scholarly journals Pharmacokinetics, Tissue Distribution, and Metabolism Study of Icariin in Rat

2017 ◽  
Vol 2017 ◽  
pp. 1-17 ◽  
Author(s):  
Shunjun Xu ◽  
Jiejing Yu ◽  
Jingjing Zhan ◽  
Liu Yang ◽  
Longgang Guo ◽  
...  
Keyword(s):  
Tissue Distribution ◽  
Internal Standard ◽  
Biological Response ◽  
Rat Plasma ◽  
Immune System Diseases ◽  
Liquid Chromatographic Method ◽  
Herba Epimedii ◽  
Distribution Studies ◽  
Liquid Chromatographic

Icariin is one of the predominant flavonoids contained in Herba Epimedii (Yin-yang-huo in Chinese), a well-known Chinese medicine for the treatment of cancers and immune system diseases. Although Herba Epimedii has been widely used in China and there are so many and various research reports on the herbal drug and its main flavones, very limited data is available on the tissue distribution and biotransformation of icariin. In the present study, a liquid chromatographic method combined with electrospray ionization tandem mass spectrometry was developed to quantify the concentration of icariin in rat plasma and various tissues collected at different time points after oral administration of the total flavonoid extract of Herba Epimedii at a dose of 0.69 g/kg (corresponding to 42 mg/g icariin). Biological samples were processed by simple protein precipitation. Genistein was chosen as internal standard. The method was successfully applied to plasma pharmacokinetic and tissue distribution studies of icariin in rat. As a result, it was worth noting that the tissue distribution characteristics of icariin exhibited a significant gender difference. Moreover, in vivo metabolism of icariin was also investigated. A total of 11 potential metabolites were found in rat feces collected in different time periods after oral and intramuscular administration of icariin. In vivo metabolic pathways were involved in hydrolysis, demethylation, oxidation, and conjugation. The preclinical data would be useful for fully understanding in vivo disposition of this compound and interpreting the mechanism of its biological response.

scholarly journals HPLC-MS/MS-Mediated Analysis of the Pharmacokinetics, Bioavailability, and Tissue Distribution of Schisandrol B in Rats

2021 ◽  
Vol 2021 ◽  
pp. 1-12 ◽  
Author(s):  
Dahu Liang ◽  
Zijing Wu ◽  
Yanhao Liu ◽  
Chao Li ◽  
Xianghong Li ◽  
...  
Keyword(s):  
Tissue Distribution ◽  
Oral Bioavailability ◽  
Internal Standard ◽  
Rat Plasma ◽  
Absolute Bioavailability ◽  
Sprague Dawley ◽  
Linear Calibration ◽  
Tissue Homogenates ◽  
Distribution Studies

Schisandrol B, a lignan isolated from dried Schisandra chinensis fruits, has been shown to exhibit hepatoprotective, cardioprotective, renoprotective, and memory-enhancing properties. This study sought to design a sensitive and efficient HPLC-MS/MS approach to measuring Schisandrol B levels in rat plasma and tissues in order to assess the pharmacokinetics, oral bioavailability, and tissue distributions of this compound in vivo. For this analysis, bifendate was chosen as an internal standard (IS). A liquid-liquid extraction (LLE) approach was employed for the preparation of samples that were subsequently separated with an Agilent ZORBAX Eclipse XDB-C18 (4.6 × 150 mm, 5 μm) column with an isocratic mobile phase consisting of methanol and water containing 5 mM ammonium acetate and 0.1% formic acid (90 : 10, v/v). A linear calibration curve was obtained over the 5–2000 ng/mL and 1–1000 ng/mL ranges for plasma samples and tissue homogenates, respectively. This established method was then successfully applied to investigate the pharmacokinetics, oral bioavailability, and tissue distributions of Schisandrol B in Sprague-Dawley (SD) rats that were intravenously administered 2 mg/kg of Schisandrol B monomer, intragastrically administered Schisandrol B monomer (10 mg/kg), or intragastrically administered 6 mL/kg SCE (equivalent to 15 mg/kg Schisandrol B monomer). The oral absolute bioavailability of Schisandrol B following intragastric Schisandrol B monomer and SCE administration was approximately 18.73% and 68.12%, respectively. Tissue distribution studies revealed that Schisandrol B was distributed throughout several tested tissues, with particular accumulation in the liver and kidneys. Our data represent a valuable foundation for future studies of the pharmacologic and biological characteristics of Schisandrol B.

scholarly journals Development and Validation of UPLC-MS/MS Method for the Determination of Aripiprazole in Rat Plasma Using Liquid-Liquid Extraction: Pharmacokinetic and Bioequivalence Application

2020 ◽  
Vol 32 (10) ◽  
pp. 2671-2676
Author(s):  
Ashish Raghuvanshi ◽  
Urooj A. Khan ◽  
Uzma Parveen ◽  
Anshul Gupta ◽  
Gaurav K. Jain
Keyword(s):  
Internal Standard ◽  
Rat Plasma ◽  
Liquid Extraction ◽  
Single Step ◽  
Liquid Liquid Extraction ◽  
Validation Parameters ◽  
Tandem Mass Spectrometric ◽  
Liquid Chromatographic

A selective, simple, sensitive and rapid ultra-performance liquid chromatographic tandem mass spectrometric (UPLC-MS/MS) method for the detection of aripiprazole in rat plasma has been developed and validated using aripiprazole-D8 as internal standard (IS). A simple single step sample preparation process was accomplished by liquid-liquid extraction (LLE). The post-treatment samples were chromato-graphed and analyzed on a UPLC bridged ethyl hybrid (BEH) C-18 column using mobile phase composition of acetonitrile: 0.1% formic acid in water::70:30 (v/v). Aripiprazole was analyzed by MS detector in positive electrospray ionization mode (ESI). Multiple reactions monitoring (MRM) was employed to observed the transition for aripiprazole (m/z 448.35→285.09) and aripiprazole-D8 (m/z 456.2→293.2). The developed method was validated and found linear in the working range of 2-1025 ng/mL with correlation coefficient, r2 = 0.99951 and quantification limit of 2.02 ng/mL. All validation parameters were in accordance with the ICH guidelines and met the acceptance criteria. The method was found to be accurate (recovery, 97.07 to 103.64%, precise (% CV, 2.68 to 7.70%), rapid (run time 4 min) and specific. The validated method was successfully used for the determination of plasma concentration of aripiprazole after single oral administration in rats and hence could be useful for in vivo pharmacokinetic study and bioequivalence testing of aripiprazole formulations.

scholarly journals A Validated HPLC-MS/MS Assay for 14-O-[(4,6-Diaminopyrimidine-2-yl)thioacetyl] Mutilin in Biological Samples and Its Pharmacokinetic, Distribution and Excretion via Urine and Feces in Rats

Molecules ◽  
2019 ◽  
Vol 24 (4) ◽  
pp. 790 ◽  
Author(s):  
Yunxing Fu ◽  
Yu Liu ◽  
Yunpeng Yi ◽  
Jianping Liang ◽  
Qingfeng Wu ◽  
...  
Keyword(s):  
Tissue Distribution ◽  
Matrix Effects ◽  
Limit Of Detection ◽  
Internal Standard ◽  
Pharmacokinetic Profile ◽  
Rat Plasma ◽  
Gram Positive Bacteria ◽  
The Matrix ◽  
Tissue Homogenates

14-O-[(4,6-Diaminopyrimidine-2-yl)thioacetyl] mutilin (DPTM), a novel pleuromutilin candidate with a substituted pyrimidine moiety, has been confirmed to possess excellent antibacterial activity against Gram-positive bacteria. To illustrate the pharmacokinetic profile after intravenous (i.v.), intramuscular (i.m.) and oral (p.o.) administrations with DPTM, as well as tissue distribution and excretion via urine and feces in vivo, a specific, sensitive and robust HPLC-MS/MS method was first developed to determine DPTM in rat plasma, various tissues, urine and feces. The plasma, tissues, urine and feces samples were treated by protein precipitation with acetonitrile using tiamulin fumarate as an internal standard (IS). This method which was achieved on an HPLC system detector equipped with an ESI interface, was sensitive with 5 ng/mL as the lower limit of detection and exhibited good linearity (R2 > 0.9900) in the range of 5–4000 ng/mL for plasma, various tissues, urine and feces, as well as intra-day precision, inter-day precision and accuracy. The matrix effects ranged from 94.2 to 109.7% with RSD ≤ 9.4% and the mean extraction recoveries ranged from 95.4 to 109.5% in plasma, tissue homogenates, urine and feces (RSD ≤ 9.9). After i.v., i.m. and p.o. administrations, DPTM was rapidly absorbed and metabolized in rats with the half-life (t1/2) of 1.70–1.86, 3.23–3.49 and 4.38–4.70 for 10, 25 and 75 mg/kg doses, respectively. The tissue distribution showed that DPTM was diffused into all the tested tissues, especially into the intestine and lung. Excretion via urine and feces studies demonstrated that DPTM was mainly excreted by feces after administration.

scholarly journals Tetrasaccharide iteration synthesis of a heparin-like dodecasaccharide and radiolabelling for in vivo tissue distribution studies

2013 ◽  
Vol 4 (1) ◽  
Author(s):  
Steen U. Hansen ◽  
Gavin J. Miller ◽  
Claire Cole ◽  
Graham Rushton ◽  
Egle Avizienyte ◽  
...  
Keyword(s):  
Tissue Distribution ◽  
Distribution Studies

In vivo levels of diadenosine tetraphosphate and adenosine tetraphospho-guanosine in Physarum polycephalum during the cell cycle and oxidative stress

1986 ◽  
Vol 6 (4) ◽  
pp. 1179-1186
Author(s):  
P N Garrison ◽  
S A Mathis ◽  
L D Barnes
Keyword(s):  
Oxidative Stress ◽  
Cell Cycle ◽  
Physarum Polycephalum ◽  
Fold Increase ◽  
Luciferase Assay ◽  
Diadenosine Tetraphosphate ◽  
Liquid Chromatographic Method ◽  
Different Strains ◽  
Liquid Chromatographic

Cellular levels of diadenosine tetraphosphate (Ap4A) and adenosine tetraphospho-guanosine (Ap4G) were specifically measured during the cell cycle of Physarum polycephalum by a high-pressure liquid chromatographic method. Ap4A was also measured indirectly by a coupled phosphodiesterase-luciferase assay. No cell cycle-specific changes in either Ap4A or Ap4G were detected in experiments involving different methods of assay, different strains of P. polycephalum, or different methods of fixation of macroplasmodia. Our results on Ap4A are in contrast with those reported previously (C. Weinmann-Dorsch, G. Pierron, R. Wick, H. Sauer, and F. Grummt, Exp. Cell Res. 155:171-177, 1984). Weinmann-Dorsch et al. reported an 8- to 30-fold increase in Ap4A in early S phase in P. polycephalum, as measured by the phosphodiesterase-luciferase assay. We also measured levels of Ap4A, Ap4G, and ATP in macroplasmodia treated with 0.1 mM dinitrophenol. Ap4A and Ap4G transiently increased three- to sevenfold after 1 h and then decreased concomitantly with an 80% decrease in the level of ATP after 2 h in the presence of dinitrophenol. These results do not support the hypothesis that Ap4A is a positive pleiotypic activator that modulates DNA replication, but they are consistent with the hypothesis proposed for procaryotes that Ap4A and Ap4G are signal nucleotides or alarmones of oxidative stress (B.R. Bochner, P.C. Lee, S.W. Wilson, C.W. Cutler, and B.N. Ames, Cell 37:225-232, 1984).

Liquid Chromatographic Method for Identity, Assay, and Content Uniformity of Five Tricyclic Drugs

1985 ◽  
Vol 68 (2) ◽  
pp. 168-171
Author(s):  
Edward G Lovering ◽  
Normand Beaulieu ◽  
Robert C Lawrence ◽  
Roger W Sears
Keyword(s):  
Hydrochloric Acid ◽  
Active Ingredient ◽  
Dilute Hydrochloric Acid ◽  
Chromatographic Method ◽  
Internal Standard ◽  
Peak Height ◽  
Content Uniformity ◽  
Liquid Chromatographic Method ◽  
Liquid Chromatographic ◽  
Better Than

Abstract A liquid chromatographic (LC) procedure has been developed for the assay, content uniformity, and identification of single active ingredient solid and liquid formulations of amitriptyline, chlorpromazine, imipramine, thioridazine, and trifluoperazine. The drugs are extracted from their formulations with methanol or dilute hydrochloric acid, and identified by comparison of retention times with those of known standards; drugs are quantitated against these standards with rf/-norephedrine hydrochloride as the internal standard. The precision of replicate injections is better than 2.5% for peak area and better than 1% for peak height. The precision of triplicate determinations of tablet composites is better than 2.2%.

Liquid Chromatographic Determination of Diazepam in Tablets: Collaborative Study

1985 ◽  
Vol 68 (3) ◽  
pp. 545-546
Author(s):  
Michael Tsougros
Keyword(s):  
Collaborative Study ◽  
Internal Standard ◽  
Chromatographic Determination ◽  
Reverse Phase ◽  
Photometric Detection ◽  
Liquid Chromatographic Method ◽  
Liquid Chromatographic Determination ◽  
The Mean ◽  
Liquid Chromatographic

Abstract A stability indicating liquid chromatographic method for the determination of diazepam in tablets was collaboratively studied by 6 laboratories. The method uses a Cig reverse phase column, a methanolwater mobile phase, p-tolualdehyde as the internal standard, and photometric detection at 254 nm. The collaborators were supplied with a synthetic tablet powder and 3 commercial tablet samples. The mean recovery of diazepam from the synthetic tablet powder was 100.2%. For all samples analyzed, the coefficient of variation was < 1.5%. The method has been adopted official first action.

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