Capsule pharmaceutical dosage form comprising a suspension formulation of an indolinone derivative

Abstract

The present invention relates to a suspension formulation containing the active substance 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulphonate, to a capsule pharmaceutical dosage form containing said suspension formulation, to a process for preparing said suspension formulation, to a process for preparing said capsule comprising said suspension formulation and to the packaging material for the finished capsule.

Description

[0001]The present invention relates to a suspension formulation containing the active substance 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulphonate, to a capsule pharmaceutical dosage form containing said suspension formulation, to a to process for preparing said suspension formulation, to a process for preparing said capsule comprising said suspension formulation and to the packaging material for the finished capsule.BACKGROUND TO THE INVENTION[0002]Some pharmacologically active substances may have biopharmaceutical and / or physicochemical properties which make them difficult to formulate into common administration forms. Such substances may be conveniently administered in liquid form either in a lipophilic or hydrophilic carrier system, either as a solution or a suspension, either mixed with a single carrier excipient or mixed with a complex carrier medium made up of several compone...

AI Technical Summary

Problems solved by technology

Some pharmacologically active substances may have biopharmaceutical and / or physicochemical properties which make them difficult to formulate into common administration forms.

In many instances the choice of formulation will be limited by solvent capacity, and in others the drug will not be sufficiently soluble in any lipid formulations.

They have to be accurately prepared and even slight variations in the composition cannot be tolerated without irreversibly upsetting the system, and destroying its beneficial properties.

This precipitation process may be irreversible and lead to an under-dosing of the patient.

As a consequence, the pharmacologically active substance may not be correctly or reproducibly absorbed.

These factors may influence the liberation of the active substance from the dosage form and hence alter the extent of patient's exposure during the shelf-life of the product.

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