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Journal of Pharmacy and Pharmacology

Angelika Drynda, Bożena Obmińska-Mrukowicz, Ewa Zaczyńska, Michał Zimecki, Stanisław Ryng, Marcin Mączyński
OBJECTIVES: Immunoregulatory properties of 06K derivative (4-(4-chlorophenyl)-1-(5-amino-3-methylisoxazole-4-carbonyl)-thiosemicarbazide) in mouse in vivo models were investigated. METHODS: Several in vivo models were used: humoral and cellular immune response, carrageenan inflammatory reaction and determination of lymphocyte subsets in non-immunized mice. KEY FINDINGS: The compound administered before or after immunization with sheep erythrocytes (sheep red blood cell (SRBC)) elevated the number of plaque-forming cells (PFC), and this effect was stronger at lower doses...
October 26, 2016: Journal of Pharmacy and Pharmacology
Anand Joshi, Matthew Halquist, Zacharoula Konsoula, Yongzhen Liu, J P Jones, Christian Heidbreder, Phillip M Gerk
OBJECTIVES: The aim of this study was to improve the oral bioavailability of buprenorphine by inhibiting presystemic metabolism via the oral co-administration of 'Generally Recognized as Safe' compounds, thus providing an orally administered drug product with less variability and comparable or higher exposure compared with the sublingual route. METHODS: The present studies were performed in Sprague Dawley rats following either intravenous or oral administration of buprenorphine/naloxone and oral co-administration of 'Generally Recognized as Safe' compounds referred to as 'adjuvants'...
October 26, 2016: Journal of Pharmacy and Pharmacology
Makiko Kobayashi, Yusuke Hattori, Tetsuo Sasaki, Makoto Otsuka
OBJECTIVES: The purposes of this study were to clarify the amorphization by ball milling of atorvastatin calcium sesquihydrate (AT) and to analyse the change in dissolution kinetics. METHODS: The amorphous AT was prepared from crystal AT by ball milling and analysed in terms of the changes of its physicochemical properties by powder X-ray diffraction analysis (XRD), thermal analysis and infrared spectroscopy (IR). Moreover, to evaluate the usefulness of the amorphous form for pharmaceutical development, intrinsic solubility of the ground product was evaluated using a dissolution kinetic method...
October 26, 2016: Journal of Pharmacy and Pharmacology
Simone Hansmann, Adam Darwich, Alison Margolskee, Leon Aarons, Jennifer Dressman
OBJECTIVES: The aim of this study was (1) to determine how closely physiologically based pharmacokinetic (PBPK) models can predict oral bioavailability using a priori knowledge of drug-specific properties and (2) to examine the influence of the biopharmaceutics classification system class on the simulation success. METHODS: Simcyp Simulator, GastroPlus(™) and GI-Sim were used. Compounds with published Biowaiver monographs (bisoprolol (BCS I), nifedipine (BCS II), cimetidine (BCS III), furosemide (BCS IV)) were selected to ensure availability of accurate and reproducible data for all required parameters...
October 26, 2016: Journal of Pharmacy and Pharmacology
Eliza de Oliveira Cardoso, Bruno José Conti, Karina Basso Santiago, Fernanda Lopes Conte, Lucas Pires Garcia Oliveira, Rodrigo Tavanelli Hernandes, Marjorie de Assis Golim, José Maurício Sforcin
OBJECTIVES: Propolis is a natural product with a complex chemical composition. Its isolated compounds exert biological activities; however, its synergistic effects are unknown. The involvement of phenolic acids (caffeic - Caf, dihydrocinnamic - Cin and p-coumaric - Cou) alone or in combination was investigated in the action of propolis in human monocytes. METHODS: Cell viability was analysed by MTT assay; TNF-α, IL-6 and IL-10 production by enzyme-linked immunosorbent assay (ELISA); cell markers expression by flow cytometry; colony-forming units were counted to assess the microbicidal activity; and H2 O2 production was analysed by colorimetric assay...
October 24, 2016: Journal of Pharmacy and Pharmacology
Hariane Côco, Larissa Pernomian, Priscila C Pereira, Mayara S Gomes, Katia C Marchi, Alexandre H Lopes, Thiago M Cunha, Carlos R Tirapelli, Ana M de Oliveira
OBJECTIVES: To investigate the mechanisms underlying the effects of chronic restraint stress on the vascular contractile response induced by angiotensin (Ang) II in rat carotid. METHODS: Concentration-response curves for AngII were obtained in endothelium-intact or endothelium-denuded carotid rings, in the absence or presence of SC-560 (COX-1 inhibitor), SC-236 (COX-2 inhibitor), wortmannin (PI3 K-Akt inhibitor), ML171 (NOX-1 inhibitor), VAS2870 (NOX-4 inhibitor), tiron (O2- scavenger) or PEG-catalase (H2 O2 scavenger)...
October 24, 2016: Journal of Pharmacy and Pharmacology
Mahfoozur Rahman, Sarwar Beg, Amita Verma, Fahad A Al Abbasi, Firoz Anwar, Sumant Saini, Sohail Akhter, Vikas Kumar
OBJECTIVES: The present review explores the therapeutic application of herbals in rheumatoid arthritis (RA) therapy, and how nano/submicromedicine can be fit in the scope of its therapeutic delivery in RA has been addressed. KEY FINDINGS: Incorporation of bioactive such as polyphenols, thymoquinone, resveratrol, hesperidin, curcumin, celastrol and gambogic acid in a dose-dependent manner showed quite high efficacy for the treatment of RA. It can be attributed to their targeting ability against various inflammatory mediators including nitric oxide (NO), cytokines, chemokines, adhesion molecules, NF-kβ, lipoxygenase (LOXs) and arachidonic acid (AA)...
October 24, 2016: Journal of Pharmacy and Pharmacology
Toru Otori, Sumio Matzno, Atushi Kawase, Masahiro Iwaki, Tetsutaro Kimachi, Keiji Nishiwaki, William C Figoni, Ryuta Tominaga, Mai Asahide, Mayumi Nishikata, Yoshikazu Ishii, Kenji Matsuyama
OBJECTIVES: To avoid the chelate formation between levofloxacin (LVFX) and aluminium hydroxide in gastrointestinal tract, an ethoxycarbonyl 1-ethyl hemiacetal ester of levofloxacin (LVFX-EHE) was synthesised as a prodrug. METHODS: The effects of aluminium hydroxide on the bioavailability of LVFX following oral administration of LVFX-EHE were investigated in rats. Furthermore, the effects of aluminium hydroxide on small intestinal absorption of LVFX and LVFX-EHE when subjected to a hydrolysis experiment using in situ everted gut sac were investigated, and the minimal inhibitory concentrations (MICs) of LVFX and LVFX-EHE for various intestinal bacteria were measured...
October 24, 2016: Journal of Pharmacy and Pharmacology
Tsuyoshi Chiba, Keiko Noji, Shohei Shinozaki, Sachina Suzuki, Keizo Umegaki, Kentaro Shimokado
OBJECTIVES: Non-alcoholic fatty liver disease (NAFLD) is associated with impaired liver function, and resveratrol could suppress NAFLD progression. This study examined the effects of NAFLD on the expression of major cytochrome P450 (CYP) subtypes in the liver and whether the expression could be attenuated by resveratrol. METHODS: C57BL/6 mice (male, 10 weeks of age) were fed a high-fat and high-sucrose (HFHS) diet to induce NAFLD. Major Cyp subtype mRNA expression in the liver was measured by real-time RT-PCR...
October 19, 2016: Journal of Pharmacy and Pharmacology
Naoyuki Makita, Jun Ishiguro, Keisuke Suzuki, Futoshi Nara
OBJECTIVES: Recently, there has been a growing interest in the mechanism of action of dichloroacetate (DCA) for T-cell differentiation; however, this mechanism has not been elucidated in detail. Therefore, this study aimed to investigate the mechanism of action of DCA for Treg and Th17 differentiation with pyruvate dehydrogenase kinase (PDHK) inhibitor (AZD7545) and PDHK knockdown. METHODS: Inhibitory activity of DCA and AZD7545 against recombinant PDHK and intracellular PDH phosphorylation was measured...
October 19, 2016: Journal of Pharmacy and Pharmacology
Juliana Maria de Mello Andrade, Natasha Maurmann, Patricia Pranke, Izabel Cristina Casanova Turatti, Norberto Peporine Lopes, Amélia T Henriques
OBJECTIVES: The hexane (HEX) and dichloromethane (DCM) fractions from Blechnum binervatum, Blechnum brasiliense and Blechnum occidentale were studied about phytochemicals and biological properties using multitarget approach. METHODS: The chemical composition was performed by gas chromatography coupled with mass spectrometry detector (GC-MS) analysis. Antioxidant capacity was evaluated against free radicals and on lipid peroxidation. Monoamine oxidases (MAO) and cholinesterases enzymatic modulation, as well as effects on rat and human cells, were assessed...
October 17, 2016: Journal of Pharmacy and Pharmacology
Matthew R Wilson, David S Jones, Gavin P Andrews
OBJECTIVES: This research examined the application of hot melt extrusion (HME) in the preparation of matrix formulations containing hydroxypropyl cellulose (HPC) as a base polymer in combination with methyl cellulose (MC) and hydroxypropyl methylcellulose (HPMC). METHODS: The limit to which formulations could control drug release under varying paddle speeds, high alcohol environments and high and low drug loads was investigated on a Caleva 10 ST dissolution tester...
October 17, 2016: Journal of Pharmacy and Pharmacology
Lucas Pires Garcia Oliveira, Fernanda Lopes Conte, Eliza de Oliveira Cardoso, Bruno José Conti, Karina Basso Santiago, Marjorie de Assis Golim, Maria Teresa Cruz, José Maurício Sforcin
OBJECTIVES: Geopropolis (GEO) in combination with doxorubicin (DOX) reduced HEp-2 cells viability compared to GEO and DOX alone. A possible effect of this combination on the innate immunity could take place, and its effects were analysed on THP-1 cell - a human leukaemia monocytic cell line used as a model to study monocyte activity and macrophage activity, assessing cell viability, expression of cell markers and cytokine production. METHODS: THP-1 cells were incubated with GEO, DOX and their combination...
October 17, 2016: Journal of Pharmacy and Pharmacology
Soumitra Shome, Anupam Das Talukdar, Manabendra Dutta Choudhury, Mrinal Kanti Bhattacharya, Hrishikesh Upadhyaya
OBJECTIVES: Nanotechnology-based drug delivery systems can resolve the poor bioavailability issue allied with curcumin. The therapeutic potential of curcumin can be enhanced by making nanocomposite preparation of curcumin with metal oxide nanoparticles, poly lactic-co-glycolic acid (PLGA) nanoparticles and solid lipid nanoparticles that increases its bioavailability in the tissue. KEY FINDINGS: Curcumin has manifold therapeutic effects which include antidiabetic, antihypertensive, anticancer, anti-inflammatory and antimicrobial properties...
October 17, 2016: Journal of Pharmacy and Pharmacology
Liz Jamieson, Ian C K Wong, Finella Craig, Nanna Christiansen, Karen Brombley, Catherine Tuleu, Emily Harrop
OBJECTIVES: This paper seeks to highlight from a UK perspective the current lack of a research evidence base in paediatric palliative care that has resulted in a paucity of available medicines with appropriate formulations (strength and dosage form) to provide symptom management for children with life-limiting illnesses and to raise awareness of this group of 'therapeutic orphans'. Currently, clinicians have limited, often unsuitable medication choices for their paediatric palliative care patients, with little hope of moving away from the status quo...
October 13, 2016: Journal of Pharmacy and Pharmacology
Dina S El-Agamy
OBJECTIVES: This study aimed to evaluate the potential protective effects of pirfenidone (PFD) against concanavalin A (Con A)-induced hepatitis in mice. METHODS: Autoimmune model of hepatitis was established using single intravenous injection of Con A. Mice were randomly assigned into four groups as follows: control group; Con A group; and two groups, receiving PFD in two dose levels (200, 300 mg/kg) for 5 days before Con A administration. Extent of hepatitis was studied using biochemical, histopathological and immunohistochemical estimations...
October 13, 2016: Journal of Pharmacy and Pharmacology
Cinzia Pagano, Maria Cristina Tiralti, Luana Perioli
OBJECTIVES: Folic acid (FA) is an important source for the prevention of many diseases. However, its use is limited because the very low solubility (<10 mg/l particularly in the gastric environment) responsible for the incomplete adsorption of the administered dose. This study proposes a technological strategy to overcome this problem enhancing FA dissolution rate by means of a formulation able to make completely bioavailable the whole administered dose. METHODS: Folic acid was intercalated in the layered double hydroxides (LDHs) MgAl-LDH and ZnAl-LDH...
October 13, 2016: Journal of Pharmacy and Pharmacology
Girlaine Pereira da Silva, Daniele Corrêa Fernandes, Mariana Vieira Vigliano, Eduardo Nunes da Fonseca, Shirley Vânia Moura Santos, Paulo Roberto Marques, Maria da Graça Justo, Kátia Costa de Carvalho Sabino, Marsen Garcia Pinto Coelho
OBJECTIVES: Echinodorus macrophyllus (Kunth) Micheli (Alismataceae) is popularly used as an infusion to treat inflammatory diseases. This work fractionated the aqueous extract of E. macrophyllus (AEEm) to improve its anti-inflammatory effects. METHODS: Aqueous extract of E. macrophyllus was fractionated by Sephadex LH-20 and analysed by HPLC-DAD. Anti-inflammatory action was evaluated, in vivo, by air pouch model (total leucocyte, protein and leukotriene B4 (LTB4 )), and, in vitro, by neutrophil migration (transwell assay) and its Mac1 expression (flow cytometry), and RAW 264...
October 10, 2016: Journal of Pharmacy and Pharmacology
Waseem Kaialy, Hussaini Bello, Kofi Asare-Addo, Ali Nokhodchi
OBJECTIVES: The aim of this work was to investigate the use of liquisolid technique to sustain the release of a model highly soluble drug, diltiazem HCl, from liquisolid matrices containing Polyox, a recently proposed matrix-forming hydrophilic polymer as an alternative to hypromellose. METHODS: Polyox-based liquisolid formulations prepared using several non-volatile solvents (i.e. polysorbate 80, polyethylene glycol, polyethylene glycol 200 and polyethylene glycol 600) and then characterised using differential scanning calorimetry and powder X-ray diffraction...
October 7, 2016: Journal of Pharmacy and Pharmacology
Bruno J Conti, Karina B Santiago, Eliza O Cardoso, Paula P Freire, Robson F Carvalho, Marjorie A Golim, José M Sforcin
OBJECTIVES: Dendritic cells (DCs) are antigen-presenting cells, essential for recognition and presentation of pathogens to T cells. Propolis, a resinous material produced by bees from various plants, exhibits numerous biological properties, highlighting its immunomodulatory action. Here, we assayed the effects of propolis on the maturation and function of human DCs. METHODS: DCs were generated from human monocytes and incubated with propolis and LPS. NF-κB and cytokines production were determined by ELISA...
October 7, 2016: Journal of Pharmacy and Pharmacology
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