Tamper-resistant tablet providing immediate drug release

Abstract

The invention relates to a tamper-resistant tablet comprising(i) a matrix material in an amount of more than one third of the total weight of the tablet; and(ii) a plurality of particulates in an amount of less than two thirds of the total weight of the tablet; wherein said particulates comprise a pharmacologically active compound and a polyalkylene oxide; and form a discontinuous phase within the matrix material;and method of using said tablet to treat pain and other conditions.

Description

PRIORITY[0001]This application claims priority of U.S. Provisional Patent Application No. 61 / 512,939, filed on Jul. 29, 2011, and European Patent Application No. 11 006 253.6, filed on Jul. 29, 2011, the contents of both of which patent applications are incorporated herein by reference.FIELD OF THE INVENTION[0002]The invention relates to tamper-resistant tablets comprising a matrix material and a plurality of particulates which comprise a pharmacologically active compound and form a discontinuous phase within the matrix material.BACKGROUND OF THE INVENTION[0003]A large number of pharmacologically active substances have a potential for being abused or misused, i.e. they can be used to produce effects which are not consistent with their intended use. Thus, e.g. opioids which exhibit an excellent efficacy in controlling severe to extremely severe pain, are frequently abused to induce euphoric states similar to being intoxicated. In particular, active substances which have a psychotropi...

AI Technical Summary

Benefits of technology

This patent explains how to make blockbuster drugs that are resistant to tampering and can be quickly released in the body. We found that adding little pieces of the active ingredient into a more important material can speed up the release. We also found that mixing different materials together and compacting them into tablets can make the drugs disintegrate faster and release more quickly. Overall, this allows us to create the best drug form for patient compliance and tablet production.

Problems solved by technology

A large number of pharmacologically active substances have a potential for being abused or misused, i.e. they can be used to produce effects which are not consistent with their intended use.

However, the presence of such aversive agents is principally not desirable and there is a need to provide sufficient tamper-resistance without relying on aversive agents and / or antagonists.

Such pharmaceutical dosage forms are useful for avoiding drug abuse of the pharmacologically active compound contained therein, as they may not be powdered by conventional means and thus, cannot be administered in powdered form, e.g. nasally.

The properties of capsules, however, are not satisfactory in every respect, e.g. with respect to disintegration time, patient compliance (e.g. swallowability) and ease of manufacture.

Further, capsules frequently contain gelatine thus causing the risk of bovine spongiform encephalopathy (BSE, or TSE).

As far as tamper-resistant dosage forms are concerned, capsules are disadvantageous as they can typically be opened easily thereby releasing the ingredients in powdery or particulate form without requiring any mechanical impact.

The properties of these tamper-resistant dosage forms, however, are not satisfactory in every respect.

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