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Felodipine

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https://www.readbyqxmd.com/read/29331439/interactions-of-dimethylaminoethyl-methacrylate-copolymer-with-non-acidic-drugs-demonstrated-high-solubilization-in-vitro-and-pronounced-sustained-release-in-vivo
#1
Wiebke Saal, Nicole Wyttenbach, Jochem Alsenz, Martin Kuentz
Recent work demonstrated remarkable solubilization effects of methacrylate-copolymer Eudragit EPO (EPO) not only with acidic drugs but interestingly also with poorly soluble basic compounds. The current work studied EPO-mediated solubilization effects first in vitro using felodipine (FLP) and tamoxifen (TMX) as model compounds. EPO-containing solutions were subsequently compared in a rat pharmacokinetic study against reference solutions and suspensions. Surprisingly, solution formulations with EPO did not result in an increased relative oral bioavailability...
January 10, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/29309155/mutual-impact-of-phase-separation-crystallization-and-water-sorption-in-amorphous-solid-dispersions
#2
Christian Luebbert, Maximilian Wessner, Gabriele Sadowski
The molecular integration of poorly-water-soluble active pharmaceutical ingredients (APIs) in a suitable polymeric matrix is a possible approach to enhance the dissolution behavior and solubility of these APIs. Like all newly-developed pharmaceutical formulations, these formulations (often denoted as amorphous solid dispersions (ASDs)) need to undergo storage stability tests at defined relative humidity (RH) and temperature conditions. In a previous work (Int. J. Pharm. 532 (2017) 635-646), it was shown that thermodynamic modeling can be successfully used to predict the long-term stability of ASDs against API crystallization and moisture-induced amorphous-amorphous phase separation (MIAPS)...
January 8, 2018: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29305982/melt-extrusion-process-for-adjusting-drug-release-of-poorly-water-soluble-drug-felodipine-using-different-polymer-matrices
#3
Eirini Palazi, Evangelos Karavas, Panagiotis Barmpalexis, Margaritis Kostoglou, Stavroula Nanaki, Evi Christodoulou, Dimitrios N Bikiaris
The purpose of the present study was to use commercial available polymers like PVP/PEG, soluplus® and kollidon® SR to prepare immediate and sustained release formulations of felodipine by hot melt mixing method. Solid dispersions containing 5, 10, 20 and 30wt% drug have been prepared in a Haake-Buchler Reomixer at melt temperatures 130°C and mixing times 10min. As was found from DSC and XDR studies completely amorphous and miscible solid dispersions can be prepared. In all cases a single glass transition was recorded, which is depending from the used drug amount...
January 3, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29302871/screen-for-inhibitors-of-crystal-growth-to-identify-desirable-carriers-for-amorphous-solid-dispersions-containing-felodipine
#4
Jinping Fu, Lin Cui, Congbin Yang, Hui Xiong, Guobin Ren, Xingyuan Ma, Qiufang Jing, Fuzheng Ren
The solvent-shift method was used to identify appropriate polymers that inhibit the growth of felodipine crystals by monitoring particle size in supersaturated drug solutions in the presence of different polymers. We speculated that there would be an intermolecular interaction between the selected polymer (zein) and felodipine by extrapolating the inhibitory effect on crystal growth and then used the selected polymer as a carrier to prepare solid dispersions. The formulations were characterized by crystalline properties, thermodynamics of mixing, dissolution behavior, and physical stability...
January 4, 2018: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29232282/selected-food-herb-drug-interactions-mechanisms-and-clinical-relevance
#5
Cecilia N Amadi, Amaka A Mgbahurike
BACKGROUND: Food/Herb-drug interactions have become a major problem in health care. These interactions can lead to loss of therapeutic efficacy or toxic effects of drugs. AREAS OF UNCERTAINTY: To probe the clinical relevance of such interactions, the impact of food/herb intake on the clinical effects of drug administration has to be evaluated. Failure to identify and efficiently manage food-drug interactions can lead to serious consequences. A comprehensive knowledge of the mechanisms that underpin variability in disposition will help optimize therapy...
November 22, 2017: American Journal of Therapeutics
https://www.readbyqxmd.com/read/29205040/a-new-method-of-constructing-drug-polymer-temperature-composition-phase-diagram-relevant-to-the-hot-melt-extrusion-platform
#6
Yiwei Tian, David S Jones, Conor Donnelly, Timothy Brannigan, Shu Li, Gavin P Andrews
Current experimental methodologies used to determine the thermodynamic solubility of an API within a polymer typically involves establishing the dissolution/melting endpoint of the crystalline API within a physical mixture, or through the use of the glass transition temperature measurement of a de-mixed amorphous solid dispersion. The measurable "equilibrium" points for solubility are normally well above the glass transition temperature of the system meaning extrapolation is required in order to predict the drug solubility at pharmaceutical relevant temperatures...
December 5, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29204927/augmented-bioavailability-of-felodipine-through-an-%C3%AE-linolenic-acid-based-microemulsion
#7
Mahendra Singh, Jovita Kanoujia, Poonam Parashar, Malti Arya, Chandra B Tripathi, V R Sinha, Shailendra K Saraf, Shubhini A Saraf
The oral bioavailability of felodipine, a dihydropyridine calcium channel antagonist, is about 15%. This may be due to poor water solubility, and a lower intestinal permeability than a BCS class I drug, and hepatic first-pass metabolism of the drug. Many drugs are unpopular due to solubility issues. The goal of this study was to develop and optimize a felodipine-containing microemulsion to improve the intestinal permeability and bioavailability of the drug. The felodipine microemulsions were developed with the selected components, i...
December 4, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/29192124/drugs-and-scaffold-that-inhibit-cytochrome-p450-27a1-cyp27a1-in-vitro-and-in-vivo
#8
Morrie Lam, Natalia Mast, Irina Pikuleva
Cytochrome P450 27A1 (CYP27A1) is a ubiquitous enzyme that hydroxylates cholesterol and other sterols. Complete CYP27A1 deficiency due to genetic mutations is detrimental to human health, whereas 50% of activity retention is not and does not affect the whole body cholesterol levels. CYP27A1 is considered as a potential therapeutic target in breast cancer and age-related neurodegenerative diseases; however CYP27A1 inhibition should be 50%. Herein, 131 pharmaceuticals were tested for their effect on CYP27A1-mediated cholesterol 27-hydroxylation by in vitro enzyme assay...
November 30, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/29133204/investigating-phase-separation-in-amorphous-solid-dispersions-via-raman-mapping
#9
Christian Luebbert, Christian Klanke, Gabriele Sadowski
The bioavailability of poorly-water-soluble active pharmaceutical ingredients (APIs) can be significantly improved by so-called amorphous solid dispersions (ASDs). However, the long-term stability of ASDs might be impaired by API recrystallization and/or amorphous phase separation (APS). So far, no methods have been reported to quantify APS in ASDs. In this work, phase-separation kinetics as well as the compositions of the two amorphous phases evolving due to APS were quantitatively determined for the first time using confocal Raman spectroscopy...
November 11, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29107791/complexes-of-felodipine-nanoparticles-with-zein-prepared-using-a-dual-shift-technique
#10
Fuzheng Ren, Jinping Fu, Hui Xiong, Lin Cui, Guobin Ren, Haiying Guan, Qiufang Jing
To improve the dissolution of felodipine, felodipine-zein complexes were prepared using a dual shift technique, with zein as both stabilizer and carrier. The complexes were characterized by particle size, zeta potential, morphology, crystalline properties and release behavior. The complexes could be prepared in high yield and showed good redispersibility. The mean diameters of the felodipine particles in complexes were 150-300 nm, with negative zeta potentials of -30 mV to -25 mV after re-hydration, and the particle sizes of the complexes were in the range 10-80 μm...
October 28, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29050316/pharmacokinetics-and-drug-drug-interaction-between-enalapril-enalaprilat-and-felodipine-extended-release-er-in-healthy-subjects
#11
Dai Li, Sumei Xu, Yulu Wang, Dan Li, Xiaomin Li, Jing Pan, Pingsheng Xu
Since angiotensin-converting enzyme (ACE) inhibitors and calcium antagonists have complimentary mechanisms of action, enalapril, an ACE inhibitor, is used in combination with felodipine, a vascular selective dihydropyridine calcium antagonist, for the treatment of hypertension. The present study was designed to investigate the possible drug-drug interaction between these two agents in Chinese healthy subjects. A randomized, open-label, multiple-dose, 3-treatment, 3-period, 6-sequence cross-over study enrolling 12 healthy subjects (six male and six female subjects) was performed...
September 19, 2017: Oncotarget
https://www.readbyqxmd.com/read/29043811/investigation-of-the-intra-and-interlaboratory-reproducibility-of-a-small-scale-standardized-supersaturation-and-precipitation-method
#12
Jakob Plum, Cecilie M Madsen, Alexandra Teleki, Jan Bevernage, Claudia da Costa Mathews, Eva M Karlsson, Sara Carlert, Rene Holm, Thomas Müller, Wayne Matthews, Alice Sayers, Krista Ojala, Konstantin Tsinsman, Ram Lingamaneni, Christel As Bergström, Thomas Rades, Anette Müllertz
The high number of poorly water-soluble compounds in drug development has increased the need for enabling formulations to improve oral bioavailability. One frequently applied approach is to induce supersaturation at the absorptive site, e.g., the small intestine, increasing the amount of dissolved compound available for absorption. However, due to the stochastic nature of nucleation, supersaturating drug delivery systems may lead to inter- and intrapersonal variability. The ability to define a feasible range with respect to the supersaturation level is a crucial factor for a successful formulation...
November 7, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29041879/-adherence-to-therapy-in-the-outpatient-setting-the-ability-to-identify-and-assess-the-effectiveness-of-therapy
#13
T F Ageev, D M Smirnova, D A Deev, V T Fofanova
AIM: To assess adherence of patients to antihypertensive therapy, to determine the role of various factors affecting adherence to treatment by outpatients, and to assess clinical efficacy of a calcium antagonist felodipine. MATERIAL AND METHODS: We examined 5 474 women and men aged >18 years who at visit to a local internist had office systolic arterial pressure (AP) 140-179 and diastolic AP up to 100 mm Hg both on and without hypotensive therapy. Examination included registration of risk factors and concomitant therapy...
July 2017: Kardiologiia
https://www.readbyqxmd.com/read/29031978/monitoring-the-phase-behavior-of-supersaturated-solutions-of-poorly-water-soluble-drugs-using-fluorescence-techniques
#14
Francesco Tres, Stephen D Hall, Michael A Mohutsky, Lynne S Taylor
Phase transformations of poorly water-soluble drugs, in low concentration, supersaturated aqueous solutions are of considerable interest. Herein, fluorescence lifetime and steady-state fluorescence spectroscopy were employed to investigate the fluorescence properties of the autofluorescent compound, felodipine (a 1,4-dihydropyridine calcium channel blocker), when present as free drug in solution, drug-rich aggregates and crystals. Measurements were also performed in the absence and presence of liver microsomes...
October 11, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28987539/statistical-investigation-of-the-full-concentration-range-of-fasted-and-fed-simulated-intestinal-fluid-on-the-equilibrium-solubility-of-oral-drugs
#15
Jeremy Perrier, Zhou Zhou, Claire Dunn, Ibrahim Khadra, Clive G Wilson, Gavin Halbert
Upon oral administration the solubility of a drug in intestinal fluid is a key property influencing bioavailability. It is also recognised that simple aqueous solubility does not reflect intestinal solubility and to optimise in vitro investigations simulated intestinal media systems have been developed. Simulated intestinal media which can mimic either the fasted or fed state consists of multiple components each of which either singly or in combination may influence drug solubility, a property that can be investigated by a statistical design of experiment technique...
October 5, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28986196/effect-of-composition-of-simulated-intestinal-media-on-the-solubility-of-poorly-soluble-compounds-investigated-by-design-of-experiments
#16
Cecilie Maria Madsen, Kung-I Feng, Andrew Leithead, Nicole Canfield, Søren Astrup Jørgensen, Anette Müllertz, Thomas Rades
The composition of the human intestinal fluids varies both intra- and inter-individually. This will influence the solubility of orally administered drug compounds, and hence, the absorption and efficacy of compounds displaying solubility limited absorption. The purpose of this study was to assess the influence of simulated intestinal fluid (SIF) composition on the solubility of poorly soluble compounds. Using a Design of Experiments (DoE) approach, a set of 24 SIF was defined within the known compositions of human fasted state intestinal fluid...
October 3, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28971609/coffee-inhibition-of-cyp3a4-in%C3%A2-vitro-was-not-translated-to-a-grapefruit-like-pharmacokinetic-interaction-clinically
#17
George K Dresser, Brad L Urquhart, Julianne Proniuk, Alvin Tieu, David J Freeman, John Malcolm Arnold, David G Bailey
Grapefruit can augment oral medication bioavailability through irreversible (mechanism-based) inhibition of intestinal CYP3A4. Supplementary data from our recent coffee-drug interaction clinical study showed some subjects had higher area under the plasma drug concentration - time curve (AUC) and plasma peak drug concentration (Cmax) of the CYP3A4 probe felodipine compared to aqueous control. It was hypothesized that coffee might interact like grapefruit in responsive individuals. Beans from six geographical locations were consistently brewed into coffee that was separated chromatographically to a methanolic fraction for in vitro inhibition testing of CYP3A4 metabolism of felodipine at 1% coffee strength...
October 2017: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/28867448/moisture-induced-phase-separation-and-recrystallization-in-amorphous-solid-dispersions
#18
Christian Luebbert, Gabriele Sadowski
Active Pharmaceutical Ingredients (APIs) are often dissolved in polymeric matrices to control the gastrointestinal dissolution and to stabilize the amorphous state of the API. During the pharmaceutical development of new formulations, stability studies via storage at certain temperature and relative humidity (RH) have to be carried out to verify the long-term thermodynamic stability of these formulations against unwanted recrystallization and moisture-induced amorphous-amorphous phase separation (MIAPS). This study focuses on predicting the MIAPS of API/polymer formulations at elevated RH...
September 1, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28791379/felodipine-inhibits-ox-ldl-induced-reactive-oxygen-species-production-and-inflammation-in-human-umbilical-vein-endothelial-cells
#19
Jie Qi, Jian-Bao Zheng, Wen-Ting Ai, Xiao-Wei Yao, Lei Liang, Gong Cheng, Xi-Ling Shou, Chao-Feng Sun
Oxidative stress and inflammation are involved in the pathogenesis of atherosclerosis. Calcium channel blockers (CCBs) inhibit the development of atherosclerosis, although the underlying molecular basis has not been completely elucidated. The present study was designed to investigate the effects of felodipine, a CCB, on inflammation and oxidative stress in human umbilical vein endothelial cells (HUVECs) and to examine the underlying mechanisms of action. Oxidized low‑density lipoprotein (ox‑LDL) was used to induce an inflammatory response in HUVECs...
October 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28749696/influence-of-physiological-gastrointestinal-surfactant-ratio-on-the-equilibrium-solubility-of-bcs-class-ii-drugs-investigated-using-a-four-component-mixture-design
#20
Zhou Zhou, Claire Dunn, Ibrahim Khadra, Clive G Wilson, Gavin W Halbert
The absorption of poorly water-soluble drugs is influenced by the luminal gastrointestinal fluid content and composition, which control solubility. Simulated intestinal fluids have been introduced into dissolution testing including endogenous amphiphiles and digested lipids at physiological levels; however, in vivo individual variation exists in the concentrations of these components, which will alter drug absorption through an effect on solubility. The use of a factorial design of experiment and varying media by introducing different levels of bile, lecithin, and digested lipids has been previously reported, but here we investigate the solubility variation of poorly soluble drugs through more complex biorelevant amphiphile interactions...
August 22, 2017: Molecular Pharmaceutics
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