口服抗妇炎胶囊大鼠血浆中移行成分的鉴定  

Identification of transitional components on oral anti-gynecitis capsules absorbed into plasma

作　　者：黄家宇 王铭菊 刘星村 胡滨 吴军 汤磊 李莉 HUANG Jiayu;WANG Mingju;LIU Xingcun;HU Bin;WU Jun;TANG Lei;LI Li(School of Pharmacy,Guizhou Medical University,Guiyang 550025,Guizhou,China;Department of Quality,Long-Range Pharmaceuticals LTD,Guiyang 550018,Guizhou,China)

机构地区：[1]贵州医科大学药学院,贵州贵阳550025 [2]贵州远程制药有限责任公司质量部,贵州贵阳550018

出　　处：《贵州医科大学学报》2023年第10期1166-1173,共8页Journal of Guizhou Medical University

基　　金：贵州省科技计划项目(黔科中引地〔2022〕4017)。

摘　　要：目的鉴定口服抗妇炎胶囊大鼠血浆中的移行成分。方法称取苦参碱、槐定碱、盐酸小檗碱对照品加甲醇制成对照品溶液,取抗妇炎胶囊内容物分别配制成110 g/L抗妇炎胶囊灌胃给药样品溶液和50 g/L体外样品溶液;成年雌性Sprague Dawley(SD)大鼠12只随机均分为给药组(0.02 mL/g灌胃抗妇炎胶囊药液)和空白组(灌服同等体积的生理盐水),2次/d、连续3 d;末次给药后麻醉取肝门静脉血离心,得含药血浆样品和空白血浆样品,采用超高效液相色谱-离子阱-飞行时间质谱联用(UPLC-IT-TOF-MS)技术检测2组大鼠血浆样品、对照品溶液、给药样品溶液和体外样品溶液,通过对比分析5种样品的总离子图、提取离子图、质谱信息(保留时间、精确质荷比及碎片离子),并结合相关文献的数据对抗妇炎胶囊的入血成分进行鉴定。结果鉴定了11个移行成分,包括原型成分8个及代谢产物3个,入血的原型成分主要为生物碱类;氧化、还原以及葡萄糖醛酸化反应是该制剂在体内的主要代谢途径。结论建立的UPLC-IT-TOF-MS分析方法可鉴定口服抗妇炎胶囊大鼠血浆中的移行成分。Objective To explore the identification of the ingredients absorbed into the blood of treated with oral anti-gynecitis capsules.Methods The reference substance of matrine,sophoridine,berberine hydrochloride was added methanol to make the reference solutions.110 g/L of anti-gynecitis capsules sample solution for intragastric administration and 50 g/L in vitro sample solution was prepared by taking the contents of anti-gynecitis capsules.Twelve adult female Sprague Dawley(SD)rats were randomly divided into a control group(n=6)and a treatment group(n=6).The treatment group was gavaged with the content of anti-gynecitis capsules while the control group was given an equal dose of physiological saline.Subsequently,rat liver portal vein blood was taken for centrifugation and the plasma ingredients of the two groups of rats,reference solution,drug-containing plasma,and sample solution of anti-gynecitis capsules were detected by ultra high performance liquid chromatography ion trap time of flight mass spectrometry(UPLC-IT-TOF-MS)technology.The total ion maps and extract ion maps,mass spectrometry information(retention time,accurate mass charge ratio,and fragment ions)of five kinds of samples were compared and analyzed to identify the blood ingredients of anti-gynecitis capsules based on relevant literature data.Results By comparing the information on the total ion chromatogram,extraction chromatogram and the mass spectrogram of anti-gynecitis capsules,rat serum with drug and blank serum sample was used to confirm the constituents of anti-gynecitis capsules in vivo.Eleven transitional ingredients were identified including three metabolites and eight prototype ingredients,the prototype ingredients were mainly alkaloids.oxidation,reduction;glucuronization reactions were the main metabolic pathways of this formulation in the body.Conclusion The UPLC-IT-TOF-MS analysis method established in this study can identify the ingredients in blood of anti-gynecitis capsules.

关 键 词：抗妇炎胶囊 超高效液相色谱-离子阱-飞行时间质谱 血清药物化学 移行成分 代谢产物 代谢途径 

分 类 号：R284.1[医药卫生—中药学]