Transdermal penetrant formulations containing cannabidiol
Inventors
Fitzsimmons, Nathan • Beal, Ryan • McMahon, Audrene • Sand, Brandon • Martinez, Kilmar
Assignees
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Publication Number
US-11026896-B2
Publication Date
2021-06-08
Expiration Date
Abstract
Disclosed herein is a transdermal delivery formulation for transdermal delivery of a Cannabidiol, with or without one or more additional active agents through the dermis, including the skin, nail or hair follicle of a subject, wherein the formulation comprises a) a transdermal delivery formulation in an amount less than about 60% w/w, comprising i. one or more phosphatides, ii. glucose, and iii. one or more fatty acids; b) water in an amount less than about 50% w/w, a Cannabidiol with or within one or more additional active agents.
Core Innovation
The invention provides a method of treating a patient with an ailment by applying a transdermal formulation to the skin of the patient. The ailments identified for treatment include pain, seizures or Parkinson’s disease. The disclosed approach is directed to a low content transdermal delivery matrix comprising phosphatides, glucose, and fatty acids with limited water content, and is contrasted with prior transdermal products that include lecithin or lecithin organogel systems.
The transdermal formulation comprises cannabidiol, phosphatidylcholine, glucose, benzyl alcohol, deionized water, safflower oil, oleic acid, stearic acid, and isopropyl palmitate, with all amounts expressed as percent by weight relative to the total weight of the transdermal formulation. The formulation is defined by specific concentration ranges for each recited component.
The disclosure further describes formulation component options and properties, including pH adjustment within a stated range, stability concepts, and additional delivery concepts such as kit/patch delivery. The document includes example formulations and therapeutic indications for cannabidiol across multiple conditions, and it presents in vivo mouse topical pharmacokinetic data comparing lecithin-based formulations versus lecithin-alternative formulations, using Cmax, tmax, and AUC to characterize plasma exposure.
Claims Coverage
The provided independent claim covers transdermal treatment of pain, seizures, or Parkinson’s disease using a specific cannabidiol-containing formulation with defined weight-percent ranges for cannabidiol, phosphatidylcholine, glucose, benzyl alcohol, deionized water, safflower oil, oleic acid, stearic acid, and isopropyl palmitate. Dependent claims further constrain cannabidiol concentration, specify a formulation pH range, add surfactant and nonionic detergent, and narrow safflower oil by requiring linoleic acid.
Transdermal application of cannabidiol-containing formulation for specified ailments
Applying a transdermal formulation to the skin of a patient, wherein the ailment is pain, seizures or Parkinson’s disease.
Cannabidiol within a defined weight-percent range
Cannabidiol at a concentration from 1% to 7% (w/w).
Phosphatidylcholine within a defined weight-percent range
Phosphatidylcholine at a concentration from 4% to 15% (w/w).
Glucose within a defined weight-percent range
Glucose at a concentration from 0% to 3% (w/w).
Benzyl alcohol within a defined weight-percent range
Benzyl alcohol at a concentration from 0.25% to 5% (w/w).
Deionized water within a defined weight-percent range
Deionized water at a concentration from 10% to 75% (w/w).
Safflower oil within a defined weight-percent range
Safflower oil at a concentration from 1% to 20% (w/w).
Oleic acid within a defined weight-percent range
Oleic acid at a concentration from 0.2% to 7.5% (w/w).
Stearic acid within a defined weight-percent range
Stearic acid at a concentration from 0.1% to 7% (w/w).
Isopropyl palmitate within a defined weight-percent range
Isopropyl palmitate at a concentration from 5% to 30% (w/w).
The inventive coverage is directed to transdermal treatment of pain, seizures, or Parkinson’s disease using a cannabidiol-containing transdermal formulation defined by concentration ranges for phosphatidylcholine, glucose, benzyl alcohol, deionized water, safflower oil, oleic acid, stearic acid, and isopropyl palmitate. The dependent claims further refine the formulation by cannabidiol concentration and additional formulation constraints.
Stated Advantages
Improved skin/dermal penetration versus prior transdermal products.
Documented Applications
Therapeutic indications for cannabidiol delivered via transdermal formulations for pain, seizures/epilepsy, Parkinson’s disease, and multiple other listed conditions including Crohn’s disease, multiple sclerosis, AIDS/HIV, ulcerative colitis, and cancer.
In vivo mouse topical pharmacokinetic evaluation of lecithin-based versus lecithin-alternative formulations using Cmax, tmax, and AUC to characterize sustained plasma exposure.
Illustrative patient dosing outcomes for severe pain, seizures, and Parkinson’s.
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