TRANSDERMAL THERAPEUTIC SYSTEM COMPRISING NORELESTROMIN FOR CONTRACEPTION AND HORMONE REPLACEMENT

• US 20100150993A1
• Filed: 10/10/2007
• Published: 06/17/2010
• Est. Priority Date: 10/26/2006
• Status: Active Grant

• Current Assignee: LTS Lohmann Therapie-Systeme AG
• Original Assignee: LTS Lohmann Therapie-Systeme AG
• Inventors: Eifler, René, Theobald, Frank
• Granted Patent: US 9,220,691 B2
• Time in Patent Office: Days
• US Class Current: 424/449
• CPC Class Codes: A61K 31/565 not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
• CPC Class Codes: A61K 31/567 substituted in position 17 alpha, e.g. mestranol, norethandrolone
• CPC Class Codes: A61K 31/57 substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
• CPC Class Codes: A61K 9/7069 obtained otherwise than by reactions only involving carbon to carbon unsaturated bonds, e.g. polysiloxane, polyesters, polyurethane, polyethylene oxide
• CPC Class Codes: A61P 15/18 Feminine contraceptives
• CPC Class Codes: A61P 5/30 Oestrogens
• CPC Class Codes: A61P 5/34 Gestagens

Abstract

The present invention relates to a transdermal therapeutic system for applying the active ingredient norelgestromin onto the skin, optionally in combination with estrogens. It further relates to the use of such systems for hormonal contraception, and for hormone replacement therapy.

Claims

1. A transdermal therapeutic system for administration of norelgestromin comprising an active ingredient-impermeable backing layer, at least active ingredient-containing matrix layer, optionally a detachable protective layer, whereby the matrix layer contains at least:

a) a therapeutically effective dose at norelgestromin,

b) one or more silicone polymers,

c) one or more substances selected consisting of the group of diethylene glycol monoethyl ether, butanediol and 1,2-propanediol.

2. The transdermal therapeutic system as claimed in claim 1, characterized that it additionally comprises an active ingredient or its derivatives selected from the group consisting of estradiol, ethinylestradiol, and estriol.

3. The transdermal therapeutic system as claimed in claim 1, characterized that it additionally comprises an active ingredient having an agonistic effect at the estradiol receptor.

4. The transdermal therapeutic system as claimed in claim 1, characterized in that it additionally comprises one or more fatty acid salts.

5. The transdermal therapeutic system as claimed in claim 1, characterized in that it additionally comprises a polymer or combinations of such polymers selected from the group consisting of ethyl-, methyl cellulose, polyvinylpyrrolidone and lactose.

6. The transdermal therapeutic system as claimed in claim 1, characterized in that it additionally comprises one or more substances or combinations thereof selected of the group consisting of silicone oil, glycerol esters of hydrogenated resin acids, hydroabietic alcohol resin esters, hydroabietic acid resin esters, hydrogenated methyl esters of terpentine resins, esters of partially hydrogenated terpentine resins and esters of terpentine resins.

7. The transdermal therapeutic system as claimed in claim 1, characterized in that it additionally comprises a substance or combinations of such substances selected from the group consisting of tragacanth, bentonite, lactose, and colloidal silicon dioxide.

8. The transdermal therapeutic system as claimed in claim 1, characterized in that it contains additionally one or more antioxidants.

9. The transdermal therapeutic system as claimed in claim 1, characterized in that it is transparent or translucent.

10. The transdermal therapeutic system as claimed in claim 1, characterized in that it additionally comprises a nonwoven supporting layer.

11. The transdermal therapeutic system as claimed in claim 10, characterized in that the active ingredient is dissolved or suspended in a solvent, or a combination of active ingredient, is applied to the nonwoven.

12. The transdermal therapeutic system as claimed in claim 10, characterized in that the nonwoven consists of polyethylene terephthalate, regenerated cellulose, cellulose nitrate or polyethylene.

13. The transdermal therapeutic system as claimed in claim 1, characterized in that it consists of a plurality of layers which differ in their composition and/or active ingredient content.

14. A method of providing hormonal contraception to a patient in need thereof which comprises administering the transdermal therapeutic system of claim 1 to the patient.

15. A method of providing hormone replacement to a patient in need thereof which comprises administering the transdermal therapeutic system of claim 1 to the patient.

16. The transdermal therapeutic system as claimed in claim 4, wherein the one or more fatty acid salts is sodium laurate.