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Details for Patent: 7,214,381

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Details for Patent: 7,214,381

Title:Composition for transdermal and/or transmucosal administration of active compounds that ensures adequate therapeutic levels
Abstract: The present invention refers to a pharmaceutical composition suitable for the transdermal or transmucosal administration of one or more active agents, in form of a gel or a solution, comprising as a permeation enhancers a combination of: a) saturated fatty alcohol of formula CH.sub.3--(CH.sub.2).sub.n--CH.sub.2OH or saturated fatty acid CH.sub.3--(CH.sub.2).sub.n--CH.sub.2COOH wherein n is an integer number 8/22, preferably 8/12, most preferably 10, or unsaturated fatty alcohol or fatty acid of formula: CH.sub.3(C.sub.nH.sub.2(n-1))--OH or CH.sub.3(C.sub.nH.sub.2(n-1))--COOH wherein n is an integer number 8/22, b) a ternary vehicle or carrier consisting of a C.sub.1/C.sub.4 alkanol, a polyalcohol in particular propylenglycol and water, c) optionally also a monoalkylether of diethylenglycol.
Inventor(s): Carrara; Dario (Buenos Aires, AR), Porto; Gabriel (Basel, CH), Rodriguez; Jorge (Buenos Aires, AR)
Assignee: Antares Pharma IPL AG (Zug, CH)
Filing Date:Aug 03, 2001
Application Number:10/343,570
Claims:1. A pharmaceutical composition in the form of a solution, cream, lotion, spray, ointment, gel, aerosol, tablet, suppository or patch device for transdermal or transmucosal administration of one or more active agents to a subject, comprising as a permeation enhancing mixture: a fatty component in an amount of 0.1% to 20% by weight and comprising one of a saturated fatty alcohol of formula CH.sub.3--(CH.sub.2).sub.n--CH.sub.2OH, a saturated fatty acid of formula CH.sub.3--(CH.sub.2).sub.n--CH.sub.2COOH, an unsaturated fatty alcohol of formula CH.sub.3(C.sub.nH.sub.2(n-1))--OH, or a fatty acid of formula CH.sub.3(C.sub.nH.sub.2(n-1))--COOH, wherein n is an integer of between 8 and 22; and a vehicle comprising 5% to 75% by weight of a C.sub.1 C.sub.4 alkanol, 0.5% to 50% of a polyalcohol, water, and up to 40% by weight of a monoalkylether of diethyleneglycol, with all weights calculated based on the total weight of the composition and provided that the total weights of the components does not exceed 100%, wherein the one or more active agents are selected from the group consisting of an androgen hormone, an antihypothyroid hormone, an antihypertensive agent, and a calcium regulator.

2. The pharmaceutical composition of claim 1, wherein the fatty component is present in an amount of 0.1% to 10%, the alkanol is present in an amount of 15% to 65%, the polyalcohol is present in an amount of 3% to 20%, and the monoalkylether of diethyleneglycol is present in an amount of 0.2% to 25%.

3. The pharmaceutical composition of claim 2, wherein the fatty component is present in an amount of 0.2% to 3%, the alkanol is present in an amount of 20% to 55%, the polyalcohol is present in an amount of 4% to 10%, and the monoalkylether of diethyleneglycol is present in an amount of 2% to 8%.

4. A pharmaceutical composition in the form of a gel for transdermal or transmucosal administration of one or more active agents to a subject, comprising as a permeation enhancing mixture a fatty component in an amount of 0.2% to 3% by weight and comprising one of a saturated fatty alcohol of formula CH.sub.3--(CH.sub.2).sub.n--CH.sub.2OH, a saturated fatty acid of formula CH.sub.3--(CH.sub.2).sub.n--CH.sub.2COOH, an unsaturated fatty alcohol of formula CH.sub.3(C.sub.nH.sub.2(n-1))--OH, or a fatty acid of formula CH.sub.3(C.sub.nH.sub.2(n-1))--COOH, wherein n is an integer of between 8 and 22, and a vehicle comprising 20% to 55% by weight of a C.sub.1 C.sub.4 alkanol, 4% to 10% of a polyalcohol, water, and 2% to 8% by weight of a monoalkylether of diethyleneglycol; a gelling agent in an amount of 0.2 to 3% by weight; and a pH regulator in an amount of 0.05% to 2% by weight, with the weights calculated based on the total weight of the composition and the total weights of the components not exceeding 100% wherein the one or more active agent are selected from the group consisting of an androgen hormone, a sedative or anxyolitic, an antihypothyroid hormone, an antihypertensive agent, and a calcium regulator.

5. The pharmaceutical composition of claim 4, wherein the gelling agent is a polyacrylic acid or a cellulose derivative.

6. The pharmaceutical composition of claim 5, wherein the gelling agent is carbopol, hydroxypropylmethylcellulose, carboxymethylcellulose, ethylhydroxyethyl cellulose, hydroxypropylcellulose, hydroxyethylcellulose, polyvinylpyrrolidone, a polyoxyethylene/polyoxypropylene copolymer, polyvinylalcohol, a natural gum, an alginate, or a pectin.

7. The pharmaceutical composition of claim 4, wherein the fatty component is a saturated or unsaturated fatty alcohol where n is an integer of between 8 and 12, the polyalcohol is a glycol, the alkanol is ethanol, the monoalkylether of diethyleneglycol is diethylene glycol monoethylether and the pH regulator is an tertiary amine or sodium hydroxide.

8. The pharmaceutical composition of claim 7, wherein the fatty component is lauryl alcohol or dodecanol, the polyalcohol is propylene glycol and the pH regulator is triethanolamine or tromethamine.

9. A pharmaceutical composition in the form of a solution, cream, lotion, spray, ointment, gel, aerosol, tablet, suppository or patch device for transdermal or transmucosal administration of one or more active agents to a subject, comprising as a permeation enhancing mixture: a fatty component in an amount of 0.1% to 20% by weight and comprising one of a saturated fatty alcohol of formula CH.sub.3--(CH.sub.2).sub.n--CH.sub.2OH, a saturated fatty acid of formula CH.sub.3--(CH.sub.2).sub.n--CH.sub.2COOH, an unsaturated fatty alcohol of formula CH.sub.3(C.sub.nH.sub.2(n-1))--OH, or a fatty acid of formula CH.sub.3(C.sub.nH.sub.2(n-1))--COOH, wherein n is an integer of between 8 and 22; a vehicle comprising 5% to 75% by weight of a C.sub.1 C.sub.4 alkanol, 0.5% to 50% of a polyalcohol, water, and up to 40% by weight of a monoalkylether of diethyleneglycol, with all weights calculated based on the total weight of the composition and provided that the total weights of the components does not exceed 100%, and one or more of a flavor agent, saborizant, sweetener or solubilizant in an amount sufficient to impart desired properties to the composition; wherein the one or more active agents are selected from the group consisting of an androgen hormone, a sedative or anxyolitic, an antihypothyroid hormone, an antihypertensive agent, and a calcium regulator.

10. The pharmaceutical composition of claim 1, wherein the active agent is an androgen hormone.

11. The pharmaceutical composition of claim 10, wherein the androgen hormone is Testosterone or a Testosterone derivatives selected from the group consisting of 17-Methyltestosterone, Testosterone 17 beta-Cypionate, Testosterone Enanthate, Testosterone Nicotinate, Testosterone Phenylacetate, or Testosterone Propionate.

12. The pharmaceutical composition of claim 4, wherein the active agent is a sedative or anxyolitic.

13. The pharmaceutical composition of claim 12, wherein the sedative or anxyolitic is a benzodiazepine or an amide.

14. The pharmaceutical composition of claim 13, wherein the sedative or anxyolitic is butoctamide, diethylbromoacetamide, or isovalcryl-diethylamide.

15. The pharmaceutical composition of claim 1, wherein the active agent is an antihypothyroid hormone.

16. The pharmaceutical composition of claim 1, wherein the active agent is an antihypertensive agent.

17. The pharmaceutical composition of claim 1, wherein the active agent is a calcium regulator.

18. The pharmaceutical composition of claim 17, wherein the calcium regulator is calcitonin, calcifediol, or parathyroid hormone.

19. A pharmaceutical composition in the form of a gel for transdermal or transmucosal administration of an androgen hormone to a subject, comprising as a permeation enhancing mixture: a fatty component in an amount of 0.1% to 20% by weight and comprising one of a saturated or unsaturated fatty alcohol of formula CH.sub.3--(CH.sub.2).sub.n--CH.sub.2OH, wherein n is an integer of between 8 and 12; a vehicle comprising 5% to 75% by weight of ethanol, 0.5% to 50% of propylene glycol, water, and 0.2 to 40% by weight of diethylene glycol monoethylether; a gelling agent of carbopol or a cellulose derivative in an amount of 0.2 to 3% by weight; a pH regulator of a tertiary amine or sodium hydroxide in an amount of 0.05% to 2% by weight, with all weights calculated based on the total weight of the composition and provided that the total weights of the components does not exceed 100%; and optionally, one or more of a flavor agent, saborizant, sweetener or solubilizant in an amount sufficient to impart desired properties to the composition.
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