Transdermal delivery system including an interface mediator
Inventors
Emgenbroich, Marco • Leonhard, Johannes Josef • Kassner, Kristina • Lappert, Aurélia
Assignees
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Publication Number
US-12427119-B2
Publication Date
2025-09-30
Expiration Date
Abstract
The present invention relates to aransdermal therapeutic system for the transdermal administration of a systemically active agent having a self-adhesive layer structure. The transdermal therapeutic system includes (A) a backing layer, and (B) a dried biphasic layer. The dried biphasic layer has (a) an outer phase having a composition comprising 75% to 100% of a polymer or polymer mixture, and (b) an inner phase having a composition that includes at least one active agent. The inner phase forms dispersed deposits in the outer phase, with the dried biphasic layer including (c) from 0.1% to 3.5% of an interface mediator other than silicone oil, with the interface mediator having with a kinematic viscosity of from 10 cSt to 100 000 cSt at 25° C.
Core Innovation
The invention provides a transdermal therapeutic system for the transdermal administration of at least one systemically active agent, using a self-adhesive layer structure that includes a backing layer and a dried biphasic layer. The dried biphasic layer has a hydrophobic outer phase and a hydrophilic inner phase, where the inner phase forms dispersed deposits in the outer phase. The inner phase and outer phase define an interface, and the dispersed deposits have a maximum droplet size of 5 μm to 25 μm.
A key aspect is the inclusion of 0.1% to 3.5% of an interface mediator other than silicone oil. The interface mediator is hydrophobic and has a kinematic viscosity of 10 cSt to 100 000 cSt at 25°C. The interface mediator fills cavities at the interface between the inner phase and outer phase, while the outer phase includes 75% to 100% of a polymer or polymer mixture having a dynamic viscosity above 150 Pa·s at 160°C.
In embodiments focused on rotigotine, the system provides a dried biphasic layer with a hydrophobic outer phase comprising 75% to 100% pressure-sensitive adhesive polysiloxane(s) and a hydrophilic inner phase comprising rotigotine base, with dispersed deposits formed in the outer phase. The same interface mediator constraints (other than silicone oil, present at 0.1% to 3.5% and with specified kinematic viscosity) apply so the interface mediator fills cavities at the inner/outer interface, while maintaining dispersed deposits having a maximum droplet size of 5 μm to 25 μm.
Claims Coverage
Two independent claims are directed to a transdermal therapeutic system with a self-adhesive layer structure and a dried biphasic layer, differentiated by whether the claim is generic for selected systemically active agents or specifically for rotigotine dosing and outer/inner phase compositions. Across both independent claims, the inventive features include the hydrophobic/hydrophilic biphasic structure, the specified interface mediator other than silicone oil, and the droplet-size-limited dispersed deposits controlled at the inner/outer interface.
Self-adhesive transdermal therapeutic system with backing and dried biphasic layer
A transdermal therapeutic system for transdermal administration of at least one systemically active agent comprising a backing layer and a dried biphasic layer, wherein the dried biphasic layer has an outer phase with 75% to 100% of a polymer or polymer mixture (dynamic viscosity above 150 Pa·s at 160°C) and an inner phase with the active agent forming dispersed deposits in the outer phase, with an interface defined between inner and outer phases.
Interface mediator other than silicone oil filling interface cavities
Including 0.1% to 3.5% of an interface mediator other than silicone oil that is hydrophobic and has kinematic viscosity of 10 cSt to 100 000 cSt at 25°C, wherein the interface mediator fills cavities at the interface between the inner phase and outer phase.
Hydrophobic outer phase, hydrophilic inner phase, and droplet-size-limited dispersed deposits
Wherein the outer phase is hydrophobic, the inner phase is hydrophilic, and the dispersed deposits have a maximum droplet size of 5 μm to 25 μm.
Selected systemically active agent set
Wherein the at least one active agent is selected from the group of rotigotine, fentanyl, oxybutynine, and fesoterodine.
Rotigotine-specific self-adhesive transdermal therapeutic system with specified areal dose and biphasic phases
A transdermal therapeutic system for transdermal administration of rotigotine containing 2.0 mg/cm2 to 4.0 mg/cm2 rotigotine base in a self-adhesive layer structure comprising a backing layer and a dried biphasic layer having a hydrophobic outer phase of 75% to 100% pressure-sensitive adhesive polysiloxane(s) and a hydrophilic inner phase comprising rotigotine base forming dispersed deposits in the outer phase.
Hydrophobic interface mediator other than silicone oil with specified viscosity and interface cavity filling
Including 0.1% to 3.5% of a hydrophobic interface mediator other than silicone oil with kinematic viscosity of 10 cSt to 100 000 cSt at 25°C, wherein the inner phase and outer phase define an interface and the interface mediator fills cavities at the interface between the inner phase and outer phase.
Polysiloxane solution viscosity and solids content limits (heptane)
Wherein the polysiloxanes have a solution viscosity at 25°C and 60% solids content in heptane from greater than 150 mPa·s to about 700 mPa·s, and the dispersed deposits have a maximum droplet size of 5 μm to 25 μm.
The independent claims share the core structural concept of a dried hydrophobic/hydrophilic biphasic layer in a self-adhesive transdermal therapeutic system, combined with a hydrophobic interface mediator other than silicone oil that fills interface cavities and is specified by kinematic viscosity and amount. Claim 1 covers at least one systemically active agent selected from rotigotine, fentanyl, oxybutynine, and fesoterodine, while claim 17 specifically requires rotigotine base delivery with a defined areal dose and polysiloxane-based outer phase composition.
Stated Advantages
Improves long-term stability.
Reduces maximum droplet size.
Enables continuous delivery.
Documented Applications
Treatment of patients with Parkinson’s disease or Parkinson’s plus syndrome using a specified transdermal therapeutic system over a 7-day period.
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