Validated UPLC-MS/MS method for quantification of seven compounds in rat plasma and tissues: Application to pharmacokinetic and tissue distribution studies in rats after oral administration of extract ofEclipta prostrataL.

2018 ◽  
Vol 32 (6) ◽  
pp. e4191 ◽  
Author(s):  
Guangyan Du ◽  
Lingling Fu ◽  
Jun Jia ◽  
Xu Pang ◽  
Haiyang Yu ◽  
...  
Keyword(s):  
Oral Administration ◽  
Tissue Distribution ◽  
Rat Plasma ◽  
Distribution Studies

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 Quantitative determination of monotropein in rat plasma and tissue by LC–MS/MS and its application to pharmacokinetic and tissue distribution studies

2018 ◽  
Vol 28 (4) ◽  
pp. 451-456 ◽  
Author(s):  
Qiang Zhou ◽  
He Yan ◽  
Rui Li ◽  
Xingliang Li ◽  
Jingyan Wei
Keyword(s):  
Quantitative Determination ◽  
Tissue Distribution ◽  
Rat Plasma ◽  
Distribution Studies

Pharmacokinetics and brain distribution studies of 6-hydroxykynurenic acid and its structural modified compounds

2021 ◽  
Author(s):  
Zhuowei Shen ◽  
Haihong Hu ◽  
Jie Pan ◽  
Mingcheng Xu ◽  
Fengting Ou ◽  
...  
Keyword(s):  
Oral Administration ◽  
Brain Homogenate ◽  
Ultra Performance Liquid Chromatography ◽  
Rat Plasma ◽  
Isopropyl Ester ◽  
Brain Distribution ◽  
Apparent Permeability ◽  
Apparent Permeability Coefficient ◽  
Distribution Studies ◽  
The Brain

Abstract Objectives 6-Hydroxykynurenic acid (6-HKA) is an organic acid component in extracts of Ginkgo biloba leaves and acts as a major contributor to neurorestorative effects, while its oral bioavailability was low. Therefore, using prodrug method to improve the bioavailability and brain content of 6-HKA is significant. Methods Three structural modified compounds of 6-HKA were synthesized, and ultra performance liquid chromatography-tandem mass spectrometry methods for quantification of these structural modified compounds in rat plasma and rat brain homogenate were established and comprehensively validated. The methods were effectively applied to investigate the effects of structural modification on apparent permeability coefficients in cells, the pharmacokinetics and the brain distribution in rats. Key findings The results illustrated that esterification can greatly improve the apparent permeability coefficient and bioavailability of 6-HKA. Comparing with direct oral administration of 6-HKA, the bioavailability of isopropyl ester was greatly improved (from 3.96 ± 1.45% to 41.8 ± 15.3%), and the contents of 6-HKA in rat brains (49.7 ± 9.2 ng/g brain) were significantly higher after oral administration. Conclusions The bioavailability and the brain content of 6-HKA can be improved by the prodrug method. Among three structural modified compounds, isopropyl-esterified 6-HKA was the most promising treatment.

Quantification of rosiglitazone in rat plasma and tissues via LC‐MS/MS ‐ method development, validation, and its application in pharmacokinetic and tissue distribution studies

2022 ◽  
Author(s):  
Kusuma Kumari Garikapati ◽  
Ammu V. V. V. Ravi Kiran ◽  
Praveen Thaggikuppe Krishnamurthy ◽  
Narenderan S. T ◽  
Babu. B ◽  
...  
Keyword(s):  
Tissue Distribution ◽  
Method Development ◽  
Rat Plasma ◽  
Distribution Studies

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 Pharmacokinetics, Tissue Distribution and Excretion of a Novel Diuretic (PU-48) in Rats

Pharmaceutics ◽  
2018 ◽  
Vol 10 (3) ◽  
pp. 124 ◽  
Author(s):  
Zhi-Yuan Zhang ◽  
Hua Zhang ◽  
Dan Liu ◽  
Ying-Yuan Lu ◽  
Xin Wang ◽  
...  
Keyword(s):  
Oral Administration ◽  
Tissue Distribution ◽  
High Performance ◽  
Peak Plasma ◽  
Plasma Concentrations ◽  
Area Under The Curve ◽  
Pharmacokinetic Profile ◽  
Rat Plasma ◽  
Drug Candidate ◽  
Liquid Chromatography Tandem Mass

Methyl 3-amino-6-methoxythieno [2,3-b] quinoline-2-carboxylate (PU-48) is a novel diuretic urea transporter inhibitor. The aim of this study is to investigate the profile of plasma pharmacokinetics, tissue distribution, and excretion by oral dosing of PU-48 in rats. Concentrations of PU-48 within biological samples are determined using a validated high performance liquid chromatography-tandem mass spectrometry (LC-MS/MS) method. After oral administration of PU-48 (3, 6, and 12 mg/kg, respectively) in self-nanomicroemulsifying drug delivery system (SNEDDS) formulation, the peak plasma concentrations (Cmax), and the area under the curve (AUC0–∞) were increased by the dose-dependent and linear manner, but the marked different of plasma half-life (t1/2) were not observed. This suggests that the pharmacokinetic profile of PU-48 prototype was first-order elimination kinetic characteristics within the oral three doses range in rat plasma. Moreover, the prototype of PU-48 was rapidly and extensively distributed into thirteen tissues, especially higher concentrations were detected in stomach, intestine, liver, kidney, and bladder. The total accumulative excretion of PU-48 in the urine, feces, and bile was less than 2%. This research is the first report on disposition via oral administration of PU-48 in rats, and it provides important information for further development of PU-48 as a diuretic drug candidate.

scholarly journals Determination of Epimedin B in Rat Plasma and Tissue by LC-MS/MS: Application in Pharmacokinetic and Tissue Distribution Studies

2017 ◽  
Vol 2017 ◽  
pp. 1-9 ◽  
Author(s):  
Qianru Feng ◽  
Shunjun Xu ◽  
Jiejing Yu ◽  
Shuai Sun ◽  
Liu Yang
Keyword(s):  
Tissue Distribution ◽  
Rat Plasma ◽  
Precipitation Method ◽  
Tissue Homogenate ◽  
Spectrometric Method ◽  
Female Rat ◽  
Mass Spectrometric Method ◽  
Tandem Mass Spectrometric ◽  
Distribution Studies

A simple, sensitive, and specific liquid chromatography tandem mass-spectrometric method was developed and validated for the determination of epimedin B in rat plasma and tissue samples. After being processed with a protein precipitation method, these samples were separated on an Agilent Eclipse XDB-C18 column with an isocratic mobile phase consisting of acetonitrile and 0.1% formic acid aqueous solution (32 : 68, v/v). The calibration curve of epimedin B was linear over the concentration range from 1 to 500 ng/mL in plasma and tissue homogenate. The method was then applied to pharmacokinetic and tissue distribution studies after a single oral administration of Herba Epimedii extract to SD rats. Results showed that epimedin B reached the plasma peak concentration at 0.4 h and the terminal elimination half-life was 1.6 h in rat plasma, and the plasma area under the curve from time zero to infinity (AUC0–∞) was 14.35 μg/L·h. The concentration distribution of epimedin B in rat tissue was in the following order: liver > ovary > womb > lung > kidney > spleen > heart > brain, indicating that the compound could be widely distributed in rat, and the reproductive system may be the principal target of epimedin B for female rat.

scholarly journals Determination of Oxaliplatin by a UHPLC-MS/MS Method: Application to Pharmacokinetics and Tongue Tissue Distribution Studies in Rats

2021 ◽  
Vol 15 (1) ◽  
pp. 52
Author(s):  
Xiuqing Gao ◽  
Robert Y. L. Tsai ◽  
Jing Ma ◽  
Yang Wang ◽  
Xiaohua Liu ◽  
...  
Keyword(s):  
Tissue Distribution ◽  
Lower Limit ◽  
Limit Of Detection ◽  
Rat Plasma ◽  
Patch Application ◽  
Icp Ms ◽  
Platinum Based Chemotherapy ◽  
Limit Of Quantitation ◽  
Distribution Studies

Oxaliplatin (OXP), a third-generation platinum-based chemotherapy drug, was often indirectly analyzed via total platinum by an ICP-MS because it was difficult to directly quantify using an LC-MS/MS method, due to its instability, bad column separability and severe MS signal inhibition. Here, we developed and validated a specific, sensitive and reproducible LC-MS/MS method for the quantification of OXP itself in rat plasma and tongue tissue on a SCIEX 4000 QTRAP® MS/MS system equipped with a Phenomenex Lux 5u Cellulose-1 column (250 × 4.6 mm, 5 μm). This method was validated at the lower limit of detection (LOD) and the lower limit of quantitation (LLOQ) of 5 ng/mL and 10 ng/mL, with linearity of 10–5000 ng/mL (r2 > 0.99) and 10–2500 ng/mL (r2 > 0.99), in rat plasma and tongue homogenates, respectively. The intra- and inter-day precision (CV%) and accuracy (RE%) were within 15% for LLOQ, low-, medium- and high-quality control samples. The mean extraction recoveries were around 50% and 80% for plasma and tongue homogenates, respectively. This assay was successfully applied to pharmacokinetics study following intravenous administration of OXP, as well as tongue tissue distribution after 1 h and 4 h of a novel oral mucosal patch application.

Antileishmanial Activity, Pharmacokinetics and Tissue Distribution Studies of Mannose Grafted Piperine Lipid Nano Spheres

Planta Medica ◽  
2010 ◽  
Vol 76 (05) ◽  
Author(s):  
PR Veerareddy ◽  
V Vobalaboina ◽  
N Ali
Keyword(s):  
Tissue Distribution ◽  
Antileishmanial Activity ◽  
Distribution Studies
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