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The present invention is directed to compositions, and methods for the delivery of drugs. Devices for the transdermal delivery of drugs are also provided. Specifically, the present invention relates to hydrogel compositions comprising water and a base mixture, in which the base mixture comprises: (i) a gelling agent consisting of methycellulose or at least one natural gum, or a mixture thereof; (ii) at least one natural gum: (iii) glucose; (iv) propylparaben; (v) methyl paraben; and (vi) sodium chloride.

InventeursDennis Lee Schmirler, Edward Malcolm Portman, Michael S. Christensen
Examinateur principal: Kathryne E. Shelborne
Classification américaine actuelle424/449; 424/430; 424/443; 424/455; 424/484
Classification internationale: A61K 970

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Citations

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Référencé par

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Revendications

1. A composition consisting essentially of:

(a) 3-12% of a base mixture consisting essentially of: 50-80% (by weight) methyl cellulose, 15-25% of a natural gum selected from the xanthin and guar gums, 3-7% glucose, 2-3.5% propylparaben, 1.5-3% methylparaben, 1-3% sodium chloride and 0.75-3.5% pectin;
(b) 0.5-15% by weight of a substituted urea of the formula R--NH--CO--NH.sub.2, wherein R is hydrogen, hydroxyl or lower alkyl having from 1 to 8 carbon atoms selected from the group consisting of methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl, hexyl, heptyl and octyl;
(c) 5-20% by weight of a hormone selected from the group consisting of progesterone, progestin, estrogen, and testosterone, or a mixture of any two or more of the foregoing;
(d) 0-20% by weight propylene glycol; and
(e) 20-80% by weight water;

in which said base mixture and water form a hydrogel.

2. A composition consisting essentially of:

(a) about 9% by weight of a base mixture consisting essentially of: about 63% (by weight) methyl cellulose, about 21% guar gum, about 5% glucose, about 3.5% propylparaben, about 3% methylparaben, about 1.5% sodium chloride and about 3% pectin;
(b) about 2% by weight of a substituted urea of the formula: R--NH--CO--NH.sub.2, wherein R is hydrogen, hydroxyl or lower alkyl having from 1 to 8 carbon atoms selected from the group consisting of methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl, hexyl, heptyl and octyl;
(c) about 10% by weight of progesterone;
(d) about 20% by weight propylene glycol; and
(e) 59% by weight water; in which said base mixture and water form a hydrogel.

3. A composition consisting essentially of:

(a) about 9% by weight of a base mixture consisting essentially of: about 63% (by weight) methyl cellulose, about 21% guar gum, about 5% glucose, about 3.5% propylparaben, about 3% methylparaben, about 1.5% sodium chloride and about 3% pectin;
(b) about 2% by weight butylurea;
(c) about 10% by weight of progesterone;
(d) about 20% by weight propylene glycol; and
(e) about 59% by weight water;

in which said base mixture and water form a hydrogel.

4. A composition consisting essentially of:

(a) a base mixture consisting essentially of methyl cellulose, guar gum, glucose, propylparaben, methyl paraben, sodium chloride and pectin;
(b) butylurea
(c) progesterone
(d) propylene glycol; and
(e) water;

in which said base mixture and water from a hydrogel.

5. A method of treating or preventing a condition responsive to hormone replacement therapy comprising placing a composition of claim 1 or 2, said composition comprising a therapeutically effective amount of said hormone or mixture of hormones, in contact with the skin of a subject in need of such treatment.

6. The method of claim 5 wherein said condition is selected from the group consisting of premenstrual syndrome, menopause, infertility, osteoporosis, dysfunctional bleeding, corpus luteum failure, senile vulvo-vaginitis, and hypogonadism.

7. A method of providing contraception to a male or female subject comprising placing a composition of claim 1 or 2, said composition comprising a therapeutically effective amount of said hormone or mixture of hormones, in contact with the skin of a subject in need of contraception.

8. The method of claim 7 wherein said subject is female and said hormone or mixture of hormones is selected from the group consisting of progesterone, progestin, estrogen, and a mixture of any two or more of the foregoing.

9. The method of claim 8 wherein said hormone is a mixture of one or more estrogens and one or more protesting.

10. The method of claim 8 wherein said hormone is a mixture of progesterone and one or more estrogens.

11. The method of claim 8 wherein said hormone is selected from the group consisting of progesterone and progestins.

12. The method of claim 7 wherein said subject is a male and said hormone is testosterone.

13. A method of delivering a therapeutically effective amount of a hormone or mixture of hormones to the bloodstream of a subject comprising contacting the skin of said subject with a composition of claim 1 or 2 comprising a therapeutically effective amount of said hormone or mixture of hormones.

14. A method for treating vaginal yeast infection comprising placing a composition of claim 1 or 2 inside the vagina of a female subject suffering from yeast infection.

15. A method for providing contraception to a female subject comprising placing a composition of claim 1 or 2 inside the vagina of a female subject in need of contraception.

16. A method for treating vaginal dryness comprising placing a composition of claim 1 or 2 inside the vagina of a female subject suffering from vaginal dryness.

17. A method for vaginal delivery of a drug comprising placing a composition of claim 1 or 2 inside the vagina of a female subject.