Transdermal therapeutic system containing asenapine and polysiloxane or polyisobutylene
Inventors
Mohr, Patrick • RIETSCHER, René • Eifler, René • BOURQUAIN, Olga
Assignees
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Publication Number
US-12485099-B2
Publication Date
2025-12-02
Expiration Date
Abstract
The present invention relates to a transdermal therapeutic system (TTS) for the transdermal administration of asenapine comprising a self-adhesive layer structure comprising a therapeutically effective amount of asenapine, said self-adhesive layer structure comprising: A) a backing layer; B) an asenapine-containing layer comprising: 1. asenapine in the form of the free base; and 2. a polymer selected from the group consisting of polysiloxanes and polyisobutylenes in an amount of more than 50% by weight based on the total weight of the asenapine-containing layer; and C) optionally an additional skin contact layer.
Core Innovation
The invention relates to a transdermal therapeutic system for the transdermal administration of asenapine that uses a self-adhesive layer structure. The self-adhesive layer structure comprises a backing layer and an asenapine-containing layer, and optionally an additional skin contact layer.
The asenapine-containing layer comprises asenapine in free base form, and a polysiloxane or polyisobutylene polymer that comprises more than 50% by weight of the asenapine-containing layer. The asenapine-containing layer further comprises an acrylic polymer.
The system is evaluated using Franz diffusion cell testing and in vitro skin permeation profiles, including cumulative permeated amount/utilization. The described approach relates to passive transdermal delivery with sustained dosing, reduced plasma fluctuation, improved bioavailability/high active utilization, and minimized skin irritation.
Claims Coverage
The independent claim coverage is centered on a self-adhesive multilayer transdermal therapeutic system for asenapine. Four inventive features are identified, focused on the layer structure and composition of the asenapine-containing layer.
Self-adhesive transdermal therapeutic system with backing and asenapine-containing layer
A transdermal therapeutic system for the transdermal administration of asenapine comprising a self-adhesive layer structure comprising a therapeutically effective amount of asenapine, the self-adhesive layer structure comprising a backing layer, an asenapine-containing layer, and optionally an additional skin contact layer.
Asenapine in free base form within an asenapine-containing layer
An asenapine-containing layer comprising asenapine in free base form.
Dominant polysiloxane or polyisobutylene polymer composition in the asenapine-containing layer
A polysiloxane or polyisobutylene polymer, wherein the polysiloxane or polyisobutylene polymer comprises more than 50% by weight of the asenapine-containing layer.
Additional acrylic polymer in the asenapine-containing layer
Wherein the asenapine-containing layer comprises an additional acrylic polymer.
Overall, the claim set is directed to a self-adhesive asenapine transdermal therapeutic system in which asenapine is in free base form within an asenapine-containing layer dominated by a polysiloxane or polyisobutylene polymer (>50% by weight), and the asenapine-containing layer additionally includes an acrylic polymer.
Stated Advantages
Overcomes limitations of sublingual asenapine, including taste, consent issues, and compliance, and supports first-pass avoidance.
Targets passive transdermal delivery with sustained dosing (approximately 24 h).
Reduces plasma fluctuation.
Improves bioavailability/high active utilization.
Minimizes skin irritation.
Documented Applications
Transdermal administration of asenapine using the described transdermal therapeutic system.
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