Confirming oral bioavailability of novel oestradiol analogues by liquid chromatography-tandem mass spectrometry in a murine model

2018 ◽  
Vol 29 (17) ◽  
Author(s):  
Mothibeli KT ◽  
Mercier AE ◽  
Cromarty AD ◽  
Rheeder M ◽  
Naidoo V ◽  
...  
Molecules ◽  
2019 ◽  
Vol 24 (11) ◽  
pp. 2037 ◽  
Author(s):  
Subindra Kazi Thapa ◽  
Mahesh Upadhyay ◽  
Tae Hwan Kim ◽  
Soyoung Shin ◽  
Sung-Joo Park ◽  
...  

Desoxo-narchinol A is one of the major active constituents from Nardostachys jatamansi, which has been reported to possess various pharmacological activities, including anti-inflammatory, antioxidant, and anticonvulsant activity. A simple and sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the quantification of desoxo-narchinol A in two different biological matrices, i.e., rat plasma and mouse plasma, using sildenafil as an internal standard (IS). The method involved simple protein precipitation with acetonitrile and the analyte was separated by gradient elution using 100% acetonitrile and 0.1% formic acid in water as a mobile phase. The MS detection was performed with a turbo electrospray in positive ion mode. The lower limit of quantification was 10 ng/mL in both rat and mouse plasma. Intra- and inter-day accuracies were in the ranges of 97.23–104.54% in the rat plasma and 95.90–110.11% in the mouse plasma. The precisions were within 8.65% and 6.46% in the rat and mouse plasma, respectively. The method was applied to examine the pharmacokinetics of desoxo-narchinol A, and the oral bioavailability of desoxo-narchinol A was 18.1% in rats and 28.4% in mice. The present results may be useful for further preclinical and clinical studies of desoxo-narchinol A.


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