Crush resistant delayed-release dosage forms

Abstract

The invention relates to a dosage form comprising a physiologically effective amount of a physiologically active substance (A), a synthetic, semi-synthetic or natural polymer (C), optionally one or more physiologically acceptable auxiliary substances (B) and optionally a synthetic, semi-synthetic or natural wax (D), wherein the dosage form exhibits a resistance to crushing of at least 400 N and wherein under physiological conditions the release of the physiologically active substance (A) from the dosage form is at least partially delayed.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application claims priority from German Patent Application No. 10 2005 005 446.3, filed on Feb. 4, 2005 and U.S. patent application Ser. No. 10 / 718,112 filed on Nov. 20, 2003.BACKGROUND OF THE INVENTION[0002]The present invention relates to a dosage form for administering a physiologically active substance (A), wherein the dosage form is mechanically stabilised, such that it cannot be comminuted by conventional methods, such as pounding, crushing, grinding in a mortar etc., or at least comminuted only with very great difficulty. The substance (A) is released from the dosage form according to the invention under physiological conditions with an at least partially delayed release profile.[0003]Numerous physiologically active substances, such as nutritional supplements, pharmaceutical substances etc., are provided as delayed-release formulations, i.e., in contrast to conventional formulations (for example “immediate release” formulation...

AI Technical Summary

Benefits of technology

[0023]As a consequence of the resistance to crushing, delayed release is maintained and an overdose due to improper handling of the dosage form is effectively prevented.

Problems solved by technology

Such pharmaceutical substances are therefore generally unsuitable for “immediate release” formulations, in particular if it is desired to administer said formulations only two or three times daily.

However, older patients in particular frequently have difficulties in taking solid dosage forms, such as tablets, gelatine capsules, etc.

However, the comminution of dosage forms with such apparatuses is problematic if the dosage forms are delayed-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.

Delayed-release formulations may also cause problems for small children.

For instance, children frequently cannot distinguish solid dosage forms from sweets.

If children find such dosage forms, for example because their parents have carelessly left them lying around in the home, there is a risk that the children may think that the dosage forms are sweets and put them in their mouths and chew them.

If said dosage forms are delayed-release formulations, which contain a pharmaceutical substance in a dosage intended for adults, the child may in such a case already be at risk of overdose due to the relatively large amount of pharmaceutical substance contained therein.

By chewing the dosage form and thus cancelling out the delayed-release action, this risk is increased still further, however, since the excessively high dose already contained therein is additionally released over a greatly reduced period of time, a situation which would be very hazardous even for an adult and which may have all the more drastic consequences for a child.

The chewing of delayed-release formulations may also lead to an overdose of the substance contained therein in adults.

This method has the disadvantage, however, that the physiologically active substance is nonetheless administered in non-delayed form and that the organism is additionally exposed to a further physiologically active substance, for example an antidote, or to a defensive reaction, such as for example vomiting.

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