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https://www.readbyqxmd.com/read/28212300/amorphous-amorphous-phase-separation-in-api-polymer-formulations
#1
Christian Luebbert, Fabian Huxoll, Gabriele Sadowski
The long-term stability of pharmaceutical formulations of poorly-soluble drugs in polymers determines their bioavailability and therapeutic applicability. However, these formulations do not only often tend to crystallize during storage, but also tend to undergo unwanted amorphous-amorphous phase separations (APS). Whereas the crystallization behavior of APIs in polymers has been measured and modeled during the last years, the APS phenomenon is still poorly understood. In this study, the crystallization behavior, APS, and glass-transition temperatures formulations of ibuprofen and felodipine in polymeric PLGA excipients exhibiting different ratios of lactic acid and glycolic acid monomers in the PLGA chain were investigated by means of hot-stage microscopy and DSC...
February 15, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28134976/multicomponent-solid-forms-of-felodipine-preparation-characterisation-physicochemical-and-in-vivo-studies
#2
Renu Chadha, Mohit Sharma, Jamshed Haneef
OBJECTIVES: This study aimed to improve biopharmaceutical parameters of the poorly soluble antihypertensive drug, felodipine, by preparing multicomponent solid forms using three coformers, viz. imidazole, nicotinamide and malonic acid. METHODS: The multicomponent solid forms were prepared by mechanochemical synthesis and characterised by various analytical techniques. These solid forms were further assessed for their physicochemical parameters. Pharmacokinetic and in-vivo antihypertensive activity was performed in rats...
March 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27987515/-study-on-the-properties-of-felodipine-solid-dispersions-prepared-by-different-technologies
#3
N Q Shi, H Zhang, Y Zhang, B Feng, Z Q Li, X R Qi
OBJECTIVE: To prepare felodipine/copovidone solid dispersions, which were made based on different preparation technologies. Insoluble felodipine was selected as the model drug in this research. This drug belonged to Biopharmaceutics Classification System II (BCSII) with insoluble property and good permeability across intestinal mucosa simultaneously. A comparative study was carried out for further investigating their corresponding pharmaceutical properties. METHODS: Felodipine/copovidone solid dispersions were achieved by four methods including spray-drying method, microwave-induced fusion quench cooling method, freeze-drying method and co-precipitation method...
December 18, 2016: Beijing da Xue Xue Bao. Yi Xue Ban, Journal of Peking University. Health Sciences
https://www.readbyqxmd.com/read/27986292/molecular-dynamics-simulation-of-amorphous-hydroxypropylmethylcellulose-and-its-mixtures-with-felodipine-and-water
#4
Tian-Xiang Xiang, Bradley D Anderson
Understanding drug-polymer molecular interactions, their miscibility, supersaturation potential, and the effects of water uptake may be invaluable for selecting amorphous polymer dispersions that can maximize the oral bioavailability of poorly water-soluble drugs. Molecular dynamics simulations were performed using a model for hydroxypropylmethylcellulose (HPMC) resembling the substitution patterns found experimentally. HPMC at low and high water contents (0.9%-23.0% wt/wt) and mixtures with a hydrophobic drug, felodipine (FEL), were constructed...
December 13, 2016: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27940083/statistical-investigation-of-simulated-fed-intestinal-media-composition-on-the-equilibrium-solubility-of-oral-drugs
#5
Zhou Zhou, Claire Dunn, Ibrahim Khadra, Clive G Wilson, Gavin W Halbert
Gastrointestinal fluid is a complex milieu and it is recognised that gut drug solubility is different to that observed in simple aqueous buffers. Simulated gastrointestinal media have been developed covering fasted and fed states to facilitate in vitro prediction of gut solubility and product dissolution. However, the combination of bile salts, phospholipids, fatty acids and proteins in an aqueous buffered system creates multiple phases and drug solubility is therefore a complex interaction between these components, which may create unique environments for each API...
March 1, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27934534/partitioning-into-colloidal-structures-of-fasted-state-intestinal-fluid-studied-by-molecular-dynamics-simulations
#6
Michael Holmboe, Per Larsson, Jamshed Anwar, Christel A S Bergström
We performed molecular dynamics (MD) simulations to obtain insights into the structure and molecular interactions of colloidal structures present in fasted state intestinal fluid. Drug partitioning and interaction were studied with a mixed system of the bile salt taurocholate (TCH) and 1,2-dilinoleoyl-sn-glycero-3-phosphocholine (DLiPC). Spontaneous aggregation of TCH and DLiPC from unconstrained MD simulations at the united-atom level using the Berger/Gromos54A7 force fields demonstrated that intermolecular hydrogen bonding between TCH molecules was an important factor in determining the overall TCH and DLiPC configuration...
December 6, 2016: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/27779454/effects-of-lercanidipine-hydrochloride-versus-felodipine-sustained-release-on-day-to-day-home-blood-pressure-variability
#7
Mengdan Xu, Ying Wu, Hao Wang, Xin Xu, Shuiping Zhao, Mei Zhang, Huigen- Jin, Jinchuan Yan, Bangning Wang, Jianbin Gong, Xiang Lu, Jianqiang Peng, Qiuyan Dai
OBJECTIVE: The objective of this study was to compare the effectiveness of lercanidipine with felodipine in patients with mild-to-moderate hypertension on day-to-day home blood pressure variability. METHODS: This is a sub-study of a multicenter, randomized, open-label, parallel group and active controlled clinical trial. Hypertensive patients aged 18-75 (i.e. diastolic blood pressure ≥90 mmHg and <110 mmHg; systolic blood pressure ≥140 mmHg and <180 mmHg) and 24 h mean BP >130/80 mmHg) were eligible for this study...
October 2016: Current Medical Research and Opinion
https://www.readbyqxmd.com/read/27754044/os-14-01-an-estimated-optimal-hypertension-level-of-goals-on-drug-therapy-from-the-fever-trial
#8
Xuezhong Zhang, Yuqing Zhang, Lisheng Liu, Alberto Zanchetti
OBJECTIVE: There is some debate as to optimal BP goals with antihypertensive treatment derived mostly in post-hoc analysis of large trials. Because there was limited number of subjects and outcomes within the larger study which may cloud the analytical accuracy of the findings. We suggest a new method to estimate the J-curve. DESIGN AND METHOD: Felodipine Event Reduction (FEVER) study randomized 9711 Chinese hypertensive patients to more or less intense anti-hypertensive treatment with 159,844 BP measurements...
September 2016: Journal of Hypertension
https://www.readbyqxmd.com/read/27732883/optical-isomers-of-dihydropyridine-calcium-channel-blockers-display-enantiospecific-effects-on-the-expression-and-enzyme-activities-of-human-xenobiotics-metabolizing-cytochromes-p450
#9
Martina Štěpánková, Kristýna Krasulová, Aneta Dořičáková, Ondřej Kurka, Pavel Anzenbacher, Zdeněk Dvořák
Dihydropyridine calcium channel blockers (CCBs) are used as anti-hypertensives and in the treatment of angina pectoris. Structurally, CCBs have at least one chiral center in the molecule, thereby existing in two or more different enantiomers. In the current paper we examined effects of benidipine, felodipine and isradipine enantiomers on the expression and enzyme activities of human xenobiotics-metabolizing cytochromes P450. All CCBs dose-dependently activated aryl hydrocarbon receptor (AhR) and pregnane X receptor (PXR), as revealed by gene reporter assays...
November 16, 2016: Toxicology Letters
https://www.readbyqxmd.com/read/27681386/xylitol-as-a-potential-co-crystal-co-former-for-enhancing-dissolution-rate-of-felodipine-preparation-and-evaluation-of-sublingual-tablets
#10
Mona F Arafa, Sanaa A El-Gizawy, Mohamed A Osman, Gamal M El Maghraby
Dissolution enhancement is a promising strategy for improving drug bioavailability. Co-crystallization of drugs with inert material can help in this direction. The benefit will become even greater if the inert material can form co-crystal while maintaining its main function as excipient. Accordingly, the objective of the current study was to investigate xylitol as a potential co-crystal co-former for felodipine with the goal of preparing felodipine sublingual tablets. Co-crystallization was achieved by wet co-grinding of the crystals deposited from methanolic solutions containing felodipine with increasing molar ratios of xylitol (1:1, 1:2 and 1:3)...
September 28, 2016: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/27642964/os-14-01-an-estimated-optimal-hypertension-level-of-goals-on-drug-therapy-from-the-fever-trial
#11
Xuezhong Zhang, Yuqing Zhang, Lisheng Liu, Alberto Zanchetti
OBJECTIVE: There is some debate as to optimal BP goals with antihypertensive treatment derived mostly in post-hoc analysis of large trials. Because there was limited number of subjects and outcomes within the larger study which may cloud the analytical accuracy of the findings. We suggest a new method to estimate the J-curve. DESIGN AND METHOD: Felodipine Event Reduction (FEVER) study randomized 9711 Chinese hypertensive patients to more or less intense anti-hypertensive treatment with 159,844 BP measurements...
September 2016: Journal of Hypertension
https://www.readbyqxmd.com/read/27594210/an-investigation-into-the-use-of-polymer-blends-to-improve-the-printability-of-and-regulate-drug-release-from-pharmaceutical-solid-dispersions-prepared-via-fused-deposition-modeling-fdm-3d-printing
#12
Muqdad Alhijjaj, Peter Belton, Sheng Qi
FDM 3D printing has been recently attracted increasing research efforts towards the production of personalized solid oral formulations. However, commercially available FDM printers are extremely limited with regards to the materials that can be processed to few types of thermoplastic polymers, which often may not be pharmaceutically approved materials nor ideal for optimizing dosage form performance of poor soluble compounds. This study explored the use of polymer blends as a formulation strategy to overcome this processability issue and to provide adjustable drug release rates from the printed dispersions...
November 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27562708/three-dimensional-structural-insight-of-laser-drilled-orifices-in-osmotic-pump-tablets
#13
Li Wu, Lebing Wang, Shuxia Wang, Tiqiao Xiao, Min Chen, Qun Shao, Peter York, Vikaramjeet Singh, Xianzhen Yin, Jingkai Gu, Jiwen Zhang
The orifice drilled in the membrane as a channel for drug delivery is the key functional part of the osmotic pumps for a controlled drug release system. Reported conventional microscopic evaluations of these orifices have been limited to measurement of two-dimensional cross-section diameters. This study was aimed at establishing a novel method to measure quantitatively the three-dimensional architectures of orifices based on synchrotron radiation X-ray microcomputed tomography (SR-μCT). Quantitative analysis of architectures extracted from captopril osmotic pumps drilled by a range of operating parameters indicated that laser power correlated with the cross section area, volume, surface area and depth of the orifices, while scanning speed of laser beam showed inverse relationships with the above structure characters...
October 10, 2016: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27508676/-op-lb01-03-benefits-of-early-blood-pressure-control-on-cardiovascular-outcomes-a-subgroup-analysis-of-the-felodipine-event-reduction-fever-study
#14
Y Zhang, X Zhang, L Liu, A Zanchetti
OBJECTIVE: In the setting of rapidly increasing trend of hypertension, a post-hoc subgroup analysis of the Felodipine Event Reduction (FEVER) Study was conducted to determine the effects of early blood pressure control on cardiovascular (CV) outcomes. DESIGN AND METHOD: The FEVER Study was a double-blind randomized trial conducted in 9711 Chinese hypertensive patients in which the CV outcomes were significantly reduced by felodipine compared with placebo. In this analysis, patients were regrouped to either the uncontrolled BP group (SBP/DBP, > = 140/90 mmHg) or the controlled BP group (<140/90 mmHg) at 1 and 6 months...
September 2016: Journal of Hypertension
https://www.readbyqxmd.com/read/27508576/-op-8d-02-first-in-man-treatment-of-severe-bp-variability-with-baroreflex-activation-therapy
#15
M D Lobo, M Y Adeel, C B Wolff, P O Julu, M Shah, D M Collier, M Saxena, C Floyd, T Brier, V Kapil, O Mukhtar, A Radunovic, N Sutcliffe, F Sharif
OBJECTIVE: Profound BP variability (BPV) is a major cause of cardiovascular morbidity and poor quality of life as there are no optimal pharmacological strategies to help patients. We hypothesised that in a patient with baroreflex dysfunction and preserved efferent baroreflex pathway, carotid sinus stimulation may help control BP, BPV and heart rate variability (HRV). DESIGN AND METHOD: A 52 year old man was referred with profound HR and BPV. Home SBPs were in a range of 60-250 mmHg and DBPs were 40-130 mmHg and heart rate (HR) of 60-200 bpm (confirmed with ABPM, see Figure) despite multiple medications including felodipine 30 mg daily, terazosin 16 mg daily, doxazosin 8 mg daily, bisoprolol 20 mg daily and butrans patch 17...
September 2016: Journal of Hypertension
https://www.readbyqxmd.com/read/27488902/studying-the-propensity-of-compounds-to-supersaturate-a-practical-and-broadly-applicable-approach
#16
Henrik Palmelund, Cecilie Maria Madsen, Jakob Plum, Anette Müllertz, Thomas Rades
Supersaturating drug delivery systems can enhance the oral bioavailability of poorly soluble drug compounds. Supersaturation of such compounds has been studied in many different ways; however, a more standardized method is required. The rationale of choosing suitable concentrations of supersaturation to study has previously been very inconsistent. This makes comparisons between studies and compounds difficult, as the propensity of compounds to supersaturate varies greatly. This study presents a standardized method to study the supersaturation of drug compounds...
October 2016: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27472680/treatment-efficacy-of-anti-hypertensive-drugs-in-monotherapy-or-combination-atom-systematic-review-and-meta-analysis-of-randomized-clinical-trials-according-to-prisma-statement
#17
REVIEW
Marco A Paz, Alejandro de-La-Sierra, Marc Sáez, María Antonia Barceló, Juan José Rodríguez, Sonia Castro, Cristina Lagarón, Josep M Garrido, Pilar Vera, Gabriel Coll-de-Tuero
BACKGROUND: The relative efficacy of antihypertensive drugs/combinations is not well known. Identifying the most effective ones and the patients' characteristics associated with best performance of the drugs will improve management of hypertensive patients. OBJECTIVE: To assess the blood pressure (BP) reduction attributed to antihypertensive drugs and identify characteristics associated with BP decrease. DATA SOURCES: MEDLINE, Cochrane Central Register of Controlled Trials from inception through July 2012 and selected papers...
July 2016: Medicine (Baltimore)
https://www.readbyqxmd.com/read/27372548/practical-estimation-of-amorphous-solubility-enhancement-using-thermoanalytical-data-determination-of-the-amorphous-crystalline-solubility-ratio-for-pure-indomethacin-and-felodipine
#18
Peter J Skrdla, Philip D Floyd, Philip C Dell'orco
Use of amorphous phases can mitigate the low in vivo exposures of poorly soluble, crystalline active pharmaceutical ingredients. However, it remains challenging to accurately predict the solubility enhancement offered even by a pure amorphous phase relative to the crystalline form. In this work, a methodology is presented that allows estimation of the amorphous:crystalline solubility ratio, α, using only measured thermodynamic quantities for each of the pure phases. With this approach, α values of 7.6 and 4...
September 2016: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27329674/probing-adsorption-of-dspe-peg2000-and-dspe-peg5000-to-the-surface-of-felodipine-and-griseofulvin-nanocrystals
#19
Hanna A Rydberg, Marianna Yanez Arteta, Staffan Berg, Lennart Lindfors, Kalle Sigfridsson
Nanosized formulations of poorly water-soluble drugs show great potential due to improved bioavailability. In order to retain colloidal stability, the nanocrystals need to be stabilized. Here we explore the use of the poly(ethylene glycol) (PEG) conjugated phospholipids DSPE-PEG2000 and DSPE-PEG5000 as stabilizers of felodipine and griseofulvin nanocrystals. Nanocrystal stability and physicochemical properties were examined and the interaction between the PEGylated lipids and the nanocrystal surface as well as a macroscopic model surface was investigated...
August 20, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27299377/accelerated-physical-stability-testing-of-amorphous-dispersions
#20
Mehak Mehta, Raj Suryanarayanan
The goal was to develop an accelerated physical stability testing method of amorphous dispersions. Water sorption is known to cause plasticization and may accelerate drug crystallization. In an earlier investigation, it was observed that both the increase in mobility and decrease in stability in amorphous dispersions was explained by the "plasticization" effect of water (Mehta et al. Mol. Pharmaceutics 2016, 13 (4), 1339-1346). In this work, the influence of water concentration (up to 1.8% w/w) on the correlation between mobility and crystallization in felodipine dispersions was investigated...
August 1, 2016: Molecular Pharmaceutics
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