IP Library Granted Patent US 8,343,962
Granted Patent B2
US 8,343,962 · App. 12/848,792 · Granted Jan 1, 2013

Topical formulation

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Quick Facts
Patent No.
US 8,343,962
App. No.
12/848,792
Granted
Jan 1, 2013
Kind
B2
Abstract

It has been discovered that certain combinations compounds are excellent penetration enhancers and, as such, can be incorporated in a topical formulation to facilitate administration of active agents. The increased penetration enhancement can also lead to a reduction in the total concentration of skin irritants in the formulation. There is described herein a topical formulation comprising (i) at least one active agent; (ii) a first compound, and (iii) a second compound, wherein the first compound and second compound are different, and each is selected from the group consisting of N-lauroyl sarcosine, sodium octyl sulfate, methyl laurate, isopropyl myristate, oleic acid, glyceryl oleate and sodium lauryl sulfoacetate.

Claims (29)

1. A topical formulation comprising: (i) at least one active agent, (ii) a first compound, and (iii) a second compound, wherein the first compound and second compound are different, and each is selected from the group consisting of N-lauroyl sarcosine, sodium octyl sulfate, methyl laurate, isopropyl myristate, oleic acid, glyceryl oleate and sodium lauryl sulfoacetate.

2. The topical formulation of claim 1 , wherein the first compound comprises sodium lauryl sulfoacetate and the second compound comprises isopropyl myristate.

3. The topical formulation of claim 1 , wherein the first compound comprises sodium lauryl sulfoacetate and the second compound comprises methyl laurate.

4. The topical formulation of claim 1 , wherein the first compound comprises isopropyl myristate and the second compound comprises N-lauryl sarcosine.

5. The topical formulation of claim 1 , wherein the first compound comprises glyceryl monooleate and the second compound comprises methyl laurate.

6. The topical formulation of claim 1 , wherein the first compound comprises N-lauroyl sarcosine and the second compound comprises oleic acid.

7. The topical formulation of claim 1 , wherein the first compound comprises sodium octyl sulfate and the second compound comprises oleic acid.

8. The topical formulation of claim 1 , wherein the first compound comprises glyceryl oleate and the second compound comprises sodium octyl sulfate.

9. The topical formulation of claim 1 , further comprising a biologically acceptable excipient.

10. The topical formulation of claim 1 , wherein the total concentration of the first compound and the second compound is up to about 50 wt. %, 40 wt. %, 35 wt. %, 30 wt. %, 25 wt %, 20 wt. %, 15 wt. %, 10 wt. %, 7.5 wt. % or 5 wt. %, per unit volume of the formulation.

11. The topical formulation of claim 1 , wherein the total concentration of the first compound and the second compound is in the range of from about 2 wt. % to about 5 wt %, per unit volume of the formulation.

12. The topical formulation of claim 1 , wherein the total concentration of the first compound and the second compound is in the range of from about 2 wt. % to about 4 wt %, per unit volume of the formulation.

13. The topical formulation of claim 1 , wherein the weight ratio of the first compound to the second compound is in the range of from about 1:9 to about 9:1.

14. The topical formulation of claim 1 , wherein the weight ratio of the first compound to the second compound is in the range of from about 1:4 to about 4:1.

15. The topical formulation of claim 1 , wherein the weight ratio of the first compound to the second compound is in the range of from about 1:3 to about 3:1.

16. The topical formulation of claim 1 , wherein the weight ratio of the first compound to the second compound is in the range of from about 1:2 to about 2:1.

17. The topical formulation of claim 1 , wherein the weight ratio of the first compound to the second compound is about 1:1.

18. The topical formulation of claim 1 , wherein the at least one active agent is an α-aryl alkanoic acid.

19. The topical formulation of claim 18 , wherein the α-aryl alkanoic acid is an anti-inflammatory drug, such as a non-steroidal anti-inflammatory drug (NSAID), or an analgesic.

20. The topical formulation of claim 18 , wherein the α-aryl alkanoic acid is selected from the group consisting of bromfenac, diclofenac, fenoprofen, flurbiprofen, ibuprofen, indomethacin, ketoprofen, ketorolac, naproxen, sulindac and tolmetin, and pharmaceutically acceptable salts and solvates thereof and mixtures thereof.

21. The topical formulation of claim 20 , wherein the α-aryl alkanoic acid is selected from the group consisting of diclofenac, ibuprofen and ketoprofen, and pharmaceutically acceptable salts and solvates thereof, and mixtures thereof.

22. The topical formulation of claim 1 , wherein the at least one active agent is acetaminophen or an NSAID selected from the group consisting of aspirin, celecoxib, diflunisal, etodolac, etoricoxib, meclofenamic acid, mefenamic acid, meloxicam, nabumetone, oxaprozin, piroxicam, salsalate, and rofecoxib, and pharmaceutically acceptable salts and solvates thereof, and mixtures thereof.

23. The topical formulation of claim 1 , wherein the at least one active agent is a phenethylamine.

24. The topical formulation of claim 23 , wherein the phenethylamine is selected from the group consisting of antidepressants, anti-anxiety agents, anticholinergic agents, cholinergics, dopaminergics, stimulants, serotonin antaogonists, serotonin inhibitors, anti-emetics, antihistamines and/or antipsychotics.

25. The topical formulation of claim 24 , wherein the phenethylamine is selected from the group consisting of bupropion, amphetamine, hydroxyamphetamine, dextroamphetamine, methamphetamine, ephedrine, epinephrine, pseudoephedrine, dopamine, epinephryl borate, etafedrine, norepinephrine and oxidopamine, and pharmaceutically acceptable salts and solvates thereof, and mixtures thereof.

26. The topical formulation of claim 25 , wherein the phenethylamine is bupropion or a pharmaceutically acceptable salt or solvate thereof.

27. The topical formulation of claim 1 , wherein the at least one active agent is a steroid.

28. The topical formulation of claim 27 , wherein the steroid is selected from the group consisting of hormones, glucosteroids, androgens, adrenocortical steroids, anabolics, estrogens and/or progestin.

29. The topical formulation of claim 27 , wherein the steroid is testosterone or a pharmaceutically acceptable salt or solvate thereof.

Assignments (6)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 18, 2016
From: NUVO RESEARCH INC.
To: CRESCITA THERAPEUTICS INC.
Reel/Frame 039476/0616 →
CHANGE OF NAME Recorded Sep 14, 2012
From: FQUBED, INC.
To: NUVO RESEARCH US INC.
Reel/Frame 028973/0233 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 14, 2012
From: NUVO RESEARCH US, INC.
To: NUVO RESEARCH INC.
Reel/Frame 028973/0919 →
MERGER Recorded Sep 14, 2012
From: NUVO RESEARCH US INC.
To: NUVO RESEARCH US, INC.
Reel/Frame 028973/0924 →
CORRECT THE NAME OF THE ASSIGNEE RECORDED AT REEL 025125/FRAME 0691ASSIGNORS CONFIRM THE ASSIGNMENT Recorded Sep 14, 2012
From: KISAK, EDWARD T.; NEWSAM, JOHN M.; KING-SMITH, DOMINIC; KARANDE, PANKAJ; MITRAGOTRI, SAMIR
To: FQUBED, INC.
Reel/Frame 029012/0035 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 12, 2010
From: KISAK, EDWARD T.; NEWSAM, JOHN M.; KING-SMITH, DOMINIC; KARANDE, PANKAJ; MITRAGOTRI, SAMIR
To: FQUBED INC.
Reel/Frame 025125/0691 →