Topical formulations comprising a steroid
View Patent ↗The application provides formulations for the topical administration of an active agent comprising at least one steroid, in the form of topical sprays that are propellant-free, and/or substantially non-foaming, and/or alcohol-free. The present application also provides processes for preparing such compositions and methods of using them in management of skin diseases or disorders such as psoriasis, dermatoses, and other associated skin diseases or disorders.
1. A dispensing device for administration of a topical composition comprising a steroid; said device comprising:
a propellant-free topical composition, a container, a pump dispenser, a dip tube, a metering valve, and an actuator;
wherein, upon actuation, the pump dispenser dispenses the composition through a dip tube into a metering valve, and through the actuator fitted with an orifice, such that the composition is consistently released in the form of a substantially uniform spray
where about 90% of the droplets have sizes ranging from about 1 to about 500 μm and does not foam at the application site.
2. The device according to claim 1 , wherein the device produces very fine uniform droplets at a specified spray rate from about 20 to about 500 mg/actuation.
3. The device according to claim 1 , wherein the device produces very fine uniform droplets at a specified spray rate from about 100 to about 200 mg/actuation.
4. The device according to claim 1 , wherein the device provides a reproducible spray pattern covering an area of about 0.1 to about 10 cm 2 depending on the distance from the application site.
5. The device according to claim 1 , wherein the device dispenses about 160 μl of the composition per actuation of the pump.
6. A method of administration of a topical composition comprising a steroid; said method comprising:
providing a dispensing device according to claim 1 , and
actuating the pump dispenser to dispense the composition through the dip tube into the metering valve, and through the actuator fitted with the orifice, such that the composition is consistently released in the form of a substantially uniform spray,
where about 90% of the droplets have sizes ranging from about 1 to about 500 μm and does not foam at the application site.
7. The method of administration according to claim 6 , wherein said method produces very fine uniform droplets at a specified spray rate from about 20 to about 500 mg/actuation.
8. The method of administration according to claim 6 , wherein said method produces very fine uniform droplets at a specified spray rate from about 100 to about 200 mg/actuation.
9. The method of administration according to claim 6 , wherein the device provides a reproducible spray pattern covering an area of about 0.1 to about 10 cm 2 depending on the distance from the application site.
10. The method of administration according to claim 6 , wherein the device dispense about 160 μl of a composition per actuation of the pump.
11. A propellant-free topical composition, comprising:
a) a steroid;
b) an emulsifying agent from about 0.25% w/w to about 45% w/w of the composition;
c) a skin penetration enhancer from about 0.001% w/w to about 15% w/w of the composition; and
d) a water-immiscible substance;
wherein the composition is non-foaming, propylene glycol-free and alcohol-free.
12. The composition according to claim 11 , wherein the steroid is selected from the group comprising of alclometasone dipropionate, beclomethasone dipropionate, betamethasone dipropionate, betamethasone valerate, fluocinolone acetonide, halobetasol propionate, hydrocortisone aceponate, hydrocortisone acetate, hydrocortisone valerate, hydrocortisone butyrate, mometasone furoate, triamcinolone acetonide, clocortolone pivalate, clobetasol propionate, desoximetasone, fluticasone propionate, and combinations thereof.
13. The composition according to claim 11 , wherein the steroid is betamethasone dipropionate.
14. The composition according to claim 11 , wherein the steroid is clobetasol propionate.
15. The composition according to claim 11 , wherein said composition is stable for at least 3 months at 25° C.
16. The composition according to claim 11 , wherein dispersed phase droplets of the composition have an average particle size of less than about 2000 nm.
17. The composition according to claim 11 , wherein dispersed phase droplets of the composition have an average particle size of less than about 500 μm.
18. The composition according to claim 11 , wherein said composition is an aqueous-based composition having viscosity in the range of from about 10 to about 15,000 centipoise.
19. The composition according to claim 11 , wherein said composition provides less than about 10% drug release in 1 hour when evaluated using a Franz diffusion cell fitted with polysulphone 0.2 μm membrane, and the receptor media is a mixture of ethanol and water 20:80 by volume with a replacement volume of 12 ml.
20. A method of treating a skin condition comprising administering a pharmaceutically effective amount of the composition according to claim 11 to a subject in need thereof, wherein the condition is selected from one or more of the group of conditions consisting of atopic dermatitis, seborrhoeic dermatitis, eczema, plaque psoriasis, erythroderma psoriasis, and psoriasis of the scalp, steroid responsive dermatoses, erythema, and contact sensitivity reactions.