scholarly journals A Simple HPLC Method for the Quantitative Determination of Silybin in Rat Plasma: Application to a Comparative Pharmacokinetic Study on Commercial Silymarin Products

Molecules ◽  
2019 ◽  
Vol 24 (11) ◽  
pp. 2180 ◽  
Author(s):  
Eun-Sol Ha ◽  
Dong-Gyun Han ◽  
Seong-Wook Seo ◽  
Ji-Min Kim ◽  
Seon-Kwang Lee ◽  
...  
Keyword(s):  
Pharmacokinetic Study ◽  
Gradient Elution ◽  
Rat Plasma ◽  
Hplc Method ◽  
Pharmacokinetic Studies ◽  
Active Constituent ◽  
Promising Alternative ◽  
Comparative Pharmacokinetic ◽  
Bioanalytical Method

Silybin (SBN) is a major active constituent of silymarin, a mixture of flavonoids found in fruits and seeds of milk thistle. The aim of this study was to describe a simple bioanalytical method for quantifying SBN in rat plasma. A simple protein deproteinization procedure with acetonitrile (ACN) was employed for plasma sample preparation. A reversed column and gradient elution of a mobile phase (mixture of phosphate buffer (pH 5.0) and ACN) were used for chromatographic separation. The selectivity, linearity (50–5000 ng/mL), precision, accuracy, recovery, matrix effect, and stability for this method were validated as per the current Food and Drug Administration (FDA) guidelines. Our method for SBN was applied to a comparative pharmacokinetic study on four different commercial silymarin products. This in vivo rat study demonstrated that product #4 significantly enhanced the relative oral bioavailability of SBN, as compared to product #1–3. Therefore, the bioanalytical method proposed herein could serve as a promising alternative for preclinical pharmacokinetic studies on silymarin products and, by extension, clinical use after partial modification and validation.

scholarly journals An LC-MS/MS Method for Simultaneous Determination of the Toxic and Active Components of Cortex Periplocae in Rat Plasma and Application to a Pharmacokinetic Study

2019 ◽  
Vol 2019 ◽  
pp. 1-10 ◽  
Author(s):  
Zhen Li ◽  
Yang Li ◽  
Jin Li ◽  
Rui Liu ◽  
Jia Hao ◽  
...  
Keyword(s):  
Oral Administration ◽  
Multiple Reaction Monitoring ◽  
Gradient Elution ◽  
Rat Plasma ◽  
Pharmacokinetic Studies ◽  
Simple Liquid ◽  
Active Components ◽  
Limit Of Quantification ◽  
Liquid Chromatography Tandem Mass

A sensitive and simple liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated to simultaneously determine the toxic and other active components including isovanillin, scopoletin, periplocin, periplogenin, and periplocymarin after oral administration of cortex periplocae extract to rats. Plasma samples were prepared by protein precipitation with methanol. All compounds were separated on a C18 column with gradient elution using acetonitrile and formic acid aqueous solution (0.1%, v/v) as the mobile phase at a flow rate of 0.3 mL/min. The detection of all compounds was accomplished by multiple-reaction monitoring (MRM) in the positive electrospray ionization mode. The LC-MS/MS method exhibited good linearity for five analytes. The lower limit of quantification (LLOQ) was 0.48 ng/mL for scopoletin, periplogenin, and periplocymarin; 2.4 ng/mL for isovanillin and periplocin. The extraction recoveries of all compounds were more than 90% and the RSDs were below 10%. It was found that the absorption of scopoletin and periplocin was rapid in vivo after oral administration of cortex periplocae extract. Furthermore, periplocymarin possessed abundant plasma exposure. The results demonstrated that the validated method was efficiently applied for the pharmacokinetic studies of isovanillin, scopoletin, periplocin, periplogenin, and periplocymarin after oral administration of cortex periplocae extract.

scholarly journals DETERMINATION OF 5H-BENZO[2,3][1,4]OXAZEPINO[5,6-B]INDOLES IN RAT PLASMA BY REVERSED-PHASE HIGH-PERFORMANCE LIQUID CHROMATOGRAPHIC-ULTRAVIOLET METHOD: APPLICATION TO PHARMACOKINETIC STUDIES

2017 ◽  
Vol 10 (12) ◽  
pp. 425 ◽  
Author(s):  
Ashok K Singh ◽  
Vinit Raj ◽  
Amit Rai ◽  
Amit K Keshari ◽  
Pranesh Kumar ◽  
...  
Keyword(s):  
High Performance ◽  
Gradient Elution ◽  
High Performance Liquid Chromatographic ◽  
Rat Plasma ◽  
Reversed Phase ◽  
Pharmacokinetic Studies ◽  
Relative Standard ◽  
Liquid Chromatographic

Objective: Recently, we reported newly synthesized 5H-benzo[2,3][1,4]oxazepino[5,6-b]indole) derivatives and proved their cytotoxicity against hepatocellular carcinoma specific Hep-G2 cell lines. We attempted herein to describe a reversed-phase high-performance liquid chromatographic method for the determination of three most active compounds 6a, 10a, and 15a in rat plasma to predict their pharmacokinetics parameters before in vivo study.Methods: A rapid and sensitive reversed-phase high-performance liquid chromatographic was employed for the determination of 6a, 10a, and 15a in rat plasma. Each compound was separated by a gradient elution of acetonitrile and water with 1 mL/min flow rate. The detector was set at 270, 285, and 275 nm for 6a, 10a, and 15a and the recorded elution times were 2.00, 2.87, and 1.88 min, respectively.Results: The calibration curve was linear with R2 of 0.938, 0.875, and 0.923 over the concentration range of 0.1–50 μg/mL. The inter- and intra-day variations of the assay were lower than 12.26%; the average recovery of 6a, 10a, and 15a was 97.31, 92.56, and 95.23 % with relative standard deviation of 2.12%, 3.25%, and 2.28%, respectively. The Cmax and Tmax were ~ 46.34, 18.56, and 25.65 μg/mL and 2.0, 4.0, and 4.0 h for 6a, 10a, and 15a, respectively, which indicate a robust method of detection in the present experiment.Conclusion: The study suggests that all of the three compounds have a lower rate of absorption, higher volume of distribution, and lower clearance rate, indicating good therapeutic response for in vivo activity. 

scholarly journals Development and Validation of an Ultra-Performance Liquid Chromatography Method for the Determination of Wedelolactone in Rat Plasma and its Application in a Pharmacokinetic Study

Molecules ◽  
2019 ◽  
Vol 24 (4) ◽  
pp. 762
Author(s):  
Qing Chen ◽  
Xiaoxue Wu ◽  
Xuemin Gao ◽  
Hua Song ◽  
Xuan Zhu
Keyword(s):  
Liquid Chromatography ◽  
Pharmacokinetic Study ◽  
Theoretical Basis ◽  
Ultra Performance Liquid Chromatography ◽  
Rat Plasma ◽  
Pharmacokinetic Parameters ◽  
Pharmacokinetic Studies ◽  
Chromatography Method ◽  
Relative Standard

Wedelolactone is a coumarin ether with significant hepatoprotective effects. However, there are few pharmacokinetic studies of wedelolactone, which will affect the studies of its efficacy and potential toxicity. In this study, a selective ultra-performance liquid chromatography (UPLC) method was developed to confirm the pharmacokinetic parameters of wedelolactone in rat plasma. The chromatographic separation was carried out on a Kromasil C18 UPLC column (250 × 4.6 mm; 5.0 μm) by gradient mobile phase of methanol-water containing 0.5% acetic acid (v/v). Perfect linearity was obtained and the samples were stable under different conditions. The intra-day and inter-day precisions (relative standard deviation, %) were within 3.81% and accuracies (relative error, %) ranged from −4.01% to 7.12%. The extraction recoveries in rat plasma ranged from 95.98% to 108.93%. This rapid method was successfully applied in the pharmacokinetic study of wedelolactone in rat plasma. Following the oral administration of 5.00 mg/kg wedelolactone, the wedelolactone was rapidly absorbed. Pharmacokinetic parameters were used to quantitatively describe the dynamic changes of wedelolactone in vivo, providing a theoretical basis for pharmacological research on drugs and preclinical medication. The study of wedelolactone can provide a theoretical basis and quick analysis for the study of other traditional Chinese medicine. This may lead to breakthroughs in the pharmacokinetic study of complex Chinese medicines.

scholarly journals A METHOD FOR DETERMINING 1,4-BENZOTHIAZINE DERIVATIVES IN RAT PLASMA BY HPLC AND ITS APPLICATION TO A PHARMACOKINETIC STUDY

2017 ◽  
Vol 9 (12) ◽  
pp. 82 ◽  
Author(s):  
Amit Rai ◽  
Vinit Raj ◽  
Ashok K. Singh ◽  
Amit K. Keshari ◽  
Sudipta Saha
Keyword(s):  
Pharmacokinetic Study ◽  
High Performance ◽  
Gradient Elution ◽  
Rat Plasma ◽  
Hplc Method ◽  
Array Detector ◽  
Hplc Separation ◽  
Rp Hplc ◽  
Photodiode Array Detector ◽  
Photodiode Array

Objective: The objective of the study was to develop, optimize and validate of a new reverse-phase high-performance liquid chromatography (RP-HPLC) method for the determining 1,4-benzothiazine derivatives (AR13 and AR15) in a biological sample of rat plasma. The 1,4-benzothiazine derivatives are produced by the synthetic reactions.Methods: RP-HPLC separation was performed using an ODS-2 Hypersil column with gradient elution mobile phase consisting of water-acetonitrile for AR13 and AR15 (1:9 v/v, 3:7 v/v) at room temperature 1 ml/min flow rate, and interfaced with photodiode array detector (PDA) detector, 233 nm, 235 nm respectively.Results: A linear response was obtained between (range from 0.100-10.00 mg/ml) AR13 and (range from 0.096–9.88 mg/ml) AR15 with correlation coefficient 0.999 and 0.998. The linearity range of both AR13 and AR15 was 101.65±1.5 and 98.78±1.7.Conclusion: It was concluded that the method was simple, accurate, sensitive, accurate and reproducible and has been successfully applied to the pharmacokinetic study of AR13 and AR15 in rat plasma.

Bioanalytical Method Development and Validation of Cilnidipine and Metoprolol Succinate by RP-HPLC: Its Pharmacokinetic Application

2021 ◽  
Vol 01 ◽  
Author(s):  
Ramanlal N. Kachave ◽  
Suvarna H. Shelke
Keyword(s):  
Oral Administration ◽  
Pharmacokinetic Study ◽  
Chromatographic Method ◽  
Method Development ◽  
Antihypertensive Agents ◽  
Rat Plasma ◽  
Reversed Phase ◽  
Pharmacokinetic Studies ◽  
Metoprolol Succinate

Background: Cilnidipine and Metoprolol Succinate are antihypertensive agents used in the treatment of hypertension. Methods: Pharmacokinetic study of Cilnidipine and Metoprolol Succinate in rat plasma was carried out using the chromatographic method. The Chromatographic method was achieved on a reversed-phase C18 column, using acetonitrile and pH 4.0 water as ratio of 80:20 v/v as mobile phase, and a flow rate of 1.2 ml/min, and UV detection at 231 nm. In-vivo pharmacokinetic studies were performed on rats. Rats were treated with Cilnidipine (1mg/kg) and Metoprolol Succinate (1 mg/kg) orally, and blood samples were collected (0), 0.5, 1, 2, 4, 6, 8, 12, and 24 h post-treatment. Results: The retention time of Plasma, Cilnidipine, and Metoprolol Succinate were found to be 2.3, 3.1, and 5.5 min, respectively. Linearity was acceptable in the concentration range of 2-10 and 10-50 for Cilnidipine and Metoprolol Succinate, respectively. The intra-day and inter-day variance was less than 2. The mean recovery of Cilnidipine and Metoprolol Succinate were 100.12 and 100.15, respectively. The assay was successfully applied to a pharmacokinetic study in the rat after oral administration. After oral administration, maximal concentration (Cmax) of Cilnidipine and Metoprolol Succinate being 460.01 and 642.13 (μg g/mL), half-life found at 2.0 and 3.904 hours, respectively. Conclusion: The present method was successfully applied to a pharmacokinetic study of Cilnidipine and Metoprolol Succinate in rat plasma after oral administration.

Simultaneous determination of vasicine and its major metabolites in rat plasma by UPLC-MS/MS and its application to in vivo pharmacokinetic studies

RSC Advances ◽  
2015 ◽  
Vol 5 (95) ◽  
pp. 78336-78351 ◽  
Author(s):  
Wei Liu ◽  
Dandan He ◽  
Yudan Zhu ◽  
Xuemei Cheng ◽  
Hao Xu ◽  
...  
Keyword(s):  
Simultaneous Determination ◽  
Pharmacokinetic Study ◽  
Rat Plasma ◽  
Pharmacokinetic Studies ◽  
Butyrylcholinesterase Activity

An UPLC-MS/MS method was developed to simultaneously determinate vasicine and its main metabolites and applied to the pharmacokinetic study. In addition, the anti-butyrylcholinesterase activity of component in plasma was evaluatedin vitro.

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