Rapid determination of isocorydine in rat plasma and tissues using liquid chromatography--tandem mass spectrometry and its applications to pharmacokinetics and tissue distribution.

A rapid and sensitive method for the determination of isocorydine in rat plasma and tissues was developed using liquid chromatography-tandem mass spectrometry (LC-MS/MS). The biological samples were processed by extracting with diethyl ether-dichloromethane (3:2, v/v) and tetrahydropulmatine was used as the internal standard (IS). Detection of the analytes was achieved using positive ion mode electrospray ionization in the multiple reaction monitoring mode. The MS/MS ion transitions monitored were m/z 342.0→279.0 and 356.0→191.9 for isocorydine and IS, respectively. The maximum plasma concentration (C(max) 2496.8 ± 374.4 µg/L) was achieved at 0.278 ± 0.113 h (T(max)) and the half-life (t(1/2)) of isocorydine was 0.906 ± 0.222 h after a 20 mg/kg oral administration. As for a 2 mg/kg intravenous (i.v.) administration, the C(max) and clearance (CL) were 1843.3 ± 338.3 µg/L and 2.381 ± 0.356 L/h/kg, respectively. Based on the AUC(0-∞) obtained from oral and i.v. administration, the absolute bioavailability (F) was estimated as 33.4%. Tissue distribution results indicated that isocorydine underwent a rapid and wide distribution into tissues and it could effectively cross the blood-brain barrier.

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Changchuan Guo, Caihong Yu, Li Li, Yuqing Wang, Shengjia Wang, Weihong Wang, Haihong Hu, Siyun Xu, Lushan Yu, Huidi Jiang, Su Zeng. Rapid determination of isocorydine in rat plasma and tissues using liquid chromatography--tandem mass spectrometry and its applications to pharmacokinetics and tissue distribution. Xenobiotica; the fate of foreign compounds in biological systems. 2012 May;42(5):466-76

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PMID: 22352392

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