Transdermal, hormone-delivering therapeutic system

• US 6,274,165 B1
• Filed: 08/25/1999
• Issued: 08/14/2001
• Est. Priority Date: 01/14/1997
• Status: Expired due to Fees

• Current Assignee: LTS Lohmann Therapie-Systeme AG
• Original Assignee: LTS Lohmann Therapie-Systeme AG
• Inventors: Seibertz, Frank, Meconi, Reinhold
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): GHALI, ISIS A D
• Application Number:
  US09/341,212
• Time in Patent Office: 720 Days
• Field of Search: 424/449, 424/448, 424/447
• US Class Current: 424/448
• 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 31/57 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: A61K 9/7076 the adhesive comprising ingredients of undetermined constitution or reaction products thereof, e.g. rosin or other plant resins

Abstract

An active compound-containing patch for the controlled delivery of oestradiol or its pharmaceutically acceptable derivatives, alone or in combination with gestagens, to human or animal skin, having an active compound-containing reservoir based on ethylcellulose and contact adhesives comprising adhesive resins is characterized by a contact adhesive having a high plasticizer content.

Claims

1. Active compound-containing patch for the controlled delivery of oestradiol or its pharmaceutically acceptable derivatives alone or in combination with gestagen to human or animal skin consisting essentially of an active compound-containing reservoir based on ethylcellulose and contact adhesives wherein the contact adhesive has a proportion of plasticizer of at least 15% by weight.

2. The patch of claim 1 wherein the contact adhesive comprises adhesive resins specifically excluding n-substituted o-toluidines.

3. The patch of claim 2 further comprising esters of optionally hydrogenated colophony as a tackifying resin.

4. The patch of claim 2 further comprising an emulsifier content in the contact adhesive of at least 15% by weight.

7. The patch of claim 2 further comprising a content of antioxidants and adsorption enhancers in the contact adhesive.

8. The patch of claim 2 further comprising a content of absorption enhancers.

9. The patch of claim 2 further comprising a content of antioxidants.

5. An active compound-containing patch for the controlled delivery of oestradiol or its pharmaceutically acceptable derivatives alone or in combination to human or animal skin comprising:

5-25% by weight of ethylcellulose

10-70% by weight of tackifying resin

20-40% by weight of plasticizer and emulsifiers

1-10% by weight of oestradiol content

1-15% by weight of gestagen.

6. The patch of claim 5 wherein the gestagen comprises norethindrone acetate.

10. Active compound-containing patch for the controlled delivery of estradiol or its pharmaceutically acceptable derivatives alone or in combination with gestagen to human or animal skin consisting of:

(a) an active compound-containing reservoir based on ethyl cellulose;

(b) contact adhesive wherein the contact adhesive has a proportion of plasticizer of at least 15% by weight;

(c) esters of optionally hydrogenated colophony as a tackifying resin;

(d) a content of absorption enhancers; and

(e) a content of antioxidants.

11. The active compound-containing pouch according to claim 10 wherein said plasticizer is isopropyl myristate.

12. The active compound-containing pouch according to claim 10 wherein said plasticizer is polyoxyethylene-(9) nonylphenol.

13. The active compound-containing pouch according to claim 10 wherein said plasticizer is polyoxyethylene-(2)-oleyl alcohol.

14. The active compound containing pouch according to claim 10 wherein said plasticizer is polyoxyethylene-(4)-lauryl alcohol.

15. The active compound containing pouch according to claim 10 wherein said plasticizer is medium chain triglycerides.

16. The active compound-containing pouch according to claim 10 wherein said plasticizer is 2-Octyldodecanol.

17. The active compound patch for the controlled delivery of estradiol or its pharmaceutically acceptable derivatives alone or in combination with gestagen to human or animal skin consisting essentially of:

(a) an active compound-containing reservoir based on ethyl cellulose;

(b) contact adhesives wherein the contact adhesive has a proportion of plasticizer of at least 15% by weight and an emulsifier content of at least 15% by weight,

(c) esters of optionally hydrogenated colophony as a tackifying resin;

(d) a content of absorption enhancers; and

(e) a content of antioxidants and specifically excluding N-substituted o-toluidines.