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[食物对健康志愿者中异烟肼生物利用度的影响]

[Influence of food on the bioavailability of isoniazid in health volunteers].

作者信息

Zwolska Z, Niemirowska-Mikulska H, Augustynowicz-Kopeć E

机构信息

Zakładu Mikrobiologii, Instytutu Gruźlicy i Chorób Płuc w Warszawie.

出版信息

Pneumonol Alergol Pol. 1998;66(7-8):412-21.

Abstract

From the theoretical point of view, food intake exerts a complex influence on the bioavailability of drugs. It may interfere with tablet disintegration, drug dissolution and drug transit through the gastrointestinal tract, may also affect the metabolic transformation of drugs in the gastrointestinal wall and the liver. The knowledge about the influence of food is very important in treatment of tuberculosis, where the drugs are taken once daily or even less frequently. We studied the isoniazid concentrations in blood serum of 20 volunteers (12 slow and 8 fast acetylators of INH) both sexes, after the drug intake 2 hours before breakfast and immediately after breakfast. Concentrations of INH were tested by biological method with Mycobacterium aurum REB as a standard strain. The results have shown, that Cmax (3.55 +/- 0.29 versus 2.56 +/- 0.49 in fast acetylators and 4.34 +/- 0.2 versus 3.67 +/- 0.37 in slow acetylators), tmax (0.75 +/- 0.26 versus 1.31 +/- 0.37 in fast acetylators and 0.87 +/- 0.31 versus 1.79 +/- 0.62 in slow acetylators and AUC0-t (6.6 +/- 1.34 versus 5.47 +/- 1.5 in fast acetylators and 21.82 +/- 2.57 versus 18.61 +/- 2.57 in slow acetylators) are significantly decreased after ingestion of INH with breakfast.

摘要

从理论角度来看,食物摄入对药物的生物利用度有着复杂的影响。它可能会干扰片剂崩解、药物溶解以及药物在胃肠道中的转运,还可能影响药物在胃肠道壁和肝脏中的代谢转化。在结核病治疗中,药物每日服用一次甚至频率更低,了解食物的影响非常重要。我们研究了20名志愿者(12名异烟肼慢乙酰化者和8名快乙酰化者)在早餐前2小时服药以及早餐后立即服药后血清中的异烟肼浓度。异烟肼浓度通过以金杆菌REB作为标准菌株的生物学方法进行检测。结果表明,与早餐一同服用异烟肼后,快乙酰化者的Cmax(分别为3.55±0.29和2.56±0.49)、tmax(分别为0.75±0.26和1.31±0.37)以及AUC0-t(分别为6.6±1.34和5.47±1.5)显著降低,慢乙酰化者的Cmax(分别为4.34±0.2和3.67±0.37)、tmax(分别为0.87±0.31和1.79±0.62)以及AUC0-t(分别为21.82±2.57和18.61±2.57)也显著降低。

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