Multiparticles safeguarded against ethanolic dose-dumping
First Claim
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1. An oral pharmaceutical dosage form comprising a pharmacologically active ingredient embedded in a matrix material, wherein:
- the pharmacologically active ingredient is one selected from pharmacologically active ingredients classified in Anatomical Therapeutic Chemical Classification System (ATC), class Nervous System;
the matrix material comprises a mixture of an alkyl cellulose and a heteropolysaccharide;
the alkyl cellulose is present in the dosage form in an amount of at least 50 wt.-% relative to the total weight of the dosage form;
the heteropolysaccharide is present in the dosage form in an amount of below 50 wt.-% relative to the total weight of the dosage form;
the total content of alkyl cellulose and heteropolysaccharide is at least 60 wt.-% relative to the total weight of the dosage form;
the pharmaceutical dosage form releases by 60 minutes more than 60% of the pharmacologically active ingredient when release of the pharmacologically active ingredient from the pharmaceutical dosage form is measured with a paddle apparatus at 50 rpm, at 37±
5°
C., in 900 mL 0.1 M HCl (pH 1.0) or simulated intestinal fluid at pH 6.8 (phosphate buffer) or pH 4.5; and
the pharmaceutical dosage form provides resistance against dose dumping in aqueous ethanol.
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Abstract
The invention relates to an oral pharmaceutical dosage form providing resistance against dose dumping in aqueous ethanol and comprising a pharmacologically active ingredient embedded in a matrix material,
- wherein the matrix material comprises an alkyl cellulose and a heteropolysaccharide; and
- wherein the relative weight ratio of heteropolysaccharide to alkyl cellulose is within the range of from 1:20 to 20:1; and
wherein the total content of alkyl cellulose and heteropolysaccharide is at least 35 wt.-%, relative to the total weight of the dosage form. A process of producing the dosage form and methods of using the dosage form, for example to treat pain, are also disclosed.
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Citations
16 Claims
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1. An oral pharmaceutical dosage form comprising a pharmacologically active ingredient embedded in a matrix material, wherein:
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the pharmacologically active ingredient is one selected from pharmacologically active ingredients classified in Anatomical Therapeutic Chemical Classification System (ATC), class Nervous System; the matrix material comprises a mixture of an alkyl cellulose and a heteropolysaccharide; the alkyl cellulose is present in the dosage form in an amount of at least 50 wt.-% relative to the total weight of the dosage form; the heteropolysaccharide is present in the dosage form in an amount of below 50 wt.-% relative to the total weight of the dosage form; the total content of alkyl cellulose and heteropolysaccharide is at least 60 wt.-% relative to the total weight of the dosage form; the pharmaceutical dosage form releases by 60 minutes more than 60% of the pharmacologically active ingredient when release of the pharmacologically active ingredient from the pharmaceutical dosage form is measured with a paddle apparatus at 50 rpm, at 37±
5°
C., in 900 mL 0.1 M HCl (pH 1.0) or simulated intestinal fluid at pH 6.8 (phosphate buffer) or pH 4.5; andthe pharmaceutical dosage form provides resistance against dose dumping in aqueous ethanol. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16)
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Specification