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https://www.readbyqxmd.com/read/29031229/-99m-tc-duramycin-for-cell-death-imaging-impact-of-kit-formulation-purification-and-species-difference
#1
Luca Palmieri, Filipe Elvas, Christel Vangestel, Koon Pak, Brian Gray, Sigrid Stroobants, Steven Staelens, Leonie Wyffels
INTRODUCTION: [(99m)Tc]duramycin is a SPECT tracer for cell death imaging. We evaluated the impact of kit formulation, purification and species difference on the pharmacokinetic profile and cell death targeting properties of [(99m)Tc]duramycin in order to define the optimal conditions for (pre-)clinical use. METHODS: Three kits were prepared (A: traditional formulation, B: containing 1/3 of ingredients, C: containing HYNIC-PEG12-duramycin). Following labeling, the kits were used without purification, or with SPE or HPLC purification...
September 14, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29031222/apolipoproteins-adsorption-and-brain-targeting-evaluation-of-baicalin-nanocrystals-modified-by-combination-of-tween80-and-tpgs
#2
Yang Liu, Yueqin Ma, Junnan Xu, Yingchong Chen, Jin Xie, Pengfei Yue, Qin Zheng, Ming Yang
To help baicalin pass across BBB and improve its targeting in brain, we designed a novel formulation strategy of baicalin nanocrystals that preferentially adsorbing apolipoprotein E (ApoE) and repelling protein adsorption of opsonins. Intravenous baicalin nanocrystals suspensions (BCL-NS) modified by different surfactant were prepared by high-pressure homogenization. The targeting potential of surface-modified BCL-NS with mean particles size of about 250nm was assessed by in vitro protein adsorption studies using two-dimensional polyacrylamide gel electrophoresis (2-D PAGE), and further evaluated in vivo pharmacokinetics...
October 5, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/29031170/a-dose-escalation-study-of-bi-daily-once-weekly-oral-docetaxel-either-as-modradoc001-or-modradoc006-combined-with-ritonavir
#3
Vincent A de Weger, Frederik E Stuurman, Jeroen J M A Hendrikx, Johannes J Moes, Emilia Sawicki, Alwin D R Huitema, Bastiaan Nuijen, Bas Thijssen, Hilde Rosing, Marianne Keessen, Marja Mergui-Roelvink, Jos H Beijnen, Jan H M Schellens, Serena Marchetti
INTRODUCTION: Two solid dispersions of docetaxel (denoted ModraDoc001 capsule and ModraDoc006 tablet (both 10 mg)) were co-administered with 100 mg ritonavir (/r) and investigated in a bi-daily once weekly (BIDW) schedule. Safety, maximum tolerated dose (MTD), pharmacokinetics (PK) and preliminary activity were explored. METHODS: Adult patients with metastatic solid tumours were included in two dose-escalation arms. PK sampling was performed during the first week and the second or third week...
October 11, 2017: European Journal of Cancer
https://www.readbyqxmd.com/read/29029280/pharmacokinetics-and-safety-results-from-the-phase-3-randomized-open-label-study-of-intravenous-posaconazole-in-patients-at-risk-of-invasive-fungal-disease
#4
Oliver A Cornely, Michael N Robertson, Shariq Haider, Andrew Grigg, Michelle Geddes, Mickael Aoun, Werner J Heinz, Issam Raad, Urs Schanz, Ralf G Meyer, Sarah P Hammond, Kathleen M Mullane, Helmut Ostermann, Andrew J Ullmann, Stefan Zimmerli, M L P S Van Iersel, Deborah A Hepler, Hetty Waskin, Nicholas A Kartsonis, Johan Maertens
No abstract text is available yet for this article.
October 3, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/29029267/evaluation-of-universal-versus-genotype-guided-efavirenz-dose-reduction-in-pregnant-women-using-population-pharmacokinetic-modelling
#5
Adeniyi Olagunju, Alessandro Schipani, Oluseye Bolaji, Saye Khoo, Andrew Owen
Objectives: Lack of data on the pharmacokinetics of efavirenz in pregnant women at the 400 mg reduced dose currently prevents universal roll-out. Population pharmacokinetic modelling was used to explore pharmacokinetic endpoints at 200, 400 and 600 mg daily doses in pregnant women stratified by CYP2B6 metabolic status. Methods: The analysis was based on 252 plasma efavirenz concentrations from 77 pregnant women (77 sparse, 175 intensive) who received antiretroviral regimens containing 600 mg of efavirenz...
September 26, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/29029190/pharmacokinetics-of-igf-i-in-papp-a2-deficient-patients-growth-response-and-effects-on-glucose-and-bone-density
#6
Catalina Cabrera-Salcedo, Tomoyuki Mizuno, Leah Tyzinski, Melissa Andrew, Alexander A Vinks, Jan Frystyk, Halley Wasserman, Catherine M Gordon, Vivian Hwa, Philippe Backeljauw, Andrew Dauber
Context: PAPP-A2 cleaves IGFBP-3 and -5 releasing free IGF-I. Homozygous mutations in PAPP-A2 result in growth failure with elevated total but low free IGF-I. Objective: To determine the 24-hour pharmacokinetic profile of free and total IGF-I after a dose of rhIGF-I. We describe the growth response and effects on glucose metabolism and bone mineral density (BMD) after one year of rhIGF-I therapy. Design and patients: Three affected siblings, their heterozygous parents, and two healthy controls participated...
September 28, 2017: Journal of Clinical Endocrinology and Metabolism
https://www.readbyqxmd.com/read/29029135/small-increase-in-dolutegravir-trough-but-equivalent-total-dolutegravir-exposure-with-simeprevir-in-hiv-hcv-seronegative-volunteers
#7
Christine E MacBrayne, Jose Castillo-Mancilla, James R Burton, Samantha MaWhinney, Charlotte B Wagner, Kestutis Micke, Jordan Fey, Ryan T Huntley, Bayli Larson, Lane R Bushman, Jennifer J Kiser
Background: Dolutegravir, an HIV integrase strand-transfer inhibitor, and simeprevir, an HCV NS3/4A PI, have the potential to interact as dolutegravir is a P-glycoprotein, uridine glucuronosyl transferase 1A1 and cytochrome P450 3A substrate and simeprevir has been shown to mildly inhibit these. Objectives: To compare dolutegravir and simeprevir pharmacokinetics (PK) when given separately versus in combination. Methods: Healthy volunteers received: (i) 150 mg of simeprevir once daily for 7 days; (ii) 50 mg of dolutegravir once daily for 7 days; and (iii) 150 mg of simeprevir once daily plus 50 mg of dolutegravir once daily for 7 days, with randomization to treatment sequence...
October 4, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/29029042/does-pharmacokinetic-pharmacodynamic-model-guided-anaesthesia-improve-outcome-after-hip-fracture-surgery
#8
M Coburn, R D Sanders
No abstract text is available yet for this article.
October 4, 2017: British Journal of Anaesthesia
https://www.readbyqxmd.com/read/29028925/influence-of-bayesian-optimization-on-the-performance-of-propofol-target-controlled-infusion
#9
J P van den Berg, D J Eleveld, T De Smet, A V M van den Heerik, K van Amsterdam, B J Lichtenbelt, T W L Scheeren, A R Absalom, M M R F Struys
Background: Target controlled infusion (TCI) systems use population-based pharmacokinetic (PK) models that do not take into account inter-individual residual variation. This study compares the bias and inaccuracy of a population-based vs a personalized TCI propofol titration using Bayesian adaptation. Haemodynamic and hypnotic stability, and the prediction probability of alternative PK models, was studied. Methods: A double-blinded, prospective randomized controlled trial of 120 subjects undergoing cardiac surgery was conducted...
October 3, 2017: British Journal of Anaesthesia
https://www.readbyqxmd.com/read/29028921/smartpilot%C3%A2-view-guided-anaesthesia-improves-postoperative-outcomes-in-hip-fracture-surgery-a-randomized-blinded-controlled-study
#10
D Leblanc, M Conté, G Masson, F Richard, A Jeanneteau, G Bouhours, J M Chrétien, L Rony, E Rineau, S Lasocki
Background: Both under-dosage and over-dosage of general anaesthetics can harm frail patients. We hypothesised that computer-assisted anaesthesia using pharmacokinetic/pharmacodynamic models guided by SmartPilot® View (SPV) software could optimise depth of anaesthesia and improve outcomes in patients undergoing hip fracture surgery. Methods: This prospective, randomized, single-centre, blinded trial included patients undergoing hip fracture surgery under general anaesthesia...
September 27, 2017: British Journal of Anaesthesia
https://www.readbyqxmd.com/read/29028616/simultaneous-determination-of-a-novel-c-met-axl-dual-target-small-molecule-inhibitor-bpi-9016m-and-its-metabolites-in-human-plasma-by-liquid-chromatography-tandem-mass-spectrometry-application-in-a-pharmacokinetic-study-in-chinese-advanced-solid-tumor-patients
#11
Xinge Cui, Xin Zheng, Ji Jiang, Fenlai Tan, Lieming Ding, Pei Hu
BPI-9016M is a novel dual-target small-molecule inhibitor targeting c-Met and AXL, which was developed by Betta Pharmaceuticals Co., Ltd (Hangzhou, China). It has great potential in the treatment of advanced cancer. A high throughput quantitation method, based on liquid chromatography-tandem mass spectrometry, was developed and validated for the simultaneous determination of BPI-9016M and its main metabolite, M1 and M2-2, in human plasma with a sample preparation method of precipitation of protein. Liquid chromatographic separation was performed with a gradient elution of formic acid-10mM ammonium acetate aqueous solution (1:1000, v/v) and acetonitrile at a flow rate of 0...
October 8, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/29028605/the-construction-and-characterization-of-hybrid-paclitaxel-in-micelle-in-liposome-systems-for-enhanced-oral-drug-delivery
#12
Yimu Li, Zheng Chen, Yanan Cui, Guangxi Zhai, Lingbing Li
In this study, novel paclitaxel (PTX) loaded hybrid liposomes for oral PTX delivery were prepared through incorporating PTX loaded polyion complex micelles comprised of positively charged Pluronic F127-Polyethylenimine (PF127-PEI) copolymer and negatively charged sodium cholate (CA) into liposomes consisted of phospholipid molecules. According to the results, this kind of PTX-loaded hybrid liposomes showed improved PTX encapsulation efficiency, sustained PTX release, and enhanced PTX absorption in intestine...
October 5, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/29028535/baicalin-and-its-metabolites-suppresses-gluconeogenesis-through-activation-of-ampk-or-akt-in-insulin-resistant-hepg-2-cells
#13
Tao Wang, Hongmei Jiang, Shijie Cao, Qian Chen, Mingyuan Cui, Zhijie Wang, Dandan Li, Jing Zhou, Tao Wang, Feng Qiu, Ning Kang
Scutellaria baicalensis Georgi (S. baicalensis), as a traditional Chinese herbal medicine, is an important component of several famous Chinese medicinal formulas for treating patients with diabetes mellitus. Baicalin (BG), a main bioactive component of S. baicalensis, has been reported to have antidiabetic effects. However, pharmacokinetic studies have indicated that BG has poor oral bioavailability. Therefore, it is hard to explain the pharmacological effects of BG in vivo. Interestingly, several reports show that BG is extensively metabolized in rats and humans...
September 23, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29028382/simultaneous-determination-of-metolazone-and-valsartan-in-plasma-by-on-line-spe-coupled-with-liquid-chromatography-tandem-mass-spectrometry
#14
Jiezhao Zhou, Meiling Chen, Ying Li, Fanglin Yu, Xiaohui Cheng, Yang Yang, Yan Liu, Xiangyang Xie, Zhiping Li, Hui Zhang, Xingguo Mei
Combination of metolazone (0.5 mg) and valsartan (80 mg) has been verified as a promising therapy treatment for hypertension. In order to facilitate to pharmacokinetic research, it needs a method for the simultaneously determination of metolazone and valsartan in biological samples. However, there are no relative reports so far. In order to facilitate to pharmacokinetic research, an on-line solid phase extraction coupled with liquid chromatography-tandem mass spectrometry method for the simultaneous determination of metolazone and valsartan in beagle dog plasma was developed and validated in this study...
October 2017: European Journal of Mass Spectrometry
https://www.readbyqxmd.com/read/29028311/radiolabeled-antibody-conjugated-manganese-oxide-nanoparticles-for-tumor-vasculature-targeted-positron-emission-tomography-and-magnetic-resonance-imaging
#15
Yonghua Zhan, Sixiang Shi, Emily B Ehlerding, Stephen A Graves, Shreya Goel, Jonathan W Engle, Jimin Liang, Jie Tian, Weibo Cai
Manganese oxide nanoparticles (Mn3O4 NPs) have attracted a great deal of attention in the field of biomedical imaging because of their ability to create an enhanced imaging signal in MRI as novel potent T1 contrast agents. In this study, we present tumor vasculature-targeted imaging in mice using Mn3O4 NPs through conjugation to the anti-CD105 antibody TRC105 and radionuclide copper-64 ((64)Cu, t1/2: 12.7 h). The Mn3O4 conjugated NPs, (64)Cu-NOTA-Mn3O4@PEG-TRC105, exhibited sufficient stability in vitro and in vivo...
October 13, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/29028117/comparison-of-weight-based-dosing-strategies-for-intravenous-immunoglobulin-in-patients-with-hematologic-malignancies
#16
Sarah E Stump, Allison J Schepers, Alexis R Jones, Maurice D Alexander, Jessica J Auten
STUDY OBJECTIVE: Intravenous immunoglobulin (IVIG) is a weight-based therapy used to treat and prevent infections in patients with hematologic malignancies. Traditionally, IVIG doses have been calculated using actual body weight (ABW). However, limited pharmacokinetic (PK) data suggest dosing strategies using ideal body weight (IBW) or adjusted body weight (adjBW) may be appropriate given the small volume of distribution of IVIG. The objective of this study was to compare the effectiveness of using a precision-dosing strategy (IBW or adjBW) to a traditional-dosing strategy (ABW) for IVIG in patients with hematologic malignancies or those undergoing hematopoietic stem cell transplant, as well as to perform an IVIG drug use analysis...
October 13, 2017: Pharmacotherapy
https://www.readbyqxmd.com/read/29027832/clinical-evaluation-of-p-glycoprotein-inhibition-by-venetoclax-a-drug-interaction-study-with-digoxin
#17
Manoj S Chiney, Rajeev M Menon, Orlando F Bueno, Bo Tong, Ahmed Hamed Salem
1. Venetoclax is a novel, small molecule B-cell lymphoma-2 (BCL-2) inhibitor that has demonstrated clinical efficacy in a variety of haematological malignancies. Since venetoclax is an inhibitor of P glycoprotein (P-gp) transporter, a study was conducted in healthy, female volunteers to evaluate the effect of venetoclax on the pharmacokinetics of digoxin, a P-gp probe substrate. 2. Volunteers received a single oral dose of digoxin (0.5 mg) with or without a single oral dose of venetoclax (100  mg). Serial blood samples were obtained for pharmacokinetic assessments of digoxin and venetoclax and serial urine samples were obtained for measurement of digoxin concentrations...
October 13, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29027831/evaluation-of-brain-targeting-in-rats-of-salvianolic-acid-b-nasal-delivery-by-the-microdialysis-technique
#18
Suiling Zhang, Yajun Shi, Lizhi Tang, Jing Wang, Dongyan Guo, Mei Wang, Xiaofei Zhang
The purpose of this study was to investigate the biodistribution of Salvianolic acid B in rats blood and brain after intranasal administration and explore its feasibility and evaluate its brain targeting effect. The concentration of Salvianolic acid B in blood and brain following nasal administration (32 mgċkg(-1)) was measured combining with microdialysis sampling and liquid chromatograph-mass spectrometer/MS detection technology. After the microdialysis samples were corrected with in vivo recoveries, the pharmacokinetic parameters were obtained by using non-compartment model and the brain targeting evaluated by the value of drug targeting index (DTI)...
October 13, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29027677/comparison-of-plasma-pharmacokinetics-of-tanreqing-solution-between-intratracheal-aerosolization-and-intravenous-injection-in-rats
#19
Cui Li, Siyu Liu, Gan Luo, Guohua Wang, Baoxian Zhang, Qixia Nie
A rapid ultra high performance liquid chromatography tandem mass spectrometry method was developed for the simultaneous analysis of baicalin, oroxylin A-7-O-β-D-glucoronide and chlorogenic acid in rats plasma, and it was applied to comparison of pharmacokinetics of Tanreqing solution between intratracheal aerosolization and intravenous injection. Results of the analytical method validation assay showed high sensitivity, accuracy and suitable recovery. Results of pharmacokinetics showed a similar decline phase for baicalin, oroxylin A-7-O-β-D-glucoronide and chlorogenic acid in two different delivery routes...
October 13, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/29027654/pharmacokinetic-drug-drug-interactions-in-the-intensive-care-unit-single-centre-experience-and-literature-review
#20
Piotr Łój, Aleksanda Olender, Weronika Ślęzak, Łukasz J Krzych
BACKGROUND: Drug-drug interactions constitute a serious health hazard in everyday clinical practice in critically ill patients. Drug-drug interactions may be pharmacokinetic or pharmacodynamic in their nature. We aimed to investigate the quantity and quality of possible drug-drug interactions, and their possible side effects in intensive care unit patients in a 12-month period. METHODS: This retrospective study covered data on pharmacological treatment of 43 consecutive patients (11 females, 32 males) aged 62 ± 15 years, hospitalized between January 2015 and February 2016...
October 13, 2017: Anaesthesiology Intensive Therapy
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