Absorption enhancers for drug administration

Abstract

A composition including a surfactant and at least one alkyl glycoside and / or saccharide alkyl ester and a drug. The surfactant composition(s) when admixed with a drug is non-toxic and non-irritating, while stabilizing and increasing the bioavailability of the drug. The invention also provides compositions that enhance absorption of drugs via the oral, ocular, nasal, nasolacrimal, inhalation or pulmonary, oral cavity (sublingual or Buccal cell) or CSF delivery route of a patient, including but not limited to insulin, glucagon and exendin-4.

Description

CROSS REFERENCE TO RELATED APPLICATION(S) [0001] This application claims the benefit of priority under 35 U.S.C. § 119(e) of U.S. application Ser. No. 60 / 649,958 filed Feb. 3, 2005, now pending; the benefit under 35 USC § 119(e) of U.S. application Ser. No. 60 / 637,284 filed Dec. 17, 2004, now pending; the benefit under 35 USC § 119(e) of U.S. application Ser. No. 60 / 632,038 filed Nov. 30, 2004, now pending; the benefit under 35 USC § 119(e) of U.S. application Ser. No. 60 / 609,890 filed Sep. 14, 2004, now pending; and the benefit under 35 USC § 119(e) of U.S. application Ser. No. 60 / 604,296 filed Aug. 25, 2004, now pending. The disclosure of each of the prior applications is considered part of and is incorporated by reference in the disclosure of this application.FIELD OF THE INVENTION [0002] The invention relates generally to non-irritating, non-toxic compositions providing enhanced bioavailability and more specifically to alkyl glycoside or saccharide alkyl ester compositions for d...

AI Technical Summary

Benefits of technology

[0004] The present invention is based, in part, on the development of a therapeutic composition containing a drug enhancing agent useful for increasing the absorption and bioavailability of the drug, while at the same time avoiding various adverse toxic effects of drug. In particular, the drug enhancing agents of the invention contain a non-toxic surfactant consisting of at least an alkyl glycoside and / or saccharide alkyl ester. One advantage of the therapeutic compositions of the invention is that they permit administration and delivery of the therapeutic agents with high bioavailabilities at concentrations of enhancing agents that are dramatically below their so-called “no observable adverse effect levels” (their NOAEL's). Accordingly, the present invention provides compositions, including alkyl glycosides and / or saccharide alkyl esters and a therapeutic agent (e.g. small molecule organic drug molecules, low molecular weight peptides such as Exenatide, GLP-1 and the like, proteins, and non-peptide therapeutic polymers such as low molecular weight heparin and inhibitory RNA), methods of administering and using the compositions e.g. via the oral, ocular, nasal, nasolacrimal, inhalation or pulmonary, oral cavity (sublingual or Buccal cell) or cerebral spinal fluid (CSF) delivery route, and methods of ameliorating a disease state in a subject by administration of such compositions

[0005] In one aspect, the present invention relates to a surfactant composition having at least one alkyl glycoside and / or at least one saccharide alkyl ester, and when admixed, mixed or blended with a therapeutic agent, a drug, or biologically active compound, the surfactant stabilizes the biological activity and increases the bioavailability of the drug.

Problems solved by technology

Yet, surfactants are frequently irritating to the skin and other tissues, including mucosal membranes such as those found in the nose, mouth, eye, vagina, rectum, esophagus, intestinal tract, and the like.

Many surfactants also cause proteins to denature, thus destroying their biological activity.

Another serious limitation to the development and use of such agents is the ability to deliver them safely, non-invasively, efficiently and stably to the site of action.

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