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Hplc pharmacokinetics

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https://www.readbyqxmd.com/read/29348104/disposition-kinetics-of-omeprazole-in-healthy-female-volunteers-in-faisalabad
#1
Sadia Ashraf, Tanweer Khaliq, Ijaz Javed, Bilal Aslam, Nazia Qadir, Nadia Noor
Omeprazole (OMP) a proton pump inhibitor is widely used to suppress gastric acid secretions of parietal cells of stomach and metabolized predominantly by CYP2C19. The objective of the present study was to investigate the pharmacokinetics and dosage regimen of OMP, after its single oral administration in eight healthy adult female subjects. Blood samples were collected at different time intervals after oral administration and their pH was measured. Plasma concentration of OMP was determined by high performance liquid chromatography (HPLC) system equipped with UV-visible Detector...
January 2018: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29346367/assessment-of-serum-pharmacokinetics-and-urinary-excretion-of-albendazole-and-its-metabolites-in-human-volunteers
#2
Laura Ceballos, Alejandro Krolewiecki, Marisa Juárez, Laura Moreno, Fabian Schaer, Luis I Alvarez, Rubén Cimino, Judd Walson, Carlos E Lanusse
BACKGROUND: Soil Transmitted Helminth (STH) infections negatively impact physical and mental development in human populations. Current WHO guidelines recommend morbidity control of these infections through mass drug administration (MDA) using albendazole (ABZ) or mebendazole. Despite major reductions in STH associated morbidity globally, not all programs have demonstrated the expected impact on prevalence of parasite infections. These therapeutic failures may be related to poor programmatic coverage, suboptimal adherence or the exposure of parasites to sub-therapeutic drug concentrations...
January 2018: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/29342239/hplc-estimation-ex-vivo-everted-sac-permeability-and-in-vivo-pharmacokinetic-studies-of-darunavir
#3
Vasanti M Suvarna, Preeti C Sangave
Darunavir ethanolate (DRV) is an efficient protease inhibitor (PI) used in the treatment of human immunodeficiency virus (HIV) type-1 patients. An isocratic reversed-phase HPLC method was developed to monitor concentration of darunavir in in vitro intestinal fluid samples in everted sac absorption model in the presence of bioenhancers, viz., piperine, quercetin, naringenin. The method was validated and successfully applied to everted sac and pharmacokinetic studies in rats. The absorption profiles of DRV and apparent permeability coefficients were determined...
January 12, 2018: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/29342170/determination-of-2-4-dichlorophenoxyacetic-acid-2-4-d-in-rat-serum-for-pharmacokinetic-studies-with-a-simple-hplc-method
#4
Xiao Chen, Hongling Zhang, Yanjian Wan, Xi Chen, Yuanyuan Li
2,4-Dichlorophenoxyacetic acid (2,4-D) is a chlorophenoxy herbicide used worldwide. We describe a high-performance liquid chromatography (HPLC) method with UV detection for the determination of 2,4-D in female and male rat serum. This allows to observe the change of serum 2,4-D concentration in rats with time and its pharmacokinetics characteristics with a simple, rapid, optimized and validated method. The serum samples are pretreated and introduced into the HPLC system. The analytes are separated in a XDB-C18 column with a mobile phase of acetonitrile (solvent A) and 0...
2018: PloS One
https://www.readbyqxmd.com/read/29341904/a-rapid-and-simple-lc-ms-ms-method-for-personalized-busulfan-dosing-in-pediatric-patients-undergoing-hematological-stem-cell-transplantation-hsct
#5
Yi Xiao, Xiaohan Li, Xiaowei Fu
BACKGROUND: Busulfan is commonly used as a conditioning regimen before hematological stem cell transplantation (HSCT). There is a big inter-individual variability in busulfan exposure and the narrow therapeutic index, especially in pediatric population. Therefore, to achieve therapeutic efficacy and safety concurrently, personalized busulfan dosing, guided by pharmacokinetic study with serial plasma samples, is needed a few hours afterwards. METHODS: We used liquid-chromatography-mass spectrometry (HPLC-MS/MS) to develop, validate, and implementation of a fast, sensitive, and accurate method for busulfan measurement...
January 13, 2018: Clinica Chimica Acta; International Journal of Clinical Chemistry
https://www.readbyqxmd.com/read/29336615/pharmacokinetic-bioequivalence-safety-and-acceptability-of-ornibel%C3%A2-a-new-polymer-composition-contraceptive-vaginal-ring-etonogestrel-ethinylestradiol-11-00-3-474%C3%A2-mg-compared-with-nuvaring%C3%A2-etonogestrel-ethinylestradiol-11-7-2-7%C3%A2-mg
#6
Jaime Algorta, Maria Diaz, Raquel de Benito, Marc Lefebvre, Eric Sicard, Milton Furtado, Pedro Antonio Regidor, Celestino Ronchi
OBJECTIVE: To show the clinical development of Ornibel® (ExeltisHealthcare, Spain) a contraceptive vaginal ring manufactured with a new polymer composition and containing etonogestrel/ethinylestradiol, compared to Nuvaring® (MSD, Spain). SUBJECTS AND METHODS: Randomised, single dose, 2-period, 2-sequence, 2-stage crossover, comparative bioavailability study conducted in 40 healthy female subjects. All subjects received both treatments for 28 days in each of two periods, separated by a 28 days washout...
January 16, 2018: European Journal of Contraception & Reproductive Health Care
https://www.readbyqxmd.com/read/29333466/evaluation-of-the-possible-utilization-of-68ga-dotatoc-in-diagnosis-of-adenocarcinoma-breast-cancer
#7
Samaneh Zolghadri, Mojdeh Naderi, Hassan Yousefnia, Behrouz Alirezapour, Davood Beiki
Objectives: Studies have indicated advantageous properties of [DOTA-DPhe1, Tyr3] octreotide (DOTATOC) in tumor models and labeling with gallium. Breast cancer is the second leading cause of cancer mortality in women, and most of these cancers are often an adenocarcinoma. Due to the importance of target to non-target ratios in the efficacy of diagnosis, the pharmacokinetic of 68Ga-DOTATOC in an adenocarcinoma breast cancer animal model was studied in this research, and the optimized time for imaging was determined...
2018: Asia Oceania Journal of Nuclear Medicine & Biology
https://www.readbyqxmd.com/read/29323165/biotransformation-and-tissue-distribution-of-protopine-and-allocryptopine-and-effects-of-plume-poppy-total-alkaloid-on-liver-drug-metabolizing-enzymes
#8
Ya-Jun Huang, Pi Cheng, Zhuo-Yi Zhang, Shi-Jie Tian, Zhi-Liang Sun, Jian-Guo Zeng, Zhao-Ying Liu
In this study, the biotransformation in the plasma, urine and feces of rats following oral administration of protopine (PRO) and allocryptopine (ALL)were explored using HPLC-QqTOF MS. An HPLC-MS/MS method for the determination of tissues was developed and applied to the tissue distribution study in rats following intragastric administration of Plume Poppy Total Alkaloid for 3 weeks. A total of ten PRO metabolites and ten ALL metabolites were characterized in rats in vivo. Among these metabolites, six PRO metabolites and five ALL metabolites were reported for the first time...
January 11, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29319909/inhibitory-effects-of-sulfonylureas-and-non-steroidal-anti-inflammatory-drugs-on-in-vitro-metabolism-of-canagliflozin-in-human-liver-microsomes
#9
Sara Algeelani, Dalal Alkhelb, David J Greenblatt
Canagliflozin, used to treat type 2 diabetes mellitus (T2DM), is commonly co-administered with sulfonylureas. The objective of the present study was to evaluate the possible inhibitory effect of sulfonylureas and non-steroidal anti-inflammatory drugs (NSAIDs) on canagliflozin metabolism in vitro. Three sulfonylurea derivatives were evaluated as inhibitors: chlorpropamide, glimepiride, and gliclazide. Two other NSAIDs were used as positive control inhibitors: niflumic acid and diclofenac. The rate of formation of canagliflozin metabolites was determined by HPLC analysis of vitro incubations of canagliflozin as a substrate with and without inhibitors, using human liver microsomes (HLMs)...
January 10, 2018: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/29319234/comparative-pharmacokinetics-of-trandolapril-its-active-metabolite-and-verapamil-in-human-plasma-of-egyptian-population-using-hplc-ms-ms
#10
Ragaa Magdy, Ahmed H El-Khatib, Ahmed Hemdan, Omar Abd Elaziz, Maha Farouk, Michael W Linscheid
Trandolapril and verapamil are commonly used antihypertensive drugs. However, there is a lack of available data on the change of their pharmacokinetics in patients with liver or kidney impairment and hence the need for dose adjustment. In the presented work, a high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method was developed and validated for the monitoring of trandolapril, its active metabolite trandolaprilat, and verapamil in human plasma of patients with renal impairment and/or liver insufficiency...
January 10, 2018: Drug Testing and Analysis
https://www.readbyqxmd.com/read/29305638/pharmacokinetics-of-dacarbazine-dtic-in-pregnancy
#11
Ira Kantrowitz-Gordon, Karen Hays, Olumide Kayode, Aditya R Kumar, Henry G Kaplan, Joel M Reid, Stephanie L Safgren, Matthew M Ames, Thomas R Easterling, Mary F Hebert
PURPOSE: The purpose of this report is to describe, for the first time, the pharmacokinetics of dacarbazine (DTIC) and its metabolites [5-[3-methyl-triazen-1-yl]-imidazole-4-carboxamide (MTIC), 5-[3-hydroxymethyl-3-methyl-triazen-1-yl]-imidazole-4-carboxamide (HMMTIC) and 5-aminoimidazole-4-carboxamide (AIC)] during pregnancy (n = 2) and postpartum (n = 1). METHODS: Non-compartmental DTIC, MTIC, HMMTIC, and AIC pharmacokinetics (PK) were estimated in one case at 29 week gestation and 18 day postpartum and a second case at 32 week gestation, in women receiving DTIC in combination with doxorubicin, bleomycin, and vinblastine for treatment of Hodgkin's lymphoma...
January 5, 2018: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/29302995/preparation-of-curcumin-self-micelle-solid-dispersion-with-enhanced-bioavailability-and-cytotoxic-activity-by-mechanochemistry
#12
Qihong Zhang, Nikolay E Polyakov, Yulia S Chistyachenko, Mikhail V Khvostov, Tatjana S Frolova, Tatjana G Tolstikova, Alexandr V Dushkin, Weike Su
An amorphous solid dispersion (SD) of curcumin (Cur) with disodium glycyrrhizin (Na2GA) was prepared by mechanical ball milling. Curcumin loaded micelles were self-formed by Na2GA when SD dissolved in water. The physical properties of Cur SD in solid state were characterized by differential scanning calorimetry, X-ray diffraction studies, and scanning electron microscope. The characteristics of the sample solutions were analyzed by reverse phase HPLC, UV-visible spectroscopy, 1H NMR spectroscopy, gel permeation LC, and transmission electron microscopy...
November 2018: Drug Delivery
https://www.readbyqxmd.com/read/29298479/gastric-emptying-and-small-bowel-water-content-after-administration-of-grapefruit-juice-compared-to-water-and-iso-caloric-solutions-of-glucose-and-fructose-a-four-way-crossover-mri-pilot-study-in-healthy-subjects
#13
Michael Grimm, Mirko Koziolek, Marwa Saleh, Felix Schneider, Grzegorz Garbacz, Jens Peter Kuhn, Werner Weitschies
Grapefruit juice (GFJ) is known to affect the bioavailability of drugs in different ways. Despite the influence on gastrointestinal enzymes and transporters, the influence on gastrointestinal fluid kinetics is regarded to be relevant for the absorption of several drugs. Thus, it was the aim of this pilot study to investigate the gastric and intestinal volumes after intake of GFJ compared to isocaloric fructose and glucose solutions and water. The gastric and small intestinal volume kinetics after intake of 240 mL of GFJ, 10...
January 3, 2018: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29295501/the-herb-drug-pharmacokinetic-interaction-of-5-fluorouracil-and-its-metabolite-5-fluoro-5-6-dihydrouracil-with-a-traditional-chinese-medicine-in-rats
#14
Ju-Han Liu, Yung-Yi Cheng, Chen-Hsi Hsieh, Tung-Hu Tsai
BACKGROUND: Xiang-Sha-Liu-Jun-Zi-Tang (XSLJZT) is the most common traditional formula given to colorectal and breast cancer patients in Taiwan, according to a statistical study of the National Health Insurance Research Database. 5-Fluorouracil (5-FU) is widely used as the first line of treatment for colorectal cancer. Thus, the aim of study is to investigate the pharmacokinetic interaction of XSLJZT and 5-FU. METHODS: To investigate the herb-drug interaction of XSLJZT with 5-FU as well as its metabolite 5-fluoro-5,6-dihydrouracil (5-FDHU) using pharmacokinetics, a high-performance liquid chromatography (HPLC) system coupled with a photodiode array detector was developed to monitor 5-FU and 5-FDHU levels in rat blood...
December 23, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29286295/determination-of-tangeretin-in-rat-plasma-assessment-of-its-clearance-and-absolute-oral-bioavailability
#15
Mai Gamal Elhennawy, Hai-Shu Lin
Tangeretin (TAN) is a dietary polymethoxylated flavone that possesses a broad scope of pharmacological activities. A simple high-performance liquid chromatography (HPLC) method was developed and validated in this study to quantify TAN in plasma of Sprague-Dawley rats. The lower limit of quantification (LLOQ) was 15 ng/mL; the intra- and inter-day assay variations expressed in the form of relative standard deviation (RSD) were all less than 10%; and the assay accuracy was within 100 ± 15%. Subsequently, pharmacokinetic profiles of TAN were explored and established...
December 29, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/29285548/preclinical-evaluation-of-an-18f-trifluoroborate-methionine-derivative-for-glioma-imaging
#16
Xiangyu Yang, Zhibo Liu, Huimin Zhang, Zhu Li, Jeeva P Munasinghe, Gang Niu, Gaojun Teng, Xiaoyuan Chen
PURPOSE: 11C-methionine (MET) is one of the most commonly used amino acid tracers for PET imaging of brain tumors. In this study, we report an 18F-labeled boron-derived methionine analogue, denoted as 18F-B-MET, as a potential substitute of 11C-MET for glioma PET imaging. METHODS: 19F-B-MET was synthesized from readily available chemicals according to our previous publication. For kit development, 19F-B-MET was aliquoted in quantities of 10 nmol for on-demand one-step labeling...
December 29, 2017: European Journal of Nuclear Medicine and Molecular Imaging
https://www.readbyqxmd.com/read/29235297/-simultaneous-determination-of-8-constituents-of-desmodii-styracifolii-herba-in-rat-bile-with-hplc-ms-ms-and-their-excretion-pharmacokinetics
#17
Xue-Yan Fan, Xin Wang, Xiao-Chen Liu, Chun-Ying Wang
To establish a HPLC-MS/MS quantitative method for analysis of 8 constituents in rat bile. The method was applied in the biliary excretion study after oral administration of Desmodii Styracifolii Herba extract. The rat bile samples were collected during 0-1, 1-2, 2-4, 4-6, 6-8, 8-12, 12-24 h. Diamonsil C₁₈column (4.6 mm×150 mm, 5 μm) was adopted and eluted with methanol and 0.01% acetic acid in a gradient mode. The flow rate was 0.8 mL•min⁻¹, and the column temperature was set at 40 ℃. The detection was carried out by a triple quadrupole linearion trap mass spectrometer in the negative ion mode with an electrospray source...
October 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/29235137/development-of-hplc-with-fluorescent-detection-using-nbd-f-for-the-quantification-of-colistin-sulfate-in-rat-plasma-and-its-pharmacokinetic-applications
#18
Sui Ouchi, Kazuaki Matsumoto, Maki Okubo, Yuta Yokoyama, Junko Kizu
Colistin sulfate, composed of a mixture of colistin A sulfate (CLA) and colistin B sulfate (CLB), is available for treating life-threatening infections caused by multidrug-resistant Gram-negative bacteria. In this study, the CLA and CLB were quantified separately. Colistin sulfate was extracted from rat plasma with a solid-phase extraction C18 cartridge and reacted with 4-fluoro-7-nitro-2,1,3-benzoxadiazole (NBD-F), and the fluorescent derivatives were subjected to reversed phase high-performance liquid chromatography analysis and used to investigate the pharmacokinetics of CLA and CLB in rat plasma...
December 12, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/29229354/comparative-clinical-trial-of-the-variability-factors-of-the-exposure-indices-used-for-the-drug-monitoring-of-two-tacrolimus-formulations-in-kidney-transplant-recipients
#19
Pierre Marquet, Laetitia Albano, Jean-Baptiste Woillard, Lionel Rostaing, Nassim Kamar, Charlotte Sakarovitch, Philippe Gatault, Matthias Buchler, Bernard Charpentier, Eric Thervet, Elisabeth Cassuto
BACKGROUND: Several studies found differences in tacrolimus whole blood trough levels (C0) or area-under-the curve (AUC) between the twice-daily (Tac-BID) and once-daily (Tac-OD) formulations given to kidney transplant recipients at equal doses. As C0 is widely used as a surrogate of the AUC for individual dose adjustment, this study investigated the correlation and proportionality between C0 and the 24h-AUC, depending on the formulation, time post-transplantation, pharmacogenetics traits and other individual characteristics...
December 8, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/29216583/hplc-ms-ms-analysis-of-mesupron-and-its-application-to-a-pharmacokinetic-study-in-rats
#20
Changmin Park, Joong Gyu Ha, Seungmok Choi, Eunyoung Kim, Keumhan Noh, Beom Soo Shin, Wonku Kang
Mesupron, the first-in-class inhibitor of urokinase-type plasminogen activator (uPA) is known to regulate cell proliferation and migration, and is under investigation for the treatment of metastatic breast cancer. In this study, a quantification method was developed for the determination of mesupron in rat plasma using liquid chromatography with a tandem mass spectrometry (LC-MS/MS). After protein precipitation with acetonitrile including itraconazole (internal standard, IS), the analytes were chromatographed on a reversed phased column with a mobile phase of acetonitrile and water (7:3, v/v, including 0...
December 4, 2017: Journal of Pharmaceutical and Biomedical Analysis
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