Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-10576156-B2
Publication Date
2020-03-03
Expiration Date
Abstract
The present invention provides compositions and methods and for increasing the bioavailability of therapeutic agents in a subject. The compositions include at least one alkyl glycoside and at least one therapeutic agent, wherein the alkylglycoside has an alkyl chain length from about 10 to about 16 carbon atoms.
Core Innovation
The invention relates to an intranasal pharmaceutical composition and related drug-delivery platform that uses a nonionic alkyl glycoside, specifically dodecyl-beta-D-maltoside, in an aqueous solution formulated for intranasal delivery. The composition includes epinephrine and is formulated to provide systemic absorption of epinephrine upon delivery to a subject. The composition has a pH of about 2.0 to 5.0.
The platform uses alkyl glycosides and saccharide alkyl esters as delivery-enhancing excipients intended to increase therapeutic drug bioavailability while maintaining stability and avoiding irritation and toxicity. The described design emphasizes systemic exposure measures such as Cmax and Tmax, including reducing Tmax and reducing first-pass clearance.
The document also describes compositions formulated for multiple administration routes and dosage forms, including oral solid/fast-dispersing and enteric or controlled-release formulations, as well as mucosal delivery approaches. Therapeutic agents can include peptides, oligonucleotides/siRNA, and a variety of other drugs, with epinephrine used in the intranasal composition of the independent claim.
Claims Coverage
The partial content includes one independent claim and dependent claims. Across the claims, there are 4 main inventive features centered on intranasal epinephrine delivery using dodecyl-beta-D-maltoside at a defined concentration range and acidic pH, with refinements specifying systemic absorption performance via Cmax and Tmax comparisons and thresholds.
Intranasal aqueous epinephrine with dodecyl-beta-D-maltoside at acidic pH
An intranasal pharmaceutical composition comprising epinephrine and between about 0.05% and 0.5% (w/v) of an alkylglycoside, wherein the alkylglycoside is dodecyl-beta-D-maltoside, wherein the composition is an aqueous solution formulated for intranasal delivery to a subject, and provides systemic absorption of epinephrine upon delivery to the subject, and wherein the composition has a pH of about 2.0 to 5.0.
Cmax fold-improvement for epinephrine with alkylglycoside
A pharmaceutical composition that provides an epinephrine Cmax in a subject at least about 2-fold greater than when the epinephrine is administered without an alkylglycoside.
Tmax reduction for epinephrine with alkylglycoside
A pharmaceutical composition as in claim 1 that provides an epinephrine Tmax in a subject that is about twofold or less compared with administration without the alkylglycoside.
Absolute Tmax threshold for epinephrine
A pharmaceutical composition that provides an epinephrine Tmax of about 0.3 hours or less in a subject.
The claims cover an intranasal aqueous epinephrine composition using dodecyl-beta-D-maltoside at about 0.05% to 0.5% (w/v) with a pH of about 2.0 to 5.0 to provide systemic absorption, with dependent refinements requiring improved Cmax and reduced epinephrine Tmax via quantitative comparisons and an absolute Tmax threshold.
Stated Advantages
Increases therapeutic drug bioavailability while maintaining stability and avoiding irritation and toxicity.
Provides systemic absorption upon intranasal delivery.
Reduces first-pass clearance and improves systemic exposure measures such as Cmax and Tmax.
Provides reduced Tmax compared to administration without an alkylglycoside.
Documented Applications
Intranasal delivery to a subject to provide systemic absorption of epinephrine.
Oral solid/fast-dispersing dosage forms and enteric or controlled-release formulations for therapeutic drugs.
Mucosal delivery approaches including ocular, nasal, inhalation, and CSF delivery routes.
Interested in licensing this patent?