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Xenobiotica
the fate of foreign compounds in biological systems
Volume 48, 2018 - Issue 1
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Animal Pharmacokinetics and Metabolism

Pharmacokinetics and tissue distribution of crotonoside

, , &
Pages 28-36 | Received 29 Sep 2016, Accepted 20 Dec 2016, Published online: 19 Jan 2017
 

Abstract

1. Crotonoside is a bioactive ingredient from Croton Herba with a strong antitumour activity. This study aimed to develop a highly sensitive and selective high-performance liquid chromatography (HPLC) method to quantify crotonoside in biological samples for pharmacokinetics and distribution studies.

2. Protein precipitation by perchloric acid was used to separate crotonoside from the biological samples, and the recovery rates for crotonoside and the internal standard (luteoloside) were  >80%. All calibration curves examining the crotonoside levels in plasma and tissues were linear (all correlation coefficients > 0.99).

3. The response to crotonoside appeared to be dose disproportional to the maximum plasma concentration and the area under the time–concentration curve in plasma over the range of 12.5–50.0 mg/kg, and crotonoside was highly distributed in tissues after intravenous administration. The highest crotonoside level was detected in the liver (28.79 ± 14.96 μg/g), whereas crotonoside was undetected in the brain.

Declaration of interest

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of this article.

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