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Abuse-resistant oral dosage forms and method of use thereof

a technology of abuse-resistant substances and oral dosage forms, which is applied in the direction of drug compositions, biocide, heterocyclic compound active ingredients, etc., can solve the problems of high potential abuse of oxycodone, high potency of addiction or abuse of such drugs, and euphoric “high” experienced by abusers, and achieve the effect of antagonizing the opioid effect of an opioid agonis

Inactive Publication Date: 2008-07-10
MEHTA ATUL M
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0010]An embodiment of the present invention is directed to an opioid-antagonist oral dosage form wherein the opioid antagonist does not release unless the oral dosage form is crushed or ground up, thereby antagonizing the opioid effect of an opioid agonist.

Problems solved by technology

Although they are effective in reducing the perceived pain by a patient, opioid agonists also have the characteristic of possibly being physically and psychologically addictive to the patient if used repeatedly over an extended period of time.
Thus, the potential for addiction to or abuse of such drugs is an issue of concern whenever prescribing such drugs as analgesics.
For example, oxycodone is an opioid agonist which has a high potential for abuse.
Thus, in this way the abuser is able to receive a relatively large single dose of the oxycodone, resulting in a euphoric “high” being experienced by the abuser.

Method used

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  • Abuse-resistant oral dosage forms and method of use thereof
  • Abuse-resistant oral dosage forms and method of use thereof

Examples

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Effect test

examples

[0049]In these examples, embodiments of the oral dosage form of the invention were prepared as follows.

Step 1: Applying an Opioid Antagonist Layer to a Biologically Inert Pellet

[0050]

IngredientsExample 1Example 2naltrexone hydrochloride50grams531gramshydroxypropylmethyl cellulose50grams530grams(HPMC) (methocel E6 10%solution) (i.e., 90% water)purified water175grams1050gramssimethicone 30% emulsion1gram10grams(i.e., 70% water)25 / 30 mesh sugar spheres750grams413gramstotal weight:805.3grams1000gramsNote:the water is evaporated during this process and is thus not part of the total weight.

Method

[0051]An opioid-antagonist suspension was prepared by mixing the methocel E6 10% solution (binder agent), the naltrexone hydrochloride (opioid antagonist), the simethicone 30% emulsion (antifoam agent) and the purified water (in the amounts listed above for each example). This opioid-antagonist suspension was then sprayed onto the 25 / 30 mesh sugar spheres using a fluid bed processor, resulting in ...

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Abstract

An opioid-antagonist oral dosage form which does not release a therapeutically effective amount of the opioid antagonist when the oral dosage form is orally administered to a human being, but whereby a physical alteration of the oral dosage form results in a release of the therapeutically effective amount of the opioid antagonist. An embodiment of the oral dosage form includes an opioid-antagonist layer coated onto a biologically inert pellet, and a non-releasing membrane coated onto the opioid-antagonist layer. Optionally, the oral dosage form can also include an opioid agonist, such that a method of preventing the abuse of an oral dosage form of an opioid agonist is provided by forming the oral dosage form including an opioid agonist and an opioid antagonist.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]The present application is a continuation of prior co-pending U.S. application Ser. No. 10 / 409,992, filed Apr. 8, 2003, the entire disclosure of which is hereby incorporated by reference.FIELD OF THE INVENTION[0002]The invention relates to an abusive-resistant substance, such as an opioid-antagonist, oral dosage form which does not release the opioid antagonist in a therapeutically effective amount when the oral dosage form is orally administered to a human being, but whereby a physical alteration of the oral dosage form results in a release of the opioid antagonist in an amount effective to prevent the abuse. The oral dosage form can further include an abusable substance, such as an opioid agonist, in order to prevent the abuse of the opioid agonist. A preferred embodiment of the invention includes naltrexone as the abuse-resistant substance in an oral dosage form.BACKGROUND OF THE INVENTION[0003]Opioid agonists, or opioids, are drugs wh...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/52A61K9/14A61K31/485A61K9/32A61KA61K9/16A61K9/22A61K9/24A61K9/48A61K9/50A61K9/54A61K9/58A61K9/60A61K9/62A61K9/64
CPCA61K9/4808A61K9/5026A61K9/1676A61K31/485A61K9/5078A61P25/00A61P25/36
Inventor MEHTA, ATUL M.
Owner MEHTA ATUL M
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