Dermal delivery compositions and methods
Inventors
ARNOLD, Charles G. • Kydonieus, Agis • Rossi, Thomas M. • ALTOMARI, Alfred F.
Assignees
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Publication Number
US-9364487-B2
Publication Date
2016-06-14
Expiration Date
Abstract
A composition for transdermal delivery of a progestin for progestin hormone therapy is disclosed. Also disclosed is a transdermal delivery device comprising the composition. For progestin-only hormone therapy, the composition contains an anti-oxidant and does not contain an estrogen. For therapy involving a progestin and an estrogen, the composition contains the progestin, the estrogen and an additional anti-oxidant. Methods of improving the stability of progestin-containing compositions comprising oxidative agents are also disclosed. The methods comprise including one or more anti-oxidants in the compositions.
Core Innovation
The disclosed transdermal delivery systems provide an adhesive polymer matrix composition for transdermal delivery of levonorgestrel in which the matrix comprises a polymeric pressure sensitive adhesive, levonorgestrel, a skin permeation enhancer comprising an organic solvent, polyvinyl pyrrolidone or a PVP copolymer, and an anti-oxidant. The composition lacks an estrogen, and the anti-oxidant protects against oxidative degradation of the levonorgestrel by the organic solvent or the PVP or PVP copolymer.
In progestin-only embodiments, the anti-oxidant is described as protecting against oxidative degradation caused by components including the polyacrylate PSA, DMSO, or the PVP/VA copolymer. The stability of levonorgestrel is stated to be improved over compositions lacking the anti-oxidant, and also improved over compositions comprising ethinyl estradiol while lacking an anti-oxidant.
A related concept is described for improving the stability of a progestin transdermal delivery composition that comprises a polymeric PSA, levonorgestrel, a skin permeation enhancer comprising an organic solvent, and PVP or a PVP copolymer, wherein the composition lacks an estrogen. The method comprises adding an anti-oxidant to the composition, thereby improving stability relative to a composition lacking the anti-oxidant.
Claims Coverage
The partial content includes four independent claims. Each claim centers on an anti-oxidant in an estrogen-free levonorgestrel transdermal composition that also includes a polymeric PSA, PVP or a PVP copolymer, and a skin permeation enhancer with an organic solvent, where the anti-oxidant protects against oxidative degradation and improves stability.
Anti-oxidant protected levonorgestrel in estrogen-free adhesive polymer matrix
An adhesive polymer matrix composition for transdermal delivery of levonorgestrel with a polymeric PSA, levonorgestrel, a skin permeation enhancer comprising an organic solvent, PVP or a PVP copolymer, and an anti-oxidant that protects against oxidative degradation of the levonorgestrel by the organic solvent or the PVP or PVP copolymer; wherein the composition lacks an estrogen and the stability is improved over the stability of such composition lacking the anti-oxidant.
Adding an anti-oxidant to improve stability of estrogen-free progestin transdermal composition
A method of improving the stability of a progestin transdermal delivery composition comprising a polymeric PSA, levonorgestrel, a skin permeation enhancer comprising an organic solvent, and PVP or a PVP copolymer, wherein the composition lacks an estrogen; the method comprising adding an anti-oxidant to the composition, thereby improving the stability of the composition over the stability of such composition lacking the anti-oxidant.
Contraceptive progestin-only transdermal composition with DMSO and PVP/VA and antioxidant stability improvements
A contraceptive progestin-only composition for transdermal delivery of levonorgestrel comprising a polyacrylate PSA, levonorgestrel, a skin permeation enhancer comprising DMSO, PVP/VA copolymer, and an anti-oxidant; wherein the anti-oxidant protects against oxidative degradation of the levonorgestrel by the polyacrylate PSA, the DMSO, or the PVP/VA copolymer; the composition lacks an estrogen; and the stability of the levonorgestrel is improved over compositions lacking the anti-oxidant and improved over compositions comprising ethinyl estradiol and lacking the anti-oxidant.
Estrogen-free contraceptive progestin-only transdermal composition limited to PSA, levonorgestrel, solvent enhancer, PVP, and antioxidant
A contraceptive progestin-only composition for transdermal delivery of levonorgestrel wherein the composition lacks estrogen and consists of a pressure sensitive adhesive, levonorgestrel, one or more skin permeation enhancers at least one of which is an organic solvent, PVP or a PVP copolymer, and an anti-oxidant.
Across the independent claims, the inventive coverage is directed to estrogen-free levonorgestrel transdermal PSA/PVP-based compositions where an anti-oxidant protects levonorgestrel from oxidative degradation associated with solvent and/or PSA/PVP components and results in improved stability; in specific contraceptive embodiments, DMSO and PVP/VA and explicit stability comparisons are required.
Stated Advantages
Improved stability of the composition over the stability of a composition lacking the anti-oxidant.
Improved stability of levonorgestrel over the stability of levonorgestrel in an estrogen-free composition lacking an anti-oxidant.
Improved stability of levonorgestrel over the stability of levonorgestrel in a composition comprising ethinyl estradiol and lacking an anti-oxidant.
Documented Applications
Contraceptive progestin-only transdermal delivery of levonorgestrel with an estrogen-free composition including levonorgestrel, PSA, PVP or PVP copolymer, a skin permeation enhancer, and an anti-oxidant.
Method of improving the stability of a progestin transdermal delivery composition comprising levonorgestrel, polymeric PSA, a skin permeation enhancer comprising an organic solvent, and PVP or a PVP copolymer, wherein the composition lacks an estrogen, by adding an anti-oxidant.
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