Pharmaceutical dosage form

Abstract

The invention relates to a pharmaceutical dosage form, preferably with controlled release of a pharmacologically active compound (A) contained therein, the pharmaceutical dosage form very preferably being tamper-resistant and most preferably having a breaking strength B1 of at least 500 N in direction of extension E1 and having a breaking strength B2 of less than 500 N in direction of extension E2.

Description

[0001]This application is a division of U.S. patent application Ser. No. 12 / 358,415 filed Jan. 23, 2009, now allowed, which claims foreign priority of European Patent Application No. 08018221.5 filed Oct. 17, 2008; European Patent Application No. 08001416.0 filed Jan. 25, 2008; and European Patent Application No. 08001415.2 filed Jan. 25, 2008, the disclosures of which are incorporated herein by reference.FIELD OF THE INVENTION[0002]The invention relates to a pharmaceutical dosage form, preferably a tablet for oral administration.BACKGROUND ART[0003]For many pharmaceutically active compounds it is still preferred to have them orally administered by way of tablets. It is also well known that depending on how a pharmaceutically active ingredient is formulated into a tablet its release pattern can be modified. In this regard, tablets providing a retarded release profile are of primary importance. With retarded release tablets care has to be taken that under no circumstances the pharmac...

AI Technical Summary

Benefits of technology

The invention is a tablet that allows for better control over the release of its active ingredients. This means that the tablet can be designed to have a specific release profile that can be controlled for both immediate and retarded release. The tablet can also have a modified outer shape without losing its strength, and has increased storage stability compared to conventional tablets.

Problems solved by technology

This may cause serious adverse effects or even death depending on the active ingredient and potency thereof.

This is particularly unpleasant if for a specific formulation an approved optimized release profile has already been found which can not be reproduced with the modified formulation.

Given the huge expenditures necessary to bring a new drug formulation up to and through clinical testing the above scenario has indeed proven to be rather unsatisfactory.

Many pharmaceutical active compounds, in addition to having excellent activity in their appropriate application, also have abuse potential, i.e., they can be used by an abuser to bring about effects other than those intended.

Pharmaceutical dosage forms exhibiting an increased breaking strength, however, may not be powdered by conventional means and thus, cannot be administered nasally thereby avoiding drug abuse.

It is known that many patients, particularly older patients frequently have difficulties in taking solid pharmaceutical dosage forms, such as tablets, gelatine capsules, etc.

However, the comminution of pharmaceutical dosage forms with such apparatuses is problematic if the pharmaceutical dosage forms are prolonged-release formulations.

Depending on the physiological activity of the substance, this may cause considerable side-effects however, and in extreme cases may even lead to the death of the patient.

Pharmaceutical dosage forms having an increased breaking strength, however, cannot be comminuted by tablet crushers and thus, have to be swallowed as a whole thereby avoiding any (unintentional) overdose.

With respect of pharmaceutical dosage forms exhibiting an increased breaking strength, however, the variation of the content, the nature of the pharmaceutical excipients and / or the surface area to volume ratio also affects the mechanical properties.

Particular problems arise when the dose of the pharmacologically active compound and thus, also the total weight of the pharmaceutical dosage form is comparatively high.

Depending upon the content and the nature of the pharmacologically active compound and of the pharmaceutical excipients, the retardant effect of the polymer may be so strong that the pharmaceutical dosage form cannot be adapted to a specific dosing regimen, e.g., twice daily, particularly when the increased breaking strength is to be maintained.

On the one hand, a decrease of the content of the retardant polymer for the purpose of accelerating drug release would substantially affect the mechanical properties of the pharmaceutical dosage form and in a worst case scenario, would completely diminish its specific and unique mechanical properties (breaking strength).

Further, a decrease of the content of the matrix polymer beyond a certain limit may cause a deterioration or even loss of other desired properties, such as storage stability.

A poor storage stability results, e.g., in a change of the release profile over time.

As highly dosed pharmaceutical dosage forms have comparatively high total weights anyway, a further increase of the total weight is disadvantageous and could deteriorate patient compliance (e.g. swallowability).

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