著者

大谷 道輝 川端 志津 假家 悟 内野 克喜 伊藤 敬 小瀧 一 籾山 邦男 森川 亜紀 瀬尾 巖 西田 紀子

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.122, no.5, pp.323-329, 2002-05-01 (Released:2003-02-18)

参考文献数

19

被引用文献数

11 13

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The effect of the intake of 200g of grapefruit pulp (corresponding to one grapefruit) on the pharmacokinetics of the calcium antagonists nifedipine (NF) and nisoldipine (NS) were investigated in 8 healthy Japanese male volunteers. A crossover design was used for the study: group I did not ingest any grapefruit (control group); group II ingested grapefruit 1 h after drug administration; and group III ingested grapefruit 1 h before drug administration. The intake of grapefruit pulp increased the plasma concentrations of both NF and NS, an effect that has previously been reported with grapefruit juice. The increase was most marked when grapefruit was eaten before drug administration. For both NF and NS, subjects who ingested grapefruit 1 h before drug administration exhibited a greater Cmax and AUC0—24 than did subjects in the control group. For NF, the Cmax was 1.4 times higher and the AUC0—24 1.3 times larger in group III than in group I. For NS, the Cmax was 1.5 times higher and the AUC0—24 1.3 times larger in group III than in group I. The increase in the AUC0-24 was significant for both drugs (p<0.05). The finding that the ratios of Cmax and AUC0—24 for unchanged drug and metabolites did not vary greatly among the three groups for either drug suggests that the increase in serum concentration produced by grapefruit intake may be due to other factors than an inhibitory effect on drug metabolism. Also, the increases in Cmax and AUC0—24 of NS produced by grapefruit intake were smaller than those produced by grapefruit juice intake, indicating that grapefruit pulp and juice have different effects on the pharmacokinetics.

著者

大谷 道輝 川端 志津 假家 悟 内野 克喜 伊藤 敬 小瀧 一 籾山 邦男 森川 亜紀 瀬尾 巖 西田 紀子

出版者

公益社団法人日本薬学会

雑誌

藥學雜誌 (ISSN:00316903)

巻号頁・発行日

vol.122, no.5, pp.323-329, 2002-05-01

被引用文献数

1 13

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The effect of the intake of 200g of grapefruit pulp (corresponding to one grapefruit) on the pharmacokinetics of the calcium antagonists nifedipine (NF) and nisoldipine (NS) were investigated in 8 healthy Japanese male volunteers. A crossover design was used for the study: group I did not ingest any grapefruit (control group); group II ingested grapefruit 1 h after drug administration; and group III ingested grapefruit 1 h before drug administration. The intake of grapefruit pulp increased the plasma concentrations of both NF and NS, an effect that has previously been reported with grapefruit juice. The increase was most marked when grapefruit was eaten before drug administration. For both NF and NS, subjects who ingested grapefruit 1 h before drug administration exhibited a greater C_<max> and AUC_<0-24> than did subjects in the control group. For NF, the C_<max> was 1.4 times higher and the AUC_<0-24> 1.3 times larger in group III than in group I. For NS, the C_<max> was 1.5 times higher and the AUC_<0-24> 1.3 times larger in group III than in group I. The increase in the AUC_<0-24> was significant for both drugs (p<0.05). The finding that the ratios of C_<max> and AUC_<0-24> for unchanged drug and metabolites did not vary greatly among the three groups for either drug suggests that the increase in serum concentration produced by grapefruit intake may be due to other factors than an inhibitory effect on drug metabolism. Also, the increases in C_<max> and AUC_<0-24> of NS produced by grapefruit intake were smaller than those produced by grapefruit juice intake, indicating that grapefruit pulp and juice have different effects on the pharmacokinetics.