HPLC‐MS/MS based comparative pharmacokinetics of 12 bioactive components in normal and osteoporosis rats after oral administration of You‐Gui‐Wan

The total flavonoids of Desmodium styracifolium are the flavonoid extracts purified from Desmodii Styracifolii Herba, which has conventionally been used for treating urolithiasis in China. In this study, a sensitive and simple liquid chromatography‐tandem mass spectrometry method was developed to simultaneously determine five active components of the extracts in rat plasma. Chromatographic separation of the analytes (schaftoside, vicenin‐1, vicenin‐2, vicenin‐3, and isovitexin) was performed on an ACQUITY UPLC HSS T3 Column under gradient elution conditions. The calibration curves were linear over ranges from 0.5 to 100 ng/ml for schaftoside, vicenin‐1, vicenin‐2, and vicenin‐3, and 0.2–20 ng/ml for isovitexin. The relative standard deviation of intra‐ and inter‐day precisions were ≤6.8% and ≤8.3%, respectively, and the accuracies (relative error) were within ±7.6%. The recoveries of the analytes ranged between 97.3% and 100.3%, and the matrix effects ranged from 98.6% to 113.8%. The method was successfully applied to the pharmacokinetic studies of the five active ingredients of Desmodium styracifolium, for the first time, in both normal and urolithiasis model rats. Results revealed that the plasma levels of these components were significantly increased under the pathological state. This study provided valuable information facilitating the clinical investigation of this medicine.

Section: Discussionmentioning

confidence: 99%

Comparative pharmacokinetic studies of five C‐glycosylflavones in normal and urolithiasis model rats following administration of total flavonoids from Desmodium styracifolium by liquid chromatography‐tandem mass spectrometry

Chen

Zhang

et al. 2022

“…However, several flavonoids, such as epimedin A, epimedin B, and epimedin C, are similar in structure and polarity, and it is therefore difficult to achieve good separation by the UPLC-UV method. Mass spectrometry has high sensitivity and high selectivity, so the multiple reaction monitoring mode can be used to determine the components from different channels, thus avoiding the interference of other components and making the determination method simple and efficient [20]. In addition, in the analysis of biological samples, the compounds to be determined are often present at very low concentrations, and the quantitative limit of UPLC-QQQ-MS is lower.…”

Section: Discussionmentioning

confidence: 99%

Study on the synergistic and attenuating mechanism of the combination of Epimedium and Ligustri lucidi fructus based on pharmacokinetics

Wang

Cao

Feng

et al. 2022

Epimedium has a wide range of clinical applications; however, there have been numerous reports of adverse reactions in recent years, which has resulted in it being changed from a widely recognized “nontoxic” to a “potentially toxic” traditional Chinese medicine. The combination of Epimedium and Ligustri lucidi fructus is commonly used in the clinic. The purpose of this study was to investigate the pharmacokinetic characteristics of Epimedium and Ligustri lucidi fructus to explore the possible synergism and reduction in toxicity. Based on liquid chromatography tandem mass spectrometry, a method was established for the determination of icariin, epimedin A, epimedin B, epimedin C, baohuoside Ⅰ, and specnuezhenide in biological samples and was successfully applied to study the pharmacokinetics of the drug pair. The results showed that the five flavonoids (specnuezhenide could not be detected) could be rapidly absorbed into the blood, and the second peak time in vivo was earlier after the combination, indicating that the metabolic pathway may be changed. In addition, combination with Ligustri lucidi fructus could significantly reduce the concentration of 5 flavonoids in vivo and increase their elimination rate, which may attenuate their virulence, thus providing a reference for the rational clinical use of Epimedium.

“…There were two different peaks at 0.75 and 2 h, respectively, in the concentration-time curve of GB. This is called the double-peak phenomenon, and it might be due to hepatic-intestinal circulation [41], uneven distribution of P-GP in the gastrointestinal tract [42], or the compatibility of herbal materials [43,44]. This is the first study on the pharmacokinetics of LA in rat plasma, the C max and area under the curve (AUC) were much lower than other analytes except TE and it could not be detected in plasma after 6 h. Just like PA and AL, LA is a monoterpene glycoside isolated from several species of Paeoniae and it has high polarity and low GI absorption (predicted from the structure, lipophilicity, and size of the molecule) which might cause poor bioavailability.…”

Section: Discussionmentioning

confidence: 99%

“…There were two different peaks at 0.75 and 2 h, respectively, in the concentration‐time curve of GB. This is called the double‐peak phenomenon, and it might be due to hepatic‐intestinal circulation [41], uneven distribution of P‐GP in the gastrointestinal tract [42], or the compatibility of herbal materials [43, 44].…”

Section: Discussionmentioning

confidence: 99%

Phytochemical identification of Xiaoer Huanglong Granule and pharmacokinetic study in the rat using its seven major bioactive components

Liu

You

Yang

et al. 2022

Xiaoer Huanglong Granule is the only Chinese Patent Medicine widely used for treating attention deficit hyperactivity disorder. However, not much is known about the bioactive components and pharmacokinetics of Xiaoer Huanglong Granule even after it was successfully introduced into clinical use. This study analyzed the components in the medication and rat plasma after oral administration with the help of the UNIFI platform and Masslynx. A total of 119 and 37 components were detected in the medication and plasma, respectively, using an ultra‐performance liquid chromatography‐tandem mass spectrometer. We established a rapid and sensitive simultaneous determination of one triterpene saponin, three monoterpene glycosides, and three lignans in rat plasma by solid‐phase extraction. The determination was accomplished within 7.50 min via gradient elution. The values of the lower limit of quantitation were validated at 0.08 ng/ml for tenuifolin, 0.8 ng/ml for lactiflorin, 1.828 ng/ml for albiflorin, 2 ng/ml for paeoniflorin, gomisin B, and gomisin D, 10 ng/ml for schisandrin. The results from validations of other methods were all acceptable (relative standard deviation ≤ 14.94%). This is the first report on the identification and pharmacokinetics studies of components in Xiaoer Huanglong Granule. Moreover, the pharmacokinetic behavior of lactiflorin was studied for the first time.