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Claims for Patent: 5,223,261

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Claims for Patent: 5,223,261

Title: Transdermal estradiol delivery system
Abstract:A pressure-sensitive adhesive sheet material for delivering estradiol to skin, the sheet material comprising a backing with a layer of a pressure-sensitive adhesive adjacent thereto, said pressure-sensitive adhesive layer comprising a pressure-sensitive adhesive polymer, two or more skin penetration-enhancing ingredients and estradiol. The sheet material is useful for systemic treatment of conditions associated with estradiol deficiency. Methods of using such adhesive sheet material are also described.
Inventor(s): Nelson; Gregory R. (St. Paul, MN), Zerbe; Horst-Georg (St. Paul, MN), Moore; Cheryl L. (St. Paul, MN), Wick; Steven M. (St. Paul, MN)
Assignee: Riker Laboratories, Inc. (St. Paul, MN)
Application Number:07/815,908
Patent Claims: 1. An adhesive-coated sheet material comprising:

(a) a flexible backing; and

(b) a pressure-sensitive adhesive coating contiguously adhered to one surface of said backing and comprising a homogeneous mixture of:

(i) an acrylic copolymer comprising about 91 to 98 percent by weight of a hydrophobic monomeric acrylic or methacrylic acid ester of an alkyl alcohol based on the weight of all monomers in said copolymer, the alkyl alcohol containing 4 to 10 carbon atoms and 2 to 9 percent by weight of a reinforcing monomer selected from the group consisting of acrylic acid; methacrylic acid; an alkyl acrylate or methacrylate containing 1 to 3 carbon atoms in the alkyl group acrylamide; methacrylamide; a lower alkyl-substituted acrylamide; diacetone acrylamide; N-vinyl-2-pyrrolidone; a vinyl ether; vinyl ester and a substituted ethylene;

(ii) estradiol in an amount by weight of about 0.2 to 12 percent of the total weight of said adhesive coating; and

(iii) a skin penetration enhancer combination comprising isopropyl myristate and glyceryl monolaurate in amounts of about 5 to 20 percent and about 1 to 6 percent by weight, respectively, based on the weight of said adhesive-coating, with the relative amounts being selected so as to enhance the penetration of said estradiol through skin as compared to when said adhesive coating is free of said skin penetration enhancers;

said sheet material being further characterized in that over a prolonged period it adheres suitably to skin and provides for substantially continuous transdermal delivery of estradiol to a subject in an amount which is therapeutically effective for treating a condition associated with estradiol deficiency.

2. An adhesive-coated sheet material according to claim 1, wherein said adhesive copolymer comprises said acrylic of methacrylic acid ester in an amount of about 94 to 98 percent by weight.

3. An adhesive-coated sheet material according to claim 2, wherein said adhesive copolymer comprises isooctyl acrylate as the A monomer and acrylamide as the B monomer.

4. An adhesive-coated sheet material according to claim 1, wherein the amount of estradiol in said adhesive coating is about 1 to 5 percent by weight of said adhesive coating.

5. An adhesive-coated sheet material according to claim 1, wherein the amount of estradiol in said adhesive coating is about 2 to 3.5 percent by weight of said adhesive coating.

6. An adhesive-coated sheet material according to claim 1, wherein said isopropyl myristate and glyceryl monolaurate are present in amounts by weight of about 5 to 15 percent and 2 to 4 percent, respectively, based on the weight said adhesive coating.

7. An adhesive-coated sheet material according to claim 1, wherein said skin penetration enhancer combination further comprises about 4 to 18 percent by weight of ethyl oleate based on the weight of said adhesive coating, and wherein the total amount by weight of isopropyl myristate and ethyl oleate is less than about 30 percent based on the weight of said adhesive coating.

8. A method of treating a condition associated with estradiol deficiency wherein an adhesive-coated sheet material according to claim 1 is applied and adhered to the skin of a mammal to permit systemic delivery of estradiol to said mammal.

9. An adhesive-coated sheet material comprising:

(a) a flexible backing; and

(b) a pressure-sensitive adhesive coating contiguously adhered to one surface of said backing and comprising a homogeneous mixture of:

(i) an acrylic copolymer comprising (1) about 60 to 80 percent by weight of a hydrophobic monomeric acrylic or methacrylic acid ester of an alkyl alcohol based on the weight of all monomers in said copolymer, the alkyl alcohol containing 4 to 10 carbon atoms; (2) about 4 to 9 percent by weight based on the weight of all monomers in said copolymer of a reinforcing monomer selected from the group consisting of acrylic acid, methacrylic acid, an alkyl acrylate or methacrylate containing 1 to 3 carbon atoms in the alkyl group, acrylamide, methacrylamide, a lower alkyl-substituted acrylamide, diacetone acrylamide, and N-vinyl-2-pyrrolidone; and (3) about 15 to 35 percent by weight of vinyl acetate based on the weight of all monomers in said copolymer;

(ii) estradiol in an amount by weight of about 0.2 to 12 percent of the total weight of said adhesive coating; and

(iii) a skin penetration enhancer combination comprising isopropyl myristate and glyceryl monolaurate in amounts of about 5 to 20 percent and about 1 to 6 percent by weight, respectively, based on the weight of said adhesive coating with the relative amounts being selected so as to enhance the penetration of said estradiol through skin as compared to when said adhesive coating is free of said skin penetration enhancers; said sheet material being further characterized in that over a prolonged period it adheres suitably to skin and provides substantially continuous transdermal delivery of estradiol to a subject in an amount which is therapeutically effective for treating a condition associated with estradiol deficiency.

10. An adhesive-coated sheet material according to claim 9, wherein said ester is isooctyl acrylate and said reinforcing monomer is acrylamide.

11. An adhesive-coated sheet material according to claim 9, wherein the amount of estradiol in said adhesive coating is about 1 to 5 percent by weight of said adhesive coating.

12. An adhesive-coated sheet material according to claim 9, wherein the amount of estradiol in said adhesive coating is about 2 to 3.5 percent by weight of said adhesive coating.

13. An adhesive-coated sheet material according to claim 10, wherein said isopropyl myristate and glyceryl monolaurate are present in amounts by weight of about 5 to 15 percent and 2 to 4 percent, respectively, based on the weight of said adhesive coating.

14. An adhesive-coated sheet material according to claim 9, wherein said skin penetration enhancer combination further comprises about 4 to 18% by weight of ethyl oleate based on the weight of said adhesive coating, and wherein the total amount by weight of isopropyl myristate and ethyl oleate is less than about 30% by weight based on the weight of said adhesive coating.

15. A method of treating a condition associated with estradiol deficiency wherein an adhesive-coated sheet material according to claim 9 is applied and adhered to the skin of a mammal to permit systemic delivery of estradiol to said mammal.
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