4.6 Article

Study on the pharmacokinetics, tissue distribution and excretion of laurolitsine from Litsea glutinosa in Sprague-Dawley rats

期刊

PHARMACEUTICAL BIOLOGY
卷 59, 期 1, 页码 884-892

出版社

TAYLOR & FRANCIS LTD
DOI: 10.1080/13880209.2021.1944221

关键词

Aporphine alkaloid; LC-MS; MS

资金

  1. Natural Science Foundation of Hainan Province [2019RC208]
  2. Key Research and Development Program of Hainan Province [ZDYF2019157]
  3. Natural Science Foundation of China [81760628]

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This study established a simple, rapid and accurate LC-MS/MS method to determine laurolitsine in different rat samples, and successfully applied it in a pharmacokinetic study. The results described the pharmacokinetics, bioavailability, tissue distribution, and excretion of laurolitsine.
Context Laurolitsine is an aporphine alkaloid and exhibits potent antihyperglycemic and antihyperlipidemic effects in ob/ob mice. Objective To investigate the pharmacokinetics, tissue distribution and excretion of laurolitsine. Materials and methods A LC-MS/MS method was established and validated to determine laurolitsine concentrations in the biological matrix of rats (plasma, tissue homogenate, urine and faeces). 10 Sprague-Dawley (SD) rats were used for plasma exposure study: 5 rats were injected with 2.0 mg/kg of laurolitsine via the tail vein, and the other 5 rats were administered laurolitsine (10.0 mg/kg) by gavage. 25 SD rats used for tissue distribution study and 5 SD rats for urine and faeces excretion study: rats administered laurolitsine (10.0 mg/kg) by gavage. After administered, serial blood, tissue, urine and faeces were collected. Analytical quantification was performed by a previous LC-MS/MS method. The pharmacokinetics, bioavailability, tissue distribution and excretion of laurolitsine were described. Results The pharmacokinetic parameters of oral and intravenous administration with T-max were 0.47 and 0.083 h, t(1/2) were 3.73 and 1.67 h, respectively. Oral bioavailability was as low as 18.17%. Laurolitsine was found at a high concentration in the gastrointestinal tract, liver, lungs and kidneys (26 015.33, 905.12, 442.32 and 214.99 ng/g at 0.5 h, respectively) and low excretion to parent laurolitsine in urine and faeces (0.03 and 1.20% in 36 h, respectively). Conclusions This study established a simple, rapid and accurate LC-MS/MS method to determine laurolitsine in different rat samples and successful application in a pharmacokinetic study.

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