Influence of food on the bioavailability of "real" and "apparent" hydralazine from conventional and slow-release preparations.

Influence of food on the bioavailability of "real" and "apparent" hydralazine from conventional and slow-release preparations.
复制标题

食物对常规和缓释制剂中“真实”和“表观”肼屈嗪生物利用度的影响。

DOI:
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发表时间:
1982
期刊:
Drug-nutrient interactions
影响因子:
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通讯作者:
A. Melander
A. Melander
中科院分区:
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文献类型:
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作者:
H. Liedholm;E. Wåhlin;A. Hanson;A. Melander

文献摘要

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在健康志愿者中,在禁食状态下单剂量给药并与 1840 kJ(440 kcal)的标准化早餐一起研究伴随食物摄入对肼屈嗪生物利用度的影响。通过气相色谱法测定肼屈嗪的“真实”(推测为活性)和“表观”(=总量=“真实”肼+摄入肼后形成的对酸不稳定的腙)。在摄入常规肼苯达嗪片剂后,同时摄入食物似乎增强了“表观”和“真实”肼苯达嗪的生物利用度。另一方面,食物摄入并没有显着影响缓释制剂中肼屈嗪的生物利用度。与传统制剂相比,食物对肼屈嗪生物利用度的增强作用可能是由于首过代谢减少。
The influence of concomitant food intake on the bioavailability of hydralazine was studied in healthy volunteers following single-dose administrations in the fasting state and together with a standardized breakfast meal of 1840 kJ (440 kcal). Both "real" (presumably active) and "apparent" (= total = "real" hydralazine + acid-labile hydrazones formed after hydralazine ingestion) hydralazine were determined by gas chromatography. Concomitant food intake seemed to enhance the bioavailability of both "apparent" and "real" hydralazine following ingestion of conventional hydralazine tablets. On the other hand, food intake did not significantly affect hydralazine bioavailability from a slow-release preparation. The enhanced effect of food on hydralazine bioavailability from the conventional preparation is probably due to reduced first-pass metabolism.