High-dose controlled-release tablets - based on pure drug cores with release-controlling layer of water-swellable polymer and pore-forming agent.

摘要

High-dose controlled-release tablets which disintegrate into small subunits under physiological conditions comprise compressed granules and an outer tablet phase. The granules comprise a core of pure drug and a release-controlling layer (I) comprising a water-swellable polymer (WSP) and a pore-forming agent (PFA). Also claimed are the granules themselves. Another release-controlling layer (II) may be interposed between (I) and the core, where (II) comprises a WSP and opt. additional drug. (I) is present in an amt. of 40-90% of the core wt. or 10-100% in the case of readily water-soluble drugs. (I) comprises 20-50 wt. % WSP and 50-80 wt. % PFA, or 70-90 wt. % WSP and 10-30 wt. % PFA in the case of drugs with medium to high water-solubility. The WSP is an emulsion-polymerised copolymer of methyl and/or ethyl acrylate and methacrylate with a molecular wt. of ca. 800,000 (e.g. Eudgrit NE-30D'). USE/ADVANTAGE - The tablets may be used for admin. of drugs with low, medium or high water-solubility, e.g. theophylline, diprophylline or mexitil respectively. The tablets release the drug over long periods e.g. at least 7 hr.