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Tian Shen, Jiwei Wang, Yingjun Yu, Jinming Yu
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...
May 21, 2018: Clinical and Experimental Hypertension: CHE
Megan Truong, Leigh G Monahan, Dee A Carter, Ian G Charles
Many infectious diseases disproportionately affect people in the developing world. Cryptococcal meningitis is one of the most common mycoses in HIV-AIDS patients, with the highest burden of disease in sub-Saharan Africa. Current best treatment regimens still result in unacceptably high mortality rates, and more effective antifungal agents are needed urgently. Drug development is hampered by the difficulty of developing effective antifungal agents that are not also toxic to human cells, and by a reluctance among pharmaceutical companies to invest in drugs that cannot guarantee a high financial return...
2018: PeerJ
Jiali Chen, Yuqi Chen, Wencong Huang, Hanning Wang, Yang Du, Subin Xiong
The objectives of this study were to explore sodium dodecyl sulfate (SDS) and Soluplus on the crystallization inhibition and dissolution of felodipine (FLDP) extrudates by bottom-up and top-down approaches. FLDP extrudates with Soluplus and/or SDS were prepared by hot melt extrusion (HME), and characterized by PLM, DSC and FT-IR. Results indicated that Soluplus inhibited FLDP crystallization and the whole amorphous solid dispersions (ASDs) were binary FLDP-Soluplus (1:3) and ternary FLDP-Soluplus-SDS(1:2:0...
May 5, 2018: Journal of Pharmaceutical Sciences
Mohammed Ali Kassem, Mona Hassan Aboul-Einien, Mai Magdy El Taweel
Felodipine has a very low bioavailability due to first-pass metabolism. The aim of this study was to enhance its bioavailability by transdermal application. Felodipine-loaded transferosomes were prepared by thin-film hydration using different formulation variables. An optimized formula was designed using statistical experimental design. The independent variables were the used edge activator, its molar ratio to phosphatidylcholine, and presence or absence of cholesterol. The responses were entrapment efficiency of transferosomes, their size, polydispersity index, zeta potential, and percent drug released after 8 h...
April 30, 2018: AAPS PharmSciTech
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 pharmacodynamic interactions. Twenty-two juice-drug combinations showed potential clinical relevance...
April 2018: Journal of Food and Drug Analysis
F Vidal, R C de Souza, D C Ferreira, R G Fischer, L S Gonçalves
OBJECTIVE: The aim of the current study was to assess the association between 3 different calcium channel blockers (CCBs) (nifedipine, amlodipine and felodipine) and gingival overgrowth in patients with a diagnosis of severe refractory hypertension. METHODS: One hundred and sixty-two patients with severe refractory hypertension, taking CCBs, were selected. Gingival overgrowth was graded and periodontal measurements were recorded (probing pocket depth, clinical attachment level, plaque index and bleeding on probing)...
April 23, 2018: Journal of Periodontal Research
Sameh Ahmed, Abdulmalik Alqurshi, Abdel-Maaboud Ismail Mohamed
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 specified criteria, based on Derringer's desirability...
July 1, 2018: Talanta
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...
May 30, 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 nonpolar 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 23, 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...
June 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...
April 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. 2017 ; 532 , 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)...
February 5, 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 temperature 130°C and mixing time 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 depended from the used drug amount...
March 1, 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...
April 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
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