Quantitative determination of D-cystine in mice using LC-MS/MS and its application to the assessment of pharmacokinetics and bioavailability.

Journal: Journal of pharmaceutical analysis
Published Date:

Abstract

Cystine is the primary source material for the synthesis of glutathione. However, the pharmacokinetics and tissue distribution of cystine are largely unknown. A surrogate analyte D-cystine was employed to generate calibration curves for the determination of levels of D-cystine and endogenous cystine in mice by liquid chromatography-tandem mass spectrometry (LC-MS/MS). Validation assessments proved the sensitivity, specificity and reproducibility of the method with a lower limit of quantification (LLOQ) of 5 ng/mL over 5-5000 ng/mL in plasma. The pharmacokinetics of D-cystine were evaluated after administering injections and oral solutions, both of which minimally impacted endogenous cystine levels. The absolute bioavailability of cystine was 18.6%, 15.1% and 25.6% at doses of 25, 50 and 100 mg/kg, respectively. Intravenously injected D-cystine resulted in dramatically high plasma levels with reduced levels in the brain and liver. Intragastrically administered D-cystine resulted in high levels in the plasma and stomach with relatively low levels in the lung, kidney, heart and brain.

Authors

  • Shuning Li
    Jiangsu Province Key Laboratory of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing, Jiangsu, 210009, China.
  • Zhenyao Lu
    Jiangsu Province Key Laboratory of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing, Jiangsu, 210009, China.
  • Li Jiao
    Jiangsu Province Key Laboratory of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing, Jiangsu, 210009, China.
  • Ran Zhang
    Jiangsu Province Key Laboratory of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing, Jiangsu, 210009, China.
  • Yu Hong
    Jiangsu Province Key Laboratory of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing, Jiangsu, 210009, China.
  • Jiye Aa
    Jiangsu Province Key Laboratory of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing, Jiangsu, 210009, China.
  • Guangji Wang
    Jiangsu Province Key Laboratory of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing, Jiangsu, 210009, China.

Keywords

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