Abstract:Significant changes in pharmacokinetic parameters of EP, PEP and MEP were observed after oral administration with different combinations. The pharmacokinetic results reported here might provide reference for clinical usage of Ephedra alkaloids.
“…Therefore, a comparison with previous reports relevant to this study was necessary. The mean T max and t 1/2 of ephedrine reported in previous studies were 0.29-3.08 and 1.00-9.76 h, respectively [21][22][23][24][25]. The T max and t 1/2 of ephedrine obtained after the oral administration of SCRT were 0.85 ± 0.22 and 1.62 ± 0.74 h, respectively, within the range of the previously reported values.…”
The purpose of this study was to investigate the pharmacokinetic properties of ephedrine, paeoniflorin, and cinnamic acid after single or multiple doses of Socheongryong-tang (SCRT) were administered to rats, and to present an example of the pharmacokinetic changes following multiple doses of an herbal medicine. SCRT is a traditional herbal medicine that has been used clinically for a long time, and its main ingredients include ephedrine, paeoniflorin, and cinnamic acid. However, studies on the pharmacokinetic properties of SCRT are insufficient, and particularly, no pharmacokinetic information has been reported for multiple doses. In this study, SCRT was administered orally to rats once or multiple times, and plasma sampled at different times was quantitatively analyzed for ephedrine, paeoniflorin, and cinnamic acid using ultra-high-performance liquid chromatography-tandem mass spectrometry. There was a difference between the pharmacokinetic parameter values of each component (especially in paeoniflorin and cinnamic acid) obtained after single or multiple doses of SCRT. The actual observed values of each component obtained after multiple doses of SCRT were clearly different from the predicted results of multiple-dose simulations based on the pharmacokinetic profiles obtained after a single dose. The results confirmed that the plasma concentrations and, thus, exposures to paeoniflorin and cinnamic acid were significantly increased when SCRT was administered multiple times, whereas that of ephedrine was not. The results of this study are expected to provide useful pharmacokinetic data for the safety and efficacy evaluation of SCRT in the future and demonstrate the necessity of pharmacokinetic comparison studies according to single or multiple oral administrations of herbal medicines.
“…Therefore, a comparison with previous reports relevant to this study was necessary. The mean T max and t 1/2 of ephedrine reported in previous studies were 0.29-3.08 and 1.00-9.76 h, respectively [21][22][23][24][25]. The T max and t 1/2 of ephedrine obtained after the oral administration of SCRT were 0.85 ± 0.22 and 1.62 ± 0.74 h, respectively, within the range of the previously reported values.…”
The purpose of this study was to investigate the pharmacokinetic properties of ephedrine, paeoniflorin, and cinnamic acid after single or multiple doses of Socheongryong-tang (SCRT) were administered to rats, and to present an example of the pharmacokinetic changes following multiple doses of an herbal medicine. SCRT is a traditional herbal medicine that has been used clinically for a long time, and its main ingredients include ephedrine, paeoniflorin, and cinnamic acid. However, studies on the pharmacokinetic properties of SCRT are insufficient, and particularly, no pharmacokinetic information has been reported for multiple doses. In this study, SCRT was administered orally to rats once or multiple times, and plasma sampled at different times was quantitatively analyzed for ephedrine, paeoniflorin, and cinnamic acid using ultra-high-performance liquid chromatography-tandem mass spectrometry. There was a difference between the pharmacokinetic parameter values of each component (especially in paeoniflorin and cinnamic acid) obtained after single or multiple doses of SCRT. The actual observed values of each component obtained after multiple doses of SCRT were clearly different from the predicted results of multiple-dose simulations based on the pharmacokinetic profiles obtained after a single dose. The results confirmed that the plasma concentrations and, thus, exposures to paeoniflorin and cinnamic acid were significantly increased when SCRT was administered multiple times, whereas that of ephedrine was not. The results of this study are expected to provide useful pharmacokinetic data for the safety and efficacy evaluation of SCRT in the future and demonstrate the necessity of pharmacokinetic comparison studies according to single or multiple oral administrations of herbal medicines.
“…Moreover, the compound concentrations in the small intestine and stomach in the GU rat were higher than those in normal rats in the order of baicalin > wogonoside > saikosaponin a > glycyrrhizic acid > baicalein > berberine hydrochloride > liquiritin > saikosaponin d. Baicalin was also widely and rapidly distributed in the liver. 33 For both groups, the peak concentration appeared at 0.5 hours in the stomach and small intestine, followed by a gradual decline until the last time point measured. In the liver, the peak concentration of baicalin appeared at 0.5 hours in the normal group and 1 hour for the GU group.…”
Gastric ulcer (GU) is one of the major gastrointestinal disorder diseases, with increasing incidence and prevalence globally. Modified Xiaochaihu granules (MXCHG) have been used effectively for treating chronic gastritis and GU clinically. To investigate the pharmacokinetics and tissue distribution of MXCHG, an ultraperformance liquid chromatography-electrospray ionization-tandem mass spectrometry (UPLC-ESI-MS/MS) method was established for the simultaneous determination of 8 bioactive ingredients (baicalin, wogonoside, baicalein, liquiritin, glycyrrhizic acid, berberine hydrochloride, saikosaponin a, and saikosaponin d) in rat plasma and various tissues using puerarin as an internal standard (IS). The biological samples were pretreated by protein precipitation with acetonitrile. The chromatographic separation was carried out on a C18 column with a gradient mobile phase consisting of acetonitrile and 0.1% formic acid in water. All analytes and IS were quantitated through ESI in the positive/negative ion multiple reaction monitoring mode. The mass transitions were as follows: m/z 445.0 → 268.5 for baicalin, m/z 458.7 → 282.8 for wogonoside, m/z 269.2 → 222.6 for baicalein, m/z 417.0 → 254.8 for liquiritin, m/z 822.1 → 350.8 for glycyrrhizic acid, m/ z 336.0 → 319.9 for berberine hydrochloride, m/z 780.3 → 618.5 for saikosaponin, and m/z 415.0 → 294.6 for the IS. The validated method was successfully applied to the pharmacokinetics and tissue distribution study of 8 compounds in rat plasma and tissues after the intragastric administration of MXCHG. The results demonstrated that 8 components were distributed widely and rapidly in various rat tissues after intravenous administration. Tissue deposition of the compounds in the rats was mainly in the small intestine and stomach. The present study can provide more useful information to guide the clinical use of MXCHG and the developed analytical method can also be applied for further clinical pharmacokinetic studies.
“…The liquorice promoted the absorption of peoniflorin in peony and enhanced its concentration 14 . Glycyrrhizic acid increased AUC of some alkaloids 15 .Figure 1Structure of GA, KL, CA and BB (from A – D ).…”
A simple validated high performance liquid chromatography method was developed for the evaluation of the effect of three kinds of active ingredients in traditional Chinese medicine (TCM) on the pharmacokinetics of glycyrrhetinic acid (GA),a kind of active component from the most commonly used TCM licorice. Our results revealed that all of the calibration curves displayed good linearity. Intra- and inter-day precision for GA ranged from 2.54 to 3.98% and from 4.95 to 7.08%, respectively. The recovery rates for GA were determined to be 96.3–106.4%. All the samples showed satisfactory precision and accuracy in various stability tests. Plasma pharmacokinetic parameters including area under the concentration-time curve (AUC), elimination half-life (t
1/2
), time to peak concentration(T
max
) and peak concentration C
max
were calculated. No significant difference was found as compared the groups administrating GA with and without other ingredients from TCM.
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