异丙嗪在大鼠离体胃肠中的体外代谢转化特性研究

摘要

目的:考察异丙嗪在大鼠离体胃肠液中的代谢转化特性,研究不同胃肠段的代谢转化速率.方法:通过水浴孵育胃肠段和异丙嗪,采用高效液相色谱(HPLC)法测定孵育液中异丙嗪含量;考察低、中、高3个不同质量浓度的异丙嗪在大鼠离体肠黏膜提取液、肠浆膜提取液、肠组织匀浆液、胃黏膜提取液、胃组织匀浆液中的代谢动力学.结果:异丙嗪在大鼠离体胃肠液中均可以被迅速代谢;各胃肠段提取液以及匀浆液对异丙嗪的代谢速率存在差异;胃黏膜提取液和肠黏膜提取液具有较大的代谢速率,代谢速率和异丙嗪浓度没有正相关性.结论:异丙嗪在大鼠不同胃肠段中代谢速率具有差异性,且代谢速率和异丙嗪浓度没有正相关性.%Objective:To investigate the metabolic properties of promethazine in rat's isolated gastrointestinal tract fluid and study the metabolic rate in different gastrointestinal tract.Methods:The gastrointestinal tract and promethazine were incubated in water bath.The content of promethazine in the incubation solution was determined by HPLC.The effects of three different concentrations of promethazine on isolated rat intestinal mucosal extract,serous membrane extract,intestinal tissue homogenate,gastric mucosal extract and gastric tissue homogenate.Results:Promethazine can be rapidly metabolized in the isolated stomach and intestine of rats.The metabolic rate of different extracts and homogenates of promethazine is different.The gastric mucosal extract and intestinal mucosa extract have high metabolic rate,metabolic rate and promethazine concentration were not positively correlated.Conclusion:Promethazine has different metabolisms in rat gastrointestinal tract,and the metabolic rate and promethazine concentration have no positive correlation.