Determination of bergenin in human plasma after oral administration by HPLC‐MS/MS method and its pharmacokinetic study

Abstract

A highly sensitive, simple and selective high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method was developed and applied to the determination of bergenin concentration in human plasma. Bergenin and the internal standard (IS) thiamphenicol in plasma were extracted with ethyl acetate, separated on a C(18 )reversed-phase column, eluted with mobile phase of acetonitrile-water, ionized by negative ion pneumatically assisted electrospray and detected in the multi-reaction monitoring mode using precursor --> product ions of m/z 327.1 --> 192 for bergenin and 354 --> 185.1 for the IS, respectively. The linear range of the calibration curve for bergenin was 0.25-60 ng mL(-1), with the lowest limit of quantification of 0.25 ng mL(-1), and the intra/inter-day relative standard deviation (RSD) was less than 10%. The method is suitable for the determination of low bergenin concentration in human plasma after therapeutic oral doses, and has been first and successfully used for its pharmacokinetic studies in healthy Chinese volunteers.

Simultaneous Quantification of Bergenin, (+)-Catechin, Gallicin and Gallic acid; and Quantification of β-Sitosterol using HPTLC from Bergenia ciliata (Haw.) Sternb. Forma ligulata Yeo (Pasanbheda)

“…bergenin, gallic acid, catechin and gallicin, further the quantification of -Sitosterol is also reported for the first time from this plant. Shi et al [36] and Wang et al [37] developed and reported the methods for determination and pharmacokinetic study of bergenin in biological fluid i.e. rat plasma by RP-HPLC method and Nunomura et al [38] also reported the determination of bergenin by RP-HPLC method.…”

Diversity, pharmacology and synthesis of bergenin and its derivatives: Potential materials for therapeutic usages

“…The blood samples from healthy volunteers were collected at different intervals after oral administration of 250 mg of bergenin. The maximum concentration of 66.6 ng/mL occurred at 2.0 ± 0.9 h and the elimination half-time was 3.7 ± 2.4 h. HPLC-MS/MS method was used by Wang et al to determine bergenin in human plasma [211]. This method was found to be suitable for the determination of low bergenin concentration (lowest limit of quantification = 0.25 ng/mL) in human plasma after oral administration of bergenin tablet (250 mg) and pharmacokinetic parameters (absorption half life = 0.852 h, time to peak concentration = 2.125 h, maximum plasma concentration = 15.915 ng/mL, elimination half life = 4.198 h etc.)…”

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“…Wang et al have also developed a highly sensitive, simple and selective high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method and applied to the determination of bergenin concentration in human plasma 65 . Bergenin and the internal standard (IS) thiamphenicol in plasma were extracted with ethyl acetate and separated on a C 18 reversed-phase column.…”