Extended release tablet formulation containing pramipexole or a pharmaceutically acceptable salt thereof

Abstract

An extended release tablet formulation comprising pramipexole or a pharmaceutically acceptable salt thereof in a matrix, the matrix comprising at least two water swelling polymers, wherein one of the polymers is pregelatinized starch, and wherein another one of the polymers is an anionic polymer.

Description

RELATED APPLICATIONS [0001] This application claims priority to European Application No. 04019248.6 filed Aug. 13, 2004, which is hereby incorporated by reference in its entirety. FIELD OF THE INVENTION [0002] The present invention is directed to an extended release tablet formulation containing pramipexole or a pharmaceutically acceptable salt thereof, method for manufacturing the same, and use thereof. BACKGROUND OF THE INVENTION [0003] Pramipexole is a known dopamine D2 receptor agonist. It is structurally different from the ergot-derived drugs, e.g., bromocriptine or pergolide. It is also pharmacologically unique in that it is a full agonist and has receptor selectivity for the dopamine D2 family of dopamine receptors. [0004] Pramipexole is designated chemically as (S)-2-amino-4,5,6,7-tetrahydro-6-(propylamino)benzothiazole and has the molecular formula C10H17N3S and a relative molecular mass of 211.33. The chemical formula is as follows: [0005] The salt form commonly used is p...

AI Technical Summary

Benefits of technology

[0031] The extended release formulations according to the present invention intended for oral administration allow to select and estimate which in vitro release characteristic and timing of a formulation is most suitable to achieve the desired in vivo plasma profiles preferably with a once daily application. Therefore, two different formulation principles have been developed for a single unit matrix tablet, i.e., two formulation principles having different release rate types are provided and a different pH dependency is available. These alternative formulations are beneficial to patients as the extended release drug delivery will allow patients to treat their symptoms with a single daily dose, thereby increasing patient convenience and compliance.

[0083] (3) optionally dry screening the pre-mixture through a screen in order to segregate cohesive particles and to improve content uniformity;

Problems solved by technology

However, it has proved difficult to formulate a tablet having a suitable combination of modified, extended or sustained-release and handling properties, where the drug is one having relatively high solubility, as in the case of pramipexole dihydrochloride.

However, in practical use, it appears that any formulation having an extended or controlled release profile designed for a once daily application would meet the above requirements for which a general teaching how to adjust such a profile is missing.

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