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Details for Patent: 8,980,290

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Details for Patent: 8,980,290

Title:Transdermal compositions for anticholinergic agents
Abstract: The present invention relates generally to compositions or formulations for transdermal or transmucosal administration of anticholinergic agents such as oxybutynin. The invention utilizes a novel delivery vehicle and is a substantially malodorous-free and irritation free transdermal formulation which is substantially free of long chain fatty alcohols, long-chain fatty acids, and long-chain fatty esters. A method is disclosed for treating a subject for urinary incontinence with these formulations while reducing the incidences of peak concentrations of drug and undesirable side effects associated with oral anticholinergics.
Inventor(s): Carrara; Dario Norberto R. (Oberwil, CH), Grenier; Arnaud (Steinbrunn le haut, FR)
Assignee: Antares Pharma IPL AG (Zug, CH)
Filing Date:Nov 06, 2009
Application Number:12/614,216
Claims:1. A composition for transdermal or transmucosal administration of oxybutynin consisting essentially of: oxybutynin in an amount between 1 to 3% by weight of the composition; a delivery vehicle which consists essentially of a C2 to C4 alkanol present in an amount of 45 to no more than 65% by weight of the composition, a polyalcohol selected from the group consisting of propylene glycol, dipropylene glycol, polyethylene glycol, glycerin, and mixtures thereof in an amount greater than 15 to about 30% by weight of the composition, a monoalkyl ether of diethylene glycol in an amount between about 1 to 5% by weight of the composition, and water, so that the delivery vehicle provides permeation enhancement of oxybutynin through mammalian dermal or mucosal surfaces; and optionally at least one excipient selected from the group consisting of gelling agents, antimicrobials, preservatives, and neutralizing agents.

2. The composition of claim 1, wherein the oxybutynin is present as oxybutynin free base, as a pharmaceutically acceptable salt of oxybutynin, or as a mixture thereof.

3. The composition of claim 2, wherein the pharmaceutically acceptable salt of oxybutynin is selected from the group consisting of acetate, bitartrate, citrate, edetate, edisylate, estolate, esylate, fumarate, gluceptate, gluconate, glutamate, hydrobromide, hydrochloride, lactate, malate, maleate, mandelate, mesylate, methylnitrate, mucate, napsylate, nitrate, pamoate, pantothenate, phosphate, salicylate, stearate, succinate, sulfate, tannate and tartrate.

4. The composition of claim 1, wherein the alkanol is selected from the group consisting of ethanol, isopropanol, n-propanol, and mixtures thereof; wherein the polyalcohol is selected from the group consisting of propylene glycol, dipropylene glycol, and mixtures thereof; and wherein the monoalkyl ether of diethylene glycol is selected from the group consisting of monomethyl ether of diethylene glycol, monoethyl ether of diethylene glycol, and mixtures thereof.

5. The composition of claim 1, wherein the at least one excipient selected from the group consisting of gelling agents, antimicrobials, preservatives, and neutralizing agents is present.

6. The composition of claim 1 wherein the formulation is in the form of a topical gel, lotion, foam, cream, spray, aerosol, ointment, emulsion, microemulsion, nanoemulsion, suspension, liposomal system, lacquer, patch, bandage, or occlusive dressing.

7. The composition according to claim 1 wherein the polyalcohol is present in an amount between about 20 to 30% by weight of the composition.

8. The composition according claim 1, wherein the oxybutynin is present as oxybutynin free base; and wherein the alkanol is selected from a group consisting of ethanol, isopropanol, and a mixture thereof in an amount between about 45 and 60% by weight of the composition; the polyalcohol is propylene glycol; the monoalkyl ether of diethylene glycol is monoethyl ether of diethylene glycol; and the polyalcohol and monoethyl ether of diethylene glycol are present in a weight ratio of 8:1.

9. A method for administering oxybutynin to a mammal in need thereof which comprises topically or transdermally administering to the skin or the mucosa of a mammal a composition according to claim 1.

10. The method of claim 9, wherein the mammal is a human and the oxybutynin is administered for treating hyperactivity of the detrusor muscle with frequent urge to urinate, increased urination during the night, urgent urination, involuntary urination with or without the urge to urinate, painful or difficult urination, detrusor hyperreflexia and detrusor instability.

11. The method of claim 10, wherein a daily dose of oxybutynin of between about 40 and about 100 mg is administered upon the abdomen, shoulder, arm, or thigh of the subject.

12. A composition for transdermal or transmucosal administration of oxybutynin consisting of: oxybutynin present as oxybutynin free base, as a pharmaceutically acceptable salt of oxybutynin, or as a mixture thereof and in an amount between 1 to 3% by weight of the composition; a delivery vehicle which consists of a C2 to C4 alkanol present in an amount of between about 45 to no more than 65% by weight of the composition, a polyalcohol selected from a group consisting of propylene glycol, dipropylene glycol, polyethylene glycol, glycerin, and mixtures thereof in an amount above 15 to 30% by weight of the composition, a monoalkyl ether of diethylene glycol in an amount between about 1 to 5% by weight of the composition, and water, to provide permeation enhancement of oxybutynin through mammalian dermal or mucosal surfaces; and optionally at least one excipient selected from the group consisting of gelling agents, preservatives, and neutralizing agents.

13. The composition of claim 12, wherein the pharmaceutically acceptable salt of oxybutynin is selected from the group consisting of acetate, bitartrate, citrate, edetate, edisylate, estolate, esylate, fumarate, gluceptate, gluconate, glutamate, hydrobromide, hydrochloride, lactate, malate, maleate, mandelate, mesylate, methylnitrate, mucate, napsylate, nitrate, pamoate, pantothenate, phosphate, salicylate, stearate, succinate, sulfate, tannate and tartrate.

14. The composition of claim 12, wherein the alkanol is selected from the group consisting of ethanol, isopropanol, n-propanol, and mixtures thereof; the polyalcohol is selected from the group consisting of propylene glycol, dipropylene glycol, polyethylene glycol, glycerin, and mixtures thereof and the monoalkyl ether of diethylene glycol is selected from the group consisting of monomethyl ether of diethylene glycol, monoethyl ether of diethylene glycol, and mixtures thereof.

15. The composition of claim 12, wherein the formulation is in the form of a topical gel.

16. The composition of claim 12, wherein the alkanol is present in an amount between about 45 and 60% by weight of the composition; the polyalcohol is present in an amount between about 20 to 30% by weight of the composition; the monoalkyl ether of diethylene glycol is monoethyl ether of diethylene glycol; and the polyalcohol and monoethyl ether of diethylene glycol are present in a weight ratio of 8:1.

17. A composition for transdermal or transmucosal administration of oxybutynin consisting of: oxybutynin present as oxybutynin free base, as a pharmaceutically acceptable salt of oxybutynin, or as a mixture thereof and in an amount between 1 to 3% by weight of the composition; a delivery vehicle which consists of ethanol present in an amount of between about 45 to no more than 60% by weight of the composition, a polyalcohol selected from a group consisting of propylene glycol and dipropylene glycol in an amount above 15 to about 20% by weight of the composition, monoethyl ether of diethylene glycol in an amount between about 1 to 5% by weight of the composition, and water, to provide permeation enhancement of oxybutynin through mammalian dermal or mucosal surfaces, with the polyalcohol and monoethyl ether of diethylene glycol present in a weight ratio of 8:1; an excipient of a gelling agent so that the composition is in the form of a gel; and optionally at least one excipient selected from the group consisting of preservatives, and neutralizing agents.

18. The composition of claim 17, wherein the oxybutynin is present as oxybutynin free base in an amount of 3% by weight of the composition, the polyalcohol is propylene glycol in an amount of about 20% by weight of the composition, and the monoethyl ether of diethylene glycol is present in an amount of about 2.5% by weight of the composition.

19. The composition of claim 18, wherein gelling agent is present in an amount of 0.3% to 2%, and the neutralizing agent is hydrochloric acid.

20. The composition of claim 19, wherein the oxybutynin is present as the free base and in an amount of 3% by weight of the composition; and, the ethanol is anhydrous ethanol present in an amount of about 50.72% by weight of the composition, the polyalcohol is propylene glycol present in an amount of about 20% by weight of the composition, the monoethyl ether of diethylene glycol is present in an amount of about 2.5% by weight of the composition, the gelling agent is hydroxypropylcellulose in an amount of about 1 to 2% by weight of the composition, and the preservative is butylhydroxytoluene in an amount of about 0.05% by weight of the composition.
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