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Dialysis of drugs

Zackary M Herbst, Sayaka Shibata, Erkang Fan, Michael H Gelb
An inexpensive, in-house made microdialysis device is described that is suitable for measuring the binding of small molecules including drug candidates to serum proteins or other macromolecules. The device is based on the standard equilibrium dialysis method to measure the fraction of low molecular weight compound bound to proteins. It is constructed from a standard polypropylene 96-well plate, dialysis tubing, and low viscosity epoxy resin. The device can be readily prepared for a small fraction of the cost of a commercial, multichamber microdialysis device...
March 8, 2018: ACS Medicinal Chemistry Letters
Yoshitaka Isaka, Hideki Fujii, Yoshihiro Tsujimoto, Satoshi Teramukai, Takayuki Hamano
BACKGROUND: In dialysis patients, mortality risk due to cardiovascular diseases is remarkably high and prognosis is poor; coronary artery calcification is considered one of the major contributing factors. It is known that hyperphosphatemia is associated with coronary artery calcification. Therefore, controlling serum phosphate level and thereby mitigating vascular calcification could improve the poor prognosis of dialysis patients. However, the optimal phosphate level in dialysis patients remains unknown; hence, this study was planned to compare the effects of two types of non-calcium-based phosphate binders, and examine the effect of strict control of phosphate on coronary artery calcification...
March 13, 2018: Clinical and Experimental Nephrology
Boshra Amiri, Hasan Ahmadvand, Ali Farhadi, Aazam Najmafshar, Mohsen Chiani, Dariush Norouzian
Vinblastine (VB), as a chemotherapeutic agent, is widely used in treatment of different types of cancer. However, its clinical application is limited due to its low water solubility, side effects and multidrug resistance. The aim of this study was to increase the therapeutic efficacy of VB using drug delivery systems. For this purpose, a PEGylated niosomal formulation of vinblastine (Pn-VB) was prepared by thin film hydration method and physicochemically characterized. Drug release pattern was performed by dialysis diffusion method...
March 13, 2018: Drug Development and Industrial Pharmacy
Ali Riza Ucar, Erol Demir, Mehmet Sukru Sever
Progress in patient care and immunosuppressive medications has resulted in improved allograft survival in the early posttransplant period; however, substantial graft loss continues in the long term. Therefore, the number of dialysis patients with failed allografts is increasing progressively. These patients have a worse prognosis than naive dialysis patients. Cardiovascular causes are the leading cause of death, followed by infections and malignancies. Delay in return to dialysis, a chronic inflammatory state, infections, and cancer are contributing factors to mortality, whereas type of dialysis modality does not have a significant effect on outcomes...
March 2018: Experimental and Clinical Transplantation
Akhila Jose, Mrudula Surendran, Sajid Fazal, Bindhu-Paul Prasanth, Deepthy Menon
This work reports the potential of iron quantum clusters (FeQCs) as a hyperthermia agent for cancer, by testing its in-vitro response to shortwave (MHz range), radiofrequency (RF) waves non-invasively. Stable, fluorescent FeQCs of size ∼1 nm prepared by facile aqueous chemistry from endogenous protein haemoglobin were found to give a high thermal response, with a ΔT ∼50 °C at concentrationsas low as165 μg/mL. The as-prepared nanoclusters purified by lyophilization as well as dialysis showed a concentration, power and time-dependent RF response, with the lyophilized FeQCs exhibiting pronounced heating effects...
February 27, 2018: Colloids and Surfaces. B, Biointerfaces
Antonio Bellasi, Luigi Morrone, Maria Cristina Mereu, Carlo Massimetti, Elena Pelizzaro, Giuseppe Cianciolo, Marzia Pasquali, Vincenzo Panuccio
We herein report on a nationwide survey conducted in Italy to investigate the use of parathyroidectomy (PTX). In spite of the availability of newer and more effective drugs to control chronic kidney disease mineral bone disorder (CKD-MBD) biochemical abnormalities, PTX still remains a resource for nephrologists to use. However, observational analyses suggest that in recent years there has been a constant decline in the number of patients undergoing PTX. The reasons are not clear, though the increasing age and number of comorbidities of dialysis patients may partly explain this trend...
March 7, 2018: Journal of Nephrology
Zhi-Bin Zhao, Jie Long, Yang-Yang Zhao, Jing-Bo Yang, Wei Jiang, Qing-Zhi Liu, Kai Yan, Liang Li, Yu-Cai Wang, Zhe-Xiong Lian
Sorafenib is a kinase inhibitor approved for the treatment of primary kidney cancer, advanced primary liver cancer, and radioactive iodine resistant advanced thyroid carcinoma. However, sorafenib usually causes serious side effects, which limit its antitumor effect. Nanoparticle based drug delivery systems have been widely used to enhance the therapeutic effects and reduce the side effects of this drug by the enhanced permeability and retention (EPR) effect. Herein, to improve the therapeutic effect of sorafenib, we developed poly(ethylene glycol)-b-poly(lactic acid-co-glycolic acid) (PEG-PLGA) based nanoparticles by a dialysis method for sorafenib encapsulation...
March 7, 2018: Biomaterials Science
Houfu Liu, Yan Chen, Liang Huang, Xueying Sun, Tingting Fu, Shengqian Wu, Xiaoyan Zhu, Wei Zhen, Jihong Liu, Gang Lu, Wei Cai, Ting Yang, Wandong Zhang, Xiaohong Yu, Zehong Wan, Jianfei Wang, Scott G Summerfield, Kelly Dong, Georg C Terstappen
Little is known about the impact of the blood-nerve barrier (BNB) on drug distribution into peripheral nerves. In this study, we examined the peripheral nerve penetration of 11 small molecule drugs possessing diverse physicochemical and transport properties and ProTx-II, a tarantula venom peptide with molecular weight of 3826 daltons, in rats. Each drug was administered as constant rate intravenous infusion for 6 h (small molecules) or 24 h (ProTx-II). Blood and tissues including brain, spinal cord, sciatic nerve, and dorsal root ganglion (DRG) were collected for drug concentration measurements...
March 6, 2018: Journal of Pharmacology and Experimental Therapeutics
Eduardo C Gomes, Diego R Falci, Pedro Bergo, Alexandre P Zavascki, Maria Helena Rigatto
OBJECTIVES: To evaluate the impact of polymyxin B (PMB)- associated Acute Kidney Injury (AKI) in 1-year mortality and renal function recovery. METHODS: Patients >18 years old who survived the first 30-days after PMB therapy were followed for 1-year. The impact of AKI and Renal Failure (using RIFLE score) in 1-year mortality was analyzed, along with other confounding variables. Variables with a P value ≤0.2 were included in a forward stepwise Cox regression model...
March 1, 2018: International Journal of Antimicrobial Agents
N Segaud, I Legroux, M Hazzan, C Noel, B Cortet
INTRODUCTION: In renal transplant patients, bone loss may be related to the drugs patients are taking but also to their past history of chronic kidney disease. The purpose of this study was to assess changes in BMD 2 years after an initial assessment (performed 9 months post transplantation) and the factors associated with these changes. METHODS: This longitudinal study included patients who had undergone a renal transplantation between 2005 and 2011, and who were followed up at the Lille Regional University Hospital...
March 2, 2018: Osteoporosis International
Fazhan Wang, Xingting Bao, Aiping Fang, Huili Li, Yang Zhou, Yongmei Liu, Chunling Jiang, Jinhui Wu, Xiangrong Song
Novel ocular drug delivery systems (NODDSs) remain to be explored to overcome the anatomical and physiological barriers of the eyes. This study was to encapsulate brinzolamide (BRZ)-hydropropyl-β-cyclodextrin (HP-β-CD) inclusion complex (HP-β-CD/BRZ) into nanoliposomes and investigate its potential as one of NODDS to improve BRZ local glaucomatous therapeutic effect. HP-β-CD/BRZ was firstly prepared to enhance the solubility of poorly water-soluble BRZ. The HP-β-CD/BRZ loaded nanoliposomes (BCL) were subsequently constructed by thin-film dispersion method...
2018: Frontiers in Pharmacology
Joseph Meletiadis, Maria Siopi, Athanassios Tsakris, Johan W Mouton, Spyros Pournaras
The lack of a quantifiable marker for echinocandins activity hinders in vitro PK/PD studies for Aspergillus spp. We developed an in vitro PK/PD model simulating anidulafungin pharmacokinetics and assessing its pharmacodynamics against A. fumigatus with a new easily quantifiable, sensitive and reproducible marker. Two clinical A. fumigatus isolates previously used in animals (AZN8196,V52-35) with identical anidulafungin EUCAST (0.03 μg/ml) and CLSI (0.015 μg/ml) MEC and one (AFU79728) with MEC>16 μg/ml were tested in a two-compartment PK/PD dialysis/diffusion closed model containing a dialysis membrane tube (DM) inoculated with 103 cfu/mL...
February 20, 2018: Antimicrobial Agents and Chemotherapy
Panagiotis I Georgianos, Eleni Champidou, Vassilios Liakopoulos, Elias V Balaskas, Pantelis E Zebekakis
In the era of newly introduced hypertension guidelines recommending lower blood pressure (BP) targets for drug-treated hypertensives, the necessity for optimized management of hypertension becomes even more urgent. The concept of home BP-guided antihypertensive therapy is for long suggested as a simple and feasible approach to improve BP control rates and optimize the management of hypertension. Home BP-guided antihypertensive therapy is particularly applicable to hypertensives with chronic kidney disease (CKD) for several reasons including the following: (1) difficult-to-control BP and high BP variability in the CKD setting; (2) poor accuracy of office BP in determining hypertension control status and detecting "white-coat" and "masked" hypertension; (3) poor value of routine office BP recordings in predicting the longitudinal progression of target-organ damage; and (4) superiority of home BP over office BP recordings in prognosticating the risk of incident end-stage renal disease or death...
February 10, 2018: Journal of the American Society of Hypertension: JASH
Nilima T Pandya, Parva Jani, Jigar Vanza, Hemal Tandel
The aim of the current investigation was to develop solid lipid nanoparticles of olmesartan medoxomil using hot homogenization method to improve its oral bioavailability. Central composite design was applied to optimize the formulation variables; lipid X1 (Glyceryl monostearate) and surfactant X2 (Poloxamer: Tween 80). The particle sizes were in the nanometer range and spherical shaped for all prepared solid lipid nanoparticles formulations and the zeta potential absolute values were high, predicting good long-term stability...
February 9, 2018: Colloids and Surfaces. B, Biointerfaces
Seiko Ishikawa, Shotaro Naito, Soichiro Iimori, Daiei Takahashi, Moko Zeniya, Hidehiko Sato, Naohiro Nomura, Eisei Sohara, Tomokazu Okado, Shinichi Uchida, Tatemitsu Rai
INTRODUCTION: Sarcopenia, the age-related loss of muscle mass and function, frequently accompanies chronic kidney disease. The aim of this study was to clarify the prevalence and the risk factors for sarcopenia among patients with non-dialysis-dependent chronic kidney disease (NDD-CKD), focusing on the use of drugs. METHODS: We conducted a cross-sectional analysis on a cohort of 260 patients with NDD-CKD in a university hospital, recruited between June 2016 and March 2017...
2018: PloS One
Keith A Riccardi, Sangwoo Ryu, Jian Lin, Phillip Yates, David A Tess, Rui Li, Dhirender Singh, Brian R Holder, Brendon Kapinos, George Chang, Li Di
Fraction unbound (fu) of liver tissue, hepatocytes and other cell types is an essential parameter used to estimate unbound liver drug concentration and intracellular free drug concentration. Fu,liver and fu,cell are frequently measured in multiple species and cell types in drug discovery and development for various applications. A comparison study of 12 matrices for fu,liver and fu,cell of hepatocytes in five different species (mouse, rat, dog, monkey and human), as well as fu,cell of Huh7 and HEK-293 cell lines, was conducted for 22 structurally diverse compounds with the equilibrium dialysis method...
February 2, 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
X Yang, S Y Qian, Y M Zhu, X Xu, C F Liu, F Xu, X X Ren, Y Wang, Y C Zhang, G P Lu
Objective: To investigate the current application status of continuous blood purification (CBP) technology and equipment in pediatric intensive care unit (PICU) in China. Methods: A cross-sectional survey was conducted to understand the current popularization of CBP technology and equipment, the management of CBP equipment and consumables, and the application of CBP in different diseases. A questionnaire named Application Status of Continuous Blood Purification Technology was applied. Children's hospitals and polyclinic hospitals with the pediatric qualification (pediatric emergency or critical care unit members of Chinese Medical Association and Chinese Medical Doctor Association) were selected...
February 2, 2018: Zhonghua Er Ke za Zhi. Chinese Journal of Pediatrics
Takehide Umeda, Taro Minami, Keith Bartolomei, Eleanor Summerhill
A 54-year-old woman with type 2 diabetes mellitus, hypertension, and peripheral vascular disease developed life-threatening lactic acidosis during treatment with metformin for type 2 diabetes. The woman received metformin at 1000 mg orally twice a day for type 2 diabetes. She presented to our emergency department with a 3-day history of severe watery diarrhea, nausea, and vomiting. Her grandson whom she cared for had gastroenteritis several days prior to the onset of her symptoms. She was confused and hypotensive with a blood pressure of 70/39 mmHg...
February 9, 2018: Drug Safety—Case Reports
Aart J van der Molen, Peter Reimer, Ilona A Dekkers, Georg Bongartz, Marie-France Bellin, Michele Bertolotto, Olivier Clement, Gertraud Heinz-Peer, Fulvio Stacul, Judith A W Webb, Henrik S Thomsen
OBJECTIVES: The Contrast Media Safety Committee (CMSC) of the European Society of Urogenital Radiology (ESUR) has updated its 2011 guidelines on the prevention of post-contrast acute kidney injury (PC-AKI). The results of the literature review and the recommendations based on it, which were used to prepare the new guidelines, are presented in two papers. AREAS COVERED IN PART 2: Topics reviewed include stratification of PC-AKI risk, the need to withdraw nephrotoxic medication, PC-AKI prophylaxis with hydration or drugs, the use of metformin in diabetic patients receiving contrast medium and the need to alter dialysis schedules in patients receiving contrast medium...
February 7, 2018: European Radiology
Markus Ketteler, Christoph Wanner
SGLT2-INHIBITION IN DIABETIC AND NON-DIABETIC KIDNEY DISEASE:  The CANVAS Program Collaborative Group study confirmed nephroprotective actions by canagliflocin comparable to empagliflozin as published in the EMPA-REG Outcome study. Treatment with Liraglutide (LEADER study) also suggests nephroprotection via albuminuria reduction a decreased eGFR decline in subgroups and depending on stages of diabetic nephropathy. KDIGO CKD-MBD GUIDELINE UPDATE 2017:  In July 2017, an update of the KDIGO (Kidney Disease: Improving Global Outcomes) 2009 guideline on diagnostic and treatment chronic kidney disease - mineral and bone disorders (CKD-MBD) was published...
February 2018: Deutsche Medizinische Wochenschrift
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