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Pharmaceutics 2018, 10(3), 87;

Oral Bioavailability of Kinsenoside in Beagle Dogs Measured by LC-MS/MS: Improvement of Ex Vivo Stability of a Lactone-Containing Compound

School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China
Author to whom correspondence should be addressed.
Received: 8 June 2018 / Revised: 5 July 2018 / Accepted: 5 July 2018 / Published: 9 July 2018
(This article belongs to the Special Issue Preclinical Pharmacokinetics and Bioanalysis)
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Kinsenoside (KD), an active compound isolated from Anoectochilus roxburghii, has demonstrated multiple pharmacological activities including hepatoprotection, antihyperliposis, antihyperglycemia, and antiosteoporosis. To the best of our knowledge, there are no available data concerning its preclinical pharmacokinetics and bioavailability in beagle dogs. To support preclinical pharmacokinetic and bioavailability study, a reliable LC-MS/MS method was developed for KD concentration measurements in beagle dog plasma. The chromatographic separation was achieved on a Waters Atlantis® Hilic Silica column with an optimum mobile phase consisting of 5 mM ammonium acetate in water (pH 3.0 adjusted with acetic acid) and acetonitrile at a flow rate of 0.2 mL/min. Mass spectrometric analyses were carried out by monitoring multiple reaction monitoring transitions at m/z 265.2→102.9 for KD and m/z 174.0→128.0 for l-phenyl-d5-alanine-2,3,3-d3 (IS). The stability of KD in beagle dog whole blood and plasma was systematically evaluated. Lowering the temperature played a more critical role in stabilizing KD than decreasing the pH and adding esterase inhibitors, indicating that the major reason for instability of KD was probably due to chemical hydrolysis rather than esterase-mediated degradation. The currently developed method was validated and applied to a pharmacokinetic and bioavailability study of KD in beagle dogs following oral administration at a dose of 3 mg/kg. The absolute oral bioavailability for KD was determined to be 27.6%. Compared with typical glycosides, KD has a better bioavailability and is suitable for developing an oral dosage form. View Full-Text
Keywords: kinsenoside; LC-MS/MS; beagle dog; bioavailability kinsenoside; LC-MS/MS; beagle dog; bioavailability

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Zhang, X.; Jin, M.; Liu, Y.; Chen, Q.; Si, L.; Li, G.; Zhang, Y.; Huang, J. Oral Bioavailability of Kinsenoside in Beagle Dogs Measured by LC-MS/MS: Improvement of Ex Vivo Stability of a Lactone-Containing Compound. Pharmaceutics 2018, 10, 87.

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