Transdermal pharmaceutical formulation for minimizing skin residues
First Claim
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1. A transdermal or transmucosal pharmaceutical formulation comprising:
- at least one active agent; and
a solvent system present in an amount sufficient to solubilize the at least one active ingredient and characterized in that it includes;
(i) a pharmaceutically acceptable monoalkyl ether of diethylene glycol present in an amount of between about 1% and 30% by weight of the solvent system;
(ii) a pharmaceutically acceptable glycol present in an amount of between about 1% and 30% by weight of the solvent system, with the monoalkyl ether of diethylene glycol and glycol being present in a weight ratio of 10;
1 to 2;
1 or 1;
2 to 1;
10; and
(iii) a mixture of a C2 to C4 alcohol and water which mixture is present in an amount of between about 40% and 98% of the solvent system, wherein the C2 to C4 alcohol is present in an amount of about 5% to 80%of the mixture, and the water is present in an amount of about 20% to 95% of the mixture, so that, compared to formulations containing the same components but in different amounts and ratios, the present solvent system (a) inhibits crystallization of the at least one active ingredient on a skin or mucosal surface of a mammal, (b) reduces or prevents transfer of the formulation to clothing or to another being, (c) modulates biodistribution of the at least one active agent within different layers of skin, (d) facilitates absorption of the at least one active agent by a skin or a mucosal surface of a mammal, or (e) provides a combination of one or more of (a) through (d).
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Abstract
This invention relates to novel transdermal or transmucosal pharmaceutical formulation which reduces the occurrences of contamination of other individuals and the transference to clothing of the user. The novel formulation includes at least one pharmacologically active ingredient, and a solvent system having a monoalkylether of diethylene glycol and a glycol present in specified ratios, and a mixture of water and alcohol. The invention also relates to a method for inhibiting or delaying crystallization of an active agent in a pharmaceutical formulation.
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Citations
45 Claims
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1. A transdermal or transmucosal pharmaceutical formulation comprising:
-
at least one active agent; and
a solvent system present in an amount sufficient to solubilize the at least one active ingredient and characterized in that it includes;
(i) a pharmaceutically acceptable monoalkyl ether of diethylene glycol present in an amount of between about 1% and 30% by weight of the solvent system;
(ii) a pharmaceutically acceptable glycol present in an amount of between about 1% and 30% by weight of the solvent system, with the monoalkyl ether of diethylene glycol and glycol being present in a weight ratio of 10;
1 to 2;
1 or 1;
2 to 1;
10; and
(iii) a mixture of a C2 to C4 alcohol and water which mixture is present in an amount of between about 40% and 98% of the solvent system, wherein the C2 to C4 alcohol is present in an amount of about 5% to 80%of the mixture, and the water is present in an amount of about 20% to 95% of the mixture, so that, compared to formulations containing the same components but in different amounts and ratios, the present solvent system (a) inhibits crystallization of the at least one active ingredient on a skin or mucosal surface of a mammal, (b) reduces or prevents transfer of the formulation to clothing or to another being, (c) modulates biodistribution of the at least one active agent within different layers of skin, (d) facilitates absorption of the at least one active agent by a skin or a mucosal surface of a mammal, or (e) provides a combination of one or more of (a) through (d). - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 27, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45)
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23. A method of delaying or inhibiting crystallization of an active agent in a transdermal or transmucosal pharmaceutical formulation, characterized in that the formulation comprises at least one active agent and a solvent system, the solvent system comprising a pharmaceutically acceptable monoalkyl ether of diethylene glycol and a glycol present in a weight ratio of 10:
- 1 to 2;
1 or 1;
2 to 1;
10. - View Dependent Claims (24, 25, 26, 28, 29, 30, 31, 32, 33, 34, 35)
- 1 to 2;
Specification