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Journal of Pharmacy and Pharmacology

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https://www.readbyqxmd.com/read/28220495/influence-of-hyperglycemia-on-liver-inflammatory-conditions-in-the-early-phase-of-non-alcoholic-fatty-liver-disease-in-mice
#1
Shinichi Harada, Kei Miyagi, Tokio Obata, Yasuko Morimoto, Kazuo Nakamoto, Ke Ih Kim, Soo Ki Kim, Soo Ryang Kim, Shogo Tokuyama
OBJECTIVES: A non-alcoholic fatty liver disease (NAFLD) has high prevalence and now important issue of public health. In general, there exists strong interaction between NAFLD and diabetes, but the detailed mechanism is unclear. In this study, we determined the effects of hyperglycemia on progression in the early phase of NAFLD in mice. METHODS: Male ddY mice were fed a choline-deficient, l-amino acid-defined, high-fat diet (CDAHFD) consisting of 60% of kcal from fat and 0...
February 21, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28220483/pharmacokinetics-and-pharmacodynamics-of-metamizol-in-co-administration-with-morphine-under-acute-and-chronic-treatments-in-arthritic-rats
#2
Patricia Esmeralda Carrillo-Calzadilla, Francisco Javier López-Muñoz, Luis Alfonso Moreno-Rocha, José Raúl Medina-López, Alma Rosa Cortés-Arroyo, Adriana Miriam Domínguez-Ramírez
OBJECTIVE: To investigate the relationship between metamizol pharmacokinetics and the antinociceptive effect produced after subcutaneous administration of metamizol (177.8 mg/kg) alone or in combination with morphine (3.2 mg/kg), under acute and chronic treatments. METHODS: Antinociception was assessed using the pain-induced functional impairment model in rat (PIFIR). Serial blood samples were collected from the same animals to study the pharmacokinetics of metamizol...
February 21, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28220480/quality-and-stability-of-extemporaneous-pyridoxal-phosphate-preparations-used-in-the-treatment-of-paediatric-epilepsy
#3
Abeer H A Mohamed-Ahmed, Matthew P Wilson, Maedelyn Albuera, Ting Chen, Philippa B Mills, Emma J Footitt, Peter T Clayton, Catherine Tuleu
OBJECTIVES: To assess the pyridoxal 5'-phosphate (PLP) content and stability of extemporaneous PLP liquids prepared from dietary supplements used for the treatment of vitamin B6 -dependent epilepsy. METHODS: Pyridoxal 5'-phosphate liquids were prepared in accordance with the guidelines given to patients from marketed 50 mg PLP dietary capsules and tablets. The PLP content and its stability were evaluated under conditions resembling the clinical setting using reverse phase HPLC and mass spectrometry...
February 21, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28211640/complexation-of-oxethazaine-with-2-hydroxypropyl-%C3%AE-cyclodextrin-increased-drug-solubility-decreased-cytotoxicity-and-analgesia-at-inflamed-tissues
#4
Andressa R Prado, Fabiano Yokaichiya, Margareth Kazuyo Kobayashi Dias Franco, Camila Morais Gonçalves da Silva, Laura Oliveira-Nascimento, Michelle Franz-Montan, Maria C Volpato, Luís F Cabeça, Eneida de Paula
OBJECTIVES: Oxethazaine (OXZ) is one of the few local anaesthetics that provides analgesia at low pH, but presents poor solubility, cytotoxicity and no parenteral formulations. To address these issues, we aimed to prepare OXZ host-guest inclusion complex with hydroxypropyl-beta-cyclodextrin (HP-β-CD). METHODS: The inclusion complex was formed by co-solubilization, followed by a job plot analysis to determine stoichiometry of complexation and dialysis equilibrium analysis (based on UV/VIS absorption and fluorescence profiles of OXZ)...
February 17, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28211580/inhibition-of-pde5a1-guanosine-cyclic-monophosphate-cgmp-hydrolysing-activity-by-sildenafil-analogues-that-inhibit-cellular-cgmp-efflux
#5
Anna Subbotina, Aina W Ravna, Roy A Lysaa, Ruben Abagyan, Ryszard Bugno, Georg Sager
OBJECTIVES: To determine the ability of 11 sildenafil analogues to discriminate between cyclic nucleotide phosphodiesterases (cnPDEs) and to characterise their inhibitory potencies (Ki values) of PDE5A1-dependent guanosine cyclic monophosphate (cGMP) hydrolysis. METHODS: Sildenafil analogues were identified by virtual ligand screening (VLS) and screened for their ability to inhibit adenosine cyclic monophosphate (cAMP) hydrolysis by PDE1A1, PDE1B1, PDE2A1, PDE3A, PDE10A1 and PDE10A2, and cGMP hydrolysis by PDE5A, PDE6C, PDE9A2 for a low (1 nm) and high concentration (10 μm)...
February 17, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28211571/inhibitory-effects-of-a-standardized-extract-of-justicia-pectoralis-in-an-experimental-rat-model-of-airway-hyper-responsiveness
#6
Carlos T M Moura, Francisco J Batista-Lima, Teresinha S Brito, Alfredo A V Silva, Luan C Ferreira, Cássia R Roque, Karoline S Aragão, Alexandre Havt, Francisco N Fonseca, Luzia K A M Leal, Pedro J C Magalhães
OBJECTIVE: Justicia pectoralis is a plant useful for the treatment of respiratory diseases. Here, we studied the antiasthmatic properties of a standardized extract of J. pectoralis (Jp). METHODS: Ovalbumin (OVA)-sensitized rats were actively challenged with saline or OVA to study airway hyper-responsiveness after oral treatment with saline or Jp. The ability of Jp to inhibit hyper-reactivity was evaluated in isolated trachea mounted in isolated organ bath chamber...
February 17, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28211563/cytotoxic-analysis-and-chemical-characterization-of-fractions-of-the-hydroalcoholic-extract-of-the-euterpe-oleracea-mart-seed-in-the-mcf-7-cell-line
#7
Dayanne da S Freitas, José A Morgado-Díaz, Adriana S Gehren, Flávia C B Vidal, Raquel Maria T Fernandes, Wanderson Romão, Lilian V Tose, Fabiola N S Frazão, Maria Célia P Costa, Dulcelena F Silva, Maria do Desterro S B Nascimento
OBJECTIVES: To analyse the antineoplastic activity of fractions derived from the hydroalcoholic extract of Euterpe oleracea Mart. seed in the MCF-7 cell line and to identify the compounds responsible for the antineoplastic action. METHODS: Cells were treated with 10, 20, 40 and 60 μg/ml with the hexane, chloroform and ethyl acetate fraction (EAF) of the hydroalcoholic extract of açaí seed, for 24 and 48 h. After treatment, cell viability was measured using MTT assay and cell death was assessed using the Annexin-Pi assay...
February 17, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28155992/biopharmaceutical-informatics-supporting-biologic-drug-development-via-molecular-modelling-and-informatics
#8
REVIEW
Sandeep Kumar, Nikolay V Plotnikov, Jason C Rouse, Satish K Singh
OBJECTIVES: The purpose of this article is to introduce an emerging field called 'Biopharmaceutical Informatics'. It describes how tools from Information technology and Molecular Biophysics can be adapted, developed and gainfully employed in discovery and development of biologic drugs. KEY FINDINGS: The findings described here are based on literature surveys and the authors' collective experiences in the field of biologic drug product development. A strategic framework to forecast early the hurdles faced during drug product development is weaved together and elucidated using chemical degradation as an example...
February 3, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28134972/novel-chemical-degradation-pathways-of-proteins-mediated-by-tryptophan-oxidation-tryptophan-side-chain-fragmentation
#9
REVIEW
Christian Schöneich
OBJECTIVES: This minireview focuses on novel degradation pathways of proteins in solution via intermediary tryptophan (Trp) radical cations, which are generated via photo-induced electron transfer to suitable acceptors such as disulfide bonds. METHODS: Gas-phase mass spectrometry studies had indicated the potential for Trp radical cations to fragment via release of 3-methylene-3H-indol-1-ium from the side chain. HPLC-MS/MS analysis demonstrates that analogous fragmentation reactions occur during the exposure of peptides and proteins to light or accelerated stability testing...
January 30, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28106257/limitations-of-polyethylene-glycol-induced-precipitation-as-predictive-tool-for-protein-solubility-during-formulation-development
#10
Melanie Hofmann, Matthias Winzer, Christian Weber, Henning Gieseler
OBJECTIVE: Polyethylene glycol (PEG)-induced protein precipitation is often used to extrapolate apparent protein solubility at specific formulation compositions. The procedure was used for several fields of application such as protein crystal growth but also protein formulation development. Nevertheless, most studies focused on applicability in protein crystal growth. In contrast, this study focuses on applicability of PEG-induced precipitation during high-concentration protein formulation development...
January 20, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28033670/a-mini-review-of-non-parenteral-clonidine-preparations-for-paediatric-sedation
#11
REVIEW
Sara M Hanning, Mine Orlu Gul, Irmgard Toni, Antje Neubert, Catherine Tuleu
OBJECTIVE: To provide an overview of non-parenteral clonidine formulations and assess the feasibility of their use for paediatric sedation. METHODS: A literature search was conducted using electronic databases and a combination of search terms. Forty articles met the inclusion criteria. Publications were grouped into different dosage forms and assessed for their potential application for sedation of children in intensive care. KEY FINDINGS: Several routes of clonidine administration have been investigated for numerous indications in children, including perioperative sedation and analgesia...
December 29, 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28028813/accuracy-of-tablet-splitting-and-liquid-measurements-an-examination-of-who-what-and-how
#12
Dana Abu-Geras, Dunja Hadziomerovic, Andrew Leau, Ramzan Nazim Khan, Sajni Gudka, Cornelia Locher, Maryam Razaghikashani, Lee Yong Lim
OBJECTIVE: To examine factors that might affect the ability of patients to accurately halve tablets or measure a 5-ml liquid dose. METHODS: Eighty-eight participants split four different placebo tablets by hand and using a tablet splitter, while 85 participants measured 5 ml of water, 0.5% methylcellulose (MC) and 1% MC using a syringe and dosing cup. Accuracy of manipulation was determined by mass measurements. KEY FINDINGS: The general population was less able than pharmacy students to break tablets into equal parts, although age, gender and prior experience were insignificant factors...
December 28, 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28000299/prolonged-release-minitablets-with-carbamazepine-preliminary-observations-in-vitro
#13
Magdalena Dzajkowska, Kotlowska Hanna, Madanecka Anna, Szczepanska Maja, Doniza Dagmara, Sosnowicz Anna, Sznitowska Malgorzata
OBJECTIVE: The aim was to develop prolonged-release minitablets (MT) with carbamazepine (CBZ). METHODS: Matrix-type 3-mm MT (5 mg CBZ) were prepared by direct compression using hydrophilic (hypromellose) or hydrophobic polymers (ethylcellulose, Kollidon SR, glyceryl behenate). Coated prolonged-release MT (2.5 mm/3 mg of CBZ) were produced using ethylcellulose or Eudragit RL/RS. The release tests were performed in a basket apparatus with water or 1% sodium lauryl sulphate solution as dissolution media...
December 20, 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28155996/anti-apoptotic-effects-of-curcuma-longa-l-extract-and-its-curcuminoids-against-blue-light-induced-cytotoxicity-in-a2e-laden-human-retinal-pigment-epithelial-cells
#14
Sang-Il Park, Eun Hye Lee, So Ra Kim, Young Pyo Jang
OBJECTIVES: The purpose of the study was to investigate the protective effect of the Curcuma longa L. extract (CLE) and its curcuminoids against blue light-induced cytotoxicity in human retinal pigment epithelial (RPE) cells laded with A2E. A2E has been concerned in age-related macular degeneration (AMD). METHODS: To perform this study, A2E-accumulated ARPE-19 cells were exposed to blue light to induce cytotoxicity. The cytotoxicity and apoptotic gene expression levels were evaluated using a lactate dehydrogenase (LDH) assay and real-time PCR analysis, respectively...
March 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28155991/in-vitro-evaluation-of-enteric-coated-insulin-tablets-containing-absorption-enhancer-and-enzyme-inhibitor
#15
Chun Y Wong, Jorge Martinez, Revathy Carnagarin, Crispin R Dass
OBJECTIVES: The aim of this study was to develop an enteric coated insulin tablet formulation using polymers, absorption enhancer and enzyme inhibitor, which protect the tablets in acidic pH and enhance systemic bioavailability. METHODS: In this study, the influence of coating by cellulose acetate hydrogen phthalate solution and chosen excipients on Glut-4 transporter translocation in C2C12 skeletal muscle cells was examined. Following the determination of optimum number of coating layers, two dissolution buffers such as 0...
March 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28134992/in-vitro-and-in-vivo-evaluation-of-the-modulatory-effects-of-the-multitarget-compound-ass234-on-the-monoaminergic-system
#16
Gerard Esteban, Jolien Van Schoors, Ping Sun, Ann Van Eeckhaut, José Marco-Contelles, Ilse Smolders, Mercedes Unzeta
OBJECTIVES: To evaluate the in-vitro and in-vivo effects on monoaminergic neurotransmission of ASS234, a promising multitarget-directed ligand (MTDL), for Alzheimer's disease (AD) therapy. METHODS: In vitro was explored the effect of ASS234 on the monoaminergic metabolism in SH-SY5Y and PC12 cell lines, and remaining activity of both monoamine oxidase (MAO) isoforms was assessed. The corresponding dopamine (DA), homovanillic acid (HVA) and 3,4-dihydroxyphenylacetic acid (DOPAC) and noradrenaline (NA) levels were determined by HPLC-ED...
March 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28134988/the-essential-oil-from-the-fruits-of-the-brazilian-spice-xylopia-sericea-a-st-hil-presents-expressive-in-vitro-antibacterial-and-antioxidant-activity
#17
Renata de F Mendes, Nícolas de C C Pinto, Josiane M da Silva, Jucélia B da Silva, Raquel C Dos S Hermisdorf, Rodrigo L Fabri, Luciana M Chedier, Elita Scio
OBJECTIVES: The aims of this study were to investigate the chemical composition and the antioxidant activity and antibacterial activity of the essential oil of Xylopia sericea fruits (OXS). The fruits of this species are popularly used for medicinal purposes, and as a condiment in food preparation. METHODS: The chemical composition of OXS was analysed by GC/MS. 1,1-Diphenyl-2-picrylhydrazyl (DPPH) scavenging, β-carotene/linoleic acid bleaching and phosphomolybdenum and thiobarbituric acid-reactive substance (TBARS) assays were used to evaluate the antioxidant activity...
March 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28134976/multicomponent-solid-forms-of-felodipine-preparation-characterisation-physicochemical-and-in-vivo-studies
#18
Renu Chadha, Mohit Sharma, Jamshed Haneef
OBJECTIVES: This study aimed to improve biopharmaceutical parameters of the poorly soluble antihypertensive drug, felodipine, by preparing multicomponent solid forms using three coformers, viz. imidazole, nicotinamide and malonic acid. METHODS: The multicomponent solid forms were prepared by mechanochemical synthesis and characterised by various analytical techniques. These solid forms were further assessed for their physicochemical parameters. Pharmacokinetic and in-vivo antihypertensive activity was performed in rats...
March 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28134974/orcinol-derivative-compound-with-antioxidant-properties-protects-langerhans-islets-against-streptozotocin-damage
#19
Nancy M V Sánchez-Lira, Angélica Morales-Miranda, Gustavo García de la Mora, Juan Carlos León Contreras, Ignacio González-Sánchez, Norma Valencia, Marco Cerbón, Sumiko Morimoto
OBJECTIVE: To design and synthesize an orcinol derivative compound, 3-formyl-2,4-dihydroxy-5,6-dimethyl sodium benzoate (A4), as an antioxidant molecule and to test its effects on oxidative stress in an in-vitro model of apoptosis of pancreatic rat beta cells induced by streptozotocin (STZ). METHODS: Scavenger properties of A4 were assessed using its capacity to capture the DPPH radical in vitro. Antiapoptotic properties of A4 were analysed by electron microscopy and TUNEL assay in rat pancreatic islets in a streptozotocin model...
March 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28134973/fucosterol-isolated-from-ecklonia-stolonifera-inhibits-adipogenesis-through-modulation-of-foxo1-pathway-in-3t3-l1-adipocytes
#20
Ji-Hyun Lee, Hyun Ah Jung, Min Jae Kang, Jae Sue Choi, Gun-Do Kim
OBJECTIVES: The purpose of this study was to investigate the effects of fucosterol on adipogenesis of 3T3-L1 preadipocytes and its underlying mechanisms. METHODS: Fucosterol, isolated from brown algae, Ecklonia stolonifera. We investigated the levels of lipid accumulation using Oil Red O staining. We conducted Western blot analysis to investigate regulatory effects of fucosterol on expression of phosphoinositide 3-kinase (PI3K), Akt, extracellular signal-regulated kinase (ERK), forkhead box protein O 1 (FoxO1) in 3T3-L1 adipocytes...
March 2017: Journal of Pharmacy and Pharmacology
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