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Publication Number
US-12251374-B2
Publication Date
2025-03-18
Expiration Date
Abstract
The present invention relates to a transdermal therapeutic system for cutaneous administration of fampridine. The system includes an active ingredient-impermeable backing layer, a pressure-sensitive adhesive reservoir layer and optionally a detachable protective layer. The pressure-sensitive adhesive reservoir layer is formed from fampridine and at least one matrix polymer containing no free carboxylic acid and/or carboxylate groups, with the content of fampridine in the matrix polymer being <5% by weight. On account of the low loading and also the lack of carboxylic acid and/or carboxylate groups in the reservoir layer, it is ensured that the systems administer the active ingredient substantially at higher administration rates than is known in the prior art, and compared to known systems a comparable thermodynamic activity of the active ingredient is achieved. The present invention further relates to a process for producing corresponding transdermal therapeutic systems.
Core Innovation
The invention relates to a fampridine transdermal therapeutic system for cutaneous administration. The system comprises an active ingredient-impermeable backing layer, a pressure-sensitive adhesive reservoir layer, and optionally a detachable protective layer. Fampridine is contained in the pressure-sensitive adhesive reservoir layer together with at least one matrix polymer.
The matrix polymer(s) contain no carboxylic acid and/or carboxylate groups, and the content of fampridine in the matrix polymer is less than 5% by weight. The matrix polymer(s) ensure continuous skin-contact, and fampridine is dissolved in toluene or ethyl acetate. The system does not include a tackifier.
The transdermal therapeutic system size is in the range of from 5 to 20 cm2. The documented work addresses the need to overcome limitations associated with carboxyl-containing systems that require much higher fampridine loading to achieve administration rates, while providing an approach using matrix polymers without free carboxylic acid/carboxylate groups and low fampridine content. Experimental permeation and utilization comparisons using human skin Franz-cell measurements are also described.
Claims Coverage
The independent claim defines a fampridine transdermal therapeutic system with multiple required structural and composition limitations, including matrix polymers lacking carboxylic acid/carboxylate groups, fampridine loading below 5% by weight, system size of 5–20 cm2, continuous skin-contact, dissolution in toluene or ethyl acetate, and exclusion of a tackifier. The claim set further includes dependent claims that refine loading ranges, daily dose ranges, specific backing construction, and additive exclusions.
Transdermal therapeutic system architecture with impermeable backing and adhesive reservoir
A transdermal therapeutic system for cutaneous administration of fampridine comprising an active ingredient-impermeable backing layer, a pressure-sensitive adhesive reservoir layer and optionally a detachable protective layer.
Matrix polymers without carboxylic acid and/or carboxylate groups
The pressure-sensitive adhesive layer contains fampridine and at least one matrix polymer, wherein the matrix polymer(s) contain no carboxylic acid and/or carboxylate groups.
Low fampridine content in carboxyl-free matrix
The content of fampridine in the matrix polymer is less than 5% by weight.
System size for continuous skin contact
The size of the transdermal therapeutic system is in the range of from 5 to 20 cm2, and the matrix polymer(s) ensures continuous skin-contact.
Fampridine dissolved in toluene or ethyl acetate with no tackifier
The fampridine has been dissolved in toluene or ethyl acetate, and the system does not include a tackifier.
Overall, the claim coverage centers on delivering fampridine in a pressure-sensitive adhesive reservoir using matrix polymers that contain no carboxylic acid and/or carboxylate groups, with fampridine present at less than 5% by weight, together with required system sizing, continuous skin-contact, solvent-based dissolution in toluene or ethyl acetate, and exclusion of tackifier; dependent claims further narrow fampridine loading and dosing ranges, specify backing constructions, and exclude diffusion/penetration-regulating additives.
Stated Advantages
Substantially higher administration rates.
Comparable thermodynamic activity to prior carboxyl-containing systems with much lower drug loading.
Feasibility for oral-equivalent daily dosing.
Documented Applications
Cutaneous administration of fampridine using the described transdermal therapeutic system, including suitability discussed for multiple sclerosis.
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