Absorption enhancers for drug administration

Inactive Publication Date: 2006-03-02
UAB RES FOUND +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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 adver

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

Method used

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  • Absorption enhancers for drug administration
  • Absorption enhancers for drug administration
  • Absorption enhancers for drug administration

Examples

Experimental program
Comparison scheme
Effect test

example 1

Alkyl Glycoside and / or Sucrose Ester Formulations Do Not Cause Mucosa Irritation or Disruption

[0146] The nasal mucosa is highly vascularized and hence optimal for high drug permeation. Moreover, absorption of drug(s) through the nasal mucosa is available to the central nervous system (CNS). Although local application of drugs is desirable, a challenge for this method of administration is mucosal irritancy.

[0147] A formulation consisting of an alkyl glycoside (0.125% TDM) in a commercial over-the-counter (OTC) nasal saline was administered in vivo to human nasal epithelium over a period of over one month. The 0.125% TDM formulation is compared to the control, namely the same commercial (OTC) nasal saline, over the same period of time. Results show that during and after 33 days of daily TDM administration (i.e., the duration of the study), there is no observable irritation of the nasal mucosa (data not shown). Thus, compositions of the invention are non-toxic and non-irritable provi...

example 2

Alkyl Glycoside and / or Ester Compositions Stabilize Drugs by Increasing Drug Bioavailability and Reducing Drug Bioavailability Variance

[0149] Stability of the alkyl glycoside depends, in part, on the number of carbon atoms, or branching of the alkyl chain, with tetradecylmaltoside (TDM) having the greatest effect; but other highly branched alkyl chains including DDM also have stabilizing effects. In contrast to Hovgaard-1, which described the preference for a high alkyl glycoside to drug ratio, the instant invention shows that this ratio is much lower. For example, alkyl glycosides in the range of about 0.01% to about 6% by weight result in good stabilization of the drug; whereas Hovgaard-1 shows stabilization is only achieved at much higher ratios of alkyl glycosides to drug (10:1 and 16: 1). Even more interesting, alkyl glycosides of the invention in the range of about 0.01% to about 6% have increased bioavailability (see FIG. 1). This is in sharp contrast to Hovgaard-2, which sh...

example 3

Ocular Administration of Alkyl Saccharides Plus Insulin Produces Hypoglycemic Effects In Vivo

[0153] Normal rats were anesthetized with a mixture of xylazine / ketamine to elevate their blood glucose levels. The elevated levels of D-glucose that occur in response to anesthesia provide an optimal system to measure the systemic hypoglycemic action of drug administration, e.g. insulin-containing eye drops. This animal model mimics the hyperglycemic state seen in diabetic animals and humans. In the experimental animal group, anesthetized rats are given eye drops containing insulin. Blood glucose levels from the experimental group are compared to anesthetized animals which received eye drops without insulin. The change in blood glucose levels and the differential systemic responses reflects the effect of insulin absorbed via the route of administration, e.g. ocular route.

[0154] Adult male Sprague-Dawley rats (250-350 g) were fed ad libitum, and experiments were conducted between 10:00 a.m...

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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...

Claims

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Application Information

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IPC IPC(8): A61K38/17A61K31/70
CPCA61K47/26A61K31/70A61K9/0043A61K9/0048A61K31/4439A61P25/00A61P25/08
Inventor MEEZAN, ELIASPILLION, DENNIS J.MAGGIO, EDWARD T.
Owner UAB RES FOUND
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