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Hplc pharmacokinetics

P S Suresh, Nuggehally R Srinivas, Ramesh Mullangi
Prostate cancer is the most common cancer and one of the leading causes for cancer deaths in men. One of the commonly used approaches to treat metastatic prostate cancer was via first generation non-steroidal anti-androgens (NSAA) namely flutamide, nilutamide, bicalutamide and topilutamide. Most of the prostate cancer patients who are initially responsive develop a most aggressive form of disease called castration-resistant prostate cancer (CRPC). Second generation NSAA receptor antagonists (enzalutamide, apalutamide and darolutamide) are emerging as additional new options to treat CRPC...
June 21, 2017: Biomedical Chromatography: BMC
Samaa Alrushaid, Neal M Davies, Stephanie E Martinez, Casey L Sayre
Liquiritigenin is a chiral flavonoid present in licorice and other medicinal plants. The nature of its biological fate with respect to the individual enantiomers has not been examined. In this study, we characterize, for the first time, the stereoselective pharmacokinetics of liquiritigenin. Liquiritigenin was intravenously (20 mg/kg) and orally (50 mg/kg) administered to male Sprague-Dawley rats (n = 4 per route of administration). Concentrations in serum and urine were characterized via stereospecific reversed-phase, isocratic HPLC method with UV detection...
June 2017: Research in Pharmaceutical Sciences
Sameh Ahmed, Noha N Atia
Selective and fast chromatographic method was essential for the determination of triptans, selective serotonin receptor (5-HT1) agonists, in biological specimens. However, selective chromatographic separation of these highly basic drugs is a challenging problem on silica-based stationary phases. Zirconia-based stationary phases have been introduced as an efficient alternative for silica-based columns offering unique stability, selectivity, and retention ability for various classes of drugs. Herein, a new selective, fast and reproducible high performance liquid chromatographic method (HPLC) was developed and validated for the determination of four triptans in plasma samples namely; Sumatriptan (SMT), Zolmitriptan (ZLT), Eletriptan (ELT) and Rizatriptan (RZT)...
June 7, 2017: Journal of Pharmaceutical and Biomedical Analysis
Qingguo Tian, Juan Rogness, Min Meng, Zheng Li
AIM: Toxicokinetic and pharmacokinetic studies of therapeutic oligonucleotides require validated bioanalytical methods for sensitive and specific quantification of oligonucleotide drug candidates in biological samples. RESULTS: A peptide nucleic acid (PNA) hybridization-based HPLC-fluorescence assay was developed and validated for quantification of Arrowhead Pharmaceuticals' proprietary siRNA in rat plasma samples via hybridization and anion-exchange-HPLC (AEX-HPLC) with fluorescence detection...
June 15, 2017: Bioanalysis
Jing Zhao, Yuan Li, Ming-Xin Shi, Xue Wang, Jing-Qing Zhang
OBJECTIVES: To study the oral phamacokinetics of curcumin ethosomes in rats. METHODS: Pharmacokinetics parameters were detected by DAS 2.1.1 software analysis through data of blood concentrations harvested from HPLC after oral administration of curcumin ethosomes in rats. RESULTS: Analyzed by non-compartmental method, the area under concentration-time curve from 0 to last time [AUC(0-72h)] of curcumin ethosomes was 1.6 times larger than that of free curcumin, the peak concentration (C max) of curcumin ethosomes was 1...
March 2017: Sichuan da Xue Xue Bao. Yi Xue Ban, Journal of Sichuan University. Medical Science Edition
Q Shan, J Fan, J Wang, X Zhu, Y Yin, G Zheng
The pharmacokinetics of enrofloxacin (ENR) was studied in crucian carp (Carassius auratus gibelio) after single administration by intramuscular (IM) injection and oral gavage (PO) at a dose of 10 mg/kg body weight and by 5 mg/L bath for 5 hr at 25°C. The plasma concentrations of ENR and ciprofloxacin (CIP) were determined by HPLC. Pharmacokinetic parameters were calculated based on mean ENR or CIP concentrations using WinNonlin 6.1 software. After IM, PO and bath administration, the maximum plasma concentration (Cmax ) of 2...
June 11, 2017: Journal of Veterinary Pharmacology and Therapeutics
Fitya Syarifa Mozar, Ezharul Hoque Chowdhury
pH sensitive nanoparticles of carbonate apatite (CA) have been proven to be effective delivery vehicles for DNA, siRNAs and proteins. More recently, conventional anti-cancer drugs, such as doxorubicin, methotrexate and cyclophosphamide have been successfully incorporated into CA for intracellular delivery to breast cancer cells. However, physical and chemical properties of drug molecules appeared to affect their interactions with CA, with hydrophillic drug so far exhibiting better binding affinity and cellular uptakes compared to hydrophobic drugs...
June 7, 2017: Pharmaceutics
Feray Altan, Kamil Uney, Ayse Er, Gul Cetin, Burak Dik, Enver Yazar, Muammer Elmas
The aim of this research was to compare plasma pharmacokinetics of ceftiofur sodium (CS) in healthy calves, and in calves with experimentally induced endotoxemia. Six calves received CS (2.2 mg/kg, IM) 2 hr after intravenous administration of 0.9% NaCl (Ceft group). After a washout period, the same 6 calves received CS 2 hr after intravenous injection of lipopolysaccharide (LPS+Ceft group). Another group of 6 calves received a combination of drug therapies that included CS 2 hr after administration of 0.9% NaCl (Comb group)...
June 5, 2017: Journal of Veterinary Medical Science
Sylvestre Dammicco, Marine Goux, Christian Lemaire, Guillaume Becker, Mohamed Ali Bahri, Alain Plenevaux, Mathieu Cinier, André Luxen
INTRODUCTION: Nanofitins are low molecular weight, single chain and cysteine-free protein scaffolds able to selectively bind a defined biological target. They derive from Sac7d bacterial protein family and are highly stable over a wide range of pH (0-13) and temperature (Tm ~80°C). Their extreme stability, low cost of production and high tolerability for chemical coupling make Nanofitins a very interesting alternative to antibodies and their fragments. Here, a hexahistidine tagged model Nanofitin (H4) directed against hen egg white lysozyme was radiolabelled and injected in mice to provide a baseline biodistribution and pharmacokinetic profiles to support future Nanofitin development programs...
April 27, 2017: Nuclear Medicine and Biology
Jana Leshinsky, Andrew McLachlan, David J R Foster, Ross Norris, Vanessa R Barrs
Cats are the most common mammal to develop invasive fungal rhinosinusitis caused by cryptic species in Aspergillus section Fumigati that are resistant to azoles but susceptible to caspofungin. In this study nonlinear mixed-effects pharmacokinetic modeling and simulation was used to investigate caspofungin pharmacokinetics and explore dosing regimens in cats using caspofungin minimum effective concentrations (MECs). Plasma concentrations in healthy cats were determined using HPLC-MS/MS after administration of a single and seven consecutive daily intravenous doses of 1 mg/kg caspofungin...
2017: PloS One
Jinglong Wang, Dandan Zheng, Yingzi Wang, Chao Zhang, Xiumei Sun
To study the pharmacokinetics of Erhuang decoction extracts, a high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method was established for the determination of effective substances in rat plasma. The extracts prepared by water extraction (WE) method were given to rats by oral administration. After collected from the orbital venous plexus, plasma was treated by protein precipitation method. Then, the concentration of index components, including baicalin, liquiritin, berberine, palmatine and glycyrrhetinic acid, were determined by HPLC-MS/MS...
August 1, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
M K Watson, M G Papich, S K Chinnadurai
This study was designed to investigate the pharmacokinetics of clindamycin, a lincosamide antibiotic, in Bennett's wallabies. The pharmacokinetic properties of a single intravenous (IV) dose of clindamycin were determined in six wallabies. A single 20-min IV infusion of 20 mg/kg of clindamycin was administered, followed by blood collection prior to, and up to 12 hr after clindamycin administration. Plasma clindamycin concentrations were determined by high-pressure liquid chromatography (HPLC) with ultraviolet (UV) detection...
June 1, 2017: Journal of Veterinary Pharmacology and Therapeutics
Tae Kon Kim
In this study, a sensitive and reliable method for the quantitation of fenofibric acid in rat plasma was developed and validated using high performance liquid chromatography (HPLC). The plasma samples were prepared by deproteinization, and sildenafil was used as an internal standard. Chromatographic separation was achieved using a reversed-phase (C18) column. The mobile phase, 0.02 M ammonium acetate buffer:acetonitrile (35:65, v/v), was run at a flow rate of 1.0 mL/min, and the column eluent was monitored using an ultraviolet detector at 280 nm at room temperature...
May 30, 2017: Drug Research
Jong Bong Lee, Cecilia Adrower, Chaolong Qin, Peter M Fischer, Cornelia H de Moor, Pavel Gershkovich
There is extensive literature on in vivo studies with cordycepin, but these studies were generally conducted without validation of the various formulations, especially in terms of the solubility of cordycepin in the dosing vehicles used. Cordycepin is a promising drug candidate in multiple therapeutic areas, and there is a growing interest in studies aimed at assessing the pharmacological activity of this compound in relevant animal disease models. It is likely that many reported in vivo studies used formulations in which cordycepin was incompletely soluble...
May 30, 2017: AAPS PharmSciTech
Sonia Luque, Carol Escaño, Luisa Sorli, Jian Li, Nuria Campillo, Juan Pablo Horcajada, Esther Salas, Santiago Grau
Objectives: Limited information is available on the urinary excretion of colistin in infected patients. This study aimed to investigate the pharmacokinetics of colistimethate sodium (CMS) and formed colistin in urine in patients with multidrug-resistant (MDR) Gram-negative infections.Methods: Pharmacokinetic study conducted in 12 patients diagnosed with an infection caused by an extremely drug-resistant (XDR) P. aeruginosa and treated with intravenous CMS. Freshly urine samples were collected in 2-h interval and blood samples pre-dose (Cminss) and at the end of the CMS infusion (Cmaxss) for measurement of concentrations of CMS and formed colistin using HPLC...
May 30, 2017: Antimicrobial Agents and Chemotherapy
Anna Lucia Fallacara, Aarianna Mancini, Claudio Zamperini, Elena Dreassi, Stefano Marianelli, Mario Chiariello, Gianni Pozzi, Francesco Santoro, Maurizio Botta, Silvia Schenone
Pyrazolo[3,4-d]pyrimidine derivatives 1-5, active as c-Src inhibitors, have been selected to be formulated as drug-loaded human serum albumin (HSA) nanoparticles, with the aim of improving their solubility and pharmacokinetic properties. The present study includes the optimization of a desolvation method-based procedure for preparing HSA nanoparticles. First, characterization by HPLC-MS and Dynamic Light Scattering (DLS) showed a good entrapment efficacy, a controllable particle size (between 100 and 200nm) and an optimal stability over time, confirmed by an in vitro drug release assay...
May 17, 2017: Bioorganic & Medicinal Chemistry Letters
Xiujun Wu, Yang You, Gonglin Qu, Ran Ma, Mingxue Zhang
A simple and sensitive HPLC-MS/MS method was developed and fully validated for simultaneous determination of ginsenoside Rb1, ginsenoside Rg1, paeoniflorin, albiflorin and oxypaeoniflorin in rat plasma. Plasma samples were pretreated with protein precipitation using acetonitrile. The chromatographic separation was carried out on a C18 column with a gradient mobile phase consisting of acetonitrile and water (containing 0.1% formic acid). All analytes and digoxin (internal stand, IS) were quantitated through electrospray ionization in negative ion multiple reaction monitoring (MRM) mode...
May 30, 2017: Biomedical Chromatography: BMC
Min Xu, Huaqiao Tang, Qian Rong, Yuanli Zhang, Yinglun Li, Ling Zhao, Gang Ye, Fei Shi, Cheng Lv
Formaldehyde (FA) is an occupational and indoor pollutant. Long-term exposure to FA can irritate the respiratory mucosa, with potential carcinogenic effects on the airways. The effects of acute FA poisoning on the activities of CYP450 isoforms CYP1A2, CYP2C11, CYP2E1, and CYP3A2 were assessed by determining changes in the pharmacokinetic parameters of the probe drugs phenacetin, tolbutamide, chlorzoxazone, and testosterone, respectively. Rats were randomly divided into three groups: control, low FA dose (exposure to 110 ppm for 2 h for 3 days), and high FA dose (exposure to 220 ppm for 2 h for 3 days)...
2017: BioMed Research International
Xiao-Kui Huo, Bo Wang, Lu Zheng, Hai-Jian Cong, Ting Xiang, Shu-Mei Wang, Cheng-Peng Sun, Chao Wang, Lin Zhang, Sa Deng, Bin Wu, Xiao-Chi Ma
An accurate, precise, selective, and sensitive high performance liquid chromatography coupled to tandem mass spectrometry (HPLC-MS/MS) method was developed for the simultaneous determination of baicalin and its metabolite, baicalein 6-O-glucopyranuronoside, in normal and febrile rats plasma. Two analytes, along with hesperidin as an internal standard, were determined by multiple reactions monitoring (MRM) operated in the positive electrospray ionization (ESI) mode. Chromatographic separation was performed on an Agilent ZORBAX Extend-C18 column (100mm×2...
August 1, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Jong Suk Park, Shaheed Ur Rehman, In Sook Kim, Min Sun Choi, Chun-Soo Na, Hye Hyun Yoo
BACKGROUND: Hovenia dulcis (Rhamnaceae) fruits are popularly used as herbal medicines or dietary supplements in Asian countries due to functions such as liver protection and detoxification from alcohol poisoning. Accordingly, it is very likely for dietary supplemental products, including H. dulcis fruit extracts, to be taken with prescription drugs. OBJECTIVE: In this study, possible food-drug interactions involving H. dulcis fruit extracts were evaluated based on the inhibition of cytochrome P450 (CYP) enzyme activity...
April 2017: Pharmacognosy Magazine
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