交泰丸中抗抑郁活性成分在健康受试者体内的药动学研究
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| 篇名: | 交泰丸中抗抑郁活性成分在健康受试者体内的药动学研究 |
| TITLE: | Pharmacokinetic study of the antidepressant active components from Jiaotai pills in healthy subjects |
| 摘要: | 目的 研究交泰丸中抗抑郁活性成分在健康受试者体内的药动学特征。方法选取8名健康受试者(男性3名,女性5名),单次口服交泰丸8.55g,分别于服药前(0h)和服药后0.25~36.0h采集静脉血。血浆样品经蛋白沉淀法处理后,采用液相色谱-串联质谱(LC-MS/MS)法检测交泰丸中抗抑郁活性成分(黄连碱、小檗碱、木兰花碱、巴马汀)的血药浓度。采用DAS2.0软件,以非房室模型计算各健康受试者的药动学参数[半衰期(t1/2)、峰浓度(cmax)、达峰时间(tmax)、药-时曲线下面积(AUC)、平均驻留时间(MRT)]。结果健康受试者服用交泰丸后,4种抗抑郁活性成分的药-时曲线符合二室模型,其tmax相近,均在服药后2.00~4.00h达到血药浓度峰值;黄连碱与小檗碱的t1/2和MRT明显长于木兰花碱和巴马汀;4种抗抑郁活性成分的AUC与cmax也存在明显差异,其中木兰花碱的AUC0-t和cmax均远高于其他3种成分。结论本研究采用LC-MS/MS法分析了交泰丸中抗抑郁活性成分在健康受试者体内的药动学特征,可为交泰丸的临床应用提供参考。 |
| ABSTRACT: | OBJECTIVE To study the pharmacokinetic characteristics of antidepressant active components from Jiaotai pills in healthy subjects. METHODS Eight healthy subjects (3 males and 5 females) were recruited and given a single oral dose of 8.55 g of Jiaotai pills. Venous blood samples were collected before administration (0 h) and at intervals from 0.25 to 36.0 hours post- administration. After treating the plasma samples with protein precipitation, the blood concentrations of the antidepressant active ingredients (coptisine, berberine, magnoflorine, and palmatine) in Jiaotai pills were determined using liquid chromatography- tandem mass spectrometry (LC-MS/MS) method. DAS 2.0 software was employed to calculate the pharmacokinetic parameters of healthy subjects [half-life (t1/2), peak concentration (cmax), time to peak concentration (tmax), area under the concentration-time curve (AUC), and mean residence time (MRT)] using a non-compartmental model. RESULTS After healthy subjects took Jiaotai pills, the drug-time curve of the four antidepressant active ingredients conforms to a two-compartment model and tmax values were similar, with all reaching peak blood concentrations within 2.00 to 4.00 hours post-administration. However, the t1/2 and MRT of coptisine and berberine were significantly longer than that of magnoflorine and palmatine. There were also significant differences in the AUC and cmax among the four antidepressant active ingredients, with magnoflorine exhibiting markedly higher AUC0-t and cmax compared to the other three components. CONCLUSIONS In this study,LC-MS/MS is used to analyze the pharmacokinetic characteristics of the antidepressant active ingredients from Jiaotai pills in healthy subjects, can provide valuable references for the clinical application of Jiaotai pills. |
| 期刊: | 2026年第37卷第03期 |
| 作者: | 陈瑜洁;王一然;廖智鹏;边欣芳;王艳军;居文政 |
| AUTHORS: | CHEN Yujie,WANG Yiran,LIAO Zhipeng,BIAN Xinfang,WANG Yanjun,JU Wenzheng |
| 关键字: | 交泰丸;药动学;抑郁;黄连碱;小檗碱;木兰花碱;巴马汀;液相色谱-串联质谱法 |
| KEYWORDS: | Jiaotai pills; pharmacokinetics; depression; coptisine; berberine; magnoflorine; palmatine; LC-MS/MS method |
| 阅读数: | 5 次 |
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