Pharmacokinetic studies of phloretin in beagle dogs plasma using LC–MS/MS

• Autorzy: Libin W. , Le M. , Tian F. , Xueying L. , Shengyong Z.

Identyfikatory

DOI

10.1556/1326.2016.00097

• Języki publikacji: EN

Abstrakty

EN

A simple, sensitive, and rapid liquid chromatography–tandem mass spectrometry (LC–MS/MS) method has been developed and validated for determination of phloretin in dog plasma using darunavir as internal standard. The phloretin was separated by the Inertsil® ODS3 C18 column (150 mm × 4.6 mm, 5 μm) and determined by LC–MS/MS. The electrospray ionization (ESI) source was operated in negative ionization mode for phloretin and positive ionization mode for darunavir (internal standard, IS). The multiple reaction monitoring (MRM) transitions were chosen to be m/z 273.0 → m/z 148.9 for phloretin, m/z 443.2 → m/z 401.0 for 2′,4′,6′,4-tetra-acetylphloretin and m/z 548.1 → m/z 69.1 for IS. The method was validated for accuracy, precision, linearity, range, selectivity, lower limit of quantification (LLOQ), recovery, and matrix effect. All validation parameters met the acceptance criteria according to regulatory guidelines. 2′,4′,6′,4-Tetra-acetylphloretin, as a prodrug of phloretin, is more stable than phloretin (PH) in vitro, protecting phenolic hydroxy from being oxygenated. The method had been successfully applied to a pharmacokinetic study of administration of phloretin and 2′,4′,6′,4-tetra-acetylphloretin in beagle dogs. Significant differences of tmax, Cmax, and area under the plasma concentration curve (AUC) were observed between phloretin and 2′,4′,6′,4-tetra-acetylphloretin.

Słowa kluczowe

EN

Phloretin; 2′4′6′4-tetra-acetylphloretin; Pharmacokinetic; LC–MS/MS

• Wydawca: University of Silesia in Katowice ; Akademiai Kiado
• Czasopismo: Acta Chromatographica
• Rocznik: 2017
• Tom: Vol. 29, no. 4
• Strony: 443--447
• Opis fizyczny: Bibliogr. 35 poz., rys., tab.

Twórcy

autor

Libin W.

• College of Science, Northwest A&F University, Yangling, Shaanxi 712100, China

autor

Le M.

• Department of Medicinal Chemistry, School of Pharmacy, Fourth Military Medical University, Xi'an, China

autor

Tian F.

• Department of Medicinal Chemistry, School of Pharmacy, Fourth Military Medical University, Xi'an, China

autor

Xueying L.

• Department of Medicinal Chemistry, School of Pharmacy, Fourth Military Medical University, Xi'an, China

autor

Shengyong Z.

• College of Science, Northwest A&F University, Yangling, Shaanxi 712100, China

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Uwagi

PL

Opracowanie rekordu w ramach umowy 509/P-DUN/2018 ze środków MNiSW przeznaczonych na działalność upowszechniającą naukę (2018).