PAIT-Survey Follow-Up: Changes in Albuminuria in Hypertensive Diabetic Patients with Mild-Moderate Chronic Kidney Disease
ConclusionsThe treatments decrease the prevalence of subjects with albuminuria, showing a significant difference among the different drug combinations, favoring the use of new dihydropyridine calcium channel blockers, such as lercanidipine, combined with RAAS inhibitors, to control albuminuria in diabetic hypertensive patients. (Source: High Blood Pressure and Cardiovascular Prevention)
Source: High Blood Pressure and Cardiovascular Prevention - January 8, 2020 Category: Cardiology Source Type: research
Evaluating side ‐by‐side diffusion models for studying drug supersaturation in an absorptive environment: a case example of fenofibrate and felodipine
ConclusionThe tested models were comparable; however, Caco ‐2 cell monolayers were considered too sensitive to be used to study drug supersaturation. Further studies are needed to evaluate the observed drug‐dependent effects of absorption on drug supersaturation. (Source: Journal of Pharmacy and Pharmacology)
Source: Journal of Pharmacy and Pharmacology - December 25, 2019 Category: Drugs & Pharmacology Authors: Jannik Nicklas Eliasen,
Ragna Berthelsen,
Anne Louise Slot,
Anette M üllertz Tags: Research Paper Source Type: research
Felodipine blocks osteoclast differentiation and ameliorates estrogen-dependent bone loss in mice by modulating p38 signaling pathway.
Abstract
Postmenopausal osteoporosis is one of the most common types of osteoporosis resulting from estrogen deficiency in elderly women. In addition, hypertension is another common disease in the elderly, and it has become an independent risk factor for osteoporosis and osteoporotic fractures. Here, we report for the first time that felodipine, a first-line antihypertensive agent, significantly prevents postmenopausal osteoporosis in addition to its vasodilation properties. Real-time RT-PCR analysis revealed that treatment with felodipine significantly downregulated the genes associated with osteoclast di...
Source: Experimental Cell Research - December 22, 2019 Category: Cytology Authors: Zhang S, Li H, Tang H, Huo S, Nie B, Qu X, Yue B Tags: Exp Cell Res Source Type: research
High Content Solid Dispersions for Dose Window Extension: A Basis for Design Flexibility in Fused Deposition Modelling
ConclusionsIn pursuit of dose flexibility, this successful demonstration of dose window extension using high content solid dispersions preserves FDM design flexibility by maintaining applicability to drugs of varying potencies. The achieved uniformity of content supports the application of varying content solid dispersions to modular dosage form concepts to enhance dose flexibility. However, poor dispensing precision impedes its utilisation until appropriate compatibility between FDM hardware and materials at varying drug contents can be attained. (Source: Pharmaceutical Research)
Source: Pharmaceutical Research - December 16, 2019 Category: Drugs & Pharmacology Source Type: research
[ASAP] Phase Behavior of Amorphous Solid Dispersions of Felodipine: Homogeneity and Drug –Polymer Interactions
Molecular PharmaceuticsDOI: 10.1021/acs.molpharmaceut.9b00731 (Source: Molecular Pharmaceutics)
Source: Molecular Pharmaceutics - November 4, 2019 Category: Drugs & Pharmacology Authors: Kanika Sarpal †, Sean Delaney†§, Geoff G. Z. Zhang‡, and Eric J. Munson*†? Source Type: research
Structural characterisation of amorphous solid dispersions via metropolis matrix factorisation of pair distribution function data.
Abstract
We measure the X-ray pair distribution functions (PDFs) of a series of felodipine:copovidone amorphous solid dispersions. Using a newly-developed Metropolis Matrix Factorisation (MMF) algorithm we extract from these data the PDF of the amorphous felodipine component in isolation. Our MMF analysis allows quantification of the degree of drug crystallinity in each sample, and structural characterisation of the amorphous drug via its PDF. Comparison with atomistic simulations reveals that the (in)accessibility of conformational rotamers distinguishes amorphous and crystalline felodipine, in turn sugge...
Source: Chemical Communications - October 2, 2019 Category: Chemistry Authors: Geddes HS, Blade H, McCabe JF, Hughes LP, Goodwin AL Tags: Chem Commun (Camb) Source Type: research
Structural Characterisation of Amorphous Solid Dispersions via Metropolis Matrix Factorisation of Pair Distribution Function Data
Chem. Commun., 2019, Accepted Manuscript DOI: 10.1039/C9CC06753A, CommunicationHarry Geddes, Helen Blade, Leslie Peter Hughes, James Francis McCabe, Andrew Goodwin We measure the X-ray pair distribution functions (PDFs) of a series of felodipine:copovidone amorphous solid dispersions. Using a newly-developed Metropolis Matrix Factorisation (MMF) algorithm we extract from these data the... The content of this RSS Feed (c) The Royal Society of Chemistry (Source: RSC - Chem. Commun. latest articles)
Source: RSC - Chem. Commun. latest articles - September 21, 2019 Category: Chemistry Authors: Harry Geddes Source Type: research
Sericin Inhibits Devitrification of Amorphous Drugs.
Abstract
The purpose of the present investigation was to analyze devitrification of amorphous drugs such as lornoxicam, meloxicam, and felodipine in the presence of sericin. The binary solid dispersions comprising varying mass ratios of drug and sericin were subject to amorphization by spray drying, solvent evaporation, ball milling, and physical mixing. Further, obtained solid dispersions (SDs) were characterized by HPLC, ATR-FTIR, H1NMR, molecular docking, accelerated stability study at 40°C and 75 ± 2% RH (XRD and DSC), and in vitro dissolution studies. The HPLC analysis indicated no decomposition...
Source: AAPS PharmSciTech - August 11, 2019 Category: Drugs & Pharmacology Authors: Salunkhe N, Jadhav N, More H, Choudhari P Tags: AAPS PharmSciTech Source Type: research
A Novel Micron-Size Particulate Formulation of Felodipine with Improved Release and Enhanced Oral Bioavailability Fabricated by Coaxial Electrospray.
Abstract
The antihypertensive drug felodipine (FD) is a typical biopharmaceutics classification system (BCS) II drug; thus, improving the dissolution rate of FD is very important to enhance its bioavailability. Besides, according to the in situ "close loop" perfusion assay, we found that the jejunum is the main absorptive site, then the duodenum and ileum. Consequently, a novel micron-size particulate of FD in a core-shell structure was fabricated by a coaxial electrospray technique; within the drug delivery system, Hypromellose K4M (HPMC K4M) was selected as a sheath material to prolong the retention time...
Source: AAPS PharmSciTech - August 11, 2019 Category: Drugs & Pharmacology Authors: Yin X, Pan H, Liu H Tags: AAPS PharmSciTech Source Type: research
Novel Hot Melt Extruded Matrices of Hydroxypropyl Cellulose and Amorphous Felodipine-Plasticized Hydroxypropyl Methylcellulose as Controlled Release Systems.
Abstract
Hydroxypropyl methylcellulose (HPMC) is a hydrophilic retarding-release polymer with the limited application in hot melt extrusion (HME) due to its high glass transition temperature (Tg 181-191°C) and melt viscosity. The aim of this study is to develop hot melt extruded matrices using hydroxypropyl cellulose (HPC) and felodipine (FLDP) with HPMC for controlled release and explore the relations of their specialty, processability, and structure with the product properties. Results showed that FLDP/HPCEF/HPMC can be extruded at 160°C with torques not more than 0.5 N·m. The extruded matrices of FL...
Source: AAPS PharmSciTech - June 13, 2019 Category: Drugs & Pharmacology Authors: Yi S, Wang J, Lu Y, Ma R, Gao Q, Liu S, Xiong S Tags: AAPS PharmSciTech Source Type: research
Felodipine
(Source: Reactions Weekly)
Source: Reactions Weekly - May 31, 2019 Category: Drugs & Pharmacology Source Type: research
Impact of Subacute Exposure to T-2 Toxin and Zearalenone on the Pharmacokinetics of Midazolam as CYP3A Probe Drug in a Porcine Animal Model: A Pilot Study
In conclusion, ZEA and T-2 have a tendency to influence the pharmacokinetics (PK) of MDZ, a typical CYP3A substrate, at realistic levels of mycotoxin contamination, although the results were only significant for Ke and marginally non-significant for F, and Ka. However, a larger follow-up study should be performed to confirm the current findings. The results of the present study allow to calculate an appropriate sample size for this future research. As DON and ZEA are frequently occurring in food and feed, they can affect pharmacotherapy. Indeed, alterations in biotransformation capacities can lead to an altered exposure an...
Source: Frontiers in Pharmacology - April 15, 2019 Category: Drugs & Pharmacology Source Type: research
Inhibitory effects of antihypertensive drugs on human cytochrome P450 2J2 activity: Potent inhibition by azelnidipine and manidipine
Publication date: Available online 6 April 2019Source: Chemico-Biological InteractionsAuthor(s): Noriaki Ikemura, Satoshi Yamaori, Chinatsu Kobayashi, Shinobu Kamijo, Norie Murayama, Hiroshi Yamazaki, Shigeru OhmoriAbstractThe inhibitory effects of antihypertensive drugs (dihydropyridine calcium channel blockers, angiotensin II receptor blockers, and angiotensin-converting enzyme inhibitors) on cytochrome P450 2J2 (CYP2J2) activity were examined. Amlodipine, azelnidipine, barnidipine, benidipine, cilnidipine, efonidipine, felodipine, manidipine, nicardipine, nifedipine, nilvadipine, nisoldipine, nitrendipine, telmisartan, ...
Source: Chemico Biological Interactions - April 8, 2019 Category: Biochemistry Source Type: research
Inhibitory effects of antihypertensive drugs on human cytochrome P450 2J2 activity: Potent inhibition by azelnidipine and manidipine.
Abstract
The inhibitory effects of antihypertensive drugs (dihydropyridine calcium channel blockers, angiotensin II receptor blockers, and angiotensin-converting enzyme inhibitors) on cytochrome P450 2J2 (CYP2J2) activity were examined. Amlodipine, azelnidipine, barnidipine, benidipine, cilnidipine, efonidipine, felodipine, manidipine, nicardipine, nifedipine, nilvadipine, nisoldipine, nitrendipine, telmisartan, delapril, and quinapril inhibited luciferin-2J2/4F12 O-dealkylase activity of recombinant human CYP2J2 in a concentration-dependent manner (IC50 = 0.116-9.19 μM). Kinetic analyses of the inh...
Source: Chemico-Biological Interactions - April 5, 2019 Category: Molecular Biology Authors: Ikemura N, Yamaori S, Kobayashi C, Kamijo S, Murayama N, Yamazaki H, Ohmori S Tags: Chem Biol Interact Source Type: research
