Study on pharmacokinetics, tissue distribution, and excretion of phloretin and its prodrug 2′,4′,6′,4-Tetra-O-acetylphloretin in rats using LC–MS/MS

• Autorzy: Wang Libin , Li Xi , Mi Le , Shen Xin , Feng Tian , Liu Xueying , Wang Qingwei

Identyfikatory

DOI

10.1556/1326.2017.00363

• Języki publikacji: EN

Abstrakty

EN

2′,4′,6′,4-Tetra-O-acetylphloretin (TAPHL) is a prodrug of phloretin (PHL) in which the OH groups are protected by acetylation. A validated liquid chromatography–tandem mass spectrometry (LC–MS/MS) method for the determination of PHL in rat biological matrices was developed and applied to investigate and compare the pharmacokinetics, tissue distribution, and excretion of PHL and TAPHL in rats following a single oral administration. 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. The mean pharmacokinetic parameters of tmax, Cmax, AUC(0 − t), CL/F, and t1/2 were observed after oral administration in rats. The data showed that PHL was absorbed and eliminated rapidly from plasma after oral administration. The pharmacokinetic properties are improved, such as the tmax has been prolonged and the area under the curve (AUC) has been enhanced after oral administration of TAPHL to rats. Tissue distribution results indicated that PHL could be rapidly and widely distributed into tissues but could not effectively cross the blood–brain barrier in rats. After oral administration of TAPHL to rats, its tissue distribution to rats was similar as that after oral administration of equimolar PHL. In addition, higher recoveries of PHL following administration of TAPHL indicated that TAPHL might reduce the excretion of PHL from the body by reducing the first pass effect.

Słowa kluczowe

EN

Phloretin; 2′,4′,6′, 4-tetra-O-acetylphloretin; pharmacokinetics; tissue distribution; excretion

• Wydawca: University of Silesia in Katowice ; Akademiai Kiado
• Czasopismo: Acta Chromatographica
• Rocznik: 2019
• Tom: Vol. 31, no. 1
• Strony: 63--70
• Opis fizyczny: Bibliogr. 34 poz., rys.

Twórcy

autor

Wang Libin

• Department of Medicinal Chemistry, School of Pharmacy, Medical University of the Air Force, Xi'an, China

autor

Li Xi

• Department of Pharmacy, Tangdu Hospital, Medical University of the Air Force, Xi'an 710038, China

autor

Mi Le

• Department of Medicinal Chemistry, School of Pharmacy, Medical University of the Air Force, Xi'an, China

autor

Shen Xin

• Department of Medicinal Chemistry, School of Pharmacy, Medical University of the Air Force, Xi'an, China

autor

Feng Tian

• Department of Medicinal Chemistry, School of Pharmacy, Medical University of the Air Force, Xi'an, China

autor

Liu Xueying

• Department of Medicinal Chemistry, School of Pharmacy, Medical University of the Air Force, Xi'an, China

autor

Wang Qingwei

• Department of Pharmacy, Tangdu Hospital, Medical University of the Air Force, Xi'an 710038, China

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Uwagi

PL

Opracowanie rekordu w ramach umowy 509/P-DUN/2018 ze środków MNiSW przeznaczonych na działalność upowszechniającą naukę (2019).