Read by QxMD icon Read


Caiqin Yang, Wei Guo, Yulong Lin, Qianqian Lin, Jiaojiao Wang, Jing Wang, Yanli Zeng
In this study, a new cocrystal of felodipine (Fel) and glutaric acid (Glu) with a high dissolution rate was developed using the solvent ultrasonic method. The prepared cocrystal was characterized using X-ray powder diffraction, differential scanning calorimetry, thermogravimetric (TG) analysis, and infrared (IR) spectroscopy. To provide basic information about the optimization of pharmaceutical preparations of Fel-based cocrystals, this work investigated the thermal decomposition kinetics of the Fel-Glu cocrystal through non-isothermal thermogravimetry...
March 8, 2018: Journal of Pharmaceutical and Biomedical Analysis
Yuqi Chen, Wencong Huang, Jiali Chen, Hanning Wang, Shujuan Zhang, Subin Xiong
The aim was to explore the effects of non-polar and polar protic solvents composed of dichloromethane (DCM) and ethanol (EtOH) on the properties of felodipine (FLDP) and Soluplus in solutions, casting films and spray dried drug-rich or polymer-rich solid dispersions (SDs). Measurement of intrinsic viscosity and solubility indicated that FLDP and Soluplus were miscible. EtOH-DCM ranging from 20:80 to 50:50 induced the strongest molecular interactions for FLDP-Soluplus-solvents systems. Accordingly, the casting films and spray dried powders of FLDP and Soluplus were prepared using pure EtOH or DCM and their mixtures as solvents...
February 15, 2018: Journal of Pharmaceutical Sciences
Rania K Eid, Ebtessam A Essa, Gamal M El Maghraby
The fluidity of vesicular membrane affects vesicular transdermal drug delivery. Essential oils can be located in vesicular membrane imparting flexibility and influencing transdermal delivery. Accordingly, the objective was to investigate the effect of incorporation of essential oils in niosomes on felodipine transdermal delivery. Rigid niosomes comprising Span 60 with cholesterol (2:1, w/w) were used with clove, eucalyptus or lemon oils being incorporated in the vesicles at increasing concentrations. The vesicle size and shape was monitored using scanning electron microscopy...
February 14, 2018: Pharmaceutical Development and Technology
Chao Pi, Ting Feng, Jing Liang, Hao Liu, Dongmei Huang, Chenglin Zhan, Jiyuan Yuan, Robert J Lee, Ling Zhao, Yumeng Wei
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 was investigated and compared with Plendil (commercial FD sustained-release tablets) as a single-unit dosage form...
February 9, 2018: International Journal of Biological Macromolecules
Mahendra Singh, Jovita Kanoujia, Poonam Parashar, Malti Arya, Chandra B Tripathi, V R Sinha, Shailendra K Saraf, Shubhini A Saraf
The oral bioavailability of felodipine (FEL) is very low, i.e., about 15%. This could be due to low water solubility and hepatic first-pass effect. The objective of the present study was to develop FEL microemulsion-based gel, to bypass the first pass effect, for buccal delivery. The optimized FEL microemulsion (OPT-MEF) was used to prepare buccoadhesive gels, with varying concentrations of hydroxypropyl methylcellulose (HPMC) E4M and polycarbophil (PCP), and evaluated. The cross-linking of the PCP gelling agent was done by adjusting the pH with a neutralizing agent, triethanolamine (TEA)...
February 8, 2018: Drug Delivery and Translational Research
Wiebke Saal, Nicole Wyttenbach, Jochem Alsenz, Martin Kuentz
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...
January 10, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Christian Luebbert, Maximilian Wessner, Gabriele Sadowski
The molecular integration of poorly-water-soluble active pharmaceutical ingredients (APIs) in a suitable polymeric matrix is a possible approach to enhance the dissolution behavior and solubility of these APIs. Like all newly-developed pharmaceutical formulations, these formulations (often denoted as amorphous solid dispersions (ASDs)) need to undergo storage stability tests at defined relative humidity (RH) and temperature conditions. In a previous work (Int. J. Pharm. 532 (2017) 635-646), it was shown that thermodynamic modeling can be successfully used to predict the long-term stability of ASDs against API crystallization and moisture-induced amorphous-amorphous phase separation (MIAPS)...
January 8, 2018: Molecular Pharmaceutics
Eirini Palazi, Evangelos Karavas, Panagiotis Barmpalexis, Margaritis Kostoglou, Stavroula Nanaki, Evi Christodoulou, Dimitrios N Bikiaris
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...
January 3, 2018: European Journal of Pharmaceutical Sciences
Jinping Fu, Lin Cui, Congbin Yang, Hui Xiong, Guobin Ren, Xingyuan Ma, Qiufang Jing, Fuzheng Ren
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...
January 4, 2018: AAPS PharmSciTech
Cecilia N Amadi, Amaka A Mgbahurike
BACKGROUND: Food/Herb-drug interactions have become a major problem in health care. These interactions can lead to loss of therapeutic efficacy or toxic effects of drugs. AREAS OF UNCERTAINTY: To probe the clinical relevance of such interactions, the impact of food/herb intake on the clinical effects of drug administration has to be evaluated. Failure to identify and efficiently manage food-drug interactions can lead to serious consequences. A comprehensive knowledge of the mechanisms that underpin variability in disposition will help optimize therapy...
November 22, 2017: American Journal of Therapeutics
Yiwei Tian, David S Jones, Conor Donnelly, Timothy Brannigan, Shu Li, Gavin P Andrews
Current experimental methodologies used to determine the thermodynamic solubility of an API within a polymer typically involves establishing the dissolution/melting endpoint of the crystalline API within a physical mixture, or through the use of the glass transition temperature measurement of a de-mixed amorphous solid dispersion. The measurable "equilibrium" points for solubility are normally well above the glass transition temperature of the system meaning extrapolation is required in order to predict the drug solubility at pharmaceutical relevant temperatures...
December 5, 2017: Molecular Pharmaceutics
Mahendra Singh, Jovita Kanoujia, Poonam Parashar, Malti Arya, Chandra B Tripathi, V R Sinha, Shailendra K Saraf, Shubhini A Saraf
The oral bioavailability of felodipine, a dihydropyridine calcium channel antagonist, is about 15%. This may be due to poor water solubility, and a lower intestinal permeability than a BCS class I drug, and hepatic first-pass metabolism of the drug. Many drugs are unpopular due to solubility issues. The goal of this study was to develop and optimize a felodipine-containing microemulsion to improve the intestinal permeability and bioavailability of the drug. The felodipine microemulsions were developed with the selected components, i...
February 2018: Drug Delivery and Translational Research
Morrie Lam, Natalia Mast, Irina A Pikuleva
Cytochrome P450 27A1 (CYP27A1) is a ubiquitous enzyme that hydroxylates cholesterol and other sterols. Complete CYP27A1 deficiency owing to genetic mutations is detrimental to human health, whereas 50% of activity retention is not and does not affect the whole body cholesterol levels. CYP27A1 is considered a potential therapeutic target in breast cancer and age-related neurodegenerative diseases; however, CYP27A1 inhibition should be ≤50%. Herein, 131 pharmaceuticals were tested for their effect on CYP27A1-mediated cholesterol 27-hydroxylation by in vitro enzyme assay...
February 2018: Molecular Pharmacology
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...
January 15, 2018: International Journal of Pharmaceutics
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 to -25 mV after rehydration, and the particle sizes of the complexes were in the range 10-80 μm...
January 2018: Journal of Pharmaceutical Sciences
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
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...
December 4, 2017: Molecular Pharmaceutics
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
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...
January 2018: Journal of Pharmaceutical Sciences
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...
January 1, 2018: European Journal of Pharmaceutical Sciences
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"