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 juic...
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, accord...
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...
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 micro...
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...
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. Powde...
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 molecula...
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 indom...
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.
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, and...
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