Transdermal delivery of cannabidiol
Inventors
Plakogiannis, Fotios M. • Lather, Tamanna • Modi, Nisarg • Borovinskaya, Marina
Assignees
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Publication Number
US-12121617-B2
Publication Date
2024-10-22
Expiration Date
Abstract
Provided is a transdermal drug delivery system comprising cannabidiol, or a cannabidiol salt alone or in combinations thereof. Transdermal delivery can provide a drug plasma concentration at predetermined rate for a predetermined period of time with a simplified therapeutic regimen by decreasing dosing frequency for the treatment and/or prevention of pain and/or inflammation.
Core Innovation
The invention is a transdermal and/or topical pharmaceutical composition that includes an active agent selected from synthetic cannabidiol, natural cannabidiol, and combinations thereof, formulated into a transdermal matrix patch. The composition includes specified ranges of adhesive, solvent, suspending agent, butylated hydroxytoluene, and a penetration enhancer comprising oleic acid, with an optionally included gelling agent. The pH of the composition is maintained at approximately 4.0 to 8.0.
The transdermal matrix patch delivers the active components at a constant rate in a patient over 7 days in a therapeutic range. The described delivery intent is to provide systemic exposure while avoiding first-pass metabolism and reducing plasma peak/valley fluctuations. The disclosed goals include maintaining steady absorption and steady serum/plasma levels over time periods spanning hours to weeks, based on reported in vitro testing.
The described formulations encompass multiple forms of cannabidiol and associated components, including free base, salts, isomers, crystalline, amorphous, co-crystal forms, synthetic cannabidiol, and biosynthetic cannabinoids including biosynthetic CBD, with optional combinations with adjunct active components. The described transdermal/topical dosage forms include transdermal liquids and semisolids and patch types such as reservoir patch, matrix patch, pressure sensitive adhesive patch, extended-release film, mucoadhesive patch, and optional microneedles.
Claims Coverage
The partial content identifies one independent claim. It specifies a cannabidiol-containing transdermal matrix patch composition with defined formulation ranges and constant rate delivery over 7 days in a therapeutic range.
Cannabidiol transdermal matrix patch composition with defined formulation ranges
A transdermal and/or topical pharmaceutical composition comprising about 0.1% to about 20% of an active agent selected from synthetic cannabidiol, natural cannabidiol, and combinations thereof; about 35% to about 99% of at least one adhesive including a silicone pressure sensitive adhesive; about 5% to about 20% of at least one solvent; about 2% to about 15% of at least one suspending agent; about 0.1% to about 0.7% of butylated hydroxytoluene; and about 0.10% to about 20% of a penetration enhancer comprising oleic acid; optionally about 0.10% to about 40% of a gelling agent.
Maintained pH and constant rate therapeutic delivery over 7 days
The pH of the composition is maintained at approximately 4.0 to 8.0; the pharmaceutical composition is in the form of a transdermal matrix patch; and the pharmaceutical composition provides a constant rate of delivery of the active components in a therapeutic range in a patient over 7 days.
The claim coverage centers on a cannabidiol active agent formulated with a silicone pressure sensitive adhesive-based transdermal matrix patch, maintained at approximately pH 4.0 to 8.0, and including specified components to achieve constant rate delivery over 7 days in a therapeutic range.
Stated Advantages
Provides constant rate delivery of the active components in a therapeutic range in a patient over 7 days.
Avoids first-pass metabolism.
Reduces plasma peak/valley fluctuations.
Maintains steady absorption and steady serum/plasma levels over time periods spanning hours to weeks.
Documented Applications
Treating or preventing pain and inflammation, including neuropathic and arthritic pain.
Therapeutic delivery outcomes in relation to systemic exposure and treating or preventing pain and inflammation.
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