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Felodipine

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https://www.readbyqxmd.com/read/29133204/investigating-phase-separation-in-amorphous-solid-dispersions-via-raman-mapping
#1
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 10, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29107791/complexes-of-felodipine-nanoparticles-with-zein-prepared-using-a-dual-shift-technique
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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
#8
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
#9
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
#10
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
#11
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
#12
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
https://www.readbyqxmd.com/read/28730199/the-amorphous-state-first-principles-derivation-of-the-gordon-taylor-equation-for-direct-prediction-of-the-glass-transition-temperature-of-mixtures-estimation-of-the-crossover-temperature-of-fragile-glass-formers-physical-basis-of-the-rule-of-2-3
#13
Peter J Skrdla, Philip D Floyd, Philip C Dell'Orco
Predicting the glass transition temperature (Tg) of mixtures has applications that span across industries and scientific disciplines. By plotting experimentally determined Tg values as a function of the glass composition, one can usually apply the Gordon-Taylor (G-T) equation to determine the slope, k, which subsequently can be used in Tg predictions. Traditionally viewed as a phenomenological/empirical model, this work proposes a physical basis for the G-T equation. The proposed equations allow for the calculation of k directly and, hence, they determine/predict the Tg values of mixtures algebraically...
August 9, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/28690250/simultaneous-determination-of-felodipine-and-metoprolol-in-beagle-dog-plasma-by-online-spe-lc-ms-ms-and-its-application-in-a-pharmacokinetic-study
#14
Meiling Chen, Jiezhao Zhou, Le Mei, Fanglin Yu, Xiangyang Xie, Yan Liu, Yang Yang, Ying Li, Xingguo Mei
In order to overcome deficiencies for simultaneously determining felodipine (FDP) and metoprolol (MPL) with low recovery and low sensitivity, a new online SPE coupled with the liquid chromatography-tandem mass spectrometry (SPE-LC-MS/MS) method for the simultaneous quantitative determination of FDP and MPL in beagle dog plasma was established. The SPE extraction of FDP and MPL was performed on a Retain PEP Javelin column (10 × 2.1 mm, 5 μm), while the chromatographic separation was achieved on a ZORBAX SB-C18 (50 × 2...
2017: Analytical Sciences: the International Journal of the Japan Society for Analytical Chemistry
https://www.readbyqxmd.com/read/28625814/a-multi-technique-characterization-of-the-stability-of-surfactant-containing-solid-dispersion-based-buccal-patches-prepared-by-hot-melt-injection-moulding
#15
Muqdad Alhijjaj, Peter Belton, Sheng Qi
This study investigates the stability of typically complex multi-component hydrophilic solid dispersions that could be used in a clinical application. Felodipine solid dispersions in two types of blends consisting of PEG, PEO and Tween 80 or Vit E TPGS were prepared by hot melt-injection moulding (HMIM) across a range of drug loadings and subjected to a range of storage conditions. Microscopy, thermal analysis, spectroscopy and powder X-ray diffraction were used to characterize the systems. The semi-solid surfactant TPGS showed a better solubilizing effect on the drug than the liquid surfactant Tween 80 in the fresh state and offered some degree of protection over the chemical degradation of PEG/PEO...
August 7, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28611390/protective-and-therapeutic-effect-of-felodipine-against-bleomycin-induced-pulmonary-fibrosis-in-mice
#16
Ken-Ichiro Tanaka, Tomomi Niino, Tomoaki Ishihara, Ayaka Takafuji, Takahiro Takayama, Yuki Kanda, Toshifumi Sugizaki, Fumiya Tamura, Shota Kurotsu, Masahiro Kawahara, Tohru Mizushima
Idiopathic pulmonary fibrosis (IPF) involves alveolar epithelial injury and abnormal collagen production caused by activated fibroblasts; transforming growth factor (TGF)-β1 is implicated in this activation. In this study, we screened for chemicals capable of inhibiting TGF-β1-induced collagen production in cultured fibroblasts from medicines already in clinical use. We selected felodipine based on its extent of collagen production inhibition, clinical safety profile, and other pharmacological activity. Felodipine is a dihydropyridine Ca(2+) channel blocker that has been used clinically to treat patients with high blood pressure...
June 13, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28560506/biomimetic-dissolution-a-tool-to-predict-amorphous-solid-dispersion-performance
#17
Michael M Puppolo, Justin R Hughey, Traciann Dillon, David Storey, Susan Jansen-Varnum
The presented study describes the development of a membrane permeation non-sink dissolution method that can provide analysis of complete drug speciation and emulate the in vivo performance of poorly water-soluble Biopharmaceutical Classification System class II compounds. The designed membrane permeation methodology permits evaluation of free/dissolved/unbound drug from amorphous solid dispersion formulations with the use of a two-cell apparatus, biorelevant dissolution media, and a biomimetic polymer membrane...
November 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28480807/tri-block-co-polymer-nanocarriers-for-enhancement-of-oral-delivery-of-felodipine-preparation-in-vitro-characterization-and-ex-vivo-permeation
#18
Sinar Sayed, Basant A Habib, Ghada M Elsayed
This study aimed to prepare, optimize and characterize novel felodipine-loaded polymeric nanomicelles, using a pluronic mixture of F127 and P123. Thin-film hydration method was adopted for the preparation of different polymeric nanomicelles (T1-T12) according to a 4(1).3(1) full factorial design. Factors studied were: Pluronic®:drug ratio (P:D ratio) (10, 20, 30 and 40 w/w) and percent of hydrophilic polymer (F127%) (33.33%, 50% and 66.67% w/w). Optimization criteria were to maximize transmittance percent (T%) and entrapment efficiency percent (EE%) and to minimize particle size (PS) and polydispersity index (PDI)...
May 25, 2017: Journal of Liposome Research
https://www.readbyqxmd.com/read/28424979/studies-on-core-shell-nanocapsules-of-felodipine-in-vitro-in-vivo-evaluations
#19
Jerome K Geroge, Priya Ranjan Prasad Verma, Jayachandran Venkatesan, Jin-Young Lee, Dong-Han Yoon, Se-Kwon Kim, Sandeep Kumar Singh
The present study aimed for in vitro-in vivo-in silico simulation studies of experimentally designed (3(2)-factorial) Capmul PG-8-cored, Eudragit RSPO-Lutrol F 127 nanocapsules to ferry felodipine using GastroPlus™. The in silico parameter sensitivity analysis for pharmacokinetic parameters was initially assessed to justify the preparation of felodipine-loaded nanocapsules (FLNs) with enhanced solubility to overcome the bioavailability issues of felodipine. The overall integrated desirability ranged between 0...
November 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28375107/formulation-evaluation-and-optimization-of-the-felodipine-nanosuspension-to-be-used-for-direct-compression-to-tablet-for-in-vitro-dissolution-enhancement
#20
Dhaval Mori, Jalpa Makwana, Ramesh Parmar, Kalpesh Patel, Jayant Chavda
The oral bioavailability of felodipine very low, nearly just 15% due to its limited solubility and high first pass metabolism. The present study was aimed to improve the rate of the dissolution of Felodipine by formulating a nano suspension of it by combination of high-speed homogenization and media milling technique. Stabilizers screened in this study were Poloxamer 401, HPMC K15M and Tween 80. Concentration of stabilizers were optimized by simplex lattice design for Mean Particle Size (MPS), Poly dispersity Index (PDI), saturation solubility (SS) and in vitro drug release in 30 min...
November 2016: Pakistan Journal of Pharmaceutical Sciences
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