配合薬の薬物相互作用に関する研究(第2報) : 犬血漿中IsopropylantipyrineおよびPhenacetin濃度を指標としたIsopropylantipyrine, Phenacetin, AllylisopropylacetylureaおよびCaffeineの相互作用について

概要

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1) The plasma level profiles of isopropylantipyrine and phenacetin in beagle dogs, were investigated by oral administration. Each drug was used alone, combined with each other, or in various combinations with caffeine or allylisopropylacetylurea. These four compounds are ingredients of an analgesic combined drug on the market. 2) The individual plasma levels of isopropylantipyrine and phenacetin were both elevated by being combined with each other. The areas under the plasma-level curves for isopropylantipyrine and phenacetin in dogs were enlarged by the combination with allylisopropylacetylurea. 3) Distribution of isopropylantipyrine in several organs and tissues was compared in rats between its single use and in combination as the analgesics. The concentration of isopropylantipyrine in all organs tested was found to be twice higher in rats receiving the analgesic combination drug than in those treated with isopropylantipyrine alone. 4) Metabolism of isopropylantipyrine by hepatic microsomal enzymes in rats was inhibited non-competitively by the addition of phenacetin or allylisopropylacetylurea. 5) Based on these findings, possible reasons for combining ingredients for an analgesic combined drug were discussed.
公益社団法人日本薬学会の論文
1977-06-25