顺、反式二苯乙烯苷在小鼠体内药动学及组织分布的对比研究

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目的:建立同时测定小鼠体内顺式二苯乙烯苷与反式二苯乙烯苷浓度的方法,并进行药动学和组织分布的对比研究。方法:采用Diamonsil C18色谱柱(250 mm×4.6 mm,5μm),乙腈-甲醇-0.1%冰醋酸(11∶7∶82)为流动相,流速1.0 m L/min,以虎杖苷为内标物,检测波长285 nm和320 nm。结果:方法学验证结果表明日内、日间精密度RSD均小于9.47%,准确度RE均在-9.69%~4.18%之间,稳定性RE为-9.49%~1.33%。药代动力学参数表明,顺式二苯乙烯苷的半衰期较反式二苯乙烯苷长,生物利用度也较反式二苯乙烯苷高。二者在组织中分布广泛,相同给药剂量下各组织中反式二苯乙烯苷的浓度远远大于顺式二苯乙烯苷。结论:该方法专属性好,灵敏度高,简便快捷,适用于小鼠体内顺式二苯乙烯苷和反式二苯乙烯苷的测定。药动学及组织分布结果表明二者体内过程存在较大的差异。 OBJECTIVE: To establish a method for the simultaneous determination of cis-stilbene and trans-stilbene in mice and to compare the pharmacokinetics and tissue distribution. METHODS: Diamonsil C18 column (250 mm × 4.6 mm, 5 μm) was used with mobile phase of acetonitrile-methanol-0.1% glacial acetic acid (11:7:82) at a flow rate of 1.0 mL / , Detection wavelength 285 nm and 320 nm. Results: The validation results showed that the RSD of intra-day and inter-day precision were less than 9.47%, the accuracy REs were between -9.69% and 4.18%, and the stability REs were between -9.49% and 1.33%. Pharmacokinetic parameters show that cis-stilbene glycosides half-life longer than trans stilbene glycosides, bioavailability than trans stilbene glycosides. The two are widely distributed in tissues, and the concentrations of trans stilbene glycosides in all tissues at the same dose are far greater than that of cis-stilbene glycosides. Conclusion: The method is specific, sensitive, simple and quick and suitable for the determination of cis-stilbene and trans-stilbene in mice. Pharmacokinetics and tissue distribution results show that there is a big difference in the process between the two.
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