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关于食物摄入对磺胺类药物生物利用度的影响。

On the influence of concomitant food intake on sulfonamide bioavailability.

作者信息

Melander A, Wåhlin E, Danielson K, Rerup C

出版信息

Acta Med Scand. 1976;200(6):497-500. doi: 10.1111/j.0954-6820.1976.tb08272.x.

Abstract

The influence of food intake on the bioavailability of a frequently used short-acting sulfonamide, sulfaisomidine (Elkosin), has been examined in eight healthy volunteers. The drug was administered as a single oral dose, both on an empty stomach and together with a standardized breakfast. Numerous venous blood samples were drawn for the first eight hours after ingestion of the drug, and the concentration of unmetabolized sulfonamide in serum was assessed by spectrophotometry. The observations indicate that concomitant food intake alters neither absorption rate, peak concentration, time to reach peak concentration, elimination rate, nor total amount of sulfonamide reaching the general circulation. Thus, the absorption of orally administered sulfaisodimidine is not at all affected by concomitant intake of food. This finding contrasts with previous observations on some other sulfonamides, and it may signify a therapeutic advantage of sulfaisodimidine. In addition, the amount absorbed showed only a little interindividual variation. This suggests that the use of standardized size and interval of sulfaisodimidine dosage can be recommended. The present findings emphasize that conclusions about the absorption of a certain drug should not be derived from studies with other, albeit chemically related, compounds.

摘要

在八名健康志愿者中研究了食物摄入对常用短效磺胺类药物磺胺异嘧啶(Elkosin)生物利用度的影响。该药物以单次口服剂量给药,分别在空腹和与标准化早餐一起服用的情况下进行。在摄入药物后的前八个小时采集了大量静脉血样,并通过分光光度法评估血清中未代谢磺胺类药物的浓度。观察结果表明,同时摄入食物既不改变磺胺异嘧啶的吸收速率、峰值浓度、达到峰值浓度的时间、消除速率,也不改变进入体循环的磺胺类药物总量。因此,口服磺胺异嘧啶的吸收完全不受同时摄入食物的影响。这一发现与之前对其他一些磺胺类药物的观察结果形成对比,可能意味着磺胺异嘧啶具有治疗优势。此外(此处根据语境添加,使逻辑更连贯),吸收量仅表现出很小的个体间差异。这表明可以推荐使用标准化剂量大小和间隔的磺胺异嘧啶。目前的研究结果强调,关于某种药物吸收的结论不应从对其他虽然化学结构相关但不同的化合物的研究中得出。

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