Low-dose transdermal patches with high drug release
View Patent ↗The present invention relates to the field of pharmaceutical formulation techniques. The invention provides a low dosage pharmaceutical composition for transdermal delivery of hormones, preferably a progestin, such as a Gestodene, and an estrogen, preferably Ethinylestradiol so as to achieve plasma concentration profiles effective in inhibiting ovulation in a woman.
1. Transdermal therapeutic system containing, in order:
a) a backing layer,
b) at least one drug-containing adhesive layer comprising the active ingredients Gestodene and Ethinylestradiol in a polyisobutylene-containing matrix and optionally other pharmaceutically acceptable ingredients, and
c) a release liner;
wherein the Gestodene amount is from about 0.4 to 1.5% by weight of the drug-containing layer and the Ethinylestradiol amount is about 0.5% (w/w) by weight of the drug-containing layer.
2. Transdermal therapeutic system according to claim 1 , wherein the transdermal therapeutic system contains an additional layer with an UV absorber between the backing layer and the drug-containing adhesive layer.
3. Transdermal therapeutic system according to claim 2 , wherein the UV absorber is a Tinuvin or Tinosorb UV absorber.
4. Transdermal therapeutic system according to claim 3 , wherein the UV absorber is Tinosorb S.
5. Transdermal therapeutic system according to claim 2 , wherein the transdermal therapeutic system contains an additional intermediate or separation layer between the additional layer with an UV absorber and the drug-containing adhesive layer.
6. Transdermal therapeutic system according to claim 1 , wherein the Gestodene amount is from about 0.9 to 1.5% by weight of the drug-containing layer.
7. Transdermal therapeutic system according to claim 1 containing, in order:
a) a backing layer,
b) an adhesive layer comprising a UV absorber,
c) an intermediate layer which is impermeable to UV absorbers and/or the active ingredients Gestodene and Ethinyl Estradiol,
d) at least one polyisobutylene-containing adhesive layer comprising the active ingredients Gestodene and Ethinylestradiol and pharmaceutically acceptable ingredients,
e) a release liner.
8. Transdermal therapeutic system according to claim 1 containing Gestodene in an amount from about 0.38 to 2.3 mg.
9. Transdermal therapeutic system according to claim 1 containing Ethinylestradiol in an amount from about 0.15 to 0.6 mg.
10. Transdermal therapeutic system according to claim 1 having a size of 3 to 20 cm 2 .
11. Transdermal therapeutic system according to claim 1 containing 1.575 mg Gestodene and 0.55 mg Ethinylestradiol or 1.05 mg Gestodene and 0.55 mg Ethinylestradiol or 0.525 mg Gestodene and 0.55 mg Ethinylestradiol with a size of 11 cm 2 .
12. Transdermal therapeutic system according to claim 1 containing less than 5% of penetration enhancers.
13. Transdermal therapeutic system according to claim 1 containing dimethylisosorbide in an amount of less than 0.5% (w/w) by weight of drug-containing layer.
14. A method for contraception in women comprising administering a transdermal therapeutic system according to claim 1 .
15. Transdermal therapeutic system according to claim 1 as a dosage unit for continuous administration over 7 days.
16. Kit comprising 1-52 dosage units as claimed in claim 15 .
17. Transdermal therapeutic system according to claim 15 wherein the dosage unit has 0.525-2.1 mg Gestodene per dosage unit together with 0.55 mg Ethinylestradiol in a polyisobutylene-containing matrix with a size of 11 cm 2 .
18. Transdermal therapeutic system according to claim 17 , wherein the dosage unit contains 0.825 mg Tinosorb S.
19. Transdermal therapeutic system according to claim 17 , wherein the dosage unit contains 1.05 to 1.575 mg Gestodene.
20. A transdermal delivery system of claim 1 containing Gestodene in an amount from about 0.525 to 2.1 mg.
21. A transdermal delivery system of claim 1 containing Gestodene in an amount from about 1.05 to 1.575 mg.
22. A transdermal delivery system of claim 1 containing Ethinylestradiol in an amount from about 0.35 to 0.55 mg.
23. A transdermal delivery system of claim 1 having a size of about 5 to 15 cm 2 .
24. A transdermal delivery system of claim 1 having a size of about 8 to 12 cm 2 .
25. A transdermal delivery system of claim 1 having a size of about 10 or about 11 cm 2 .