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Pharmacokinetics and bioavailability of gelsenicine in mice by UPLC-MS/MS.
Biomed Chromatogr 2019; 33(3):e4418BC

Abstract

Gelsenicine is an indole alkaloid isolated from Gelsemium elegans Benth. In recent years, the role of G. elegans Benth preparations in anti-tumor, analgesic, dilatation and dermatological treatment has attracted attention, and it has been applied clinically, but it is easy to cause poisoning with its use. An UPLC-MS/MS method was established to determine the gelsenicine in mouse blood, and the pharmacokinetics of gelsenicine after intravenous (0.1 mg/kg) and intragastric (0.5 and 1 mg/kg) administration was studied. Deltalin was used as internal standard; a UPLC BEH C18 column was used for chromatographic separation. The mobile phase consisted of acetonitrile and 10 mmol/L ammonium acetate (0.1% formic acid) with a gradient elution flow rate of 0.4 mL/min. Multiple reaction monitoring mode was used for quantitative analysis of gelsenicine in electrospray ionization positive interface. Proteins from mouse blood were removed by acetonitrile precipitation. A validation of this method was performed in accordance with the US Food and Drug Administration guidelines. In the concentration range of 0.05-100 ng/mL, the gelsenicine in the mouse blood was linear (r > 0.995), and the lower limit of quantification was 0.05 ng/mL. In the mouse blood, the intra-day precision RSD was <12%, the inter-day precision RSD was <15%, the accuracy ranged from 89.8 to 112.3%, the average recovery was >76.8%, and the matrix effect was between 103.7 and 108.4%, which meet the pharmacokinetic research requirements of gelsenicine. The UPLC-MS/MS method is sensitive, rapid and selective, and has been successfully applied to the pharmacokinetic study of gelsenicine in mice. The absolute bioavailability of gelsenicine is 1.13%.

Authors+Show Affiliations

Yuhang Branch, Second Affiliated Hospital of Zhejiang University, Hangzhou, China.Analytical and testing Centre, School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou, China.Analytical and testing Centre, School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou, China.Analytical and testing Centre, School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou, China.Analytical and testing Centre, School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou, China.The Laboratory of Clinical Pharmacy, The People's Hospital of Lishui, Lishui, China.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

30367478

Citation

Li, Jianbo, et al. "Pharmacokinetics and Bioavailability of Gelsenicine in Mice By UPLC-MS/MS." Biomedical Chromatography : BMC, vol. 33, no. 3, 2019, pp. e4418.
Li J, Jin Y, Fu H, et al. Pharmacokinetics and bioavailability of gelsenicine in mice by UPLC-MS/MS. Biomed Chromatogr. 2019;33(3):e4418.
Li, J., Jin, Y., Fu, H., Huang, Y., Wang, X., & Zhou, Y. (2019). Pharmacokinetics and bioavailability of gelsenicine in mice by UPLC-MS/MS. Biomedical Chromatography : BMC, 33(3), pp. e4418. doi:10.1002/bmc.4418.
Li J, et al. Pharmacokinetics and Bioavailability of Gelsenicine in Mice By UPLC-MS/MS. Biomed Chromatogr. 2019;33(3):e4418. PubMed PMID: 30367478.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Pharmacokinetics and bioavailability of gelsenicine in mice by UPLC-MS/MS. AU - Li,Jianbo, AU - Jin,Yue, AU - Fu,Huiyan, AU - Huang,Yihui, AU - Wang,Xianqin, AU - Zhou,Yunfang, Y1 - 2018/11/22/ PY - 2018/07/28/received PY - 2018/10/16/revised PY - 2018/10/19/accepted PY - 2018/10/28/pubmed PY - 2019/3/5/medline PY - 2018/10/28/entrez KW - UPLC-MS/MS KW - bioavailability KW - gelsenicine KW - mouse KW - pharmacokinetics SP - e4418 EP - e4418 JF - Biomedical chromatography : BMC JO - Biomed. Chromatogr. VL - 33 IS - 3 N2 - Gelsenicine is an indole alkaloid isolated from Gelsemium elegans Benth. In recent years, the role of G. elegans Benth preparations in anti-tumor, analgesic, dilatation and dermatological treatment has attracted attention, and it has been applied clinically, but it is easy to cause poisoning with its use. An UPLC-MS/MS method was established to determine the gelsenicine in mouse blood, and the pharmacokinetics of gelsenicine after intravenous (0.1 mg/kg) and intragastric (0.5 and 1 mg/kg) administration was studied. Deltalin was used as internal standard; a UPLC BEH C18 column was used for chromatographic separation. The mobile phase consisted of acetonitrile and 10 mmol/L ammonium acetate (0.1% formic acid) with a gradient elution flow rate of 0.4 mL/min. Multiple reaction monitoring mode was used for quantitative analysis of gelsenicine in electrospray ionization positive interface. Proteins from mouse blood were removed by acetonitrile precipitation. A validation of this method was performed in accordance with the US Food and Drug Administration guidelines. In the concentration range of 0.05-100 ng/mL, the gelsenicine in the mouse blood was linear (r > 0.995), and the lower limit of quantification was 0.05 ng/mL. In the mouse blood, the intra-day precision RSD was <12%, the inter-day precision RSD was <15%, the accuracy ranged from 89.8 to 112.3%, the average recovery was >76.8%, and the matrix effect was between 103.7 and 108.4%, which meet the pharmacokinetic research requirements of gelsenicine. The UPLC-MS/MS method is sensitive, rapid and selective, and has been successfully applied to the pharmacokinetic study of gelsenicine in mice. The absolute bioavailability of gelsenicine is 1.13%. SN - 1099-0801 UR - https://www.unboundmedicine.com/medline/citation/30367478/Pharmacokinetics_and_bioavailability_of_gelsenicine_in_mice_by_UPLC_MS/MS_ L2 - https://doi.org/10.1002/bmc.4418 DB - PRIME DP - Unbound Medicine ER -