喘可治注射液在大鼠体内的药物代谢研究

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探讨喘可治注射液在大鼠体内的代谢转化。选择SD大鼠12只,分为两组,分别为对照组和肌肉注射给药组,收集给药后0~24 h、24~48 h粪便和尿液样品,给药后0.5、2和24 h血样,甲醇超声提取,沉淀蛋白,高效液相色谱-串联线性离子阱静电场轨道阱质谱仪检测。通过比较给药组和对照组的总离子流色谱图,对粪便、尿液以及血浆中推测的代谢物和标准物质的出峰时间及相关化合物的多级串联质谱数据进行了分析,结果在大鼠尿液中未检测到相关代谢产物;在大鼠给药后0.5 h血样中可检测到在喘可治注射液中含量较大的原形药物,如朝藿定C和淫羊藿苷,但未能检测到其他原形药物和相关代谢产物,而大鼠给药后2和4 h血样中则均未能检测到原形药物和相关代谢产物;在大鼠粪便中发现了12种黄酮类代谢产物,系统分析了这些代谢产物的代谢转化规律及可能结构。大鼠体内喘可治注射液所含化学成分的主要代谢转化途径为脱糖、脱水、氧化、甲基化和异构化代谢反应等。 To investigate the metabolic transformation of Chuankezhi Injection in rats. Twelve SD rats were selected and divided into two groups: control group and intramuscular injection group. Fecal and urine samples were collected at 0-24 h and 24-48 h after administration, and 0.5, 2 and 24 h blood samples, ultrasonic extraction of methanol, precipitated protein, high performance liquid chromatography - tandem linear ion trap electrostatic field orbital mass spectrometry. By comparing the total ion chromatogram of the administration group and the control group, the peak time of excreted metabolites and reference substances in stool, urine and plasma as well as the multistage tandem mass spectrometry data of the related compounds were analyzed. As a result, No relevant metabolites were detected in the urine of rats; prototype drugs such as appeudin C and icariin were detected in the blood of Chuankezhi injection at 0.5 h after administration in rats Failed to detect other prototype drugs and related metabolites, and 2 and 4 h after administration of blood samples were unable to detect prototype drugs and related metabolites; found in rat feces 12 flavonoid metabolites , Systematically analyzed the metabolic transformation of these metabolites and possible structure. The main metabolic pathway of the chemical components contained in the body of Chuankezhi injection in rats is desalination, dehydration, oxidation, methylation and isomerization reaction.
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