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The effect of parenteral nutrition fluids on the binding of therapeutic drugs to human serum in vitro.

机译:肠胃外营养液在体外对治疗药物与人血清结合的影响。

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摘要

The competitive binding of seven therapeutic drugs (carbamazepine, phenytoin, phenobarbital, procainamide, quinidine, theophylline, and valproic acid) to human serum and to five commonly used parenteral nutrition fluids in vitro was studied using equilibrium dialysis. For five of the drugs, all parenteral nutrition fluids bound less drug than human serum-phenobarbital (up to 14% less), phenytoin (up to 46% less), procainamide (up to 43% less), quinidine (up to 25% less), and valproic acid (up to 77% less)-suggesting that the presence of these fluids might increase the free fraction of these drugs in vivo. For carbamazepine, the fluids bound up to 82% more drug, suggesting that the presence of these fluids might decrease the free fraction of this drug in vivo. For theophylline, the fluids produced a minimal (no more than 5%) effect on binding to serum. The administration of parenteral nutrition fluids may significantly alter the free (active) fraction of some therapeutic drugs.
机译:使用平衡透析研究了七种治疗药物(卡马西平,苯妥英钠,苯巴比妥,普鲁卡因酰胺,奎尼丁,茶碱和丙戊酸)与人血清和五种常用肠胃外营养液的竞争性结合。对于这五种药物,所有肠胃外营养液中的药物结合量均少于人血清苯巴比妥(减少多达14%),苯妥英(减少多达46%),普鲁卡因酰胺(减少多达43%),奎尼丁(多达25%减少)和丙戊酸(减少多达77%),这表明这些液体的存在可能会增加这些药物在体内的游离分数。对于卡马西平,液体结合最多可增加82%的药物,这表明这些液体的存在可能会降低该药物在体内的游离分数。对于茶碱,液体对结合血清的影响很小(不超过5%)。肠胃外营养液的施用可能会显着改变某些治疗药物的游离(活性)部分。

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