IP Library › Granted Patent US 12,357,561
Granted Patent B2
US 12,357,561 · App. 17/933,929 · Granted Jul 15, 2025

Compositions and uses of alpha-adrenergic agents

Inventors: Frank Litvack (Los Angeles, CA); Houman Hemmati (Los Angeles, CA)
Assignee: LEVATION PHARMA LTD.
A61K9/0014A61K8/4946A61K9/0019A61K9/0048A61K31/4174A61P21/00A61P27/02A61Q1/10A61Q19/00
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Quick Facts
Patent No.
US 12,357,561
App. No.
17/933,929
Granted
Jul 15, 2025
Kind
B2
Abstract

The disclosure provides cosmetic and therapeutic compositions of alpha-adrenergic agents. Compositions of the disclosure may be used for topical, transdermal or parenteral administration to the eye or eyelid. The compositions of the disclosure may be used cosmetically to improve the appearance of the eye or therapeutically to treat ptosis.

Claims (23)

1. A method for increasing the vertical separation of the upper and lower eyelids of an eye of a subject, comprising:

administering to the exterior surface of the upper eyelid of the subject a cosmetic gel composition comprising an alpha-adrenergic agent, a permeation enhancer, and one or more cosmetic excipients,

wherein the alpha-adrenergic agent is oxymetazoline or a salt thereof,

wherein increasing the vertical separation of the upper and lower eyelids comprises retraction of the upper eyelids by about 0.5 mm or more.

2. The method of claim 1 , wherein the one or more cosmetic excipients are individually selected from sunscreens, fragrances, pigments and antioxidants.

3. The method of claim 1 , wherein the gel composition further comprises one or more dermatologically acceptable carriers.

4. The method of claim 3 , wherein the one or more dermatologically acceptable carriers are individually selected from buffers, preservatives, gelling agents, rheological modifiers and stabilizers, moisturizers, and humectants.

5. The method of claim 1 , wherein the administering comprises applying a dose to the exterior upper eyelid to the subject, wherein the dose comprises from about 0.5 mg to about 4 mg of the alpha-adrenergic agent.

6. The method of claim 1 , wherein the administering comprises applying a dose to the exterior upper eyelid to the subject, wherein the dose comprises from about 0.5 mg to about 3 mg of the alpha-adrenergic agent.

7. The method of claim 1 , wherein the administering comprises applying a dose to the exterior upper eyelid to the subject, wherein the dose comprises from about 0.5 mg to about 2 mg of the alpha-adrenergic agent.

8. The method of claim 1 , wherein the administering comprises applying a dose to the exterior upper eyelid to the subject, wherein the dose comprises about 2 mg of the alpha-adrenergic agent.

9. The method of claim 1 , wherein the administering comprises applying a dose to the exterior upper eyelid to the subject, wherein the dose comprises about 1 mg of the alpha-adrenergic agent.

10. The method of claim 1 , wherein the permeation enhancer is less than 40% by weight of the total composition.

11. The method of claim 1 , wherein the permeation enhancer comprises an alcohol.

12. The method of claim 1 , wherein the permeation enhancer is selected from ethanol, propylene glycol, dodecyl-N,N-dimethyl-aminoacetate, ethylacetate, azone, sodium dodecyl sulfate, d-limonene, oleic acid, 1,3-diphenyl-urea, N-methyl-2-pyrrolidone, beta-cyclodextrin, and dimethylsulfoxide.

13. The method of claim 12 , wherein the permeation enhancer is propylene glycol.

14. The method of claim 1 , wherein the permeation enhancer increases skin permeation of oxymetazoline or a salt thereof by about 2-fold or greater relative to a composition without the permeation enhancer.

15. The method of claim 14 , wherein the permeation enhancer increases skin permeation of oxymetazoline or a salt thereof by about 3-fold or greater relative to a composition without the permeation enhancer.

16. The method of claim 1 , wherein the permeation enhancer increases skin permeation of oxymetazoline or a salt thereof by about 0.5 mm or more relative to a composition without the permeation enhancer.

17. The method of claim 1 , wherein oxymetazoline or a salt thereof permeates through the stratum corneum and septal fat pad to contact Müller's muscle.

18. The method of claim 1 , wherein the gel composition is a controlled-release composition.

19. The method of claim 1 , wherein the increasing the vertical separation of the upper and lower eyelids comprises retracting the upper eyelid by about 1 mm or more.

20. The method of claim 1 , wherein retraction of the upper eyelids by about 0.5 mm or more comprises an increase in the vertical separation of the upper and lower eyelids relative to the position of the eyelids prior to administration of oxymetazoline or a salt.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 30, 2023
From: LITVACK, FRANK; HEMMATI, HOUMAN
To: LEVATION PHARMA LTD.
Reel/Frame 062535/0001 →
Continuity (5)
Continuation 17064327 · Oct 6, 2020
Division 16043725 · Jul 24, 2018
Continuation PCTUS2017015181 · Jan 26, 2017
Provisional Application 62287391 · Jan 26, 2016
Related Publication 20230181455A1 · Jun 15, 2023
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