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Compositions and methods for the inhibition of gastric acid secretion using derivatives of small dicarboxylic acids in combination with IBP
专利权人:
VECTA LTD.
发明人:
MARASH, MICHAEL,KOSTADINOV, ALEKSEY,ATAROT, TAL
申请号:
ES07804623
公开号:
ES2511792T3
申请日:
2007.07.19
申请国别(地区):
ES
年份:
2014
代理人:
摘要:
A pharmaceutical composition comprising as active ingredients a pharmaceutically effective amount of: (i) a parietal cell activator comprising one or more derivatives of aliphatic carboxylic acids chosen from: methyl, ethyl, propyl or butyl esters of aliphatic carboxylic acid molecules; and (ii) an irreversible inhibitor of the H + / K + ATPase gastric proton pump (IBP), in which the IBP particles are formulated as enteric coated delayed-release granules or as non-enteric dependent-release polymer coated granules weather; in which the derivatives have delayed and / or sustained parietal cell activation compared to non-derivatized acid molecules; wherein the aliphatic carboxylic acid molecules are one or more of: maleic acid, succinic acid, pyruvate, citrate, fumarate, -ketoglutarate, succinyl-CoA and oxaloacetate; and wherein the composition is formulated as: (a) pressure coated tablets or bilayer comprising enteric coated IBP in one layer and aliphatic carboxylic acid derivatives, both uncoated and coated with hydroxypropyl methyl cellulose, in a second cap; (b) an individual dosage form comprising hard gelatin capsules comprising a mixed population of microspheres chosen from among the IBP particles and microspheres comprising one more of aliphatic carboxylic acid derivatives, both uncoated and coated with hydroxypropyl methyl cellulose or alginate; or (c) a solid dosage form in which the solid dosage form is a capsule or multilaminar tablet containing the particles of the IBP and the particles of the aliphatic carboxylic acid derivative.Una composición farmacéutica que comprende como principios activos una cantidad farmacéuticamente eficaz de: (i) un activador de las células parietales que comprende uno o más derivados de ácidos carboxílicos alifáticos elegidos de entre: ésteres de metilo, de etilo, de propilo o de butilo de moléculas de ácidos carboxílicos alifáticos; y (ii) un inhibidor irreversible de la bomba de protones gástrica ATPasa de H+/K+ (IBP), en la
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中国工程科技知识中心
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