Transdermal delivery system including an emulsifier
Inventors
Wauer, Gabriel • Seibertz, Frank
Assignees
Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-12383509-B2
Publication Date
2025-08-12
Expiration Date
Abstract
The present invention relates to a transdermal therapeutic system (TTS) comprising an active agent-containing layer structure comprising A) a backing layer and B) a biphasic matrix layer, the biphasic matrix layer having a) a continuous, outer phase having a composition comprising 70 to 100% by weight of at least one polymer, b) a discontinuous, inner phase having a composition comprising the active agent and a dissolver for the active agent in amount sufficient so that the active agent forms a solution with the dissolver in the inner phase and c) an emulsifier in an amount of 0.1 to 20% by weight based on the biphasic matrix layer, processes of manufacture and uses thereof, corresponding methods of treatments therewith.
Core Innovation
The invention relates to a transdermal therapeutic system for transdermal administration of an active agent. The system comprises an active agent-containing layer structure including a backing layer and a dried biphasic matrix layer. The dried biphasic matrix layer includes a continuous outer phase with 70 to 100% by weight of at least one polymer and a discontinuous inner phase containing the active agent and a dissolver for the active agent formed as a solution in the inner phase.
The dissolver is one or more C3 to C24 carboxylic acids. The discontinuous inner phase comprises spheres having a maximum sphere size of 20 μm or less dispersed in the continuous outer phase. The dried biphasic matrix layer further contains an emulsifier in an amount of 0.1 to 20% by weight based on the dried biphasic matrix layer.
The emulsifier is a mixture of PEG/PPG-19/19 dimethicone and PEG-12 dimethicone, where PEG/PPG-19/19 dimethicone is present as a dispersion containing 40 to 60% by weight of cyclopentasiloxane and where PEG-12 dimethicone and the PEG/PPG-19/19 dimethicone dispersion are present in a weight ratio of 1:1.1 to 1:2.3. The dried biphasic matrix layer does not contain a viscosity-increasing substance and is obtained from a solvent-containing biphasic coating mixture after coating on a film and evaporating the solvent.
Claims Coverage
The independent claim covers a transdermal therapeutic system with an active agent-containing layer structure featuring 70–100% polymer continuous outer phase, a discontinuous inner phase of spheres (≤20 μm) formed from an active agent/dissolver solution using C3–C24 carboxylic acids, and a defined emulsifier system (0.1–20% by weight) in a dried biphasic matrix layer made from a solvent-containing biphasic coating mixture after coating and solvent evaporation; the layer excludes viscosity-increasing substances.
Transdermal therapeutic system with dried biphasic matrix layer
A transdermal therapeutic system comprising an active agent-containing layer structure with a backing layer and a dried biphasic matrix layer, where the dried biphasic matrix layer is obtained from a solvent-containing biphasic coating mixture after coating on a film and evaporating the solvent.
Continuous outer phase with high polymer fraction
A continuous outer phase composition comprising 70 to 100% by weight of at least one polymer in the dried biphasic matrix layer.
Discontinuous inner phase formed by active agent/dissolver solution using C3 to C24 carboxylic acids
A discontinuous inner phase composition comprising the active agent and a dissolver for the active agent in an amount sufficient so that the active agent forms a solution with the dissolver in the inner phase, wherein the dissolver is one or more C3 to C24 carboxylic acids.
Dispersed spheres with maximum sphere size of 20 μm or less
The discontinuous inner phase comprises spheres having a maximum sphere size of 20 μm or less dispersed in the continuous outer phase.
Defined emulsifier mixture in 0.1 to 20% by weight
An emulsifier in an amount of 0.1 to 20% by weight based on the dried biphasic matrix layer, wherein the emulsifier is a mixture of PEG/PPG-19/19 dimethicone and PEG-12 dimethicone, the PEG/PPG-19/19 dimethicone is present as a dispersion containing 40 to 60% by weight of cyclopentasiloxane, and the PEG-12 dimethicone and the PEG/PPG-19/19 dimethicone dispersion are present in a weight ratio of 1:1.1 to 1:2.3.
Exclusion of viscosity-increasing substance
The dried biphasic matrix layer does not contain a viscosity-increasing substance.
Overall, the claims focus on a microreservoir-type transdermal therapeutic system defined by a dried biphasic matrix layer with a high-polymer continuous outer phase, a discontinuous inner phase made from an active agent solution in C3 to C24 carboxylic acids dispersed as ≤20 μm spheres, and a specific PEG/PPG-19/19 dimethicone plus PEG-12 dimethicone emulsifier system within 0.1 to 20% by weight, produced via solvent-containing biphasic coating mixture followed by solvent evaporation while excluding viscosity-increasing substances.
Stated Advantages
Improving active agent release consistency by stabilizing deposit size and resisting coalescence under shear during manufacturing.
Providing reduced or better-controlled permeation profiles over extended times.
Documented Applications
Transdermal administration of an active agent using the disclosed transdermal therapeutic system.
Treating pain by applying a buprenorphine-containing transdermal therapeutic system to a patient’s skin for 7 days.
Interested in licensing this patent?