TRANSDERMAL HORMONE DELIVERY

• US 20180078493A1
• Filed: 08/03/2017
• Published: 03/22/2018
• Est. Priority Date: 01/27/2012
• Status: Abandoned Application

• Current Assignee: Agile Therapeutics, Inc.
• Original Assignee: Agile Therapeutics, Inc.
• Inventors: Kydonieus, Agis, Rossi, Thomas M., Arnold, Charles G., Banga, Ajay K., Sachdeva, Vishal
• Application Number:
  US15/668,505
• Publication Number:
  US 20180078493A1
• Time in Patent Office: Days
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• 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 9/0014 Skin, i.e. galenical aspects of topical compositions non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00
• CPC Class Codes: A61K 9/7053 obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
• CPC Class Codes: A61P 15/18 Feminine contraceptives

Abstract

Compositions and devices for transdermal hormone delivery are disclosed. The compositions and devices include desogestrel and enable delivery of effective amounts of progestin without the use of skin permeation enhancers.

Claims

1-19. -19. (canceled)

20. A composition for transdermal delivery of a progestin for effecting contraception in a woman, the composition being a polymeric pressure sensitive adhesive (PSA) matrix comprising a polyisobutylene (PIB) PSA, a solubility modifier, and an effective amount of desogestrel, wherein the composition

(a) has a solubility for the desogestrel of more than 3% by weight of the composition and up to 10% by weight of the composition;

(b) does not comprise a skin penetration enhancer;

(c) has a skin-contacting surface area of 5 to 20 cm²;

(d) transdermally delivers a contraceptive amount of the desogestrel when applied to the skin of a woman during a one week wear period; and

(e) comprises the desogestrel in an amount of 90% to 100% of its saturation concentration.

21. The transdermal composition of claim 20, wherein the solubility modifier comprises PVP or a PVP/VA copolymer.

22. The transdermal composition of claim 21, wherein the solubility modifier is PVP, PVP/VA, or a combination of either PVP or PVP/VA with mineral oil.

23. The transdermal composition of claim 22 wherein the PSA is a PIB comprising a mixture of about 10% high molecular weight PIB, about 50% low molecular weight PIB, and about 40% polybutene.

24. The transdermal composition of claim 23, which comprises (a) 70 to 95 wt % PIB, and (b)(i) 1 to 20 wt % mineral oil or 0.1 to 30 wt % PVP or 0.1 to 30 wt % PVP/VA or (ii) 1 to 20 wt % mineral oil and either 0.1 to 30 wt % PVP or 0.1 to 30 wt % PVP/VA.

25. The transdermal composition of claim 24 that comprises 80 to 90 wt % PIB, 5 to 15 wt % mineral oil, and 0.1 to 10 wt % PVP or PVP/VA.

26. The transdermal composition of claim 24 that has a thickness of 0.1 to 0.6 mm.

27. The transdermal composition of claim 26 that has a thickness of 0.2 to 0.4 mm.

28. The transdermal composition of claim 20 that also comprises an estrogen.

29. The transdermal composition of claim 28, wherein the estrogen is ethinyl estradiol.

30. The transdermal composition of claim 20, which comprises an antioxidant.

31. A transdermal hormone delivery device comprising:

a composition for transdermal delivery of a progestin for effecting contraception in a woman, the composition being a polymeric pressure sensitive adhesive (PSA) matrix comprising a PIB PSA, a solubility modifier and desogestrel, wherein the composition

(a) has a solubility for the desogestrel of more than 3% by weight of the composition and up to 10% by weight of the composition;

(b) does not comprise a skin penetration enhancer;

(c) has a skin-contacting surface area of 5 to 20 cm² and a thickness of 0.1 to 0.6 mm;

(d) transdermally delivers a contraceptive amount of desogestrel when applied to the skin of a woman during a one week wear period, at a rate of at least 90 micrograms per day; and

(e) comprises the desogestrel in an amount of 90% to 100% of its saturation concentration;

wherein the transdermal composition comprises a skin contacting surface and a non-skin contacting surface, with a backing layer disposed on the non-skin contacting surface of the transdermal composition, and a release liner disposed on the skin contacting surface of the transdermal composition.

32. The device of claim 31, wherein the transdermal composition comprises (a) 70 to 95 wt % PIB, and (b) (i) 1 to 20 wt % mineral oil or 0.1 to 10 wt % PVP or PVP/VA or (ii) 1 to 20 wt % mineral oil and 0.1 to 10 wt % PVP or PVP/VA.

33. The device of claim 31, wherein the transdermal composition comprises 80 to 90 wt % PIB, 5 to 15 wt % mineral oil, and 0.1 to 5 wt % PVP or PVP/VA, and has a surface area of about 15 cm².

34. The device of claim 31, wherein the transdermal composition comprises an antioxidant.

35. The device of claim 31, wherein the composition has a skin-contacting surface area of 15 cm² or less.

36. The device of claim 31, wherein the device is transparent.

37. A method of delivering a progestin to a patient in need thereof, which comprises applying to the skin of the patient a composition for transdermal delivery of the progestin, wherein the composition is a polymeric pressure sensitive adhesive (PSA) matrix comprising a polyisobutylene (PIB) PSA, a solubility modifier, and an effective amount of desogestrel, wherein the composition

(a) has a solubility for the desogestrel of more than 3% by weight of the composition and up to 10% by weight of the composition;

(b) does not comprise a skin penetration enhancer;

(c) has a skin-contacting surface area of 5 to 20 cm²;

(d) transdermally delivers a contraceptive amount of the desogestrel when applied to the skin of a woman during a one week wear period; and

(e) comprises the desogestrel in an amount of 90% to 100% of its saturation concentration.

38. The method of claim 37, wherein the composition has a skin contacting surface and a non-skin contacting surface, and is disposed within a transdermal hormone delivery device comprising a backing layer disposed on the non-skin contacting surface of the transdermal composition, and a release liner disposed on the skin contacting surface of the transdermal composition.

39. The method of claim 38 that comprises delivering a progestin to effect contraception in a woman by applying to the skin of the woman the transdermal delivery device and replacing the transdermal delivery device once each week for three of four successive weeks of a menstrual cycle, for successive menstrual cycles extending as contraception is desired.