IP Library Granted Patent US 7,897,587
Granted Patent B2
US 7,897,587 · App. 10/933,976 · Granted Mar 1, 2011

Topical dermatological formulations and use thereof

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Quick Facts
Patent No.
US 7,897,587
App. No.
10/933,976
Granted
Mar 1, 2011
Kind
B2
Abstract

A topical formulation of an androstane steroid compound of improved solubility in combinations of the solvents propylene glycol and propylene carbonate.

Claims (112)

1. An ointment consisting of on a w/w % basis

Component

%

Fluticasone

0.05

propionate

Microcrystalline

30

Wax

Sorbitan

1.5

sesquioleate

Glycerol

1.5

monostearate

Oleic acid

2.5

Butylated

0.05

hydroxytoluene

Propylene

0.825

glycol

Propylene

2.475

carbonate

Mineral oil

61.1

and the total of the propylene glycol and propylene carbonate components is about 10% or less.

2. An ointment consisting of on a w/w % basis

Component

w/w %

Fluticasone

0.02

propionate

Microcrystalline

30

Wax

Sorbitan

2

sesquioleate

Glycerol

1.5

monostearate

Oleic acid

1

Butylated

0.05

hydroxytoluene

Propylene

3.15

glycol

Propylene

1.05

carbonate

Mineral oil

61.23.

3. An ointment consisting of on a w/w % basis

Component

w/w %

Fluticasone

0.075

propionate

Microcrystalline

30

Wax

Sorbitan

3

sesquioleate

Glycerol

1.5

monostearate

Oleic acid

2.5

Butylated

0.05

hydroxytoluene

Propylene

1.25

glycol

Propylene

3.75

carbonate

Mineral oil

57.875.

4. A method for treating a skin condition selected from atopic dermatitis, eczema, erthema, pruritus, impetigo, sporiasis, and inflammation, the process comprising topically applying to the skin a composition of claim

5. A cream composition for topical administration consisting of:

(a) about 0.05-0.2 wt-% fluticasone propionate;

(b) about 2.5-20 wt-% propylene carbonate;

(c) about 2.0-20 wt-% propylene glycol;

wherein the propylene carbonate is about 4.8-95 wt-% of the combination of (b) and (c);

(d) about 1.0-10 wt-% surfactant;

(e) about 2.0-40 wt-% of one or more emollients;

(f) about 5-20 wt-% of an occlusive agent selected from the group consisting of mineral oil, wax and a mixture thereof;

(g) the balance, water;

wherein the cream is an oil-in-water emulsion.

6. The cream of claim 5 wherein the surfactant is ceteareth-20.

7. The cream of claim 5 wherein the occlusive agent is mineral oil.

8. The cream of claim 7 wherein the mineral oil is in the amount of about 1-10 wt-%.

9. The cream of claim 5 wherein the occlusive agent is a mixture of wax and mineral oil.

10. The cream of claim 9 wherein the wax is in the amount of about 5-15 wt-%.

11. The cream of claim 5 wherein the weight ratio of propylene carbonate to propylene glycol in the composition is from about 88:12 to about 45:55.

12. The cream of claim 11 wherein the weight ratio of propylene carbonate to propylene glycol in the composition is about 88:12.

13. A non-aqueous ointment consisting of on a wt/wt % basis

(a) about 0.05-0.2% fluticasone propionate;

(b) about 1-10% of a surfactant selected from the group consisting of sorbitan sesquioleate, glycerol monostearate, sorbitan monostearate, and mixtures thereof;

(c) about 40-75% mineral oil;

(d) about 2.5-7.5% propylene carbonate;

(e) about 2.5-7.5% propylene glycol, wherein the combination of (d) and (e) is about 10% or less;

(f) about 0-0.6% benzyl alcohol, butylated hydroxyanisole, butylated hydroxytolulene, butyl paraben or disodium edetate; and

(g) an effective amount of an occlusive agent consisting of at least one wax.

14. The ointment of claim 13 wherein the wax is in the amount of about 20-30 wt-%.

Assignments (5)
PATENT RELEASE Recorded Mar 20, 2015
From: ROYAL BANK OF CANADA, AS COLLATERAL AGENT
To: FOUGERA PHARMACEUTICALS INC. (F.K.A. NYCOMED US INC.)
Reel/Frame 035233/0381 →
PATENT SECURITY AGREEMENT Recorded Oct 21, 2011
From: FOUGERA PHARMACEUTICALS INC. (F.K.A. NYCOMED US INC.)
To: ROYAL BANK OF CANADA, AS COLLATERAL AGENT
Reel/Frame 027103/0716 →
CHANGE OF NAME Recorded Oct 5, 2011
From: NYCOMED US INC.
To: FOUGERA PHARMACEUTICALS INC.
Reel/Frame 027021/0146 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 7, 2010
From: THERAPEUTICS INCORPORATED
To: NYCOMED US INC.
Reel/Frame 023755/0711 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 3, 2004
From: JOHNSON, KEITH A.
To: THERAPEUTICS INCORPORATED
Reel/Frame 015781/0471 →