首页> 外国专利> PHARMACEUTICAL COMPOSITION COMPRISING P-GLYCOPROTEIN INHIBITOR AND P-GLYCOPROTEIN SUBSTRATE DRUG

PHARMACEUTICAL COMPOSITION COMPRISING P-GLYCOPROTEIN INHIBITOR AND P-GLYCOPROTEIN SUBSTRATE DRUG

机译:包含P-糖蛋白抑制剂和P-糖蛋白底物药物的药物组合物

摘要

The present invention relates to a pharmaceutical composition comprising a p-glycoprotein inhibitor and a p-glycoprotein substrate drug. The pharmaceutical composition of the present invention reduces side effects of the drug caused by activity of p-glycoprotein, and further may provide an equivalent pharmacological effect using a smaller amount of the drug. In particular, use of dabigatran etexilate, a p-glycoprotein substrate drug, with tetrazole derivative, a p-glycoprotein inhibitor, can significantly increase the bioavailability of dabigatran etexilate, and consequently the remaining amount of dabigatran etexilate in the gastrointestinal tract may be significantly reduced as the drug has the same level of bioavailability despite a reduction in the amount thereof. Also, because of the above reasons, the dosage of the drug in the gastrointestinal tract is reduced, and so the pharmaceutical composition of the present invention can reduce the risk of bleeding, a fatal drawback for patients taking a conventional dabigatran etexilate.
机译:本发明涉及包含p-糖蛋白抑制剂和p-糖蛋白底物药物的药物组合物。本发明的药物组合物减少了由对糖蛋白的活性引起的药物副作用,并且还可以使用较少量的药物来提供等效的药理作用。特别是,将达比加群酯的一种糖蛋白的底物达比加群酯与一种p-糖蛋白抑制剂四唑衍生物一起使用,可以显着提高达比加群酯的生物利用度,因此胃肠道中达比加群酯的残留量可能会大大减少。因为药物的量减少了,但具有相同水平的生物利用度。另外,由于上述原因,减少了药物在胃肠道中的剂量,因此本发明的药物组合物可以降低出血的风险,这是服用常规达比加群酯的患者的致命缺点。

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