A validated LC–MS/MS method for the quantification of amlodipine, bisoprolol, enalapril and enalaprilat—Application to pharmacokinetic study in healthy volunteers
Publication date: June 2020Source: Microchemical Journal, Volume 155Author(s): Liliya Logoyda, Sergiy Kovalenk, Moustafa Gaafar, Ahmed M. Abdel-Megied, Fawzy A. ElbarbryAbstractIn this work, a highly sensitive and rapid liquid chromatography-tandem mass spectrometry (LC–MS/MS) method for the simultaneous determination of amlodipine (AML), bisoprolol (BIS) and enalapril maleate (ENA) in the presence of its metabolite enalaprilat (ENT) in real human plasma was developed and validated using felodipine, propranolol, ramipril, and captopril, as internal standards (IS), respectively. The prepared samples were chromatograph...
Source: Microchemical Journal - February 14, 2020 Category: Chemistry Source Type: research

Small scale design of experiment investigation of equilibrium solubility in simulated fasted and fed intestinal fluid.
Abstract It is widely recognised that drug solubility within the gastrointestinal tract (GIT) differs from values determined in a simple aqueous buffer and to circumvent this problem measurement in biorelevant fluids is determined. Biorelevant fluids are complex mixtures of components (sodium taurocholate, lecithin, sodium phosphate, sodium chloride, pancreatin and sodium oleate) at various concentrations and pH levels to provide systems simulating fasted (FaSSIF) or fed (FeSSIF) intestinal media. Design of Experiment (DoE) studies have been applied to investigate FaSSIF and FeSSIF and indicate that a drug's equil...
Source: European Journal of Pharmaceutics and Biopharmaceutics - February 6, 2020 Category: Drugs & Pharmacology Authors: McPherson S, Perrier J, Dunn C, Khadra I, Davidson S, Ainousah B, Wilson CG, Halbert G Tags: Eur J Pharm Biopharm Source Type: research

Bile acid transporter mediated STC/Soluplus self-assembled hybrid nanoparticles for enhancing the oral drug bioavailability
In conclusion, STC/Soluplus SHNPs via ASBT are a potential strategy for enhancing the oral bioavailability of poorly water-soluble drugs.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 5, 2020 Category: Drugs & Pharmacology Source Type: research

Felodipine and Renal Function in Lung Transplantation: A Randomized Placebo-controlled Trial
Calcium channel blockers may ameliorate the decline in renal function caused by calcineurin inhibitors in lung transplant (LTX) recipients. We hypothesized that preoperative and 12-week postoperative treatment with the calcium channel blocker, felodipine, would reduce the decline in glomerular filtration rate (GFR). (Source: The Journal of Heart and Lung Transplantation)
Source: The Journal of Heart and Lung Transplantation - January 29, 2020 Category: Transplant Surgery Authors: M Hornum, M Iversen, P Oturai, MJ Andersen, M Zemtsovski, P Bredahl, N.H Bjarnason, K.B Christensen, J. Carlsen, CH M øller, B Feldt-Rasmussen, M Perch Tags: Original Clinical Science Source Type: research

An in vitro dissolution-digestion-permeation assay for the study of advanced drug delivery systems.
uml;m CAS Abstract Advanced drug delivery systems (ADDS) are widely explored to overcome poor aqueous solubility of orally administered drugs. However, the prediction of their in vivo performance is challenging, as in vitro models typically do not capture the interplay between processes occurring in the gut. In additions, different models are used to evaluate the different systems. We therefore present a method that allows monitoring of luminal processing (dissolution, digestion) and its interplay with permeation to better inform on the absorption of felodipine formulated as ADDS. Experiments were performed in a &...
Source: European Journal of Pharmaceutics and Biopharmaceutics - January 23, 2020 Category: Drugs & Pharmacology Authors: Alvebratt C, Keemink J, Edueng K, Cheung O, Strømme M, Bergström CAS Tags: Eur J Pharm Biopharm Source Type: research

PAIT-Survey Follow-Up: Changes in Albuminuria in Hypertensive Diabetic Patients with Mild-Moderate Chronic Kidney Disease
AbstractIntroductionAlbuminuria is an early marker of kidney disease and reduction of albuminuria translates into a decreased occurrence of cardiovascular and renal outcomes.AimsTo evaluate  the changes in the prevalence of albuminuria in diabetic hypertensive patients treated with several combinations of renin-angiotensin aldosterone system with calcium channel blockers.MethodsWe analysed data from  668 unselected patients from the PAIT survey (mean age 60.4 ± 10.2 years, prevalence of males 38%), with and without albuminuria, maintained for 6 months with the previous treatment wit...
Source: High Blood Pressure and Cardiovascular Prevention - January 9, 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 26, 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 differenti...
Source: Experimental Cell Research - December 23, 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 17, 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 suggesting de...
Source: Chemical Communications - October 3, 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 de...
Source: AAPS PharmSciTech - August 12, 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 ti...
Source: AAPS PharmSciTech - August 12, 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 matric...
Source: AAPS PharmSciTech - June 14, 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
Wim Schelstraete*, Mathias Devreese and Siska Croubels* Laboratory of Pharmacology and Toxicology, Department of Pharmacology, Toxicology and Biochemistry, Faculty of Veterinary Medicine, Ghent University, Ghent, Belgium Cytochrome P450 enzymes (CYP) are important catalyzing proteins involved in the biotransformation of endogenous and xenobiotic compounds. However, their expression and/or activity can be altered by exposure to contaminants such as mycotoxins. In vitro incubations in porcine hepatic microsomes revealed a potent inhibition of the midazolam (CYP3A) biotransformation by T-2 toxin (T-2) (Ki = 27.0 &pl...
Source: Frontiers in Pharmacology - April 16, 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 inhibitio...
Source: Chemico-Biological Interactions - April 6, 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

The importance and safety of calcium antagonists in the treatment of hypertension in pregnant women
Publication date: Available online 6 March 2019Source: Pregnancy HypertensionAuthor(s): Grzegorz Grześk, Łukasz Wołowiec, Marcin Walukiewicz, Daniel Rogowicz, Wojciech Gilewski, Joanna BanachAbstractThe use of CCBs, including newer dihydropyridine derivatives like felodipine and amlodipine, seems to be an effective, safe and more modern option in HDP therapy and during breast-feeding. (Source: Pregnancy Hypertension: An International Journal of Womens Cardiovascular Health)
Source: Pregnancy Hypertension: An International Journal of Womens Cardiovascular Health - March 6, 2019 Category: OBGYN Source Type: research

[One-year persistence of fixed-dose combinations of angiotensin-converting enzyme inhibitor and calcium channel blocker in hypertensive patients].
Abstract INTRODUCTION: The most recent European guidelines for the treatment of hypertension suggest the use of renin-angiotensin-aldosterone system antagonists (RAAS inhibitors) and calcium channel blockers (CCBs) or diuretics fixed-dose combinations (FDCs) as the first therapeutic option. In antihypertensive therapy, the patient's adherence is one of the most important factors in reducing unwanted cardiovascular events. AIM: Our aim was to assess the one-year persistence of angiotensin-converting enzyme inhibitor (ACEI) and CCB FDCs in hypertensive patients. METHOD: Authors have analysed the prescripti...
Source: Orvosi Hetilap - February 28, 2019 Category: General Medicine Authors: Simonyi G, Ferenci T, Finta E, Igaz I, Balogh S, Gasparics R, Medvegy M Tags: Orv Hetil Source Type: research

Low Dose Scanning Transmission Electron Microscopy of Organic Crystals by Scanning Moiré Fringes
Publication date: Available online 1 February 2019Source: MicronAuthor(s): Mark S’ari, James Cattle, Nicole Hondow, Rik Brydson, Andy BrownAbstractIn the pharmaceutical industry, it is important to determine the effects of crystallisation and processes, such as milling, on the generation of crystalline defects in formulated products. Conventional transmission electron microscopy and scanning transmission electron microscopy (STEM) can be used to obtain information on length scales unobtainable by other techniques, however, organic crystals are extremely susceptible to electron beam damage. This work demonstrates a br...
Source: Micron - February 2, 2019 Category: Biology Source Type: research

The Influence of Cellulosic Polymer's Variables on Dissolution/Solubility of Amorphous Felodipine and Crystallization Inhibition from a Supersaturated State.
Abstract The collective impact of cellulosic polymers on the dissolution, solubility, and crystallization inhibition of amorphous active pharmaceutical ingredients (APIs) is still far from being adequately understood. The goal of this research was to explore the influence of cellulosic polymers and incubation conditions on enhancement of solubility and dissolution of amorphous felodipine, while inhibiting crystallization of the drug from a supersaturated state. Variables, including cellulosic polymer type, amount, ionic strength, and viscosity, were evaluated for effects on API dissolution/solubility and crystalli...
Source: AAPS PharmSciTech - December 17, 2018 Category: Drugs & Pharmacology Authors: Shi NQ, Jin Y, Zhang Y, Che XX, Xiao X, Cui GH, Chen YZ, Feng B, Li ZQ, Qi XR Tags: AAPS PharmSciTech Source Type: research

Targeting Nrf2/HO-1 signaling by crocin: Role in attenuation of AA-induced ulcerative colitis in rats
In conclusion; crocin demonstrated anti-ulcerogenic and coloprotective effect mediated primarily by its antioxidant, anti-inflammatory and anti-apoptotic properties. The therapeutic impact is mediated primarily via enhancement of colon Nrf2 content by 211% in protective protocol and by 350% in curative and HO-1 signaling by 49% in protective protocol and, 288% in the curative protocol. Enhancement of Nrf2 and HO-1 signaling and down-regulation of caspase-3 activity are believed to underly the observed therapeutic effect.Graphical abstract (Source: Biomedicine and Pharmacotherapy)
Source: Biomedicine and Pharmacotherapy - December 5, 2018 Category: Drugs & Pharmacology Source Type: research

Targeting Nrf2/HO-1 signaling by crocin: Role in attenuation of AA-induced ulcerative colitis in rats.
In conclusion; crocin demonstrated anti-ulcerogenic and coloprotective effect mediated primarily by its antioxidant, anti-inflammatory and anti-apoptotic properties. The therapeutic impact is mediated primarily via enhancement of colon Nrf2 content by 211% in protective protocol and by 350% in curative and HO-1 signaling by 49% in protective protocol and, 288% in the curative protocol. Enhancement of Nrf2 and HO-1 signaling and down-regulation of caspase-3 activity are believed to underly the observed therapeutic effect. PMID: 30530041 [PubMed - as supplied by publisher] (Source: Biomedicine and pharmacotherapy = Biom...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - December 4, 2018 Category: Drugs & Pharmacology Authors: Khodir AE, Said E, Atif H, ElKashef HA, Salem HA Tags: Biomed Pharmacother Source Type: research

Application of biorelevant saliva-based dissolution for optimisation of orally disintegrating formulations of felodipine
In this study pooled human saliva was characterised and utilised as dissolution media for biorelevant oral cavity dissolution studies and to assess drug release. Lipophilic drug felodipine with challenging biopharmaceutical properties was selected for assessment in oral cavity dissolution studies. These saliva dissolution studies investigated for the first time how biorelevant dissolution can be implemented as a screening tool to guide the formulation development process and to predict dosage form performance within the mouth. In this study a combination of three dissolution enhancement strategies (cryomilling, solid dispe...
Source: International Journal of Pharmaceutics - November 19, 2018 Category: Drugs & Pharmacology Source Type: research

Predicted Amorphous Solubility and Dissolution Rate Advantages Following Moisture Sorption: Case Studies of Indomethacin and Felodipine
Publication date: Available online 15 November 2018Source: International Journal of PharmaceuticsAuthor(s): Peter J. Skrdla, Philip D. Floyd, Philip C. Dell'OrcoAbstractWater is often readily absorbed by amorphous compounds, lowering their glass transition temperature (Tg) and facilitating their recrystallization (via nucleation-and-growth). At the same time, the increase in moisture content translates to a decrease in both the thermodynamic solubility and intrinsic dissolution rate, as compared to the corresponding dry (pure) amorphous phase, e.g. see [Murdande SB, Pikal MJ, Shanker RM, Bogner RH. 2010. Solubility advanta...
Source: International Journal of Pharmaceutics - November 17, 2018 Category: Drugs & Pharmacology Source Type: research

Diversity of methyl group dynamics in felodipine: a DFT supported NMR and QENS study
CrystEngComm, 2018, Advance Article DOI: 10.1039/C8CE01605D, PaperAleksandra Pajzderska, Kacper Dru żbicki, Miguel Angel Gonzalez, Jacek Jenczyk, Jadwiga Mielcarek, Jan Wąsicki Computationally-supported NMR and neutron scattering experiments were combined to provide new insights into the structure –dynamics relationship in the most stable polymorph of felodipine. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry (Source: RSC - CrystEngComm latest articles)
Source: RSC - CrystEngComm latest articles - November 7, 2018 Category: Chemistry Authors: Aleksandra Pajzderska Source Type: research

Diversity of Methyl Group Dynamics in Felodipine: a DFT Supported NMR and Neutron Scattering Study
CrystEngComm, 2018, Accepted Manuscript DOI: 10.1039/C8CE01605D, PaperAleksandra Pajzderska, Kacper Druzbicki, Miguel A. Gonzalez, Jacek Jenczyk, Jadwiga Mielcarek, Jan Wasicki Molecular and vibrational dynamics in a widely used calcium channel blocker, felodipine form I (FLD), have been thoroughly explored by combining periodic density functional theory (plane-wave DFT) with solid-state nuclear... The content of this RSS Feed (c) The Royal Society of Chemistry (Source: RSC - CrystEngComm latest articles)
Source: RSC - CrystEngComm latest articles - October 31, 2018 Category: Chemistry Authors: Aleksandra Pajzderska Source Type: research

Identification of crucial genes and prediction of small molecules for multidrug resistance of Hodgkin's lymphomas.
CONCLUSIONS: The present study offered new insights into the molecular mechanisms of multidrug resistance and identified a series of important hub genes and small agents that might be critical for treatment of multidrug-resistant HL. PMID: 30347596 [PubMed - as supplied by publisher] (Source: Cancer Biomarkers)
Source: Cancer Biomarkers - October 25, 2018 Category: Cancer & Oncology Tags: Cancer Biomark Source Type: research

Early stages of drug crystallization from amorphous solid dispersion via fractal analysis based on chemical imaging.
z M Abstract Early stages of crystallization from amorphous solid dispersion (ASD) are typically not detected by means of standard methods like powder X-ray diffraction (XRPD). The aim of this study is therefore to evaluate if fractal analysis based on energy dispersive x-ray imaging can provide the means to identify early signs of physical instability. ASDs of the poorly water-soluble compound, felodipine (FEL) were prepared by solvent evaporation using different grades of HPMCAS, at 50wt. % drug loading. Samples were stored at accelerated conditions of 40°C. Scanning electron microscopy equipped with an ener...
Source: European Journal of Pharmaceutics and Biopharmaceutics - October 6, 2018 Category: Drugs & Pharmacology Authors: Abreu-Villela R, Schönenberger M, Caraballo I, Kuentz M Tags: Eur J Pharm Biopharm Source Type: research

Structural studies of calcium channel blockers used in the treatment of hypertension - 1 H and 13 C NMR characteristics of nifedipine analogues.
Abstract The 1 H and 13 C NMR spectroscopy in solution was applied to characterize a series of active pharmaceutical ingredients (API) belonging to the class of calcium channel blockers, a group of drug substances extremely sensitive to UV radiation: nifedipine (1), nitrendipine (2), nisoldipine (3), nimodipine (4), nilvadipine (5), felodipine (6) isradipine (7) nicardipine (8) and amlodipine besylate (9). Two-dimensional NMR experiments (COSY, HSQC, HMBC) allowed the unequivocal assignments of peaks in the 1 H and 13 C spectra in solution and in some cases enabled editing of incorrect assignments appearing in the...
Source: Magnetic Resonance in Chemistry : MRC - September 26, 2018 Category: Chemistry Authors: Szeleszczuk Ł, Zielińska-Pisklak M, Pisklak DM Tags: Magn Reson Chem Source Type: research

Validated RP-HPLC method for quantification of felodipine in rabbit plasma: Application in a bioequivalence study.
CONCLUSION: Thus, developed method is simple, convenient and suitable for the analysis of felodipine in bulk and pharmaceutical formulations. PMID: 30243471 [PubMed - as supplied by publisher] (Source: Annales Pharmaceutiques Francaises)
Source: Annales Pharmaceutiques Francaises - September 19, 2018 Category: Drugs & Pharmacology Authors: Salunkhe NH, Jadhav NR, Bhinge SD Tags: Ann Pharm Fr Source Type: research

Polyvinylpyrrolidone affects thermal stability of drugs in solid dispersions
Publication date: Available online 11 September 2018Source: International Journal of PharmaceuticsAuthor(s): Yasmine Ben Osman, Tatsiana Liavitskaya, Sergey VyazovkinAbstractThe present study explores the hypothesis that a polymer can affect the thermal stability of a drug in solid polymer-drug dispersions. The hypothesis is tested in a systematic fashion by combining isoconversional kinetic analysis with thermogravimetric measurements on several solid dispersions. Experimental systems involve three drugs: indomethacin (IMC), felodipine (FD), and nifedipine (ND) and their solid dispersions with polyvinylpyrrolidone (PVP). ...
Source: International Journal of Pharmaceutics - September 12, 2018 Category: Drugs & Pharmacology Source Type: research

Selected Food/Herb–Drug Interactions: Mechanisms and Clinical Relevance
Conclusions: This review updates our knowledge on clinical food–drug interactions with emphasis on mechanism and clinical implications. Results obtained from literature search identified interactions with selected foods/herbs generated from in vivo and in vitro studies. For example, interaction studies in humans revealed a reduction in the bioavailability of mercaptopurine when taken concurrently with substances containing xanthine oxidase (eg, cow milk); a reduction in the bioavailability of quinine with Garcinia kola; increased bioavailability/toxicity of felodipine, nifedipine, saquinavir, sildenafil with grape ...
Source: American Journal of Therapeutics - July 1, 2018 Category: Drugs & Pharmacology Tags: Systematic Review and Clinical Guidelines Source Type: research

Comparison of real-world effectiveness between valsartan and non-RAS inhibitor monotherapy on the incidence of new diabetes in Chinese hypertensive patients: An electronic health recording system based study.
This study aimed to compare the real-world effectiveness of valsartan and non renin-angiotensin system (non-RAS) agent monotherapy on the incidence of new on-set diabetes (NOD) in Chinese hypertensive patients. It was based on an electronic Health Recording System database from Minhang District of Shanghai. Hypertensive patients aged ≥18 years continuously taking either valsartan or non-RAS agent monotherapy for>12 months were included. Hazard ratios (HR) of NOD events were estimated using propensity score matching method and multivariate regression. Of 29295 patients, there were 2107 in valsartan group, 21397 in CCB...
Source: Clinical and Experimental Hypertension - May 21, 2018 Category: Cardiology Authors: Shen T, Wang J, Yu Y, Yu J Tags: Clin Exp Hypertens Source Type: research

Dry Gel Containing Optimized Felodipine-Loaded Transferosomes: a Promising Transdermal Delivery System to Enhance Drug Bioavailability.
In conclusion, topically applied lyophilized gel containing felodipine-loaded transferosomes is a promising transdermal delivery system to enhance its bioavailability. PMID: 29714001 [PubMed - as supplied by publisher] (Source: AAPS PharmSciTech)
Source: AAPS PharmSciTech - April 30, 2018 Category: Drugs & Pharmacology Authors: Kassem MA, Aboul-Einien MH, El Taweel MM Tags: AAPS PharmSciTech Source Type: research

Development of a chromatographic method with multi-criteria decision making design for simultaneous determination of nifedipine and atenolol in content uniformity testing.
Abstract A new robust and reliable high-performance liquid chromatography (HPLC) method with multi-criteria decision making (MCDM) approach was developed to allow simultaneous quantification of atenolol (ATN) and nifedipine (NFD) in content uniformity testing. Felodipine (FLD) was used as an internal standard (I.S.) in this study. A novel marriage between a new interactive response optimizer and a HPLC method was suggested for multiple response optimizations of target responses. An interactive response optimizer was used as a decision and prediction tool for the optimal settings of target responses, according to s...
Source: Talanta - April 22, 2018 Category: Chemistry Authors: Ahmed S, Alqurshi A, Mohamed AI Tags: Talanta Source Type: research

Experimental and DFT simulation study of a novel felodipine cocrystal: Characterization, dissolving properties and thermal decomposition kinetics
In conclusion, the formed cocrystal exhibited different thermal decomposition kinetics and showed different E a, A, and shelf life from the intact active pharmaceutical ingredient. Graphical abstract (Source: Journal of Pharmaceutical and Biomedical Analysis)
Source: Journal of Pharmaceutical and Biomedical Analysis - March 16, 2018 Category: Drugs & Pharmacology Source Type: research

Food-drug interactions precipitated by fruit juices other than grapefruit juice: An update review
Publication date: Available online 15 February 2018 Source:Journal of Food and Drug Analysis Author(s): Meng Chen, Shu-yi Zhou, Erlinda Fabriaga, Pian-hong Zhang, Quan Zhou This review addressed drug interactions precipitated by fruit juices other than grapefruit juice based on randomized controlled trials (RCTs). Literature was identified by searching PubMed, Cochrane Library, Scopus and Web of Science till December 30 2017. Among 46 finally included RCTs, six RCTs simply addressed pharmacodynamic interactions and 33 RCTs studied pharmacokinetic interactions, whereas seven RCTs investigated both pharmacokinetic and pharm...
Source: Journal of Food and Drug Analysis - February 15, 2018 Category: Food Science Source Type: research

Polymer blends used to develop felodipine-loaded hollow microspheres for improved oral bioavailability.
Abstract Felodipine (FD) has been widely used in anti-hypertensive treatment. However, it has extremely low aqueous solubility and poor bioavailability. To address these problems, FD hollow microspheres as multiple-unit dosage forms were synthesized by a solvent diffusion evaporation method. Particle size of the hollow microspheres, types of ethylcellulose (EC), amounts of EC, polyvinyl pyrrolidone (PVP) and FD were investigated based on an orthogonal experiment of three factors and three levels. In addition, the release kinetics in vitro and pharmacokinetics in beagle dogs of the optimized FD hollow microspheres ...
Source: International Journal of Biological Macromolecules - February 9, 2018 Category: Biochemistry Authors: Pi C, Feng T, Liang J, Liu H, Huang D, Zhan C, Yuan J, Lee RJ, Zhao L, Wei Y Tags: Int J Biol Macromol Source Type: research

Interactions of dimethylaminoethyl methacrylate copolymer with non-acidic drugs demonstrated high solubilization in vitro and pronounced sustained release in vivo.
Abstract 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. Exposure was reduced for both drugs and plasma-...
Source: European Journal of Pharmaceutics and Biopharmaceutics - January 10, 2018 Category: Drugs & Pharmacology Authors: Saal W, Wyttenbach N, Alsenz J, Kuentz M Tags: Eur J Pharm Biopharm Source Type: research

Screen for Inhibitors of Crystal Growth to Identify Desirable Carriers for Amorphous Solid Dispersions Containing Felodipine.
Abstract 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. Powder x-ray ...
Source: AAPS PharmSciTech - January 4, 2018 Category: Drugs & Pharmacology Authors: Fu J, Cui L, Yang C, Xiong H, Ren G, Ma X, Jing Q, Ren F Tags: AAPS PharmSciTech Source Type: research

Melt extrusion process for adjusting drug release of poorly water soluble drug felodipine using different polymer matrices.
Abstract 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. Hydrogen bonds and the molecul...
Source: European Journal of Pharmaceutical Sciences - January 3, 2018 Category: Drugs & Pharmacology Authors: Palazi E, Karavas E, Barmpalexis P, Kostoglou M, Nanaki S, Christodoulou E, Bikiaris DN Tags: Eur J Pharm Sci Source Type: research

Electron microscopy/energy dispersive X-ray spectroscopy of drug distribution in solid dispersions and interpretation by multifractal geometry
Publication date: 20 February 2018 Source:Journal of Pharmaceutical and Biomedical Analysis, Volume 150 Author(s): Renata Abreu-Villela, Camille Adler, Isidoro Caraballo, Martin Kuentz Much contemporary research of poorly water-soluble drugs focuses on amorphous solid dispersions (SDs) for oral drug delivery. Recently, a multifractal formalism has been introduced to describe the distribution of an inorganic carrier in SDs. The present work attempts to directly image model drugs by means of scanning electron microscopy and energy dispersive X-ray spectroscopy. The compounds amlodipine, felodipine, glyburide, and indomethac...
Source: Journal of Pharmaceutical and Biomedical Analysis - December 23, 2017 Category: Drugs & Pharmacology Source Type: research

Coffee - Antihypertensive Drug Interaction: A Hemodynamic and Pharmacokinetic Study With Felodipine
Publication date: November–December 2017 Source:Journal of Pharmacological and Toxicological Methods, Volume 88, Part 2 Author(s): George K. Dresser, Brad L. Urquhart, David J. Freeman, J. Malcolm O. Arnold, David G. Bailey (Source: Journal of Pharmacological and Toxicological Methods)
Source: Journal of Pharmacological and Toxicological Methods - November 22, 2017 Category: Drugs & Pharmacology Source Type: research

Investigating phase separation in amorphous solid dispersions via Raman mapping
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): 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 evol...
Source: International Journal of Pharmaceutics - November 20, 2017 Category: Drugs & Pharmacology Source Type: research

Statistical investigation of the full concentration range of fasted and fed simulated intestinal fluid on the equilibrium solubility of oral drugs.
In this study a design of experiment covering the full range from the lower limit of fasted to the upper limit of fed parameters and using a small number of experiments has been performed. The measured equilibrium solubility values are comparable with literature values for simulated fasted and fed intestinal fluids as well as human fasted and fed intestinal fluids. The equilibrium solubility data range is statistically equivalent to a combination of published fasted and fed design of experiment data in six (indomethacin, phenytoin, zafirlukast, carvedilol, fenofibrate and probucol) drugs with three (aprepitant, tadalafil a...
Source: European Journal of Pharmaceutical Sciences - October 5, 2017 Category: Drugs & Pharmacology Authors: Perrier J, Zhou Z, Dunn C, Khadra I, Wilson CG, Halbert G Tags: Eur J Pharm Sci Source Type: research

Effect of composition of simulated intestinal media on the solubility of poorly soluble compounds investigated by design of experiments.
, Rades T Abstract 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. The SIF were composed of phospholipid, bile salt, a...
Source: European Journal of Pharmaceutical Sciences - October 3, 2017 Category: Drugs & Pharmacology Authors: Madsen CM, Feng KI, Leithead A, Canfield N, Jørgensen SA, Müllertz A, Rades T Tags: Eur J Pharm Sci Source Type: research