Alkylglycoside compositions for drug administration
Inventors
Assignees
Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-8268791-B2
Publication Date
2012-09-18
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 pharmaceutical composition(s) that include a triptan analog combined with an alkylglycoside that increases absorption. The alkylglycoside comprises a maltose linked by glycosidic linkage to an alkyl chain comprising between 12 to 16 carbons, and is used at a concentration between 0.05% and 20% by weight.
The problem addressed is that drugs may have limited bioavailability and may show first-pass effects and/or bioavailability variance, including reduced absorption and greater variability. Background discussion characterizes the need for an absorption increasing amount of a nonionic surfactant to improve uptake and systemic exposure while maintaining non-irritating or low-toxicity performance.
The disclosed approach is positioned around delivery enhancement using fast-dispersing or fast-dissolving dosage forms and related formulation concepts, including enteric or membrane coatings and sustained contact matrices, to support improved absorption through multiple delivery routes. The document also includes reported therapeutic context for multiple drug classes and demonstrates improved pharmacokinetics and/or rapid exposure parameters for fast-dispersing forms, including examples involving alkyl glycoside excipients.
Claims Coverage
The independent claim is directed to a pharmaceutical composition combining a specified class of triptan analogs with an absorption increasing amount of a defined alkylglycoside (maltose-linked alkyl chain of 12–16 carbons at 0.05%–20% by weight). The dependent claims mainly refine the particular triptan analog, specify particular alkylglycoside members and stereochemical/anomeric forms, and optionally include EDTA.
Triptan analog with defined absorption-increasing alkylglycoside excipient
A pharmaceutical composition comprising a triptan analog selected from sumatriptan, naratriptan, zolmitriptan, eletriptan, almotriptan, frovatriptan; and an absorption increasing amount of an alkylglycoside comprising a maltose linked by glycosidic linkage to an alkyl chain comprising between 12 to 16 carbons, wherein the concentration of alkylglycoside is between 0.05% and 20% by weight.
Claim coverage centers on pairing a selected triptan analog with an absorption increasing alkylglycoside defined by maltose-linked glycosidic linkage to a C12–C16 alkyl chain at 0.05%–20% by weight. The dependent claims further narrow the specific triptan analog, specify particular maltoside species, and optionally add EDTA.
Stated Advantages
Improves drug bioavailability and stability.
Increases absorption.
Reduces mucosal irritation/non-irritation.
Increases and reduces variability of bioavailability.
Improves pharmacokinetics, including rapid exposure (e.g., Tmax) for fast-dispersing forms.
Documented Applications
Therapeutic use contexts are described for multiple drug classes including insulin, GLP-1/exendin-4 (including exendin-4), PYY, peptides/proteins, oligonucleotides/antisense/RNAi, nicotine, interferons, bisphosphonate analogs, and triptan analogs including sumatriptan.
Delivery routes for absorption enhancement are described including oral cavity, nasal, ocular, inhalation, and CSF delivery.
Interested in licensing this patent?