scholarly journals Pharmacokinetic Changes According to Single or Multiple Oral Administrations of Socheongryong-Tang to Rats: Presented as a Typical Example of Changes in the Pharmacokinetics Following Multiple Exposures to Herbal Medicines

Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 478
Author(s):  
Seung-Hyun Jeong ◽  
Ji-Hun Jang ◽  
Da-Hwa Jung ◽  
Guk-Yeo Lee ◽  
Yong-Bok Lee
Keyword(s):  
Herbal Medicine ◽  
Cinnamic Acid ◽  
High Performance ◽  
Plasma Concentrations ◽  
Herbal Medicines ◽  
Pharmacokinetic Data ◽  
Efficacy Evaluation ◽  
Multiple Doses ◽  
Pharmacokinetic Properties ◽  
Liquid Chromatography Tandem Mass

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.

scholarly journals Preclinical Pharmacokinetics of Scoparone, Geniposide and Rhein in an Herbal Medicine Using a Validated LC-MS/MS Method

Molecules ◽  
2018 ◽  
Vol 23 (10) ◽  
pp. 2716 ◽  
Author(s):  
Tun-Pin Hsueh ◽  
Tung-Hu Tsai
Keyword(s):  
Bioactive Compounds ◽  
Pharmacokinetic Study ◽  
High Performance ◽  
Low Dose ◽  
Rat Plasma ◽  
Herbal Formula ◽  
Preclinical Pharmacokinetics ◽  
Pharmacokinetic Properties ◽  
Liquid Chromatography Tandem Mass

The herbal formula Yin-Chen-Hao-Tang has been reported to have anti-fibrosis properties. The aim of this study was to reveal the pharmacokinetic characteristics of bioactive compounds in this herbal formula. A new high-performance liquid chromatography-tandem mass spectrometry method was developed and validated for simultaneous determination of scoparone, geniposide and rhein in rat plasma. A pharmaceutical herbal powder was administered to rats at doses of 1 g/kg and 3 g/kg orally. The method showed excellent linearity (r2 > 0.999) and validation was successfully conducted for the pharmacokinetic study. The results show that the Cmax values and areas under the curve of scoparone, geniposide and rhein were higher and not proportional to the dose in rat plasma, while the Tmax and half-life values were consistent in the group that received 1 g/kg. The clearance of the higher dose (3 g/kg) did not decrease proportionally to that of the low dose. The results showed the nonlinear pharmacokinetic properties of scoparone, geniposide and rhein in Yin-Chen-Hao-Tang that suggested possible accumulation of bioactive compounds through oral administration. This pharmacokinetic study reveals that an increased dose of this herbal formula would largely increase the maximum concentration and bioavailability of scoparone, geniposide and rhein.

scholarly journals Determination of Matrine in Rat Plasma after Oral Administration of Novel Korean Herbal Medicine KIOM-MA128 and Application of PK

2015 ◽  
Vol 2015 ◽  
pp. 1-6 ◽  
Author(s):  
Hyun-moon Back ◽  
Byungjeong Song ◽  
Jung-woo Chae ◽  
Hwi-yeol Yun ◽  
Jin Yeul Ma ◽  
...  
Keyword(s):  
Herbal Medicine ◽  
Oral Administration ◽  
High Performance ◽  
Rat Plasma ◽  
Pharmacokinetic Studies ◽  
Chemical Marker ◽  
Chromatography Tandem Mass Spectrometry ◽  
Accuracy And Precision ◽  
Liquid Chromatography Tandem Mass

KIOM-MA128 is a novel Korean herbal medicine with antiatopic, anti-inflammatory, and antiasthmatic effects. Matrine is thought to be a potential chemical marker of KIOM-MA128, but pharmacokinetic studies on KIOM-MA128 had not been performed. This study describes a simple and rapid method using high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) to determine the concentration of matrine in rats plasma after administration of KIOM-MA128. The isocratic mobile phase consisted of methanol and distilled water, and the flow rate was 0.15 mL/min. The accuracy and precision of the assay, as well as stability tests, were performed in accordance with FDA regulations for the validation of bioanalytical methods. The half-life andTmaxof matrine after administration of KIOM-MA128 were 4.29 ± 2.20 h and 1.8 ± 1.23 h, respectively.CmaxandAUCinfof matrine after administration of KIOM-MA128 at 4 g/kg and 8 g/kg were 595.10 ± 182.91 ng/mL, 5336.77 ± 1503.84 ng/mL·h and 850.46 ± 120 ng/mL, 9583.10 ± 888.92 ng/mL·h, respectively. The validated method was successfully applied to a pharmacokinetic study in rats after oral administration of KIOM-MA128.

scholarly journals Pharmacokinetic Properties of Sulfadoxine-Pyrimethamine in Pregnant Women

2009 ◽  
Vol 53 (10) ◽  
pp. 4368-4376 ◽  
Author(s):  
Harin A. Karunajeewa ◽  
Sam Salman ◽  
Ivo Mueller ◽  
Francisca Baiwog ◽  
Servina Gomorrai ◽  
...  
Keyword(s):  
High Performance ◽  
Plasma Concentrations ◽  
Population Pharmacokinetic ◽  
Third Trimester ◽  
Presumptive Treatment ◽  
Time Curve ◽  
Population Pharmacokinetic Modeling ◽  
Pharmacokinetic Properties ◽  
Intermittent Presumptive Treatment ◽  
Papua New Guinean

ABSTRACT To determine the pharmacokinetic disposition of sulfadoxine (SDOX) and pyrimethamine (PYR) when administered as intermittent presumptive treatment during pregnancy (IPTp) for malaria, 30 Papua New Guinean women in the second or third trimester of pregnancy and 30 age-matched nonpregnant women were given a single dose of 1,500 mg of SDOX plus 75 mg of pyrimethamine PYR. Blood was taken at baseline and 1, 2, 4, 6, 12, 18, 24, 30, 48, and 72 h and at 7, 10, 14, 28, and 42 days posttreatment in all women. Plasma samples were assayed for SDOX, N-acetylsulfadoxine (NASDOX), and PYR by high-performance liquid chromatography. Population pharmacokinetic modeling was performed using NONMEM v6.2.0. Separate user-defined mamillary models were fitted to SDOX/NASDOX and PYR. When the covariate pregnancy was applied to clearance, there was a significant improvement in the base model for both treatments. Pregnancy was associated with a significantly lower area under the concentration-time curve from 0 to ∞ for SDOX (22,315 versus 33,284 mg·h/liter), NASDOX (801 versus 1,590 mg·h/liter), and PYR (72,115 versus 106,065 μg·h/liter; P < 0.001 in each case). Because lower plasma concentrations of SDOX and PYR could compromise both curative efficacy and posttreatment prophylaxis in pregnant patients, IPTp regimens incorporating higher mg/kg doses than those recommended for nonpregnant patients should be considered.

scholarly journals New Colistin Population Pharmacokinetic Data in Critically Ill Patients Suggesting an Alternative Loading Dose Rationale

2014 ◽  
Vol 58 (12) ◽  
pp. 7324-7330 ◽  
Author(s):  
N. Grégoire ◽  
O. Mimoz ◽  
B. Mégarbane ◽  
E. Comets ◽  
D. Chatelier ◽  
...  
Keyword(s):  
Steady State ◽  
Critically Ill ◽  
Critically Ill Patients ◽  
Plasma Concentrations ◽  
Multidrug Resistant ◽  
Pharmacokinetic Analysis ◽  
Population Pharmacokinetic ◽  
Pharmacokinetic Data ◽  
Loading Dose ◽  
Liquid Chromatography Tandem Mass

ABSTRACTColistin is an old antibiotic that has recently gained a considerable renewal of interest as the last-line defense therapy against multidrug-resistant Gram-negative bacteria. It is administered as colistin methanesulfonate (CMS), an inactive prodrug, and it was shown that due to slow CMS conversion, colistin plasma concentrations increase very slowly after treatment initiation, which constitutes the rationale for a loading dose in critically ill patients. However, faster CMS conversion was observed in healthy volunteers but using a different CMS brand, which may also have a major impact on colistin pharmacokinetics. Seventy-three critically ill patients not undergoing dialysis received multiple doses of CMS. The CMS concentrations were measured by liquid chromatography-tandem mass spectrometry (LC-MS/MS), and a pharmacokinetic analysis was conducted using a population approach. We confirmed that CMS renal clearance and colistin concentrations at steady state are mostly governed by creatinine clearance, but we predict a typical maximum concentration of drug in serum (Cmax) of colistin close to 2 mg/liter, occurring 3 h after an initial dose of 2 million international units (MIU) of CMS. Accordingly, the estimated colistin half-life (t1/2) was relatively short (3.1 h), with rapid attainment of steady state. Our results are only partially consistent with other recently published results. We confirm that the CMS maintenance dose should be adjusted according to renal function in critically ill patients. However, much higher than expected colistin concentrations were observed after the initial CMS dose, with rapid steady-state achievement. These discrepancies challenge the pharmacokinetic rationale for a loading dose, which may still be appropriate for rapid bacterial eradication and an improved clinical cure rate.

scholarly journals Effects of a non-steroidal aromatase inhibitor on ovarian function in cattle

2012 ◽  
Vol 24 (4) ◽  
pp. 631 ◽  
Author(s):  
M. Jimena Yapura ◽  
Reuben J. Mapletoft ◽  
Jaswant Singh ◽  
Roger Pierson ◽  
Jonathan Naile ◽  
...  
Keyword(s):  
Aromatase Inhibitor ◽  
High Performance ◽  
Ovarian Function ◽  
Plasma Concentrations ◽  
Dominant Follicle ◽  
Follicular Wave ◽  
Chromatography Tandem Mass Spectrometry ◽  
Liquid Chromatography Tandem Mass ◽  
Arrest Growth ◽  
Phosphate Buffered Saline

Effects of the non-steroidal aromatase inhibitor letrozole on ovarian function in cattle were determined. The hypothesis that letrozole would arrest growth of the dominant follicle, resulting in emergence of a new follicular wave at a predictable post-treatment interval, was tested. Heifers were assigned randomly to four groups 4 days after follicular ablation (~2½ days after wave emergence) and given intravenous doses of 500 (n = 9), 250 (n = 10), or 125 µg kg–1 (n = 10) letrozole or phosphate-buffered saline (controls; n = 10). Blood was collected and ovarian structures were monitored daily by transrectal ultrasonography. Plasma concentrations of LH and FSH were measured by radioimmunoassay; plasma concentrations of letrozole were determined by high-performance liquid chromatography tandem mass spectrometry. A single intravenous dose of letrozole did not induce regression of the dominant follicle present at the time of treatment, nor did it directly affect FSH release. Conversely, treatment with letrozole increased endogenous concentrations of LH and extended the lifespan of the dominant follicle, which delayed the next FSH surge and subsequent follicular wave emergence. Letrozole continues to have potential as a non-steroidal treatment for controlling ovarian function in cattle.

scholarly journals Pharmacokinetic Properties of Acetyl Tributyl Citrate, a Pharmaceutical Excipient

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 177 ◽  
Author(s):  
Hyeon Kim ◽  
Min Choi ◽  
Young Ji ◽  
In Kim ◽  
Gi Kim ◽  
...  
Keyword(s):  
Oral Dosage ◽  
Pharmacokinetic Data ◽  
Metabolic Clearance ◽  
Pharmaceutical Excipient ◽  
Pharmacokinetic Properties ◽  
Liquid Chromatography Tandem Mass ◽  
Solid Oral Dosage Forms ◽  
Tandem Mass Spectrometric ◽  
Acetyl Tributyl Citrate ◽  
Oral Dosage Forms

Acetyl tributyl citrate (ATBC) is an (the Food and Drug Administration) FDA-approved substance for use as a pharmaceutical excipient. It is used in pharmaceutical coating of solid oral dosage forms such as coated tablets or capsules. However, the information of ATBC on its pharmacokinetics is limited. The aim of this study is to investigate the pharmacokinetic properties of ATBC using liquid chromatography–tandem mass spectrometric (LC–MS/MS) analysis. ATBC was rapidly absorbed and eliminated and the bioavailability was 27.4% in rats. The results of metabolic stability tests revealed that metabolic clearance may have accounted for a considerable portion of the total clearance of ATBC. These pharmacokinetic data would be useful in studies investigating the safety and toxicity of ATBC.

scholarly journals Desbutyl-Lumefantrine Is a Metabolite of Lumefantrine with PotentIn VitroAntimalarial Activity That May Influence Artemether-Lumefantrine Treatment Outcome

2011 ◽  
Vol 55 (3) ◽  
pp. 1194-1198 ◽  
Author(s):  
Rina P. M. Wong ◽  
Sam Salman ◽  
Kenneth F. Ilett ◽  
Peter M. Siba ◽  
Ivo Mueller ◽  
...  
Keyword(s):  
Confidence Interval ◽  
High Performance ◽  
Geometric Mean ◽  
Artemisinin Combination Therapy ◽  
Parent Compound ◽  
Plasma Concentrations ◽  
Liquid Chromatography Tandem Mass ◽  
The Mean ◽  
The Relationship

ABSTRACTDesbutyl-lumefantrine (DBL) is a metabolite of lumefantrine. Preliminary data fromPlasmodium falciparumfield isolates show greater antimalarial potency than, and synergy with, the parent compound and synergy with artemisinin. In the present study, thein vitroactivity and interactions of DBL were assessed from tritium-labeled hypoxanthine uptake in cultures of the laboratory-adapted strains 3D7 (chloroquine sensitive) and W2mef (chloroquine resistant). The geometric mean 50% inhibitory concentrations (IC50s) for DBL against 3D7 and W2mef were 9.0 nM (95% confidence interval, 5.7 to 14.4 nM) and 9.5 nM (95% confidence interval, 7.5 to 11.9 nM), respectively, and those for lumefantrine were 65.2 nM (95% confidence interval, 42.3 to 100.8 nM) and 55.5 nM (95% confidence interval, 40.6 to 75.7 nM), respectively. An isobolographic analysis of DBL and lumefantrine combinations showed no interaction in either laboratory-adapted strain but mild synergy between DBL and dihydroartemisinin (sums of the fractional inhibitory concentrations of 0.92 [95% confidence interval, 0.87 to 0.98] and 0.94 [95% confidence interval, 0.90 to 0.99] for 3D7 and W2mef, respectively). Using a validated ultra-high-performance liquid chromatography-tandem mass spectrometry assay and 94 day 7 samples from a previously reported intervention trial, the mean plasma DBL was 31.9 nM (range, 1.3 to 123.1 nM). Mean plasma DBL concentrations were lower in children who failed artemether-lumefantrine treatment than in those with an adequate clinical and parasitological response (ACPR) (P= 0.053 versusP> 0.22 for plasma lumefantrine and the plasma lumefantrine-to-DBL ratio, respectively). DBL is more potent than the parent compound and mildly synergistic with dihydroartemisinin. These properties and the relationship between day 7 plasma concentrations and the ACPR suggest that it could be a useful alternative to lumefantrine as a part of artemisinin combination therapy.

scholarly journals Determination of the Novel Insecticide Flupyradifurone and Its Two Metabolites in Traditional Chinese Herbal Medicines Using Modified QuEChERS and High-Performance Liquid Chromatography-Tandem Mass Spectrometry

2020 ◽  
Vol 2020 ◽  
pp. 1-9
Author(s):  
Nan Fang ◽  
Zhou Lu ◽  
Zhongbei Zhang ◽  
Zhiguang Hou ◽  
Shuang Liang ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
High Performance ◽  
Herbal Medicines ◽  
Tandem Mass ◽  
The Novel ◽  
Chinese Herbal ◽  
Chromatography Tandem Mass Spectrometry ◽  
Liquid Chromatography Tandem Mass ◽  
Traditional Chinese Herbal Medicines

In this study, an analytical method for the simultaneous determination of the novel insecticide flupyradifurone and its two metabolites in a variety of traditional Chinese herbal medicines was developed for the first time using high-performance liquid chromatography-tandem mass spectrometry. A simple and efficient method using dispersive solid-phase extraction was employed for the pretreatment of the samples. Several extractions and cleanup strategies were evaluated. The recoveries (n = 15) of flupyradifurone and its metabolites at three spiking levels were in the range 71.3%–101.7%, with corresponding intraday and interday relative standard deviations of 1.1%–14.8%. The limits of quantitation were 0.01 mg/kg for flupyradifurone and 0.1 mg/kg for its two metabolites. Overall, our developed method was sensitive and reliable for the fast screening of flupyradifurone and its two metabolites in traditional Chinese herbal medicine samples.

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