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目的:建立大鼠血浆和肠内容物中炎琥宁含量测定方法,研究炎琥宁肠溶微丸在大鼠体内肠吸收和药物动力学,为炎琥宁口服制剂的研究提供依据。方法:以大鼠为研究对象,灌胃给予炎琥宁肠溶微丸,采用高效液相色谱法测定大鼠灌胃给药后血浆和各肠段内容物中炎琥宁的药物浓度,评价其在大鼠体内的吸收和药动学特性。结果:给药后2 h小肠和大肠中未发现小丸存在,4 h小肠中小丸的数量最多,肠道内容物中炎琥宁含量最高(3593.13μg),血药浓度-时间曲线符合单室模型特征,求得主要药物动力学参数t1/2为2.69 h,Tmax为5 h,Cmax为3.02μg/mL,血药浓度时间曲线下面积为6.42μg.h/mL。结论:炎琥宁在大鼠小肠有较好吸收,制备炎琥宁肠溶微丸口服给药可行。
OBJECTIVE: To establish a method for the determination of content of melatonin in rat plasma and intestinal contents, and to study the intestinal absorption and pharmacokinetics of Yanhuaning enteric-coated pellets in rats. Methods: Rat was taken as the research object. Yanhuaning enteric-coated pellets were given by intragastric administration. The drug concentrations of Yanhuoning in plasma and intestinal segments were determined by high performance liquid chromatography Its absorption and pharmacokinetics in rats. Results: No small pellets were found in the small intestine and large intestine 2 h after administration. The number of small intestine pellets in 4 h was the highest, the content of mehtodin in intestinal contents was the highest (3593.13 μg), and the plasma concentration-time curve was in agreement with single-chamber model The main pharmacokinetic parameters t1 / 2 were 2.69 h, Tmax was 5 h, Cmax was 3.02 μg / mL, and the area under the plasma concentration time curve was 6.42 μg.h / mL. Conclusion: Yanhu Ning better absorption in the small intestine, the preparation of Yan Huaning enteric-coated pellets feasible.