QUIESCENT FOAMABLE COMPOSITIONS, STEROIDS, KITS AND USES THEREOF
First Claim
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1. A storable foamable emulsion composition adapted for delivery of an active pharmaceutical ingredient (API) to a delivery site in a subject, the composition comprising:
- a) at least one organic carrier selected from the group consisting of a hydrophobic organic carrier, an organic polar solvent, an emollient and mixtures thereof, at a concentration of about 2% to about 50% by weight;
b) at least one surface-active agent at a concentration of about 0.01% to about 5% by weight;
c) at least one polymeric agent selected from the group consisting of a bioadhesive agent, a gelling agent, a film forming agent and a phase change agent, each in a concentration of about 0.01% to about 5% by weight;
d) water;
e) an effective amount of at least one API selected from the group consisting of a steroid, a steroid derivative, and combinations thereof;
f) optionally, a further active agent; and
g) a propellant at a concentration of about 3% to about 25% by weight of the total foamable composition,wherein, at ambient temperature, the storable foamable emulsion composition is shakable, is resistant to centrifugation at about 3000 rpm for about 10 min, is substantially devoid of crystals, is resistant to at least one freeze-thaw cycle and does not phase separate within at least about one month;
wherein the at least one API remains chemically stable for at least about one month; and
wherein the composition is stored in an aerosol container and upon release expands to form a breakable foam having an average bubble size range of about 30 to about 250 micron.
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Abstract
The present invention relates to an emulsion steroid composition as a foamable vehicle in which the vehicle is stable or stabilized by the presence of at least one quiesence agent; therapeutical kit containing such composition; to methods of treatment using such composition; to methods of enhancing the stability of such composition.
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Citations
24 Claims
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1. A storable foamable emulsion composition adapted for delivery of an active pharmaceutical ingredient (API) to a delivery site in a subject, the composition comprising:
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a) at least one organic carrier selected from the group consisting of a hydrophobic organic carrier, an organic polar solvent, an emollient and mixtures thereof, at a concentration of about 2% to about 50% by weight; b) at least one surface-active agent at a concentration of about 0.01% to about 5% by weight; c) at least one polymeric agent selected from the group consisting of a bioadhesive agent, a gelling agent, a film forming agent and a phase change agent, each in a concentration of about 0.01% to about 5% by weight; d) water; e) an effective amount of at least one API selected from the group consisting of a steroid, a steroid derivative, and combinations thereof; f) optionally, a further active agent; and g) a propellant at a concentration of about 3% to about 25% by weight of the total foamable composition, wherein, at ambient temperature, the storable foamable emulsion composition is shakable, is resistant to centrifugation at about 3000 rpm for about 10 min, is substantially devoid of crystals, is resistant to at least one freeze-thaw cycle and does not phase separate within at least about one month; wherein the at least one API remains chemically stable for at least about one month; and wherein the composition is stored in an aerosol container and upon release expands to form a breakable foam having an average bubble size range of about 30 to about 250 micron. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21)
wherein the composition is an emulsion, which is flowable to a sufficient extent to be expelled by the propellant from a canister to form a bioadhesive foam of appropriate quality for topical, body cavity or mucosal application having a bioadhesivity to said delivery site, requiring a force of about −
3 g to about −
30 g to dislodge said foam from said delivery site.
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21. A composition according to claim 1 wherein:
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(a) the at least one organic carrier comprises at least one carrier selected from the group consisting of ocytyldodecanol, isopropyl myristate, mineral oil, capric/caprylic triglyceride, silicone, lanolin and glycerin; (b) the at least one a surface-active agent comprises at least one of, Polysorbate 60, Polysorbate 80, Polyoxyl 100 stearate, PEG 40 stearate, PPG 15 Stearyl Ether, and Ceteareth 20, (c) the at least one polymeric additive comprises at least one of hypromellose, polycarbophil, carbopol and additionally optionally propylene glycol; and (d) optionally further comprising a foam adjuvant comprising at least one of cetearyl alcohol, oleyl alcohol, stearyl alcohol and stearic acid.
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22. A storable foamable emulsion composition adapted for delivery of an active pharmaceutical ingredient (API) to a delivery site in a subject, the composition comprising:
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a) at least one fatty alcohol, at a concentration of about 2% to about 50% by weight; b) at least one surface-active agent at a concentration of about 0.01% to about 5% by weight; c) at least one polymeric agent selected from the group consisting of a bioadhesive agent, a gelling agent, a film forming agent and a phase change agent, each in a concentration of about 0.01% to about 5% by weight; d) water; e) an effective amount of at least one API selected from the group consisting of a steroid, a steroid derivative, a further active agent together with the steroid or derivative thereof and combinations thereof; and f) a propellant at a concentration of about 3% to about 25% by weight of the total foamable composition, wherein, at ambient temperature, the storable foamable emulsion composition is shakable, is resistant to centrifugation at about 3000 rpm for about 10 min, is substantially devoid of crystals, is resistant to at least one freeze-thaw cycle and does not phase separate within at least about one month; wherein the at least one API remains chemically stable for about at least about one month; and wherein the composition is stored in an aerosol container and upon release expands to form a breakable foam having an average bubble size range of about 30 to about 250 micron. - View Dependent Claims (23)
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24. A method of treating, alleviating or preventing a disorder of the skin, a body cavity or a mucosal surface, wherein the disorder involves inflammation as one of its etiological factors, which method comprise administering topically to a subject having the disorder in need thereof a therapeutically effective amount of a storable foamable emulsion composition comprising:
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a. at least one organic carrier selected from the group consisting of a hydrophobic organic carrier, an organic polar solvent, an emollient and mixtures thereof, at a concentration of about 2% to about 50% by weight; b. at least one surface-active agent at a concentration of about 0.01% to about 5% by weight; c. at least one polymeric additive selected from the group consisting of a bioadhesive agent, a gelling agent, a film forming agent and a phase change agent, each in a concentration of about 0.01% to about 5% by weight; d. water; e. an effective amount of at least one API selected from the group consisting of a steroid, a steroid derivative, a further active agent together with the steroid or derivative thereof and combinations thereof; and f. a propellant at a concentration of about 3% to about 25% by weight of the total foamable composition, wherein, at ambient temperature, the storable foamable emulsion composition is shakable, is resistant to centrifugation at about 3000 rpm for about 10 min, is substantially devoid of crystals, is resistant to at least one freeze-thaw cycle and does not phase separate within at least about one month; wherein the at least one API remains chemically stable for at least about one month; and wherein the composition is stored in an aerosol container and upon release expands to form a breakable bioadhesive foam having an average bubble size range of about 30 to about 250 micron.
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Specification