A61K9/0014A61K9/06A61K9/4866A61K47/32A61K47/44
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 9,283,220
App. No.
13/076,564
Granted
Mar 15, 2016
Kind
B2
Abstract

Provided are compositions comprising opioid antagonists, such as naltrexone naloxone, or nalmefene, or their pharmaceutically acceptable salts, and methods for treating conditions caused by the varicella-zoster virus therewith.

Claims (57)

1. A method for treating a vesicular eruption caused by the varicella-zoster virus, the method comprising topically administering to a subject in need thereof an effective amount of naltrexone or a pharmaceutically-acceptable salt thereof, wherein the naltrexone or the pharmaceutically-acceptable salt thereof is administered in the form of a pharmaceutical composition comprising:

a) the naltrexone or the pharmaceutically-acceptable salt thereof in an amount of about 0.1% to about 5% by weight of the pharmaceutical composition;

b) an emulsifying agent in an amount of about 2% to about 5% by weight of the pharmaceutical composition;

c) a stiffening agent in an amount of about 1% to about 45% by weight of the pharmaceutical composition;

d) a surfactant in an amount of about 0.5% to about 2.5% by weight of the pharmaceutical composition;

e) a preservative in an amount of about 0.01% to about 0.6% by weight of the pharmaceutical composition;

f) a humectant in an amount of about 1% to about 15% by weight of the pharmaceutical composition;

g) alkalizing or buffering agent in an amount of about 0.01% to about 3% by weight of the pharmaceutical composition;

h) an emollient in an amount of about 1% to about 50% by weight of the pharmaceutical composition; and

i) a solvent,

wherein the vesicular eruption regresses within 5 days of administration of the pharmaceutical composition.

2. The method of claim 1 , wherein the naltrexone or the pharmaceutically-acceptable salt thereof has less than about 10% by weight of other stereoisomers.

3. The method of claim 1 , wherein the naltrexone or the pharmaceutically-acceptable salt thereof has less than about 5% by weight of other stereoisomers.

4. The method of claim 1 , wherein the naltrexone or the pharmaceutically-acceptable salt thereof is present in an amount of about 0.5% to about 2% by weight of the pharmaceutical composition.

5. The method of claim 1 , wherein the naltrexone or the pharmaceutically-acceptable salt thereof is present in an amount of about 1% by weight of the pharmaceutical composition.

6. The method of claim 1 , wherein the pharmaceutical composition is in the form of a gel, cream, ointment, liquid, suspension, solution, emulsion, foam, or aerosol.

7. The method of claim 1 , wherein the pharmaceutical composition is administered to the subject by spreading or spraying the composition onto the affected area.

8. The method of claim 1 , wherein the naltrexone or the pharmaceutically-acceptable salt thereof is administered in a total daily dose of up to about 150 mg/cm 2 of skin.

9. The method of claim 1 , wherein the naltrexone or the pharmaceutically-acceptable salt thereof is administered in a total daily dose of about 10 mg/cm 2 to about 100 mg/cm 2 of skin.

10. The method of claim 1 , wherein the naltrexone or the pharmaceutically-acceptable salt thereof is administered in a total daily dose of about 50 mg/cm 2 of skin.

11. The method of claim 1 , wherein the pharmaceutical composition is administered 1, 2, 3, 4, or 5 times daily.

12. The method of claim 1 , further comprising administering to the subject one or more additional agents effective to treat the vesicular eruption.

13. The method of claim 12 , wherein the additional agent is acyclovir, valacyclovir, or famciclovir.

14. The method of claim 1 , wherein the administration blocks an opioid receptor in the subject.

15. The method of claim 14 , wherein the opioid receptor that is blocked is a mu (μ) opioid receptor.

16. The method of claim 14 , wherein the opioid receptor that is blocked is a delta (δ) opioid receptor.

17. The method of claim 14 , wherein the opioid receptor that is blocked is a kappa (κ) opioid receptor.

18. The method of claim 1 , wherein the method further comprises treating post-herpetic neuralgia caused by varicella-zoster virus in the subject.

19. The method of claim 1 , wherein a pain of the subject associated with the varicella-zoster virus regresses within 3 days of administration.

20. The method of claim 1 , wherein an itching of the subject associated with the varicella-zoster virus regresses within 3 days of administration.

21. The method of claim 1 , wherein a hyperesthesis of the subject associated with the varicella-zoster virus regresses within 3 days of administration.

22. The method of claim 1 , wherein an itching, pain, and hyperesthesis of the subject associated with the varicella-zoster virus regresses within 3 days of administration.

23. The method of claim 1 , wherein no additional treatment is required to treat the vesicular eruption.

24. The method of claim 1 , wherein the administration produces no side-effect in the subject.

25. The method of claim 1 , wherein the administration occurs daily.

26. The method of claim 1 , wherein the administration occurs three times daily.

27. The method of claim 1 , wherein the naltrexone or the pharmaceutically-acceptable salt thereof is administered in a total daily amount of about 1 g.

28. The method of claim 1 , wherein the pharmaceutical composition comprises:

a) the naltrexone or the pharmaceutically-acceptable salt thereof in an amount of about 0.5% to about 2% by weight of the pharmaceutical composition;

b) the emulsifying agent in an amount of about 2% to about 5% by weight of the pharmaceutical composition;

c) the stiffening agent in an amount of about 2% to about 5% by weight of the pharmaceutical composition;

d) the surfactant in an amount of about 0.5% to about 1.5% by weight of the pharmaceutical composition;

e) the preservative in an amount of about 0.01% to about 0.6% by weight of the pharmaceutical composition;

f) the humectant in an amount of about 2% to about 10% by weight of the pharmaceutical composition;

g) the alkalizing or buffering agent in an amount of about 0.01% to about 3% by weight of the pharmaceutical composition;

h) the emollient in an amount of about 15% to about 30% by weight of the pharmaceutical composition; and

i) the solvent.

29. The method of claim 1 , wherein the pharmaceutical composition comprises:

a) the naltrexone or the pharmaceutically-acceptable salt thereof in an amount of about 1% by weight of the pharmaceutical composition;

b) the emulsifying agent, wherein the emulsifying agent is cetyl alcohol in an amount of about 3.6% by weight of the pharmaceutical composition, and carboxypolymethylene in an amount of about 0.2% by weight of the pharmaceutical composition;

c) the stiffening agent in an amount of about 3.6% by weight of the pharmaceutical composition, wherein the stiffening agent is stearyl alcohol;

d) the surfactant in an amount of about 0.8% by weight of the pharmaceutical composition, wherein the surfactant is sodium lauryl sulfate;

e) the preservative, wherein the preservative is nipagin in an amount of about 0.1% by weight of the pharmaceutical composition, and nipasol in an amount of about 0.05% by weight of the pharmaceutical composition;

f) the humectant in an amount of about 5% by weight of the pharmaceutical composition, wherein the humectant is propylene glycol;

g) the alkalizing or buffering agent in an amount of about 0.03% by weight of the pharmaceutical composition, wherein the alkalizing or buffering agent is sodium hydroxide;

h) the emollient, wherein the emollient is white vaseline in an amount of about 13.5% by weight of the pharmaceutical composition, and liquid vaseline in an amount of about 5.4% by weight of the pharmaceutical composition; and

i) the solvent, wherein the solvent is water.

Assignments (4)
CHANGE OF NAME Recorded Aug 2, 2013
From: AK FARMA ILAC SANAYI VE TICARET ANONIM SIRKETI
To: IMUNEKS FARMA ILAC SANAYI VE TICARET ANONIM SIRKETI
Reel/Frame 030954/0612 →
CHANGE OF NAME Recorded Apr 18, 2013
From: AK KIMYA ITHALAT IHRACAT VE SANAYI ANONIM SIRKETI
To: AK FARMA ILAC SANAYI VE TICARET ANONIM SIRKETI
Reel/Frame 030249/0201 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 15, 2011
From: MUSTAFA NEVZAT ILAC SANAYII A.S.
To: AK KIMYA ITHALAT-IHRACAT VE SANAYII A.S.
Reel/Frame 026750/0632 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 26, 2011
From: PISAK, IBRAHIM MUSTAFA ISKENDER; BINGOL, SEMRA; SELAMOGLU, MEHMET LEVENT; PISAK, MEHMET
To: MUSTAFA NEVZAT ILAC SANAYII A.S.
Reel/Frame 026343/0191 →
Priority Claims (1)
TR 2010/02473 · Mar 31, 2010 · national
Continuity (1)
Related Publication 20110245278A1 · Oct 6, 2011