| LC-MS法研究血浆中氧化苦参碱及其代谢物在犬体内的药代学 |
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| 引用本文： | 王素军,王广基,李晓天,马仁玲,孙建国,盛龙生.LC-MS法研究血浆中氧化苦参碱及其代谢物在犬体内的药代学[J].中国中药杂志,2005,30(2):133-136. |
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| 作者姓名： | 王素军 王广基 李晓天 马仁玲 孙建国 盛龙生 |
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| 作者单位： | 1. 中国药科大学药,物代谢研究中心,江苏,南京,210038
2. 中国药科大学,分析测试中心,江苏,南京,210038 |
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| 基金项目： | 国家高技术研究发展计划(863计划)，国家自然科学基金，江苏省重点实验室基金 |
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| 摘 要： | 目的 :建立同时测定Beagle犬血浆中氧化苦参碱及其代谢物的LC MS分析法 ,研究氧化苦参碱及其代谢物药代学过程。方法 :采用LichrospherC18柱 (4.6mm× 2 5 0mm ,5 μm) ,柱温 2 5℃。流动相 10mmol·L-1醋酸铵水溶液 甲醇 (2 5∶75 ) ,流速 1mL·min-1;电喷雾离子化 (ESI)方式 ,采用选择性离子检测法 ,检测离子为正离子 ,氧化苦参碱SIM的离子是 M +H]+ ,m/z 2 6 5 .1;苦参碱SIM的离子是 M +H]+ ,m/z2 4 9 2。结果 :氧化苦参碱与苦参碱在 2～ 5 0 0 0ng·mL-1呈良好的线性关系 (r≥ 0. 9990 ) ,二者最小检出含量分别为 0. 6 ,0. 3ng·mL-1。日内和日间误差均小于 4.7% ,方法回收率大于 96. 5 % ;氧化苦参碱的T1/2 ,Tmax,Cmax,MRT ,AUC0→24 h为 (5. 5± 1 5 8)h ,(1.0± 0 .30 )h ,(2 4 18 3± 970 78)ng·mL-1,(3.2± 0. 6 4 )h ,(5 797 4± 90 8 16 )ng·mL-1·h ,苦参碱的T1/2 ,Tmax,Cmax,MRT ,AUC0→24 h为 (9.8± 2.77)h ,(1.9± 1.0 9)h ,(15 32. 4± 4 94 86 )ng·mL-1,(4 4± 1 97)h ,(5.5 30 5± 10 4 2.6 5 )ng·mL-1·h。结论 :氧化苦参碱和苦参碱LC MS定量法灵敏、快速、简单 ,专属性强 ;氧化苦参碱口服后在Beagle犬体内转化较多。
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| 关 键 词： | 氧化苦参碱 苦参碱 液相色谱/质谱联用 药代学 |
| 文章编号： | 1001-5302(2005)02-0133-04 |
| 收稿时间： | 2004/5/26 0:00:00 |
Pharmacokinetics of oxymatrine and its metabolite in beagle dogs by LC-MS |
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| WANG Su-jun;WANG Guang-ji;LI Xiao-tian;MA Ren-ling;SUN Jian-guo;SHENG Long-sheng.Pharmacokinetics of oxymatrine and its metabolite in beagle dogs by LC-MS[J].China Journal of Chinese Materia Medica,2005,30(2):133-136. |
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| Authors: | WANG Su-jun;WANG Guang-ji;LI Xiao-tian;MA Ren-ling;SUN Jian-guo;SHENG Long-sheng |
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| Affiliation: | Center of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing 210038, China. |
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| Abstract: | OBJECTIVE: To establish LC-MS method in the determination of oxymatrine and its metabolite in plasma and investigate their pharmacokinetics in beagle dogs. METHOD: Lichrospher C18 column (4.6 mm x 250 mm, 5 microm) was used as the analytical column maintained at 25 degrees C. The mobile phase consisted of 10 mmol x L(-1) CH3COONH4 and CH3OH (25:75). Flow rate was 1 mL x min(-1). Electrospray ionization (ESI) was carried out. The ESI ion source was set in positive ion polasity mode. The selective ion monitoring (SIM) was set at m/z 265.1 and 249.2. RESULT: The linearity ranged from 2 to 5000 ng x mL(-1) (r = 0.9991). The detection of oxymatrine and its metabolite were 0.6 and 0.3 ng x mL(-1). The RSD(%) within day and between day was less than 4.7%. The recovery of this method was more than 96.5%. The disposition was conformed to a two-compartment model. The T(1/2), Tmax, Cmax, MRT, AUC(0-->24 h) of oxymatrine were (5.5+/-1.58) h, (1.0+/-0.30) h, (2418.3 +/-970.78) ng x mL(-1), (3.2+/-0.64) h, (5797.4+/-908.16) ng x mL(-1) x h accordingly. The corresponding T(1/2), Tmax, Cmax, MRT, AUC(0-->24 h) of matrine were (9.8+/-2.77) h, (1.9+/-1.09) h, (1532.4+/-494.86) ng x mL(-1), (4.4+/-1.97) h, (5530.5+/-1042.65) ng x mL(-1) x h. CONCLUSION: This assay was highly sensitive, rapid, simple and specific enough for determining concentrations of oxymatrine and its metabolite matrine in plasma of beagle dog. |
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| Keywords: | oxymatrine matrine LC-MS pharmacokinetics |
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