Distribution and Blood Penetration of Hirudin in Various Organs and Tissues of Rabbits With Carotid Artery Injury by Ultraperformance Liquid Chromatography-Tandem Mass Spectrometry

Background: Hirudin is a major active ingredient of the traditional Chinese medicine leech. It has been proved to have good antithrombotic and anticoagulant effects. Objective: To determine the tissue distribution of hirudin and its pharmacokinetics in vivo by ultrahigh performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS). Methods: A total of 21 SPF adult New Zealand rabbits were acclimatized for 1 week, and one was randomly selected as a blank control, while the remaining 18 were randomized to the control group and the model group. The heart, liver, spleen, lung, kidney, brain, plasma, blood vessels, and colon tissues were taken by execution at 1, 3, and 6 h. The samples were assayed using the natural hirudin standard as an external standard. Results: The established UPLC-MS/MS method with good precision, accuracy, recovery, and stability of hirudin proved to be reliable. The correlation between different concentrations of natural hirudin standard and the response value was R 2 ≥ 0.9997. The results of the distribution of various tissues showed that hirudin in the two groups had the highest content in plasma and blood vessels, followed by spleen, lung, and liver tissues, and was weaker in the brain and the heart, and the content of hirudin in the control group was higher than that of the model group, and the difference was statistically significant. Conclusion: The absorption and metabolism of hirudin in rabbits with carotid artery injury mainly acted through vascular tissues and blood, and normal rabbits mainly metabolized it through spleen, lung, and liver.

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A validated UPLC-MS/MS assay tracked hirudin in rabbit tissues: levels were highest in plasma and blood vessels, followed by spleen, lung and liver, and were significantly lower in carotid-injured rabbits than in controls.

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