Pharmaceutical composition and method for treating seizure disorders
Inventors
Plakogiannis, Fotios M. • Lather, Tamanna • Modi, Nisarg • Borovinskaya, Marina
Assignees
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Publication Number
US-12186280-B2
Publication Date
2025-01-07
Expiration Date
Abstract
The present disclosure relates to the transdermal administration of cannabidiol (CBD) for the reduction of seizure frequency in the treatment of “treatment-resistant epilepsy” (TRE).
Core Innovation
The invention provides a pharmaceutical composition comprising a highly purified cannabis that comprises at least about 90% (w/w) cannabidiol (CBD) for transdermal delivery. The composition is formulated with highly purified CBD and includes propylene glycol as a solvent, oleic acid as a penetration enhancer, butylated hydroxytoluene as an antioxidant, silicon dioxide as a suspending agent, and a silicone pressure sensitive adhesive, with pH maintained at approximately 4.0 to 8.0.
The composition is provided in the form of a transdermal matrix patch and provides a constant rate of delivery of the active components in a patient. The constant rate of delivery is maintained in a therapeutic range over at least 7 days, and constant blood serum levels over time are described for the active components delivered by a transdermal patch.
The invention further encompasses transdermal use in treating seizure disorders, including treatment-resistant epilepsy and treatment-resistant pediatric epilepsy, with enumerated seizure types and syndromes. The described seizure-disorder scope includes complex partial seizures, generalized seizures such as absence and tonic-clonic, neonatal and infantile spasms, febrile seizures, juvenile myoclonic epilepsy, and syndromes including Dravet syndrome, Lennox-Gastaut, and Tuberous Sclerosis Complex.
Claims Coverage
The independent claim coverage centers on a transdermal pharmaceutical composition and delivery system using highly purified CBD (at least about 90% w/w) in a transdermal matrix patch with specified formulation parameters and a constant rate of delivery in a therapeutic range for at least 7 days. The claim set also includes seizure-disorder indication coverage, specified dosing intervals for topical application, a constant blood serum levels feature, and optional co-formulation with additional anti-epileptic agents.
Highly purified CBD transdermal matrix patch composition with specified formulation ranges
A pharmaceutical composition comprising a highly purified cannabis comprising at least about 90% (w/w) cannabidiol (CBD) for transdermal delivery, in which the composition comprises a concentration of highly purified CBD selected from about 1% to about 15% (w/w); about 5% to about 25% (w/w) of a solvent comprising propylene glycol; about 1% to about 20% (w/w) of a penetration enhancer comprising oleic acid; about 0.1% to about 0.7% of butylated hydroxytoluene; about 2% to about 15% (w/w) of at least one suspending agent comprising silicon dioxide; and about 50% to about 80% (w/w) of a silicone pressure sensitive adhesive, wherein the pH is maintained at approximately 4.0 to 8.0 and the composition is in the form of a transdermal matrix patch.
Constant rate delivery in therapeutic range over at least 7 days
The pharmaceutical composition provides a constant rate of delivery of the active components of the matrix patch in a therapeutic range in a patient over at least 7 days.
Seizure-disorder scope for transdermal patch treatment with enumerated seizure types and syndromes
A pharmaceutical composition for treating seizure disorders in a patient, wherein the seizure disorder is selected from a group including complex partial seizures, simple partial seizures, partial seizures with secondary generalization, generalized seizures including absence, grand mal (tonic clonic), status epilepticus, tonic, atonic, myoclonic, neonatal and infantile spasms, drug-induced seizures, trauma-induced seizures, febrile seizures, juvenile myoclonic epilepsy, and seizures associated with CNS mass lesions, and wherein the seizure disorder further includes epilepsy syndromes selected from Lennox-Gastaut, Dravet syndrome, Tuberous Sclerosis Complex (TSC), treatment-resistant epilepsy, and treatment-resistant pediatric epilepsy.
Specified dosing intervals for topical application of transdermal patch
A method in which a transdermal patch is topically applied at one of several specified dosing intervals to treat the seizure disorder types and epilepsy syndromes in the listed group, with dosing intervals selected from once in a day, once in two days, once in three days, once in four days, once in five days, once in six days, once in a week, and once in ten days.
Constant blood serum levels maintained over time
A method further maintains constant blood serum levels over time of the active components delivered by a transdermal patch.
Optional co-formulation with additional anti-epileptic agents
The pharmaceutical composition further includes at least one additional anti-epileptic agent selected from clobazam, levetiracetam, topiramate, stiripentol, phenobarbital, lacsamide, valproic acid, zonisamide, perampanel, and fosf(en)ytoin.
The claims focus on a transdermal matrix patch formulation of highly purified CBD with specific excipient ranges and pH control, delivering active components at a constant rate in a therapeutic range for at least 7 days. The coverage further specifies seizure-disorder indication scope, optional additional anti-epileptic agents, prescribed topical dosing intervals, and maintaining constant blood serum levels.
Stated Advantages
Provides a constant rate of delivery of the active components in a therapeutic range over at least 7 days.
Maintains constant blood serum levels over time of the active components delivered by a transdermal patch.
Documented Applications
Treatment of seizure disorders in a patient, including treatment-resistant epilepsy and treatment-resistant pediatric epilepsy, with seizure-type and syndrome coverage including Dravet syndrome, Lennox-Gastaut, Tuberous Sclerosis Complex, and seizures associated with CNS mass lesions.
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