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Compositions for oral drug administration

a technology of compositions and oral drugs, applied in the direction of carbohydrate active ingredients, animal husbandry, biocide, etc., can solve the problems of not being able to demonstrate the use of alkylsaccharides as absorption enhancers in solid dosage forms such as tablets, and achieve the effects of increasing the absorption and bioavailability of drugs, avoiding various adverse drug effects, and high bioavailability

Inactive Publication Date: 2014-06-12
AEGIS THERAPEUTICS LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention is about a therapeutic composition that contains a drug enhancing agent to increase the absorption and bioavailability of the drug while avoiding adverse toxic effects. The drug enhancing agents are made of a non-toxic surfactant made up of at least an alkyl glycoside and / or saccharide alkyl ester. The therapeutic compositions have a high bioavailability at low concentrations of the enhancing agent. The invention provides compositions and methods of use via various delivery routes to treat various disease states.

Problems solved by technology

Previously, no examples of the use of alkylsaccharides as absorption enhancers in solid dosage forms such as tablets has been demonstrated.
As a result, it was not expected that solid dosage forms containing an alkylsaccharide and the drug substance would benefit from the absorption enhancing effect of the alkylsaccharide since the slow dissolution of the alkylsaccharide in the aqueous gastrointestinal contents would not be expected to produce a sufficiently high concentration or comparable concentration to that achieved in the aqueous formulations before the drug substance and the alkylsaccharide molecules diffuse away from each other throughout the gastrointestinal contents diluting the relative concentrations of each.

Method used

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  • Compositions for oral drug administration
  • Compositions for oral drug administration
  • Compositions for oral 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

[0196]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.

[0197]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 providing...

example 2

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

[0199]Stability of the alkyl glycoside depends, in part, on the number of carbon atoms or length of the alkyl chain and other long alkyl chains, 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 con...

example 3

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

[0203]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.

[0204]Adult male Sprague-Dawley rats (250-350 g) were fed ad libitum, and experiments were conducted between 10:00 a.m. an...

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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. In various aspects, the invention provides compositions and methods for oral delivery in the form of a tablet.

Description

CROSS REFERENCE TO RELATED APPLICATION(S)[0001]This application is a continuation-in-part and claims the benefit of priority under 35 U.S.C. §120 of U.S. patent application Ser. No. 13 / 191,146, filed Jul. 26, 2011; which is a continuation-in-part of U.S. patent application Ser. No. 12 / 906,922, filed Oct. 18, 2010, currently pending, which is a continuation-in-part and claims the benefit of priority under 35 U.S.C. §120 of U.S. patent application Ser. No. 12 / 341,696, filed Dec. 22, 2008, currently pending, which is a continuation-in-part and claims the benefit of priority under 35 U.S.C. §120 of U.S. patent application Ser. No. 12 / 195,192, filed Aug. 20, 2008, currently pending, which is a continuation-in-part and claims the benefit of priority under 35 U.S.C. §120 of U.S. application Ser. No. 12 / 036,963, filed Feb. 25, 2008, currently pending, which is a continuation-in-part and claims the benefit of priority under 35 U.S.C. §120 of U.S. application Ser. No. 11 / 193,825, filed Jul. 2...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K47/26A61K31/138A61K31/137
CPCA61K47/26A61K31/138A61K31/137A61K9/0043A61K9/0048A61K9/0056A61K9/006A61K9/2018A61K9/2095A61K31/4439A61K31/70
Inventor MAGGIO, EDWARD T.
Owner AEGIS THERAPEUTICS LLC
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