IP Library Granted Patent US 10,933,018
Granted Patent B2
US 10,933,018 · App. 15/772,456 · Granted Mar 2, 2021

Isotretinoin formulations and uses and methods thereof

Inventors: Zachary Rome (Nyack, NY); Charles Rodney Greenaway Evans (Worthing, GB); Marc Barry Brown (Herts, GB); Francesco Caserta (Aldershot, GB)
Assignee: Timber Pharmaceuticals LLC
A61K9/06A61K31/198A61K31/203A61K45/06A61K47/10A61Q19/00
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Quick Facts
Patent No.
US 10,933,018
App. No.
15/772,456
Granted
Mar 2, 2021
Kind
B2
Abstract

Provided herein are novel isotretinoin formulations that provide an enhanced targeted dermal delivery system for the drug isotretinoin with improved thermodynamic activity using no to a small level of ethanol relative to existing isotretinoin gel products, and methods for treatment of ichthyosis and other skin conditions using the same.

Claims (12)

1. A pharmaceutical composition consisting of PEG 400, PEG 3350, PEG 1450, butylated hydroxytoluene (BHT), methyl paraben, propyl paraben, and about 0.01% w/w to about 0.6% w/w isotretinoin, wherein the pharmaceutical composition has 0% w/w of ethanol and 0% w/w of water, and is formulated as a gel, ointment, lotion, emulsion, or cream.

2. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition has about 69% to about 70% w/w PEG 400, about 15% w/w PEG 3350 and about 15% w/w PEG 1450.

3. The pharmaceutical composition of claim 2 , wherein the pharmaceutical composition has about 0.2% w/w methyl paraben and about 0.02% w/w propyl paraben.

4. The pharmaceutical composition of claim 3 , wherein the pharmaceutical composition has about 0.1% w/w BHT.

5. A pharmaceutical composition consisting of about 0.01% w/w to about 0.2% w/w isotretinoin, about 69% w/w to about 70% w/w PEG 400, about 15% w/w PEG 3350, about 15% w/w PEG 1450, about 0.1% w/w butylated hydroxytoluene (BHT), about 0.2% w/w methyl paraben, and about 0.02% w/w propyl paraben, wherein the pharmaceutical composition has 0% w/w of ethanol and 0% w/w of water, and is formulated as a gel, ointment, lotion, emulsion, or cream.

6. The pharmaceutical composition of claim 5 , wherein the pharmaceutical composition has about 0.01% w/w, about 0.025% w/w, about 0.05% w/w, about 0.1% w/w, about 0.15% w/w, or about 0.2% w/w isotretinoin.

7. A pharmaceutical composition consisting of 0.01% w/w to 0.2% w/w isotretinoin, 69% w/w to 70% w/w PEG 400, 14.78% w/w PEG 3350, 15% w/w PEG 1450, 0.1% w/w butylated hydroxytoluene (BHT), 0.2% w/w methyl paraben, and 0.02% w/w propyl paraben, wherein the pharmaceutical composition has 0% w/w of ethanol and 0% w/w of water, and is formulated as a gel, ointment, lotion, emulsion, or cream.

8. The pharmaceutical composition of claim 7 , wherein the pharmaceutical composition has 0.01% w/w, 0.025% w/w, 0.05% w/w, 0.1% w/w, 0.15% w/w, or 0.2% w/w isotretinoin.

9. A pharmaceutical composition consisting of PEG 400, PEG 3350, PEG 1450, butylated hydroxytoluene (BHT), methyl paraben, propyl paraben, and 0.01% w/w to 0.6% w/w isotretinoin, wherein the pharmaceutical composition has 0% w/w of ethanol and 0% w/w of water, and is formulated as a gel, ointment, lotion, emulsion, or cream.

10. The pharmaceutical composition of claim 9 , wherein the pharmaceutical composition has 69% to 70% w/w PEG 400, 15% w/w PEG 3350 and 15% w/w PEG 1450.

11. The pharmaceutical composition of claim 10 , wherein the pharmaceutical composition has 0.2% w/w methyl paraben and 0.02% w/w propyl paraben.

12. The pharmaceutical composition of claim 11 , wherein the pharmaceutical composition has 0.1% w/w BHT.

Assignments (13)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 11, 2024
From: TIMBER PHARMACEUTICALS, INC.; TIMBER PHARMACEUTICALS, LLC; BIOPHARMX, INC.
To: LEO PHARMA A/S
Reel/Frame 066782/0409 →
RELEASE OF SECURITY INTEREST Recorded Jan 23, 2024
From: LEO US HOLDING, INC.
To: TIMBER PHARMACEUTICALS, INC.; TIMBER PHARMACEUTICALS LLC
Reel/Frame 066216/0835 →
RELEASE OF SECURITY INTEREST Recorded Jan 23, 2024
From: LEO US HOLDING, INC.
To: TIMBER PHARMACEUTICALS, INC.; TIMBER PHARMACEUTICALS LLC
Reel/Frame 066216/0619 →
SECURITY INTEREST Recorded Nov 29, 2023
From: TIMBER PHARMACEUTICALS, INC.; TIMBER PHARMACEUTICALS LLC
To: LEO US HOLDING, INC.
Reel/Frame 065702/0064 →
SECURITY INTEREST Recorded Aug 31, 2023
From: TIMBER PHARMACEUTICALS, INC.; TIMBER PHARMACEUTICALS LLC
To: LEO US HOLDING, INC.
Reel/Frame 064766/0151 →
RELEASE OF SECURITY INTEREST Recorded Aug 23, 2023
From: TIMBER PHARMACEUTICALS LLC
To: PATAGONIA PHARMACEUTICALS LLC
Reel/Frame 064682/0001 →
CORRECTIVE ASSIGNMENT TO CORRECT THE FIRST PAGE OF THE UCC FINANCING STATMENT TO NAME PATAGONIA PHARMACEUTICALS LLC AS THE SECURED PARTY PREVIOUSLY RECORDED AT REEL: 060624 FRAME: 0380. ASSIGNOR(S) HEREBY CONFIRMS THE SECURITY INTEREST . Recorded Jul 29, 2022
From: TIMBER PHARMACEUTICALS LLC
To: PATAGONIA PHARMACEUTICALS LLC
Reel/Frame 060978/0984 →
SECURITY INTEREST Recorded Jul 26, 2022
From: TIMBER PHARMACEUTICALS LLC
To: PATAGONIA PHARMACEUTICALS LLC
Reel/Frame 060624/0380 →
CHANGE OF ADDRESS FOR ASSIGNEE Recorded Feb 14, 2022
From: TIMBER PHARMACEUTICALS LLC
To: TIMBER PHARMACEUTICALS LLC
Reel/Frame 059122/0532 →
RELEASE OF SECURITY INTEREST Recorded May 28, 2020
From: EMPERY DEBT OPPORTUNITY FUND, LP
To: TIMBER PHARMACEUTICALS LLC
Reel/Frame 052781/0989 →
INTELLECTUAL PROPERTY SECURITY AGREEMENT Recorded Jan 29, 2020
From: TIMBER PHARMACEUTICALS LLC
To: EMPERY DEBT OPPORTUNITY FUND, LP, AS COLLATERAL AGENT
Reel/Frame 051735/0965 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 18, 2019
From: PATAGONIA PHARMACEUTICALS, LLC
To: TIMBER PHARMACEUTICALS LLC
Reel/Frame 048930/0735 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 23, 2018
From: ROME, ZACHARY; EVANS, CHARLES RODNEY GREENAWAY; BROWN, PHD., PROFESSOR MARC BARRY; CASERTA, DR. FRANCESCO
To: PATAGONIA PHARMACEUTICALS, LLC
Reel/Frame 046686/0450 →
Continuity (3)
Provisional Application 62301759 · Mar 1, 2016
Provisional Application 62248760 · Oct 30, 2015
Related Publication 20180318245A1 · Nov 8, 2018