The influence of experimental procedures and dose on the intestinal absorption of an onium compound, benzomethamine.
The influence of experimental procedures and dose on the intestinal absorption of an onium compound, benzomethamine.
复制标题
实验程序和剂量对鎓化合物苯甲胺肠道吸收的影响。
DOI：
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发表时间：
1961
期刊：
影响因子：
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通讯作者：
E. Pelikan
中科院分区：
文献类型：
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作者：
R. R. Levine;E. Pelikan
在未麻醉的大鼠体内，使用单环和多环制剂研究了苯甲甲胺在3小时内从小肠的吸收。
在实验开始前，动物禁食并用少量水灌注肠腔，使吸收增加至对照水平以上。吸收不受肠道轻度机械操作的影响。
苯甲甲胺的吸收量被认为是依赖于在肠道中的吸收表面的相对位置。最接近幽门的肠段吸收最大。
在大量动物中研究了0.5 mg/环至10 mg/环的17个剂量水平下苯甲甲胺的吸收与剂量的函数关系。发现剂量-吸收曲线是一条复合曲线，而不是整个使用剂量范围内的单一线性函数。对应于0.5 mg/环至2.0 mg/环剂量的曲线段的斜率与2.0 mg/环至2.5 mg/环曲线段的斜率显著不同，后一段的斜率与2.5 mg/环至4或10 mg/环曲线段的斜率显著不同。剂量-吸收曲线的线性性得出结论，在至少一部分剂量-反应曲线中必须涉及不止一种苯甲甲胺穿过肠壁的转移机制。
药物溶液中存在肠粘液物质，具有均匀降低单位给药量苯甲甲胺吸收量的作用。曲线向下位移的量直接随注射溶液中粘液的量而变化。
The absorption in 3 hours of benzomethamine from the small intestine has been studied in vivo in unanesthetized rats using single- and multiple-loop preparations.
Fasting of animals and perfusing of the intestinal lumen with small quantities of water prior to the beginning of the experiments increased absorption above control levels. Absorption was unaffected by mild mechanical manipulation of the gut.
The amount of benzomethamine absorbed was found to be dependent on the relative position in the gut of the absorbing surface. Absorption was greatest in the intestinal segments closest to the pylorus.
The absorption of benzomethamine as a function of dose was studied in a large number of animals at 17 dose levels ranging from 0.5 mg/loop to 10 mg/loop. The dose-absorption curve was found to be a composite curve and not a single, linear function throughout the entire range of doses used. The slope of the segment of the curve corresponding to doses of 0.5 mg/loop to 2.0 mg/loop was significantly different from the slope of the segment of the curve from 2.0 mg/loop to 2.5 mg/loop, and the slope of the latter segment was significantly different from the slope of the curve from 2.5 mg/loop to 4 or 10 mg/loop. The alinearity of the dose-absorption curve led to the conclusion that more than one mechanism of transfer of benzomethamine across the gut wall must be involved in at least a part of the dose-response curve.
The presence of intestinal mucous material in the drug solutions had the effect of uniformly decreasing the amount of benzomethamine absorbed per quantity administered. The amount of downward displacement of the curve varied directly with the amount of mucus in the injected solutions.