Permeation enhancing compositions for anticholinergic agents
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-031/24
A61K-031/21
A61K-009/00
출원번호
US-0120306
(2005-05-02)
등록번호
US-7425340
(2008-09-16)
발명자
/ 주소
Grenier,Arnaud
Carrara,Dario Norberto R.
Besse,Celine
출원인 / 주소
Antares Pharma IPL AG
대리인 / 주소
Winston & Strawn LLP
인용정보
피인용 횟수 :
11인용 특허 :
93
초록
A transdermal or topical composition including anticholinergic agents, such as oxybutynin, a urea-containing compound and a carrier system. A method is disclosed for treating a subject for urinary incontinence while reducing the incidences of peak concentrations of drug and undesirable side effects.
대표청구항▼
What is claimed is: 1. A non-occlusive composition for topical or transdermal administration of an anticholinergic or antispasmodic agent, the composition comprising: at least one anticholinergic or antispasmodic agent of at least one of oxybutynin, flavoxate, imipramine, propantheline, phenylpropa
What is claimed is: 1. A non-occlusive composition for topical or transdermal administration of an anticholinergic or antispasmodic agent, the composition comprising: at least one anticholinergic or antispasmodic agent of at least one of oxybutynin, flavoxate, imipramine, propantheline, phenylpropanolamine, darifenacin, duloxetine, tolterodine tartrate, trospium, or solifenacin succinate or a pharmaceutically acceptable salt thereof in an amount between about 0.1 to 20% by weight of the formulation; a compound selected from the group consisting of urea, 1,3-dimethylurea, 1,1-diethylurea, 1-acetyl-1-phenylurea, isopropylideneurea, allophanic acid, hydantoic acid, allophanoyl, pyrrolidone carboxylic acid, biuret, thiobiuret, dithiobiuret, triuret and 2-(3-methylureido)-1-naphthoic acid in an amount of between about 1 to 20% by weight of the formulation for enhancing permeation of the anticholinergic or antispasmodic agent; and a carrier suitable for transdermal or topical administration and comprising the combination of an alcohol, a polyalcohol, and either a monoalkyl ether of diethylene glycol or a tetraglycol furol present in the carrier in a combined amount effective with the amount of urea-containing compound to enhance permeation of the anticholinergic or antispasmodic agent through dermal or mucosal surfaces; wherein the alcohol is present in an amount of about 30 to 70% by weight of the formulation, the polyalcohol is present in an amount of about 1 to 15% by weight of the formulation, and the monoalkyl ether of diethylene glycol or tetraglycol furol is present in an amount between about 1 to 15% by weight of the formulation. 2. The composition of claim 1, wherein the anticholinergic or antispasmodic agent is oxybutynin, oxybutynin free base, or a pharmaceutically acceptable salt thereof, the urea-containing compound is urea, the alcohol is ethanol, propanol, isopropanol, 1-butanol, 2-butanol or a mixture thereof, the polyalcohol is propylene glycol, dipropylene glycol or a mixture of thereof; the monoalkyl ether of diethylene glycol, when present, is diethylene glycol monomethyl ether, diethylene glycol monoethyl ether or a mixture thereof, and the tetraglycol, when present, is glycofurol. 3. The composition of claim 2, wherein the oxybutynin is as a racemate or an isomer. 4. 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. 5. The composition of claim 2, wherein the composition provides a steady plasma concentration of oxybutynin to a subject administered with the composition. 6. The composition of claim 1, further comprising a gelling agent, solvent, antimicrobial agent, preservative, antioxidant, buffer, humectant, sequestering agent, moisturizer, emollient, or additional permeation enhancer. 7. The composition of claim 1, wherein the composition is in the form of an ointment, cream, gel, foam, lotion, liposome, micelle, microsphere, lacquer, non occlusive dressing or a combination thereof. 8. A non-occlusive composition for topical or transdermal administration of oxybutynin, the composition comprising: oxybutynin, oxybutynin free base or a pharmaceutically acceptable salt of oxybutynin present in an amount between about 1 to 5% by weight of the formulation; a compound selected from the group consisting of urea, 1,3-dimethylurea, 1,1-diethylurea, 1-acetyl-1-phenylurea, isopropylideneurea, allophanic acid, hydantoic acid, allophanoyl, pyrrolidone carboxylic acid, biuret, thiobiuret, dithiobiuret, triuret and 2-(3-methylureido)-1-naphthoic acid present in an amount between about 1 to 10% by weight of the formulation; and a carrier present in an amount between about 40 to 80 percent by weight of the formulation, wherein the carrier comprises the combination of an alcohol, a polyalcohol, water and a monoalkyl ether of diethylene glycol or a tetraglycol furol, wherein the alcohol is present in an amount of about 30 to 70% by weight of the formulation, the polyalcohol is present in an amount of about 1 to 15 % by weight of the formulation, and the monoalkyl ether of diethylene glycol or tetraglycol furol is present in an amount of about 1 to 1500 by weight of the formulation. 9. The composition of claim 8, wherein the composition further includes a gelling agent present in an amount of about 1 to 10%, the alcohol is ethanol, propanol, isopropanol, 1-butanol, 2-butanol or a mixture thereof, the polyalcohol is propylene glycol, dipropylene glycol or a mixture of thereof the monoalkyl ether of diethylene glycol, when present, is diethylene glycol monomethyl ether, diethylene glycol monoethyl ether or a mixture thereof, and the tetraglycol, when present, is glycofurol. 10. A method for treating overactive bladder or urge and urinary incontinence in a subject, the method comprising administering to a subject in need thereof, a non-occlusive topical or transdermal composition according to claim 8. 11. The method of claim 10, wherein the oxybutynin is in the form of its free base or as a pharmaceutically acceptable salt 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. 12. The method of claim 11, wherein the method reduces peak plasma concentrations of oxybutynin, and further wherein the method lowers a number of incidences or lowers intensities of oxybutynin-associated side effects. 13. The method of claim 11, wherein the oxybutynin is in the form of its free base and the method provides a steady plasma oxybutynin concentration. 14. The method of claim 11, wherein the daily dosage of oxybutynin is about 30 to 60 milligrams over a 24-hour period, and further wherein composition is in the form of a gel. 15. The method of clam 10, wherein the oxybutynin is recemate and further wherein the subject is dosed with about 1 to about 20 mg over a 24-hour period. 16. The method of claim 10, wherein the oxybutynin is an enantiomer, and further wherein the subject is dosed with about 0.5 to about 15 mg over a 24-hour period. 17. The method of claim 10, wherein the composition further comprises a gelling agent, solvent, antimicrobial agent, preservative, antioxidant, buffer, humectant, sequestering agent, moisturizer, emollient, or additional permeation enhancer. 18. The method of claim 10, wherein the composition administered to the subject is in the form of an ointment, cream, gel, foam, lotion, liposome, micelle, microsphere, lacquer, patch, bandage, occlusive or non occlusive dressing or a combination thereof 19. A non-occlusive gel composition for topical or transdermal administration of oxybutynin, consisting essentially of: oxybutynin, oxybutynin free base or a pharmaceutically acceptable salt of oxybutynin present in an amount between about 1 to 5% by weight of the formulation; urea present in an amount of about 1 to 10% by weight of the formulation; and a carrier present in an amount of about 40 to 80 percent by weight of the formulation, wherein the carrier consists essentially of the combination of an alcohol selected from the group consisting of ethanol, propanol, isopropanol, 1-butanol, 2-butanol or a mixture thereof, a polyalcohol selected from the group consisting of propylene glycol, dipropylene glycol or a mixture thereof, a monoalkyl ether of diethylene glycol selected from the group consisting of diethylene glycol monomethyl ether, diethylene glycol monoethyl ether or a mixture thereof, or a tetraglycol furol, and water, wherein the alcohol is present in an amount of about 30 to 70 percent by weight of the formulation, the polyalcohol is present in an amount of about 1 to 15% by weight of the formulation, and the monoalkyl ether of diethylene glycol or a tetraglycol furol, whichever is included, is present in an amount of about 1 to 15% by weight of the formulation. 20. A method for treating overactive bladder or urge and urinary incontinence in a subject, the method comprising administering to a subject in need thereof, a non-occlusive topical or transdermal composition according to claim 19.
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