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Journal of Pharmacy and Pharmacology

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https://www.readbyqxmd.com/read/29341138/model-fitting-for-small-skin-permeability-data-sets-hyperparameter-optimisation-in-gaussian-process-regression
#1
Parivash Ashrafi, Yi Sun, Neil Davey, Roderick G Adams, Simon C Wilkinson, Gary Patrick Moss
OBJECTIVES: The aim of this study was to investigate how to improve predictions from Gaussian Process models by optimising the model hyperparameters. METHODS: Optimisation methods, including Grid Search, Conjugate Gradient, Random Search, Evolutionary Algorithm and Hyper-prior, were evaluated and applied to previously published data. Data sets were also altered in a structured manner to reduce their size, which retained the range, or 'chemical space' of the key descriptors to assess the effect of the data range on model quality...
January 17, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29341135/phenolic-fractions-from-nine-trifolium-species-modulate-the-coagulant-properties-of-blood-plasma-in-vitro-without-cytotoxicity-towards-blood-cells
#2
Joanna Kolodziejczyk-Czepas, Malgorzata Sieradzka, Barbara Moniuszko-Szajwaj, Pawel Nowak, Wiesław Oleszek, Anna Stochmal
OBJECTIVE: The study covers an evaluation of the influence of extracts (1-50 μg/ml), isolated from aerial parts of nine Trifolium L. species (i.e. T. alexandrinum, T. fragiferum, T. hybridum, T. incarnatum, T. pallidum, T. pratense, T. resupinatum var. majus, T. resupinatum var. resupinatum and T. scabrum) on haemostatic properties of blood plasma. METHODS: The clot formation and fibrinolysis assay (CFF), blood clotting times, the extrinsic and intrinsic coagulation pathway-dependent polymerization of plasma fibrin were measured...
January 17, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29341132/acanthoic-acid-suppresses-lipin1-2-via-tlr4-and-irak4-signalling-pathways-in-etoh-and-lipopolysaccharide-induced-hepatic-lipogenesis
#3
Jian Song, Xin Han, You-Li Yao, Ya-Mei Li, Jing Zhang, Dan-Yang Shao, Li-Shuang Hou, Ying Fan, Shun-Zong Song, Li-Hua Lian, Ji-Xing Nan, Yan-Ling Wu
OBJECTIVES: In alcoholic liver disease, alcohol and lipopolysaccharide (LPS) are major stimulation factors of hepatic lipogenesis. Our objective was to determine the protective mechanism of acanthoic acid (AA) in EtOH- and LPS-induced hepatic lipogenesis. METHODS: HSC-T6 cells were treated with ethanol (200 mm) plus LPS (1 μg/ml) for 1 h, followed by AA (10 or 20 μm) for another 6 h. C57BL/6 mice were pretreated with of AA (20 and 40 mg/kg) or equal volume of saline and then exposed to three doses of ethanol (5 g/kg body weight) within 24 h...
January 17, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29238994/intestinal-p-glycoprotein-inhibitors-benzoxanthone-analogues
#4
Song Wha Chae, Jaeok Lee, Jung Hyun Park, Youngjoo Kwon, Younghwa Na, Hwa Jeong Lee
OBJECTIVES: The inhibitors of P-glycoprotein (P-gp) which limits an access of exogenous compounds in the luminal membrane of the intestine have been studied to enhance the intestinal P-gp-mediated absorption of anticancer drugs. METHODS: Inhibition of the efflux pump by synthesized benzoxanthone derivatives was investigated in vitro and in vivo. MCF-7/ADR cell line was used for cytotoxicity assay and [3 H]-daunomycin (DNM) accumulation/efflux study. Eight benzoxanthone analogues were tested for their effects on DNM cytotoxicity...
December 13, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29238984/differing-disintegration-and-dissolution-rates-pharmacokinetic-profiles-and-gastrointestinal-tolerability-of-over-the-counter-ibuprofen-formulations
#5
Ingvar Bjarnason, Ozgur Sancak, Anne Crossley, Andrew Penrose, Angel Lanas
OBJECTIVES: Formulations of over the counter (OTC) NSAIDs differ substantially, but information is lacking on whether this alters their gastrointestinal profiles. To assess disintegration and dissolution rates and pharmacokinetics of four preparations of OTC ibuprofen and relate these with spontaneously reported gastrointestinal adverse events. METHODS: Disintegration and dissolution rates of ibuprofen tablets as (a) acid, (b) sodium salt, (c) lysine salt, and (d) as a liquid gelatine capsule were assessed...
December 13, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29238980/influence-of-paeoniflorin-and-menthol-on-puerarin-transport-across-mdck-and-mdck-mdr1-cells-as-blood-brain-barrier-in%C3%A2-vitro-model
#6
Bing Yang, Shouying Du, Yang Lu, Shan Jia, Mengdi Zhao, Jie Bai, Pengyue Li, Huichao Wu
OBJECTIVE: Our objective of this research was (1) to investigate the transport characteristics of puerarin through MDCK-MDR1 and MDCK cells and (2) to evaluate the effects of paeoniflorin and menthol on puerarin transport so as to (3) explore the enhancement mechanism. METHODS: The cytotoxicity of drugs on MDCK and MDCK-MDR1 was evaluated by the MTT assay, and the transport studies were performed in both directions. The membrane fluidity was evaluated by fluorescence recovery after photobleaching, and the membrane potential was estimated by the accumulation of DiBAC4(3) in the cells...
December 13, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29193143/anti-inflammatory-and-anti-apoptotic-effects-of-the-combination-of-ligusticum-chuanxiong-and-radix-paeoniae-against-focal-cerebral-ischaemia-via-tlr4-myd88-mapk-nf-%C3%AE%C2%BAb-signalling-pathway-in-mcao-rats
#7
Junfei Gu, Shulan Su, Jianming Guo, Yue Zhu, Ming Zhao, Jin-Ao Duan
OBJECTIVE: This study was performed to assess the anti-inflammatory and anti-apoptotic effects of the combination of Ligusticum chuanxiong and Radix Paeoniae (XS) on focal cerebral ischaemic stroke. METHODS: MCAO rats were used to evaluate the effect of XS on stroke. Cerebral water content was measured, and the levels of IFN-γ, IL-1β, IL-6 and IL-12 in serum and brain were assessed by ELISA kits. Protein expressions including p-p38, p-38, TLR-4, p-ERK, ERK, TLR-5, NF-κBp65, Myd88, Caspase-3 and Caspase-12 were examined by WB and IHC...
November 28, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29193086/transfer-rates-of-aflatoxins-from-herbal-medicines-to-decoctions-determined-by-an-optimized-high-performance-liquid-chromatography-with-fluorescence-detection-method
#8
Yujiao Nian, Haiwei Wang, Guangyao Ying, Meihua Yang, Ze Wang, Weijun Kong, Shihai Yang
OBJECTIVES: This study aimed to explore the transfer rates of aflatoxins from several contaminated herbal medicines by fungi to their decoctions. METHODS: Five types of commonly used herbal medicines including Lilii Bulbus, Hordei Fructus Germinatus, Nelumbinis Semen, Polygalae Radix and Bombyx Batryticatus were selected as the examples. Raw herbal medicine samples were treated by ultrasonication-assisted extraction with 70% methanol and immunoaffinity column clean-up, and the decoctions were prepared following the commonly used boiling method with water for 2 h...
November 28, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29193077/evaluating-bioequivalence-of-meloxicam-tablets-is-in-vitro-dissolution-test-overdiscriminating
#9
Chan Jin, Chenyao Zhao, Dachao Shen, Wenxiang Dong, Hongzhuo Liu, Zhonggui He
OBJECTIVES: The aim of the study was to assess the impact of the differences in dissolution profiles of meloxicam tablets on the in-vivo bioavailability parameters after oral administration. METHODS: Compare in-vitro dissolution testing in the recommended media to evaluate in-vivo bioequivalence outcomes for the Biopharmaceutics Classification System Class II weak acidic drugs. Nine Beagle dogs received a single oral administration of each formulation (7.5 mg) in a three-way crossover design...
November 28, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29193053/oral-insulin-delivery-existing-barriers-and-current-counter-strategies
#10
REVIEW
Ahmed Gedawy, Jorge Martinez, Hani Al-Salami, Crispin R Dass
OBJECTIVES: The chronic and progressive nature of diabetes is usually associated with micro- and macrovascular complications where failure of pancreatic β-cell function and a general condition of hyperglycaemia is created. One possible factor is failure of the patient to comply with and adhere to the prescribed insulin due to the inconvenient administration route. This review summarizes the rationale for oral insulin administration, existing barriers and some counter-strategies trialled...
November 28, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29168173/the-role-of-melatonin-on-chemotherapy-induced-reproductive-toxicity
#11
REVIEW
Hamed Haghi-Aminjan, Mohammad Hossein Asghari, Bagher Farhood, Mahban Rahimifard, Nasser Hashemi Goradel, Mohammad Abdollahi
OBJECTIVES: Reproductive malfunctions after chemotherapy still are a reason of reducing fertility and need specialized intensive care. The aim of this review was to investigate the effect of melatonin on the reproductive system under threatening with chemotherapeutic drugs. METHODS: To find the role of melatonin in the reproductive system during chemotherapy, a full systematic literature search was carried out based on Preferred Reporting Items for Systematic Reviews and Meta-Analyses guidelines in the electronic databases up to 17 April 2017 using search terms in the titles and abstracts...
November 23, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29148068/gastrodin-protects-myocardial-cells-against-hypoxia-reoxygenation-injury-in-neonatal-rats-by-inhibiting-cell-autophagy-through-the-activation-of-mtor-signals-in-pi3k-akt-pathway
#12
Xiang Li, Qinhui Zhu, Yuanyuan Liu, Zhiyong Yang, Bin Li
OBJECTIVES: This study aimed to investigate the protective effect of gastrodin (GAS) on myocardial cells with hypoxia/reoxygenation (H/R) injury in neonatal rats and explore the underlying mechanism. METHODS: Myocardial cells were extracted from neonatal rats and divided into six groups: control, H/R, H/R + Low-Concentration GAS, H/R + Middle-Concentration GAS, H/R + High-Concentration GAS and H/R + High-Concentration GAS + AKT Inhibitor groups. After 48-h treatment, cell viability, autophagosome quantity and the expression levels of LC3-II, p62, Akt, pAkt, mammalian target of rapamycin (mTOR) and uncoordinated 51-like kinase 1 (ULK1) in myocardial cells were made comparisons among each group...
November 17, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29148063/studies-on-the-curcumin-phospholipid-complex-solidified-with-soluplus-%C3%A2
#13
Jianan Wang, Lulu Wang, Lan Zhang, Dandan He, Jianming Ju, Weiguang Li
OBJECTIVES: With the purpose of developing a curcumin phospholipid complex (CPC) formulation with high performance, the CPC was prepared and solidified with Soluplus(®) in this study. METHODS: Soluplus(®) was used as a carrier to solidify CPC. The structures of the CPC and curcumin phospholipid complex - Soluplus(®) solidified powder (CSP) - were also characterized by differential scanning electron microscope, differential scanning calorimetry, Fourier transform infrared spectroscopy and X-ray diffractometer, and flowability, in-vitro dissolution and oral bioavailability were also investigated...
November 17, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29148061/endocannabinoids-modulate-gq-11-protein-coupled-receptor-agonist-induced-vasoconstriction-via-a-negative-feedback-mechanism
#14
REVIEW
Olga Karpińska, Marta Baranowska-Kuczko, Monika Kloza, Hanna Kozłowska
OBJECTIVES: The endocannabinoid (eCB) system centrally and peripherally regulates cardiovascular parameters, including blood pressure, in health and disease. The relationship between Gq/11 protein-coupled receptor activation, regulation of eCBs release (mainly 2-arachidonoylglycerol) and subsequent CB1 receptor activation was initially observed in the central nervous system. Here, we review the latest findings from systemic physiological studies which include for the first time data from pulmonary arteries...
November 17, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29125176/hplc-dad-esi-ms-ms-analysis-of-fruits-from-firmiana-simplex-l-and-evaluation-of-their-antioxidant-and-antigenotoxic-properties
#15
Mosad Ahmed Ghareeb, Tamer Mohamed, Amal Mohamed Saad, Laila Abdel-Ghany Refahy, Mansour Sobeh, Michael Wink
OBJECTIVES: The secondary metabolites of the fruits of Firmiana simplex (L.) were analysed by LC-DAD-ESI-MS/MS; furthermore, we evaluated their antioxidant and antigenotoxic properties. METHODS: The antioxidant activity was investigated using the 2,2'-diphenyl-1-picrylhydrazyl radical (DPPH), the 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) diammonium salt (ABTS) and the ferric reducing antioxidant power (FRAP) assays. The antigenotoxic potential was determined via the comet assay...
November 10, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29105086/dose-dependent-effect-of-triiodothyronine-on-the-chondrogenic-differentiation-of-mesenchymal-stem-cells-from-the-bone-marrow-of-female-rats
#16
Higor A Assis, Nathalia C Elert, André Luiz B P Azevedo, Iolanda S Braga, Rogéria Serakides, Natália de Melo Ocarino, Alfredo M de Goes, Francisco de Paula Careta, Greiciane G Paneto, Adriana M A da Silva, Jankerle N Boeloni
OBJECTIVES: Verify the in-vitro effect of triiodothyronine (T3) on the chondrogenic differentiation of female rat bone marrow mesenchymal stem cells (BMMSCs) over several time periods and at several doses. METHODS: CD54 + /CD73 + /CD90 +  BMMSCs from Wistar female rats were cultured in chondrogenic medium with or without T3 (0.01; 1; 100; 1000 nm). At seven, 14 and 21 days, the cell morphology, chondrogenic matrix formation and expression of Sox9 and collagen II were evaluated...
November 3, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29072321/standardised-evaluation-of-medicine-acceptability-in-paediatric-population-reliability-of-a-model
#17
Thibault Vallet, Fabrice Ruiz, Marc Lavarde, Anne-Marie Pensé-Lhéritier, Ameziane Aoussat
OBJECTIVES: Our novel tool to standardise the evaluation of medicine acceptability was developed using observational data on medicines use measured in a paediatric population included for this purpose (0-14 years). Using this tool, any medicine may be positioned on a map and assigned to an acceptability profile. The present exploration aimed to verify its statistical reliability. METHODS: Permutation test has been used to verify the significance of the relationships among measures highlighted by the acceptability map...
October 26, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29072315/methyl-jasmonate-a-phytohormone-with-potential-for-the-treatment-of-inflammatory-bowel-diseases
#18
REVIEW
Jean Carlos Fernando Besson, Caroline de Carvalho Picoli, Graciette Matioli, Maria Raquel Marçal Natali
OBJECTIVES: The phytohormone methyl jasmonate (MeJA) has been identified as a vital cell regulator in plants. This substance is analogous to eicosanoids and similar to that of anti-inflammatory prostaglandins. In animals and in animal cells, it displayed an efficient neuroprotective, anti-inflammatory and antioxidant action; while in tumoral strains, it demonstrates a potentially highly attractive mechanism of apoptosis induction through various cellular and molecular mechanisms. The aim of the present review was to explore two new hypotheses that explain the action of MeJA, a lipid phytohormone and its potentially anti-apoptotic mechanism for use as a therapeutic target for future treatment of Inflammatory bowel diseases (IBDs)...
October 26, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29057480/cannabinoids-concentration-variability-in-cannabis-olive-oil-galenic-preparations
#19
Chiara Carcieri, Cristina Tomasello, Marco Simiele, Amedeo De Nicolò, Valeria Avataneo, Luca Canzoneri, Jessica Cusato, Giovanni Di Perri, Antonio D'Avolio
OBJECTIVES: Knowledge of the exact concentration of active compounds in galenic preparations is crucial to be able to ensure their quality and to properly administer the prescribed dose. Currently, the need for titration of extracts is still debated. Considering this, together with the absence of a standard preparation method, the aim of this study was to evaluate cannabinoids concentrations variability in galenic olive oil extracts, to evaluate the interlot and interlaboratory variability in the extraction yield and in the preparation composition...
January 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29205370/abstracts-of-the-royal-pharmaceutical-society-rps-winter-summit-2017-london-uk-5-december-2017
#20
(no author information available yet)
No abstract text is available yet for this article.
December 2017: Journal of Pharmacy and Pharmacology
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