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. |
Citations|
| US3964482 | 17 mai 1971 | 22 juin 1976 | Alza Corporation | Drug delivery device | | US4590190 | 1 juil. 1983 | 20 mai 1986 | Nitto Electric Industrial Co., Ltd. | Method for percutaneously administering physiologically active agents using an alcohol adjuvant and a solvent | | US4593053 | 7 déc. 1984 | 3 juin 1986 | Medtronic, Inc. | Hydrophilic pressure sensitive biomedical adhesive composition | | US4637930 | 31 janv. 1985 | 20 janv. 1987 | Yamanouchi Pharmaceutical Co, Ltd. | Transdermal formulation of nicardipine hydrochloride | | US4693887 | 3 mai 1984 | 15 sept. 1987 | The Kendall Company | Microphase separated hydrogels for controlled release of bioactive materials | | US4710497 | 31 mai 1985 | 1 déc. 1987 | Nitto Electric Industrial Co., Ltd. | Method for percutaneously administering physiologically active agents | | US4746515 | 26 févr. 1987 | 24 mai 1988 | ALZA Corporation | Skin permeation enhancer compositions using glycerol monolaurate | | US4752612 | 23 janv. 1986 | 21 juin 1988 | Nitto Electrical Industrial Co., Ltd. | Method and percutaneously administering physiologically active agents using an alcohol adjuvant and a solvent | | US4797284 | 12 mars 1986 | 10 janv. 1989 | Merck & Co., Inc. | Transdermal drug delivery system | | US4818540 | 29 août 1986 | 4 avr. 1989 | Rutgers, The State University of New Jersey | Transdermal fertility control system and process | | US4861764 | 17 nov. 1986 | 29 août 1989 | Macro Chem. Corp. | Percutaneous absorption enhancers, compositions containing same and method of use | | US4863738 | 23 nov. 1987 | 5 sept. 1989 | ALZA Corporation | Skin permeation enhancer compositions using glycerol monooleate | | US4863952 | 4 oct. 1985 | 5 sept. 1989 | Nitto Electric Industrial Co., Ltd. | Method of promoting percutaneous drug absorption with 2-pyrrolidin-2-one 5-carboxylic acids and esters thereof | | US4865848 | 26 févr. 1987 | 12 sept. 1989 | ALZA Corporation | Skin permeation enhancer compositions using sucrose esters | | US4880663 | 13 juin 1988 | 14 nov. 1989 | Nordson Corporation | Method for applying a moistureproof insulative coating to printed circuit boards using triangular or dovetail shaped liquid films emitted from a flat-pattern nozzle | | US4883669 | 30 mai 1986 | 28 nov. 1989 | Rutgers, The State University of New Jersey | Transdermal absorption dosage unit for estradiol and other estrogenic steroids and process for administration | | US4900555 | 13 oct. 1988 | 13 févr. 1990 | Alza Corporation | Skin permeation enhancer compositions using sucrose esters | | US4906169 | 16 déc. 1988 | 6 mars 1990 | Rutgers, The State University of New Jersey | Transdermal estrogen/progestin dosage unit, system and process | | US4913905 | 25 mars 1988 | 3 avr. 1990 | Ciba-Geigy Corporation | Transdermal therapeutic systems for active ingredient combinations | | US4940586 | 13 oct. 1988 | 10 juil. 1990 | Alza Corporation | Skin permeation enhancer compositions using sucrose esters | | US4942158 | 13 oct. 1988 | 17 juil. 1990 | Eastman Kodak | Transdermal steroid penetrant compositions and methods utilizing isopropanol and isobutanol | | US4960771 | 12 juil. 1988 | 2 oct. 1990 | | Oxazolidinone penetration enhancing compounds | | US4973468 | 22 mars 1989 | 27 nov. 1990 | Cygnus Research Corporation | Skin permeation enhancer compositions | | US4989607 | 30 mars 1989 | 5 févr. 1991 | | Highly conductive non-stringy adhesive hydrophilic gels and medical electrode assemblies manufactured therefrom | | US5019395 | 9 août 1989 | 28 mai 1991 | Warner-Lambert Company | Compositions with enhanced penetration | | US5023084 | 16 déc. 1988 | 11 juin 1991 | Rutgers, The State University of New Jersey | Transdermal estrogen/progestin dosage unit, system and process | | US5030629 | 11 août 1989 | 9 juil. 1991 | | Compositions and method comprising heterocyclic compounds containing two heteroatoms as membrane penetration enhancers | | US5053227 | 12 juin 1990 | 1 oct. 1991 | Cygnus Therapeutic Systems | Skin permeation enhancer compositions, and methods and transdermal systems associated therewith | | US5059426 | 12 juin 1990 | 22 oct. 1991 | Cygnus Therapeutic Systems | Skin permeation enhancer compositions, and methods and transdermal systems associated therewith | | US5064654 | 20 avr. 1990 | 12 nov. 1991 | Ciba-Geigy Corporation | Mixed solvent mutually enhanced transdermal therapeutic system | | US5102666 | 11 sept. 1990 | 7 avr. 1992 | Oramed, Inc. | Calcium polycarbophil controlled release composition and method | | US5122383 | 17 mai 1991 | 16 juin 1992 | Theratech, Inc. | Sorbitan esters as skin permeation enhancers | | US5128376 | 4 sept. 1990 | 7 juil. 1992 | Nitto Denko Corporation | Method for percutaneously administering physiologically active agents using an adjuvant a solvent and a diol moderator | | US5143071 | 26 mars 1990 | 1 sept. 1992 | Nepera, Inc. | Non-stringy adhesive hydrophilic gels | | US5198223 | 9 mars 1992 | 30 mars 1993 | Alza Corporation | Transdermal formulations, methods and devices | | US5212199 | 21 avr. 1992 | 18 mai 1993 | Theratech, Inc. | Sorbitan esters as skin permeation enhancers | | US5227169 | 9 mars 1992 | 13 juil. 1993 | Theratech, Inc. | Sorbitan esters as skin permeation enhancers | | US5229423 | 6 mars 1992 | 20 juil. 1993 | Albert Einstein College of Medicine of Yeshiva University | Use of butylurea as a contraceptive agent | | US5232705 | 1 avr. 1992 | 3 août 1993 | Alza Corporation | Dosage form for time-varying patterns of drug delivery | | US5254338 | 8 févr. 1991 | 19 oct. 1993 | Showa Denko K.K. | External application base or auxiliary agent and external application composition for human being or animal containing the same | | US5296230 | 3 avr. 1989 | 22 mars 1994 | Rutgers, The State University of New Jersey | Transdermal fertility control system and process | | US5300059 | 19 nov. 1991 | 5 avr. 1994 | Hydro Slip Technologies Inc. Albert Einstein College of Medicine | Bloodbag and method of making same | | US5314694 | 26 mars 1993 | 24 mai 1994 | Alza Corporation | Transdermal formulations, methods and devices | | US5320850 | 12 févr. 1993 | 14 juin 1994 | ALZA Corporation | Transdermal delivery of the gestogen ST-1435 and devices therefor | | US5344655 | 17 mars 1993 | 6 sept. 1994 | Showa Denko K.K. | External application base or auxiliary agent and external application composition for human being or animal containing the same | | US5354790 | 31 août 1992 | 11 oct. 1994 | Nepera, Inc. | Methods for the preparation of non-stringy adhesive hydrophilic gels | | US5362497 | 13 janv. 1992 | 8 nov. 1994 | Takeda Chemical Industries, Ltd. | Transdermal therapeutic composition | | US5376377 | 17 déc. 1992 | 27 déc. 1994 | ALZA Corporation | Transdermal contraceptive formulations, methods and devices | | US5387611 | 3 juin 1993 | 7 févr. 1995 | Albert Einstein College of Medicine of Yeshiva University, a Division of Yeshiva University | Use of butylurea, nonoxynol-9 and benzalkonium chloride as anti-bacterial, anti-viral contraceptive agents | | US5405366 | 12 nov. 1992 | 11 avr. 1995 | Nepera, Inc. | Adhesive hydrogels having extended use lives and process for the preparation of same | | US5445611 | 8 déc. 1993 | 29 août 1995 | Non-Invasive Monitoring Company (NIMCO) | Enhancement of transdermal delivery with ultrasound and chemical enhancers | | US5482965 | 3 sept. 1993 | 9 janv. 1996 | | Compositions and method comprising aminoalcohol derivatives as membrane penetration enhancers for physiological active agents | | US5624906 | 8 déc. 1994 | 29 avr. 1997 | Lever Brothers Company, Division of Conopco, Inc. | Oral hygiene compositions comprising heteroatom containing alkyl aldonamide compounds |
Référencé par|
| US6455065 | 18 mai 1999 | 24 sept. 2002 | LecTec Corporation | Therapeutic method for treating acne or isolated pimples and adhesive patch therefor | | US6472425 | 16 juil. 1999 | 29 oct. 2002 | NitroMed, Inc. | Methods for treating female sexual dysfunctions | | US6514534 | 14 août 1998 | 4 févr. 2003 | Incept LLC | Methods for forming regional tissue adherent barriers and drug delivery systems | | US6562369 | 14 déc. 2000 | 13 mai 2003 | Dermatrends, Inc. | Transdermal administration of androgenic drugs hydroxide-releasing agents as permeation enhancers | | US6582724 | 4 oct. 2001 | 24 juin 2003 | Dermatrends, Inc. | Dual enhancer composition for topical and transdermal drug delivery | | US6586000 | 14 déc. 2000 | 1 juil. 2003 | Dermatrends, Inc. | Hydroxide-releasing agents as skin permeation enhancers | | US6673363 | 19 juin 2002 | 6 janv. 2004 | Dermatrends, Inc. | Transdermal and topical administration of local anesthetic agents using basic enhancers | | US6676961 | 6 mars 2002 | 13 janv. 2004 | Automated Carrier Technologies, Inc. | Transdermal patch assembly | | US6726673 | 24 mai 1999 | 27 avr. 2004 | Zars, Inc. | Methods and apparatus for improved administration of testosterone pharmaceuticals | | US6762202 | 8 mai 2001 | 13 juil. 2004 | NitroMed, Inc. | Infrared thermography and methods of use | | US6835392 | 13 mars 2003 | 28 déc. 2004 | Dermatrends, Inc. | Dual enhancer composition for topical and transdermal drug delivery |
Revendications1. 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. |