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目的:建立LC-MS法测定大鼠血浆和其他组织中苦参碱、氧化苦参碱、槐果碱、氧化槐果碱的浓度,研究复方苦参注射液在大鼠体内心、肝、脾、肺、肾等12个脏器组织的分布。方法:在血浆和组织样品中加入内标,用氯仿提取,以甲醇:10 mmolNH4Ac-0.02%HCOOH-水=90:10(v:v);CN柱分离,LC-MS法检测健康大鼠给予复方苦参注射液后3个时间点(15min、1h、4h)的血浆及组织样品中4种生物碱的浓度。结果:在给药后3个时间点,苦参碱和槐果碱在各组织中的分布量依次为:肝>肾/脾>肌肉/肠>肺/胃>心/脑>脂肪/子宫>睾丸;氧化苦参碱和氧化槐果碱在各组织中的分布量依次为:肾/肺>肌肉>肠/胃>心/脾>子宫>脂肪/睾丸>脑/肝;随着时间的推移,苦参碱和槐果碱浓度下降速度明显缓于氧化苦参碱和氧化槐果碱;苦参碱和槐果碱在肝脏分布最多,而氧化苦参碱和氧化槐果碱在肝脏分布最低。结论:复方苦参注射液4种生物碱在组织脏器中的分布,氧化态和非氧化态存在较大差异,尤其在肝脏,氧化苦参碱、氧化槐果碱浓度很低,而苦参碱、槐果碱浓度很高;而且在各组织中苦参碱和槐果碱的浓度显著高于氧化苦参碱和氧化槐果碱,与血浆中的分布相反,说明苦参碱和槐果碱相对于氧化苦参碱和氧化槐果碱而言主要分布于组织脏器中。
OBJECTIVE: To establish a method for the determination of matrine, oxymatrine, sophocarpine and oxysophocarpine in rat plasma and other tissues by LC-MS method. The effects of compound Kushen injection on heart, liver, spleen , Lung, kidney and other 12 organ tissue distribution. Methods: The internal standard was added to the plasma and tissue samples and extracted with chloroform. The rats were dosed with 10 mmol NH 4 Ac-0.02% HCOOH-water = 90: 10 (v: v) Compound Kushen injection three time points (15min, 1h, 4h) plasma and tissue samples of four alkaloid concentrations. Results: The distribution of matrine and sophocarpine in each tissue were as follows: liver> kidney / spleen> muscle / intestine> lung / stomach> heart / brain> fat / The distributions of testis, oxymatrine and oxycodone in each tissue were as follows: kidney / lung> muscle> intestine / stomach> heart / spleen> uterus> fat / testis> brain / liver; as time went by , Matrine and sophocarpine decreased significantly slower than the concentration of oxymatrine and oxidized sophocarpine; matrine and sophocarpine most distributed in the liver, and oxymatrine and oxycinnamine were the lowest in the liver distribution . CONCLUSION: The distribution of four alkaloids in compound kushen injection has obvious difference between oxidized and non-oxidized state, especially in liver, oxymatrine and oxycodone, Alkali, sophocarpine concentration is high; and matrine and sophocarpine concentrations in each tissue was significantly higher than that of oxymatrine and oxcarbosulfan, and the distribution of plasma opposite, indicating that matrine and Sophora japonica Alkaloids are mainly distributed in tissues and organs relative to oxymatrine and oxycodone.