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Pharmaceutics

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https://www.readbyqxmd.com/read/29473897/design-optimization-and-characterization-of-a-transfersomal-gel-using-miconazole-nitrate-for-the-treatment-of-candida-skin-infections
#1
Mona Qushawy, Ali Nasr, Mohammed Abd-Alhaseeb, Shady Swidan
Miconazole nitrate (MIC) is an antifungal drug used for treatment of superficial fungal infections. However, it has low skin permeability. Hence, the objective of this study was to prepare miconazole nitrate using Transfersomes to overcome the barrier function of the skin. MIC Transfersomes were prepared using a thin lipid film hydration technique. The prepared Transfersomes were evaluated with respect to entrapment efficiency (EE%), particle size, and quantity of in vitro drug released to obtain an optimized formulation...
February 23, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/29470434/pharmacokinetics-and-scintigraphic-imaging-of-the-hypoxia-imaging-agent-123-i-iaza-in-healthy-adults-following-exercise-based-cardiac-stress-%C3%A2
#2
Daria Stypinski, Stephen A McQuarrie, Alexander J B McEwan, Leonard I Wiebe
The objective of this work is to evaluate the potential effect of cardiac stress exercise on the accumulation of [123 I]IAZA, a radiopharmaceutical used to image focal tissue hypoxia, in otherwise normal myocardium in healthy volunteers, and to determine the impact of exercise on [123 I]IAZA pharmacokinetics. The underlying goal is to establish a rational basis and a baseline for studies of focal myocardial hypoxia in cardiac patients using [123 I]IAZA. Three healthy male volunteers ran the 'Bruce' treadmill protocol, a clinically-accepted protocol designed to expose myocardial ischemia in patients...
February 22, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/29439456/epinephrine-in-anaphylaxis-preclinical-study-of-pharmacokinetics-after-sublingual-administration-of-taste-masked-tablets-for-potential-pediatric-use
#3
Ousama Rachid, Mutasem Rawas-Qalaji, Keith J Simons
Epinephrine is a life-saving treatment in anaphylaxis. In community settings, a first-aid dose of epinephrine is injected from an auto-injector (EAI). Needle phobia highly contributes to EAI underuse, leading to fatalities-especially in children. A novel rapidly-disintegrating sublingual tablet (RDST) of epinephrine was developed in our laboratory as a potential alternative dosage form. The aim of this study was to evaluate the sublingual bioavailability of epinephrine 30 mg as a potential pediatric dose incorporated in our novel taste-masked RDST in comparison with intramuscular (IM) epinephrine 0...
February 11, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/29401648/chitosan-loaded-into-a-hydrogel-delivery-system-as-a-strategy-to-treat-vaginal-co-infection
#4
Diego R Perinelli, Raffaella Campana, Athanasios Skouras, Giulia Bonacucina, Marco Cespi, Francesca Mastrotto, Wally Baffone, Luca Casettari
Polymeric hydrogels are common dosage forms designed for the topical administration of antimicrobial drugs to treat vaginal infections. One of the major advantages of using chitosan in these formulations is related to the intrinsic and broad antimicrobial activity exerted on bacteria and fungi by this natural polymer. Most vaginal yeast infections are caused by the pathogenic fungus Candida albicans. However, despite the anti-Candida activity towards and strains susceptibility to low molecular weight chitosan being documented, no information is available regarding the antimicrobial efficacy of mixed hydrogels in which chitosan is dispersed in a polymeric matrix...
February 3, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/29389848/feasibility-of-using-gluconolactone-trehalose-and-hydroxy-propyl-gamma-cyclodextrin-to-enhance-bendroflumethiazide-dissolution-using-lyophilisation-and-physical-mixing-techniques
#5
Ashraf Saleh, Kenneth McGarry, Cheng Shu Chaw, Amal Ali Elkordy
PURPOSE: Hydrophobic drugs are facing a major challenge in dissolution rate enhancement and solubility in aqueous solutions; therefore, a variety of methods have been used to improve dissolution rate and/or solubility of bendroflumethiazide as a model hydrophobic drug. METHODS: In this study, two main methods (physical mixing and lyophilisation) were used with gluconolactone, hydroxyl propyl γ-ccyclodextrin, and trehalose to explore this challenge. Bendroflumethiazide, practically insoluble in water, was mixed with one of the three excipients gluconolactone, hydroxyl propyl γ-cyclodextrin, and trehalose in three different ratios 1:1, 1:2, 1:5...
February 1, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/29382038/extended-duration-vascular-endothelial-growth-factor-inhibition-in-the-eye-failures-successes-and-future-possibilities
#6
REVIEW
Michael W Stewart
Vascular endothelial growth factor (VEGF) plays a pivotal role in the development of neovascularization and edema from several common chorioretinal vascular conditions. The intravitreally injected drugs (aflibercept, bevacizumab, conbercept, pegaptanib, and ranibizumab) used to treat these conditions improve the visual acuity and macular morphology in most patients. Monthly or bimonthly injections were administered in the phase III pivotal trials but physicians usually individualize therapy with pro re nata (PRN) or treat and extend regimens...
January 27, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/29373537/pharmacokinetics-and-pharmacodynamics-of-s-ketoprofen-co-administered-with-caffeine-a-preclinical-study-in-arthritic-rats
#7
Raúl Medina-López, Nancy Vara-Gama, Olivia Soria-Arteche, Luis A Moreno-Rocha, Francisco J López-Muñoz
The purpose of the present study was to determine whether caffeine modifies the pharmacokinetics and pharmacodynamics of (S)-ketoprofen following oral administration in a gout-type pain model. 3.2 mg/kg of (S)-ketoprofen alone and combined with 17.8 mg/kg of caffeine were administered to Wistar rats and plasma levels were determined between 0.5 and 24.0 h. Additionally, antinociception was evaluated based on the protocol of the PIFIR (pain-induced functional impairment in the rat) model before blood sampling between 0...
January 26, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/29370122/minoxidil-skin-delivery-from-nanoemulsion-formulations-containing-eucalyptol-or-oleic-acid-enhanced-diffusivity-and-follicular-targeting
#8
Eman Abd, Heather A E Benson, Michael S Roberts, Jeffrey E Grice
In this work, we examined enhanced skin delivery of minoxidil applied in nanoemulsions incorporating skin penetration enhancers. Aliquots of fully characterized oil-in-water nanoemulsions (1 mL), containing minoxidil (2%) and the skin penetration enhancer oleic acid or eucalyptol as oil phases, were applied to full-thickness excised human skin in Franz diffusion cells, while aqueous solutions (1 mL) containing minoxidil were used as controls. Minoxidil in the stratum corneum (SC), hair follicles, deeper skin layers, and flux through the skin over 24 h was determined, as well as minoxidil solubility in the formulations and in the SC...
January 25, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/29370068/pharmaceutical-cocrystals-new-solid-phase-modification-approaches-for-the-formulation-of-apis
#9
REVIEW
Anna Karagianni, Maria Malamatari, Kyriakos Kachrimanis
Cocrystals can be used as an alternative approach based on crystal engineering to enhance specific physicochemical and biopharmaceutical properties of active pharmaceutical ingredients (APIs) when the approaches to salt or polymorph formation do not meet the expected targets. In this article, an overview of pharmaceutical cocrystals will be presented, with an emphasis on the intermolecular interactions in cocrystals and the methods for their preparation. Furthermore, cocrystals of direct pharmaceutical interest, along with their in vitro properties and available in vivo data and characterization techniques are discussed, highlighting the potential of cocrystals as an attractive route for drug development...
January 25, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/29364167/preventing-crystal-agglomeration-of-pharmaceutical-crystals-using-temperature-cycling-and-a-novel-membrane-crystallization-procedure-for-seed-crystal-generation
#10
Elena Simone, Rahimah Othman, Goran T Vladisavljević, Zoltan K Nagy
In this work, a novel membrane crystallization system was used to crystallize micro-sized seeds of piroxicam monohydrate by reverse antisolvent addition. Membrane crystallization seeds were compared with seeds produced by conventional antisolvent addition and polymorphic transformation of a fine powdered sample of piroxicam form I in water. The membrane crystallization process allowed for a consistent production of pure monohydrate crystals with narrow size distribution and without significant agglomeration...
January 24, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/29360788/solvation-and-aggregation-of-meta-aminobenzoic-acid-in-water-density-functional-theory-and-molecular-dynamics-study
#11
Etienne Gaines, Devis Di Tommaso
Meta-aminobenzoic acid, an important model system in the study of polymorphism and crystallization of active pharmaceutical ingredients, exist in water in both the nonionic (mABA) and zwitterionic (mABA±) forms. However, the constituent molecules of the polymorph that crystallizes from aqueous solutions are zwitterionic. This study reports atomistic simulations of the events surrounding the early stage of crystal nucleation of meta-aminobenzoic acid from aqueous solutions. Ab initio molecular dynamics was used to simulate the hydration of mABA± and mABA and to quantify the interaction of these molecules with the surrounding water molecules...
January 23, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/29346275/a-review-on-recent-advances-in-stabilizing-peptides-proteins-upon-fabrication-in-hydrogels-from-biodegradable-polymers
#12
REVIEW
Faisal Raza, Hajra Zafar, Ying Zhu, Yuan Ren, Aftab -Ullah, Asif Ullah Khan, Xinyi He, Han Han, Md Aquib, Kofi Oti Boakye-Yiadom, Liang Ge
Hydrogels evolved as an outstanding carrier material for local and controlled drug delivery that tend to overcome the shortcomings of old conventional dosage forms for small drugs (NSAIDS) and large peptides and proteins. The aqueous swellable and crosslinked polymeric network structure of hydrogels is composed of various natural, synthetic and semisynthetic biodegradable polymers. Hydrogels have remarkable properties of functionality, reversibility, sterilizability, and biocompatibility. All these dynamic properties of hydrogels have increased the interest in their use as a carrier for peptides and proteins to be released slowly in a sustained manner...
January 18, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/29342089/chitosan-gel-to-treat-pressure-ulcers-a-clinical-pilot-study
#13
Virginia Campani, Eliana Pagnozzi, Ilaria Mataro, Laura Mayol, Alessandra Perna, Floriana D'Urso, Antonietta Carillo, Maria Cammarota, Maria Chiara Maiuri, Giuseppe De Rosa
Chitosan is biopolymer with promising properties in wound healing. Chronic wounds represent a significant burden to both the patient and the medical system. Among chronic wounds, pressure ulcers are one of the most common types of complex wound. The efficacy and the tolerability of chitosan gel formulation, prepared into the hospital pharmacy, in the treatment of pressure ulcers of moderate severity were evaluated. The endpoint of this phase II study was the reduction of the area of the lesion by at least 20% after four weeks of treatment...
January 17, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/29342085/development-of-a-region-specific-physiologically-based-pharmacokinetic-brain-model-to-assess-hippocampus-and-frontal-cortex-pharmacokinetics
#14
Zaril Zakaria, Raj Badhan
Central nervous system drug discovery and development is hindered by the impermeable nature of the blood-brain barrier. Pharmacokinetic modeling can provide a novel approach to estimate CNS drug exposure; however, existing models do not predict temporal drug concentrations in distinct brain regions. A rat CNS physiologically based pharmacokinetic (PBPK) model was developed, incorporating brain compartments for the frontal cortex (FC), hippocampus (HC), "rest-of-brain" (ROB), and cerebrospinal fluid (CSF). Model predictions of FC and HC Cmax, tmax and AUC were within 2-fold of that reported for carbamazepine and phenytoin...
January 17, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/29337865/pharmacokinetics-and-drug-metabolism-in-canada-the-current-landscape-a-summary-of-this-indispensable-special-issue
#15
EDITORIAL
Neal M Davies, Kishor M Wasan
Canadian Pharmaceutical Scientists have a rich history of groundbreaking research in pharmacokinetics and drug metabolism undertaken primarily throughout its Pharmacy Faculties and within the Pharmaceutical and Biotechnology industry.[...].
January 16, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/29342903/application-of-nanoparticle-technologies-in-the-combat-against-anti-microbial-resistance
#16
REVIEW
Mayur Kumar, Anthony Curtis, Clare Hoskins
Anti-microbial resistance is a growing problem that has impacted the world and brought about the beginning of the end for the old generation of antibiotics. Increasingly, more antibiotics are being prescribed unnecessarily and this reckless practice has resulted in increased resistance towards these drugs, rendering them useless against infection. Nanotechnology presents a potential answer to anti-microbial resistance, which could stimulate innovation and create a new generation of antibiotic treatments for future medicines...
January 14, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/29342879/ophthalmic-drug-delivery-systems-for-antibiotherapy-a-review
#17
REVIEW
Marion Dubald, Sandrine Bourgeois, Véronique Andrieu, Hatem Fessi
The last fifty years, ophthalmic drug delivery research has made much progress, challenging scientists about the advantages and limitations of this drug delivery approach. Topical eye drops are the most commonly used formulation in ocular drug delivery. Despite the good tolerance for patients, this topical administration is only focus on the anterior ocular diseases and had a high precorneal loss of drugs due to the tears production and ocular barriers. Antibiotics are popularly used in solution or in ointment for the ophthalmic route...
January 13, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/29329196/is-the-skin-absorption-of-hydrocortisone-modified-by-the-variability-in-dosing-topical-products
#18
Daniel A Paterson, Jacqueline Hallier, Elizabeth Jenkins, Sarah F Cordery, M Begoña Delgado-Charro
Fingertip units have been proposed as a tool to standardize topical therapy with semisolid formulations. However, no studies to date have characterized the variability in dosing by patients using this concept and whether this variability ultimately affects the topical absorption of drugs. This work aimed to answer these two questions. A first study determined the dose measured, the area of spread and the area-normalized dose for a 1% hydrocortisone cream and ointment applied by members of the public using this dosing approach before and after brief counselling...
January 12, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/29315234/curcumin-artemisinin-coamorphous-solid-xenograft-model-preclinical-study
#19
M K Chaitanya Mannava, Kuthuru Suresh, Manish Kumar Bommaka, Durga Bhavani Konga, Ashwini Nangia
Curcumin is a natural compound present in Indian spice turmeric. It has diverse pharmacological action but low oral solubility and bioavailability continue to limit its use as a drug. With the aim of improving the bioavailability of Curcumin (CUR), we evaluated Curcumin-Pyrogallol (CUR-PYR) cocrystal and Curcumin-Artemisinin (CUR-ART) coamorphous solid. Both of these solid forms exhibited superior dissolution and pharmacokinetic behavior compared to pure CUR, which is practically insoluble in water. CUR-ART coamorphous solid showed two fold higher bioavailability than CUR-PYR cocrystal (at 200 mg/kg oral dose)...
January 9, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/29316660/regulation-of-hepatic-ugt2b15-by-methylation-in-adults-of-asian-descent
#20
Steffen G Oeser, Jon-Paul Bingham, Abby C Collier
The hepatic uridine 5'-diphosphate-glucuronosyl transferases (UGTs) are critical for detoxifying endo- and xenobiotics. Since UGTs are also dynamically responsive to endogenous and exogenous stimuli, we examined whether epigenetic DNA methylation can regulate hepatic UGT expression and differential effects of ethnicity, obesity, and sex. The methylation status of UGT isoforms was determined with Illumina Methylation 450 BeadChip arrays, with genotyping confirmed by sequencing and gene expression confirmed with quantitative reverse transcriptase polymerase chain reaction (q-RT-PCR)...
January 7, 2018: Pharmaceutics
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