Foamable pharmaceutical compositions and methods for treating a disorder
First Claim
1. A foamable delivery system which comprises:
- (i) a solvent composition selected from the group consisting of water, a volatile propellant, a C1-C6 fluid alkyl or branched alkyl alcohol, an aromatic alcohol, an ether of a sorbitol derivative, propylene carbonate, xylene, methylene chloride, ethylhexanediol, pqlysiloxanes, dimethyl ether, and mixtures thereof;
(ii) a surfactant composition selected from the group consisting of a polyoxyethylene fatty ether, a polyoxyethylene fatty ester, a fatty acid, a sulfated fatty acid surfactant, a phosphated fatty acid surfactant, a sulfosuccinate surfactant, an amphoteric surfactant, a non-ionic poloxamer surfactant, a non-ionic meroxapol surfactant, a petroleum derivative surfactant, an aliphatic amine surfactant, a polysiloxane derivative, a sorbitan fatty acid ester, pharmaceutically acceptable salts thereof, and mixtures thereof;
(iii) a propellant; and
(iv) an acid in an amount to affect the delivery system'"'"'s pH selected from the group consisting of;
(a) acetylsalicyclic acid, ascorbic acid, boric acid, carbonic acid, formic acid, ethanesulfonic acid, fumaric acid, glycerophosphoric acid, hippuric acid, hydrochloric acid, maleic acid, methanesulfonic acid, nitrous acid, oxalic acid, phosphoric acid, saccharin, sorbic acid, sulfuric acid, thiosulfuric acid, undecylenic acid, ethanolamine, and a pharmaceutically acceptable salt, ester, or solvate thereof;
(b) an alpha hydroxyacid of formula T;
(Ra)(Rb)C(OH)COOH
I or a pharmaceutically acceptable salt, lactone, or solvate thereof wherein Ra and Rb are independently selected from the group consisting of H, F, Cl, Br, and saturated or unsaturated, isomeric or non-isomeric, straight, branched, or cyclic C1-C25 alkyl, aralkyl, or aryl groups, wherein each of Ra and Rb may be optionally substituted with an OH, SH, CHO, COOH group;
(c) an alpha ketoacid of formula II;
(Ra)COCOO(Rb)
II or a pharmaceutically acceptable salt, ester, or solvate thereof wherein Ra and Rb are independently selected from the group consisting of H and saturated or unsaturated, isomeric or non-isomeric, straight, branched, or cyclic C1-C25 alkyl, aralkyl, or aryl groups, wherein Ra may be optionally substituted with an F, Cl, Br, I, OH, CHO, COOH, or alkoxy group having 1 to 9 carbon atoms;
(d) an acid of formula ITT;
or a pharmaceutically acceptable salt, ester, or solvate thereof, wherein n is 0-6;
X is H, OH, or NH2, each Y is H or OH, or X and Y are optionally taken together to form a 5-7 membered saturated or unsaturated carbocyclic ring or a 5-7 membered saturated or unsaturated heterocyclic ring, wherein one or more ring atom(s) of said heterocyclic ring is O, S, or N;
Z is H, CH3, OH, COOH, or SH, provided that Y and Z are not both OH, or Y and Z are optionally taken together to form a 5-7 membered saturated or unsaturated carbocyclic ring or a 5-7 membered saturated or unsaturated heterocyclic ring, wherein one or more ring atom(s) of said heterocyclic ring is O, S, or N; and
(e) mixtures thereof.
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Accused Products
Abstract
Novel compositions of matter comprising a foamable delivery system are provided. Novel methods for treating a disease, disorder, or condition using the novel compositions are further provided. Novel methods for making and delivering a foamable pharmaceutical composition are also provided. While the novel compositions and foamable drug delivery system may be utilized for administration of a wide variety of drugs to epithelial tissues, to treat a wide variety of diseases, disorders, or conditions, the inventive compositions and foamable drug delivery systems are particularly useful for the dermatological administration of corticosteroids and antifungal agents.
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Citations
53 Claims
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1. A foamable delivery system which comprises:
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(i) a solvent composition selected from the group consisting of water, a volatile propellant, a C1-C6 fluid alkyl or branched alkyl alcohol, an aromatic alcohol, an ether of a sorbitol derivative, propylene carbonate, xylene, methylene chloride, ethylhexanediol, pqlysiloxanes, dimethyl ether, and mixtures thereof;
(ii) a surfactant composition selected from the group consisting of a polyoxyethylene fatty ether, a polyoxyethylene fatty ester, a fatty acid, a sulfated fatty acid surfactant, a phosphated fatty acid surfactant, a sulfosuccinate surfactant, an amphoteric surfactant, a non-ionic poloxamer surfactant, a non-ionic meroxapol surfactant, a petroleum derivative surfactant, an aliphatic amine surfactant, a polysiloxane derivative, a sorbitan fatty acid ester, pharmaceutically acceptable salts thereof, and mixtures thereof;
(iii) a propellant; and
(iv) an acid in an amount to affect the delivery system'"'"'s pH selected from the group consisting of;
(a) acetylsalicyclic acid, ascorbic acid, boric acid, carbonic acid, formic acid, ethanesulfonic acid, fumaric acid, glycerophosphoric acid, hippuric acid, hydrochloric acid, maleic acid, methanesulfonic acid, nitrous acid, oxalic acid, phosphoric acid, saccharin, sorbic acid, sulfuric acid, thiosulfuric acid, undecylenic acid, ethanolamine, and a pharmaceutically acceptable salt, ester, or solvate thereof;
(b) an alpha hydroxyacid of formula T;
(Ra)(Rb)C(OH)COOH
Ior a pharmaceutically acceptable salt, lactone, or solvate thereof wherein Ra and Rb are independently selected from the group consisting of H, F, Cl, Br, and saturated or unsaturated, isomeric or non-isomeric, straight, branched, or cyclic C1-C25 alkyl, aralkyl, or aryl groups, wherein each of Ra and Rb may be optionally substituted with an OH, SH, CHO, COOH group;
(c) an alpha ketoacid of formula II;
(Ra)COCOO(Rb)
IIor a pharmaceutically acceptable salt, ester, or solvate thereof wherein Ra and Rb are independently selected from the group consisting of H and saturated or unsaturated, isomeric or non-isomeric, straight, branched, or cyclic C1-C25 alkyl, aralkyl, or aryl groups, wherein Ra may be optionally substituted with an F, Cl, Br, I, OH, CHO, COOH, or alkoxy group having 1 to 9 carbon atoms;
(d) an acid of formula ITT;
or a pharmaceutically acceptable salt, ester, or solvate thereof, wherein n is 0-6;
X is H, OH, or NH2, each Y is H or OH, or X and Y are optionally taken together to form a 5-7 membered saturated or unsaturated carbocyclic ring or a 5-7 membered saturated or unsaturated heterocyclic ring, wherein one or more ring atom(s) of said heterocyclic ring is O, S, or N;
Z is H, CH3, OH, COOH, or SH, provided that Y and Z are not both OH, or Y and Z are optionally taken together to form a 5-7 membered saturated or unsaturated carbocyclic ring or a 5-7 membered saturated or unsaturated heterocyclic ring, wherein one or more ring atom(s) of said heterocyclic ring is O, S, or N; and
(e) mixtures thereof.
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2. A pharmaceutical composition comprising:
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(A) an effective amount of one or more active therapeutic agents or pharmaceutically acceptable free bases, salts, esters, or solvates thereof; and
(B) a pharmaceutically acceptable carrier, comprising;
(i) a foamable delivery system which comprises;
(a) a solvent composition selected from the group consisting of water, a volatile propellant, a C1-C6 fluid alkyl or branched alkyl alcohol, an aromatic alcohol, an ether of a sorbitol derivative, propylene carbonate, xylene, methylene chloride, ethylhexanediol, polysiloxanes, dimethyl ether, and mixtures thereof; and
(b) a surfactant composition selected from the group consisting of a polyoxyethylene fatty ether, a polyoxyethylene fatty ester, a fatty acid, a sulfated fatty acid surfactant, a phosphated fatty acid surfactant, a sulfosuccinate surfactant, an amphoteric surfactant, a non-ionic poloxamer surfactant, a non-ionic meroxapol surfactant, a petroleum derivative surfactant, an aliphatic amine surfactant, a polysiloxane derivative, a sorbitan fatty acid ester, pharmaceutically acceptable salts thereof, and mixtures thereof;
(ii) a propellant; and
(iii) an acid in an amount to affect the composition'"'"'s pH selected from the group consisting of;
(a) acetylsalicyclic acid, ascorbic acid, boric acid, carbonic acid, formic acid, ethanesulfonic acid, fumaric acid, glycerophosphoric acid, hippuric acid, hydrochloric acid, maleic acid, methanesulfonic acid, nitrous acid, oxalic acid, phosphoric acid, saccharin, sorbic acid, sulfuric acid, thiosulfuric acid, undecylenic acid, ethanolamine, and a pharmaceutically acceptable salt, ester, or solvate thereof;
(b) an alpha hydroxyacid of formula I;
(Ra)(Rb)C(OH)COOH
Ior a pharmaceutically acceptable salt, lactone, or solvate thereof wherein Ra and Rb are independently selected from the group consisting of H, F, Cl, Br, and saturated or unsaturated, isomeric or non-isomeric, straight, branched, or cyclic C1-C25 alkyl, aralkyl, or aryl groups, wherein each of Ra and Rb may be optionally substituted with an OH, SH, CHO, COOH group;
(c) an alpha ketoacid of formula II;
(Ra)COCOO(Rb)
IIor a pharmaceutically acceptable salt, ester, or solvate thereof wherein Ra and Rb are independently selected from the group consisting of H and saturated or unsaturated, isomeric or non-isomeric, straight, branched, or cyclic C1-C25 alkyl, aralkyl, or aryl groups, wherein Ra may be optionally substituted with an F, Cl, Br, I, OH, CHO, COOH, or alkoxy group having 1 to 9 carbon atoms;
(d) an acid of formula III;
or a pharmaceutically acceptable salt, ester, or solvate thereof, wherein n is 0-6;
X is H, OH, or NH2, each Y is H or OH, or X and Y are optionally taken together to form a 5-7 membered saturated or unsaturated carbocyclic ring or a 5-7 membered saturated or unsaturated heterocyclic ring, wherein one or more ring atom(s) of said heterocyclic ring is O, S, or N;
Z is H, CH3, OH, COOH, or SH, provided that Y and Z are not both OH, or Y and Z are optionally taken together to form a 5-7 membered saturated or unsaturated carbocyclic ring or a 5-7 membered saturated or unsaturated heterocyclic ring, wherein one or more ring atom(s) of said heterocyclic ring is O, S, or N; and
(e) mixtures thereof. - View Dependent Claims (3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19)
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20. A pharmaceutical composition comprising:
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(A) an effective amount of one or more active therapeutic agents or pharmaceutically acceptable free bases, salts, esters, or solvates thereof; and
(B) a pharmaceutically acceptable carrier, comprising;
(i) a foamable delivery system which comprises;
(a) a solvent composition selected from the group consisting of water, ethanol, isopropyl alcohol, benzyl alcohol, dimethyl isosorbide, propylene carbonate, xylene, methylene chloride, ethylhexanediol, polysiloxanes, dimethyl ether, and mixtures thereof; and
(b) a surfactant composition selected from the group consisting of laureth-4, PEG-2 dilaurate, stearic acid, sodium lauryl sulfate, dioctyl sodium sulfosuccinate, cocoamphopropionate, poloxamer 188, meroxapol 258, triethanolamine, dimethicone, polysorbate 60, sorbitan monostearate, pharmaceutically acceptable salts thereof, and mixtures thereof;
(ii) a propellant; and
(iii) an acid in an amount to affect the composition'"'"'s pH selected from the group consisting of acetic acid, acetylsalicylic acid, adipic acid, ascorbic acid, aspartic acid, benzoic acid, boric acid, carbonic acid, citric acid, formic acid, ethanesulfonic acid, fumaric acid, glycerophosphoric acid, gluconic acid, glutaric acid, glycine, glyceric acid, glycolic acid, glutamic acid, hippuric acid, hydrochloric acid, lactic acid, maleic acid, malic acid, malonic acid, mandelic acid, methanesulfonic acid, mucic acid, nitrous acid, oxalic acid, pelargonic acid, phosphoric acid, propionic acid, saccharin, salicylic acid, sorbic acid, succinic acid, sulfuric acid, tartaric acid, thioglycolic acid, thiosulfuric acid, undecylenic acid, ethanolamine, naturally and synthetically derived amino acids, derivatives thereof, and mixtures thereof.
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21. A pharmaceutical composition having a starting concentration of an active therapeutic agent comprising:
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(A) an effective amount of one or more active therapeutic agents or pharmaceutically acceptable free bases, salts, esters, or solvates thereof; and
(B) a pharmaceutically acceptable carrier, comprising;
(i) a foamable delivery system which comprises;
(a) a solvent composition selected from the group consisting of water, a volatile propellant, a C1-C6 fluid alkyl or branched alkyl alcohol, an aromatic alcohol, an ether of a sorbitol derivative, propylene carbonate, xylene, methylene chloride, ethylhexanediol, polysiloxanes, dimethyl ether, and mixtures thereof; and
(b) a surfactant composition selected from the group consisting of a polyoxyethylene fatty ether, a polyoxyethylene fatty ester, a fatty acid, a sulfated fatty acid surfactant, a phosphated fatty acid surfactant, a sulfosuccinate surfactant, an amphoteric surfactant, a non-ionic poloxamer surfactant, a non-ionic meroxapol surfactant, a petroleum derivative surfactant, an aliphatic amine surfactant, a polysiloxane derivative, a sorbitan fatty acid ester, pharmaceutically acceptable salts thereof, and mixtures thereof;
(ii) a propellant; and
(iii) an acid in an amount to affect the composition'"'"'s pH selected from the group consisting of;
(a) acetylsalicyclic acid, ascorbic acid, boric acid, carbonic acid, formic acid, ethanesulfonic acid, fumaric acid, glycerophosphoric acid, hippuric acid, hydrochloric acid, maleic acid, methanesulfonic acid, nitrous acid, oxalic acid, phosphoric acid, saccharin, sorbic acid, sulfuric acid, thiosulfuric acid, undecylenic acid, ethanolamine, and a pharmaceutically acceptable salt, ester, or solvate thereof;
(b) an alpha hydroxyacid of formula I;
(Ra)(Rb)C(OH)COOH
Ior a pharmaceutically acceptable salt, lactone, or solvate thereof wherein Ra and Rb are independently selected from the group consisting of H, F, Cl, Br, and saturated or unsaturated, isomeric or non-isomeric, straight, branched, or cyclic C1-C25 alkyl, aralkyl, or aryl groups, wherein each of Ra and Rb may be optionally substituted with an OH, SH, CHO, COOH group;
(c) an alpha ketoacid of formula II;
(Ra)COCOO(Rb)
IIor a pharmaceutically acceptable salt, ester, or solvate thereof wherein Ra and Rb are independently selected from the group consisting of H and saturated or unsaturated, isomeric or non-isomeric, straight, branched, or cyclic C1-C25 alkyl, aralkyl, or aryl groups, wherein Ra may be optionally substituted with an F, Cl, Br, I, OH, CHO, COOH, or alkoxy group having 1 to 9 carbon atoms;
(d) an acid of formula III;
or a pharmaceutically acceptable salt, ester, or solvate thereof, wherein n is 0-6;
X is H, OH, or NH2, each Y is H or OH, or X and Y are optionally taken together to form a 5-7 membered saturated or unsaturated carbocyclic ring or a 5-7 membered saturated or unsaturated heterocyclic ring, wherein one or more ring atom(s) of said heterocyclic ring is O, S, or N;
Z is H, CH3, OH, COOH, or SH, provided that Y and Z are not both OH, or Y and Z are optionally taken together to form a 5-7 membered saturated or unsaturated carbocyclic ring or a 5-7 membered saturated or unsaturated heterocyclic ring, wherein one or more ring atom(s) of said heterocyclic ring is O, S, or N; and
(e) mixtures thereof, wherein said composition maintains a concentration of degradation product(s) less than about 5% of the starting concentration of said active therapeutic agent or its pharmaceutically acceptable salt, ester, or solvate. - View Dependent Claims (22)
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23. A method for treating a disease, disorder, or condition in a mammal in need thereof, comprising administering to said mammal an effective amount of a foamable pharmaceutical composition, said composition comprising:
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(i) an effective amount of one or more active therapeutic agents or pharmaceutically acceptable free bases, salts, esters, or solvates thereof;
(ii) a foarmable delivery system which comprises;
(a) a solvent composition selected from the group consisting of water, a volatile propellant, a C1-C6 fluid alkyl or branched alkyl alcohol, an aromatic alcohol, an ether of a sorbitol derivative, propylene carbonate, xylene, methylene chloride, ethylhexanediol, polysiloxanes, dimethyl ether, and mixtures thereof; and
(b) a surfactant composition selected from the group consisting of a polyoxyethylene fatty ether, a polyoxyethylene fatty ester, a fatty acid, a sulfated fatty acid surfactant, a phosphated fatty acid surfactant, a sulfosuccinate surfactant, an amphoteric surfactant, a non-ionic poloxamer surfactant, a non-ionic meroxapol surfactant, a petroleum derivative surfactant, an aliphatic amine surfactant, a polysiloxane derivative, a sorbitan fatty acid ester, pharmaceutically acceptable salts thereof, and mixtures thereof;
(iii) a propellant; and
(iv) an acid in an amount to affect the composition'"'"'s pH selected from the group consisting of;
(a) acetylsalicyclic acid, ascorbic acid, boric acid, carbonic acid, formic acid, ethanesulfonic acid, fumaric acid, glycerophosphoric acid, hippuric acid, hydrochloric acid, maleic acid, methanesulfonic acid, nitrous acid, oxalic acid, phosphoric acid, saccharin, sorbic acid, sulfuric acid, thiosulfuric acid, undecylenic acid, ethanolamine, and a pharmaceutically acceptable salt, ester, or solvate thereof;
(b) an alpha hydroxyacid of formula I;
(Ra)(Rb)C(OH)COOH
Ior a pharmaceutically acceptable salt, lactone, or solvate thereof wherein Ra and Rb are independently selected from the group consisting of H, F, Cl, Br, and saturated or unsaturated, isomeric or non-isomeric, straight, branched, or cyclic C1-C25 alkyl, aralkyl, or aryl groups, wherein each of Ra and Rb may be optionally substituted with an OH, SH, CHO, COOH group;
(c) an alpha ketoacid of formula II;
(Ra)COCOO(Rb)
IIor a pharmaceutically acceptable salt, ester, or solvate thereof wherein Ra and Rb are independently selected from the group consisting of H and saturated or unsaturated, isomeric or non-isomeric, straight, branched, or cyclic C1-C25 alkyl, aralkyl, or aryl groups, wherein Ra may be optionally substituted with an F, Cl, Br, I, OH, CHO, COOH, or alkoxy group having 1 to 9 carbon atoms;
(d) an acid of formula III;
or a pharmaceutically acceptable salt, ester, or solvate thereof, wherein n is 0-6;
X is H, OH, or NH2, each Y is H or OH, or X and Y are optionally taken together to form a 5-7 membered saturated or unsaturated carbocyclic ring or a 5-7 membered saturated or unsaturated heterocyclic ring, wherein one or more ring atom(s) of said heterocyclic ring is O, S, or N;
Z is H, CH3, OH, COOH, or SH, provided that Y and Z are not both OH, or Y and Z are optionally taken together to form a 5-7 membered saturated or unsaturated carbocyclic ring or a 5-7 membered saturated or unsaturated heterocyclic ring, wherein one or more ring atom(s) of said heterocyclic ring is O, S, or N; and
(e) mixtures thereof. - View Dependent Claims (24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34)
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35. A method for treating a skin condition in a mammal in need thereof, comprising administering to the skin of said mammal an effective amount of a foamable pharmaceutical composition, said composition comprising:
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(i) an effective amount of one or more active therapeutic agents or pharmaceutically acceptable free bases, salts, esters, or solvates thereof;
(ii) a foamable delivery system which comprises;
(a) a solvent composition selected from the group consisting of water, ethanol, isopropyl alcohol, benzyl alcohol, dimethyl isosorbide, propylene carbonate, xylene, methylene chloride, ethylhexanediol, polysiloxanes, dimethyl ether, and mixtures thereof; and
(b) a surfactant composition selected from the group consisting of laureth-4, PEG-2 dilaurate, stearic acid, sodium lauryl sulfate, dioctyl sodium sulfosuccinate, cocoamphopropionate, poloxamer 188, meroxapol 258, triethanolamine, dimethicone, polysorbate 60, sorbitan monostearate, pharmaceutically acceptable salts thereof, and mixtures thereof;
(iii) a propellant; and
(iv) an acid in an amount to affect the composition'"'"'s pH selected from the group consisting of acetic acid, acetylsalicylic acid, adipic acid, ascorbic acid, aspartic acid, benzoic acid, boric acid, carbonic acid, citric acid, formic acid, ethanesulfonic acid, fumaric acid, glycerophosphoric acid, gluconic acid, glutaric acid, glycine, glyceric acid, glycolic acid, glutamic acid, hippuric acid, hydrochloric acid, lactic acid, maleic acid, malic acid, malonic acid, mandelic acid, methanesulfonic acid, mucic acid, nitrous acid, oxalic acid, pelargonic acid, phosphoric acid, propionic acid, saccharin, salicylic acid, sorbic acid, succinic acid, sulfuric acid, tartaric acid, thioglycolic acid, thiosulfuric acid, undecylenic acid, ethanolamine, naturally and synthetically derived amino acids, derivatives thereof, and mixtures thereof.
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36. A method of making a foamable pharmaceutical composition, comprising the steps of:
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(A) admixing an effective amount of one or more active therapeutic agents or pharmaceutically acceptable free bases, salts, esters, or solvates thereof and a pharmaceutically acceptable carrier comprising;
(i) a foamable delivery system which comprises;
(a) a solvent composition selected from the group consisting of water, a volatile propellant, a C1-C6 fluid alkyl or branched alkyl alcohol, an aromatic alcohol, an ether of a sorbitol derivative, propylene carbonate, xylene, methylene chloride, ethylhexanediol, polysiloxanes, dimethyl ether, and mixtures thereof; and
(b) a surfactant composition selected from the group consisting of a polyoxyethylene fatty ether, a polyoxyethylene fatty ester, a fatty acid, a sulfated fatty acid surfactant, a phosphated fatty acid surfactant, a sulfosuccinate surfactant, an amphoteric surfactant, a non-ionic poloxamer surfactant, a non-ionic meroxapol surfactant, a petroleum derivative surfactant, an aliphatic amine surfactant, a polysiloxane derivative, a sorbitan fatty acid ester, pharmaceutically acceptable salts thereof, and mixtures thereof; and
(ii) an acid in an amount to affect the composition'"'"'s pH selected from the group consisting of;
(a) acetylsalicyclic acid, ascorbic acid, boric acid, carbonic acid, formic acid, ethanesulfonic acid, fumaric acid, glycerophosphoric acid, hippuric acid, hydrochloric acid, maleic acid, methanesulfonic acid, nitrous acid, oxalic acid, phosphoric acid, saccharin, sorbic acid, sulfuric acid, thiosulfuric acid, undecylenic acid, ethanolamine, and a pharmaceutically acceptable salt, ester, or solvate thereof;
(b) an alpha hydroxyacid of formula I;
(Ra)(Rb)C(OH)COOH
Ior a pharmaceutically acceptable salt, lactone, or solvate thereof wherein Ra and Rb are independently selected from the group consisting of H, F, Cl, Br, and saturated or unsaturated, isomeric or non-isomeric, straight, branched, or cyclic C1-C25 alkyl, aralkyl, or aryl groups, wherein each of Ra and Rb may be optionally substituted with an OH, SH, CHO, COOH group;
(c) an alpha ketoacid of formula II;
(Ra)COCOO(Rb)
IIor a pharmaceutically acceptable salt, ester, or solvate thereof wherein Ra and Rb are independently selected from the group consisting of H and saturated or unsaturated, isomeric or non-isomeric, straight, branched, or cyclic C1-C25 alkyl, aralkyl, or aryl groups, wherein Ra may be optionally substituted with an F, Cl, Br, I, OH, CHO, COOH, or alkoxy group having 1 to 9 carbon atoms;
(d) an acid of formula III;
or a pharmaceutically acceptable salt, ester, or solvate thereof, wherein n is 0-6;
X is H, OH, or NH2, each Y is H or OH, or X and Y are optionally taken together to form a 5-7 membered saturated or unsaturated carbocyclic ring or a 5-7 membered saturated or unsaturated heterocyclic ring, wherein one or more ring atom(s) of said heterocyclic ring is O, S, or N;
Z is H, CH3, OH, COOH, or SH, provided that Y and Z are not both OH, or Y and Z are optionally taken together to form a 5-7 membered saturated or unsaturated carbocyclic ring or a 5-7 membered saturated or unsaturated heterocyclic ring, wherein one or more ring atom(s) of said heterocyclic ring is O, S, or N; and
(e) mixtures thereof; and
(B) packaging said mixture in a container suitable for storage and delivery of said composition. - View Dependent Claims (37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47)
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48. A method of delivering a foamable pharmaceutical composition from a container comprising providing an expelling force generated by mechanical means to said foamable pharmaceutical composition, said foamable pharmaceutical composition comprising:
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(i) an effective amount of one or more active therapeutic agents or pharmaceutically acceptable free bases, salts, esters, or solvates thereof;
(ii) a foamable delivery system which comprises;
(a) a solvent composition selected from the group consisting of water, a volatile propellant, a C1-C6 fluid alkyl or branched alkyl alcohol, an aromatic alcohol, an ether of a sorbitol derivative, propylene carbonate, xylene, methylene chloride, ethylhexanediol, polysiloxanes, dimethyl ether, and mixtures thereof; and
(b) a surfactant composition selected from the group consisting of a polyoxyethylene fatty ether, a polyoxyethylene fatty ester, a fatty acid, a sulfated fatty acid surfactant, a phosphated fatty acid surfactant, a sulfosuccinate surfactant, an amphoteric surfactant, a non-ionic poloxamer surfactant, a non-ionic meroxapol surfactant, a petroleum derivative surfactant, an aliphatic amine surfactant, a polysiloxane derivative, a sorbitan fatty acid ester, pharmaceutically acceptable salts thereof, and mixtures thereof; and
(iii) an acid in an amount to affect the composition'"'"'s pH selected from the group consisting of;
(a) acetylsalicyclic acid, ascorbic acid, boric acid, carbonic acid, formic acid, ethanesulfonic acid, fumaric acid, glycerophosphoric acid, hippuric acid, hydrochloric acid, maleic acid, methanesulfonic acid, nitrous acid, oxalic acid, phosphoric acid, saccharin, sorbic acid, sulfuric acid, thiosulfuric acid, undecylenic acid, ethanolamine, and a pharmaceutically acceptable salt, ester, or solvate thereof;
(b) an alpha hydroxyacid of formula I;
(Ra)(Rb)C(OH)COOH
Ior a pharmaceutically acceptable salt, lactone, or solvate thereof wherein Ra and Rb are independently selected from the group consisting of H. F, Cl, Br, and saturated or unsaturated, isomeric or non-isomeric, straight, branched, or cyclic C1-C25 alkyl, aralkyl, or aryl groups, wherein each of Ra and Rb may be optionally substituted with an OH, SH, CHO, COOH group;
(c) an alpha ketoacid of formula II;
(Ra)COCOO(Rb)
IIor a pharmaceutically acceptable salt, ester, or solvate thereof wherein Ra and Rb are independently selected from the group consisting of H and saturated or unsaturated, isomeric or non-isomeric, straight, branched, or cyclic C1-C25 alkyl, aralkyl, or aryl groups, wherein Ra may be optionally substituted with an F, Cl, Br, I, OH, CHO, COOH, or alkoxy group having 1 to 9 carbon atoms;
(d) an acid of formula III;
or a pharmaceutically acceptable salt, ester, or solvate thereof, wherein n is 0-6;
X is H, OH, or NH2, each Y is H or OH, or X and Y are optionally taken together to form a 5-7 membered saturated or unsaturated carbocyclic ring or a 5-7 membered saturated or unsaturated heterocyclic ring, wherein one or more ring atom(s) of said heterocyclic ring is O, S, or N;
Z is H, CH3, OH, COOH, or SH, provided that Y and Z are not both OH, or Y and Z are optionally taken together to form a 5-7 membered saturated or unsaturated carbocyclic ring or a 5-7 membered saturated or unsaturated heterocyclic ring, wherein one or more ring atom(s) of said heterocyclic ring is O, S, or N; and
(e) mixtures thereof. - View Dependent Claims (49, 50, 51, 52, 53)
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Specification