INFLUENCE OF FOOD ON THE PHARMACOKINETICS OF KETOCONAZOLE
INFLUENCE OF FOOD ON THE PHARMACOKINETICS OF KETOCONAZOLE
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DOI：
10.1128/aac.25.1.1
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发表时间：
1984-01-01
影响因子：
4.9
通讯作者：
WILLIAMSON, PJ
中科院分区：
文献类型：
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作者：
DANESHMEND, TK;WARNOCK, DW;WILLIAMSON, PJ
8名健康成人在禁食状态下口服单剂量酮康唑（一种抗真菌剂）（200,400,600和800mg），并根据平衡块设计每周间隔一次标准早餐。在给药后32小时测定血清中的浓度。食物没有减少酮康唑的吸收或显著改变血清中酮康唑的峰值浓度；在达到峰值浓度时，有与食物有关的延迟。在400和600毫克的剂量下，食物似乎能促进吸收；在800毫克的剂量下没有看到这种效果。随着剂量的增加，酮康唑的半衰期和血清浓度-时间曲线下面积不成比例地增加，提示酮康唑的药代动力学可能具有剂量依赖性。直到800毫克的剂量，酮康唑的消除似乎不是饱和的。药物与食物一起服用不太可能是治疗失败的原因。
Eight healthy adults were given single oral doses of ketoconazole [an antifungal agent] (200, 400, 600 and 800 mg) in the fasting state and with a standard breakfast at weekly intervals according to a balanced block design. Concentrations in serum were measured up to 32 h after the dose. Food did not reduce ketoconazole absorption or significantly alter peak ketoconazole concentrations in serum; there was a food-related delay in achieving peak concentrations. At the 400 and 600 mg doses, food appeared to enhance absorption; this effect was not seen at the 800 mg dose. With an increase in dose, the half-life and area under the serum concentration-time curve increased disproportionately, suggesting that the pharmacokinetics of ketoconazole may be dose-dependent. Up to the 800 mg dose, the elimination of ketoconazole did not appear to be saturable. Administration of the drug with food is unlikely to be a cause of therapeutic failure.