PH-dependent controlled release pharmaceutical composition for non-opioids with resistance against the influence of ethanol

摘要

The invention relates to a pH-dependent controlled release pharmaceutical composition, comprising at least one pharmaceutical active ingredient, with the exception of opioids, wherein the core is coated at least by one coating layer, controlling the release of the pharmaceutical composition, wherein the coating layer comprises a polymer mixture of i) 40-95% by weight, based on dry weight of the polymer mixture, of at least one water insoluble essentially neutral vinyl polymer or copolymer, and ii) 5-60% by weight, based on dry weight of the polymer mixture, of at least one anionic polymer or copolymer, which is insoluble in a buffered medium below pH 4.0 and soluble at least in the range from pH 7.0 to pH 8.0. characterized in that the coating layer further contains 110 to 250% by weight, calculated on dry weight of the polymer mixture, of a non-porous inert lubricant and the is present in an amount of at least 60% by weight calculated on the weight of core.

主权项

1. A pH-dependent controlled release pharmaceutical composition, comprising
a core, comprising at least one pharmaceutical active ingredient, with the exception of opioids, wherein the core is coated by at least one coating layer, controlling the release of the pharmaceutical composition, wherein the coating layer comprises a polymer mixture of
i) 40-95% by weight, based on dry weight of the polymer mixture, of at least one water insoluble essentially neutral vinyl polymer or copolymer, andii) 5-60% by weight, based on dry weight of the polymer mixture, of at least one anionic polymer or copolymer, which is insoluble in a buffered medium below pH 4.0 and soluble at least in the range from pH 7.0 to pH 8.0, wherein the coating layer further comprises 110 to 250% by weight, calculated on dry weight of the polymer mixture, of a non-porous inert lubricant and the coating layer is present in an amount of at least 60% by weight calculated on the weight of core, and wherein, under in-vitro conditions according to USP paddle, 100 rpm, buffered at pH 6.8 in a medium with and without the addition of 40% (v/v) ethanol: when the pharmaceutical active ingredient is released to a degree of less than 20%, the difference in the release rate with the addition of 40% (v/v) ethanol is not more than plus or minus 15% of the corresponding release value without 40% (v/v) ethanol, and when the pharmaceutical active ingredient is released to a degree of 20-80%, the difference in the release rate with the addition of 40% (v/v) ethanol is not more than plus or minus 30% of the corresponding release value without 40% (v/v) ethanol.