Tchercansky D M, Acevedo C, Rubio M C
Cátedra de Farmacologia, Facultad de Farmacia y Bioquimica, Universidad de Buenos Aires, Argentina.
J Pharm Sci. 1994 Apr;83(4):549-52. doi: 10.1002/jps.2600830421.
The duodenal transfer and metabolism of [3H]tyramine from sacs and perfused segments of rat intestine were determined. In sacs, a linear relationship between the steady-state transfer rate of total tritium and the initial mucosal tyramine concentration was observed, suggesting that the clearance is the same at different concentrations. In duodenal perfusions, there was no significant difference in the amount of total tritium removed between control and everted tissues, whether the flow was 0.2 or 2.0 mL/min. The percentage of [3H]tyramine extracted from the gut lumen depended on the flow rate. About 30-40% of the extracted drug was metabolized; this value decreased to 20% when the rats were pretreated with pargyline. The data support the idea that the transfer mechanism for tyramine is simple diffusion.
测定了大鼠肠囊和灌注肠段中[3H]酪胺的十二指肠转运及代谢情况。在肠囊中,观察到总氚的稳态转运速率与初始黏膜酪胺浓度之间呈线性关系,这表明在不同浓度下清除率相同。在十二指肠灌注实验中,无论流速是0.2还是2.0 mL/min,对照组织和外翻组织之间去除的总氚量均无显著差异。从肠腔中提取的[3H]酪胺百分比取决于流速。约30 - 40%的提取药物被代谢;当大鼠用帕吉林预处理后,该值降至20%。这些数据支持酪胺的转运机制是简单扩散这一观点。