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Drug Research

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https://www.readbyqxmd.com/read/28427104/pharmacokinetics-and-pharmacodynamics-of-tofogliflozin-a-selective-sglt2-inhibitor-in-healthy-male-subjects
#1
Nahoko Kasahara-Ito, Hiroyuki Fukase, Yoichiro Ogama, Tomohisa Saito, Yasuhiro Ohba, Sumire Shimada, Yasuki Takano, Tomoko Ichihara, Kimio Terao, Noboru Nakamichi, Yuji Kumagai, Sachiya Ikeda
Tofogliflozin is a selective oral inhibitor of sodium-glucose co-transporter 2 for treatment of type 2 diabetes mellitus. The pharmacokinetics, pharmacodynamics, and safety of tofogliflozin were investigated in healthy male subjects. Three studies were conducted: single-ascending dose study (10-640 mg) in 56 Japanese and 24 Caucasian subjects; multiple-ascending dose study (2.5-80 mg once daily for 7 days) in 24 Japanese subjects; and food-effect study (20-40 mg) in 30 Japanese subjects. Tofogliflozin was absorbed rapidly and eliminated from the systemic circulation with a t1/2 of 5-6 h...
April 20, 2017: Drug Research
https://www.readbyqxmd.com/read/28351081/osteoarthritis-patients-experiences-of-pharmacotherapy-for-pain-management-in-iran-a-qualitative-study
#2
Vahid Zamanzadeh, Fazlollah Ahmadi, Mozhgan Behshid, Alireza Irajpoor, Parvin Zakeri-Milani
Despite the effectiveness of pharmacotherapy for pain management in patients with osteoarthritis (OA), personal biases in the selection, administration, and continuation of pharmacotherapy challenge the proper management of symptoms and the effectiveness of the therapy. This study was conducted to carry out an in-depth examination of the experiences of patients with OA about their use of pharmacotherapy for the OA pain management and the existing challenges. The present qualitative study was conducted on 17 patients with OA, 5 of their family members and 8 healthcare personnel using a conventional content analysis approach...
March 28, 2017: Drug Research
https://www.readbyqxmd.com/read/28320041/prevention-of-iron-overload-and-long-term-maintenance-of-normal-iron-stores-in-thalassaemia-major-patients-using-deferiprone-or-deferiprone-deferoxamine-combination
#3
Annita Kolnagou, Christina N Kontoghiorghe, George J Kontoghiorghes
Decrease in mortality and morbidity is observed in thalassaemia major patients with reduced iron load in comparison to heavy iron loaded patients. Effective and complete treatment of transfusional iron overload can be achieved by chelation protocols that can eliminate excess iron and maintain normal iron stores (NIS). The maintenance of NIS, i. e., serum ferritin (350 μg/L >), MRI T2* cardiac (>20 ms) and liver (>6.3 ms) relaxation time levels was monitored in 16 thalassaemia major patients (32-53 years, 12 splenectomized, 10 male, erythrocyte transfusions 120-323 ml/kg/year) for about 90 patient years...
March 20, 2017: Drug Research
https://www.readbyqxmd.com/read/28320040/mitochondria-as-a-target-for-the-cardioprotective-effects-of-cydonia-oblonga-mill-and-ficus-carica-l-in-doxorubicin-induced-cardiotoxicity
#4
Saman Gholami, Mir-Jamal Hosseini, Leila Jafari, Fatemeh Omidvar, Mohammad Kamalinejad, Vida Mashayekhi, Seyed Hojjat Hosseini, Azin Kardan, Jalal Pourahmad, Mohammad Reza Eskandari
Quince (Cydonia oblonga Mill.) and fig (Ficus carica L.) exhibit a broad spectrum of pharmacological activities. Regarding the cardiotoxic effect of doxorubicin (DOX) is mediated mainly through mitochondrial oxidative stress and dysfunction; the present study evaluated the cardioprotective effects of the aqueous extracts of Cydonia oblonga Mill. fruit (ACO) and Ficus carica L. fruit (AFC) against DOX-induced cardiotoxicity. Cardiomyocytes toxicity was induced in male Sprague Dawley rats by intraperitoneal (ip) injections of 2...
March 20, 2017: Drug Research
https://www.readbyqxmd.com/read/28320039/the-role-of-peganum-harmala-ethanolic-extract-and-type-ii-toxin-antitoxin-system-in-biofilm-formation
#5
Nasrin Valizadeh, Firuzeh Valian, Nourkhoda Sadeghifard, Shahriar Karami, Iraj Pakzad, Hossein Kazemian, Sobhan Ghafourian
Toxin antitoxin system is a regulatory system that antitoxin inhibits the toxin. We aimed to determine the role of TA loci in biofilm formation in K. pneumoniae clinical and environmental isolates; also inhibition of biofilm formation by Peganum harmala. So, 40 K. pneumoniae clinical and environmental isolates were subjected for PCR to determine the frequency of mazEF, relEB, and mqsRA TA loci. Biofilm formation assay subjected for all isolates. Then, P. harmala was tested against positive biofilm formation strains...
March 20, 2017: Drug Research
https://www.readbyqxmd.com/read/28288491/effect-of-traditional-treatment-of-diabetes-mellitus-with-xanthosoma-sagittifolium-on-the-male-reproductive-system-of-alloxan-induced-diabetic-wistar-rats
#6
Olayinka A Oridupa, Oluyemisi F Folasire, Adedotun J Owolabi, Oluwasanmi Aina
The management of diabetes mellitus (DM) targets glycemic control as well as prevention or reversal of other complications associated with the metabolic disorder. One of such complications is the infertility which has been traced to oxidative stress and DNA damage caused by DM. In this study, experimentally-induced diabetic male Wistar rats were fed with Xanthosoma sagittifolium (cocoyam) for 14 days and its effect on sperm morphology and characteristics, as well as histology of the testes were assessed. X...
March 13, 2017: Drug Research
https://www.readbyqxmd.com/read/28288490/development-in-vitro-characterization-antitumor-and-aerosol-performance-evaluation-of-respirable-prepared-by-self-nanoemulsification-method
#7
Neda Naseri, Parvin Zakeri-Milani, Hamed Hamishehkar, Younes Pilehvar-Soltanahmadi, Hadi Valizadeh
Poor water solubility and low oral bioavailability limit the clinical application of Erlotinib as an anticancer. For this purpose, we encapsulated erlotinib in the solid lipid nanoparticles (SLN) and designed a spray-dried dry powder inhalable (DPI) formulation. Erlotinib-loaded SLNs were prepared using self-nanoemulsifying and characterized for physicochemical properties. Pulmonary deposition of spray-dried DPI formulation was performed using Next Generation Impactor. The particle size and zeta potential of Erlotinib-loaded SLNs were 300 to 800 nm and -18 to -32 mV, respectively...
March 13, 2017: Drug Research
https://www.readbyqxmd.com/read/28288489/impact-of-the-herbal-breviscapine-on-the-pharmacokinetics-of-simvastatin-in-rats-the-involvement-of-cyp3a4
#8
Aixia Ju, Yang Yang Li, Zhe Qu, Qiuhong Li
The effect of breviscapine injection on the pharmacokinetics of simvastatin and the mRNA expression of hepatic cytochrome P450 (CYP) enzyme was investigated with rats. The rats were pretreated for 8 consecutive days with breviscapine injection (20 mg/kg/day, i. v.), followed by administration of simvastatin through gavage (40 mg/kg). The control rats received the corresponding volume of saline solution for the pretreatment. Blood samples were collected at varied time points after simvastatin administration and the liver was harvested after the last collection of the blood sample for measurement of the CYP3A4 mRNA expression...
March 13, 2017: Drug Research
https://www.readbyqxmd.com/read/28268238/role-of-chemically-modified-tetracyclines-in-the-management-of-periodontal-diseases-a-review
#9
Archit A Ghangurde, Kiran Kumar Ganji, Manohar L Bhongade, Bhumika Sehdev
Researchers have found that Chemically Modified Tetracyclines (CMTs) act through multiple mechanisms, affecting several parameters of osteoclast function and consequently inhibit bone resorption by altering intracellular calcium concentration and interacting with the putative calcium receptor; decreasing ruffled border area; diminishing acid production; diminishing the secretion of lysosomal cysteine proteinases (cathepsins); inducing cell retraction by affecting podosomes; inhibiting osteoclast gelatinase activity; selectively inhibiting osteoclast ontogeny or development; and inducing apoptosis or programmed cell death of osteoclasts...
March 7, 2017: Drug Research
https://www.readbyqxmd.com/read/28268237/effect-of-a-bicyclic-pyrimidine-derivative-krp-103-a-novel-selective-tachykinin-nk1-receptor-antagonist-on-bladder-function-in-guinea-pigs
#10
Asao Tanioka, Takashi Deguchi
We evaluated the pharmacological characteristics of KRP-103, chemically named as ((2-(4-acetylpiperazin-1-yl)-6-[3,5-bis(trifluorometheyl)-phenylmethyl]-4- (2-methylphenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,5]oxazocin-5-one), and its effects on lower urinary tract function in guinea pigs. In radioligand binding assay, KRP-103 showed higher selectivity for human NK1 receptor (hNK1R) than for human NK2 receptor (hNK2R) and human NK3 receptor (hNK3R) (Ki for hNK1R, hNK2R and hNK3R=0.126 nM, > 10 000 nM and > 10 000 nM)...
March 7, 2017: Drug Research
https://www.readbyqxmd.com/read/28268236/design-network-analysis-and-in-silico-modeling-of-biologically-significant-4-substituted-benzyl-2-amino-6-hydroxypyrimidine-5-carboxamide-nanoparticles
#11
Theivendren Panneerselvam, Vellaichamy Sivakumar, Subramanian Arumugam, Kunjiappan Selvaraj, Murugan Indhumathy
The synthesized 4-(4-hydroxy benzyl)-2-amino-6-hydroxy pyrimidine-5-carboxamide was chosen to perform in silico modeling with identified drug target AGT, TNF, F2 and BCL2L1. The identified human proteins are vital in the pain management and also an important target for the study of wound healing activity. The enzymes were identified by using BioGRID, string database and network analysis through Cytoscape software. The wound healing activity was evaluated by excision wound model. The observed results revealed that, the pyrimidine nanoparticles showed significant wound healing activity compared to standard and synthesized compound...
March 7, 2017: Drug Research
https://www.readbyqxmd.com/read/28255972/gastroprotective-effect-of-thymoquinone-on-water-immersion-restraint-stress-induced-ulceration-in-rats
#12
Syed Sufiyan Ahmad, Abul Kalam Najmi, Madhu Kaundal, Mohd Akhtar
To evaluated the role of thymoquinone (TQ) on stress induced ulceration progress in rats subjected to water immersion restraint as a stress (WRS) condition model. Wistar albino rats were divided into different groups; the animals were subjected to WRS. TQ (10 mg/kg) alone and TQ with ranitidine (20 mg/kg) were administered per orally as pre treatment for 7 days. On 8(th) day the animals were sacrificed, gastric juice, pH, acid secretion, acid output, ulcer index and markers of oxidative stress and histopathology were determined...
March 2, 2017: Drug Research
https://www.readbyqxmd.com/read/28222467/design-and-synthesis-of-new-1-3-4-oxadiazole-benzothiazole-and-hydrazone-derivatives-as-promising-chemotherapeutic-agents
#13
Betül Kaya, Weiam Hussin, Leyla Yurttaş, Gülhan Turan-Zitouni, Hülya Karaca Gençer, Merve Baysal, Abdullah Burak Karaduman, Zafer Asim Kaplancıklı
Looking for new cytotoxic and antimicrobial agents with improved antitumor activity, a series of hydrazide and oxadiazole derivatives were designed and synthesized using 3-methoxyphenol as starting substance. Novel N'-(arylidene)-2-(3-methoxyphenoxy)acetohydrazide derivatives (4a-f)/1-(4-substitutedphenyl)-2-[(5-[(3-methoxyphenoxy)methyl]-1,3,4-oxadiazol-2-yl)thio]ethan-1-one derivatives (6a-f)/N-(6-substitutedbenzothiazol-2-yl)-2-[(5-[(3-methoxyphenoxy)methyl]-1,3,4-oxadiazol-2-yl)thio]acetamide derivatives (7a-e) were obtained and evaluated for their in vitro antimicrobial activity against various gram-positive, gram-negative bacteria and fungi...
February 21, 2017: Drug Research
https://www.readbyqxmd.com/read/28222466/cromolyn-sodium-attenuates-paraquat-induced-lung-injury-by-modulation-of-proinflammatory-cytokines
#14
Amir Larki Harchegani, Ali Asghar Hemmati, Amir Nili-Ahmadabadi, Borhan Darabi, Somayeh Shabib
The current study aimed to investigate the effects of Cromolyn Sodium (CS) on proinflammatory cytokines in Paraquat (PQ)-induced lung damage in rat. Animals were randomly divided into 5 groups. Group 1 and 2 received nebulized vehicle and CS (8 mg/kg) for 3 consecutive weeks, respectively. Group 3 was treated with single oral dose of PQ (40 mg/kg). Groups 4 and 5 were PQ groups which received nebulized CS (6 and 8 mg/kg/day, respectively) from 1 week before to 2 weeks after PQ administration. Finally, the animals were scarified and the changes of hydroxyproline (HP) and histology were evaluated in lung tissue...
February 21, 2017: Drug Research
https://www.readbyqxmd.com/read/28212595/preparation-and-characterization-of-gold-nanoparticles-in-the-presence-of-citrate-and-soybean-seed-extract-in-an-acidic-conditions
#15
Ebrahim Izadi, Ali Rasooli, Abolfazl Akbarzadeh, Soodabeh Davaran
Through the present study, an eco-friendly method was used to synthesize the gold nanoparticles (GNPs) by using the sodium citrate and extract of the soybean seed as reducing the agents at PH 3. X-Ray diffraction (XRD) method was used to evaluate the crystal structure of as-synthesized NPs and it's revealed that this method leads to well crystallized GNPs. In order to determine the particle size and their distribution, field emission scanning microscopy (FE-SEM) and dynamic light scattering (DLS) were used...
February 17, 2017: Drug Research
https://www.readbyqxmd.com/read/28208189/advances-in-silver-nanotechnology-an-update-on-biomedical-applications-and-future-perspectives
#16
Shiva Gholizadeh-Ghaleh Aziz, Sara Gholizadeh-Ghaleh Aziz, Abolfazl Akbarzadeh
Nanotechnology is one of the most promising fields for producing new applications in nanotechnology, biotechnology, and medicine. However, only a few products have been used for nanotechnology, biotechnology, and medical purposes. Nanoparticles have been among the most usually applied nanomaterial in our health care system for hundreds of years. The most prominent nano product is nano silver which generally present at 1-100 nm in size in at least one dimension. Silver nanoparticles reveal remarkably unusual chemical, physical and biological properties and have been used for many different applications which detailed in this review...
April 2017: Drug Research
https://www.readbyqxmd.com/read/28196394/synthesis-and-evaluation-of-a-triblock-copolymer-zno-nanoparticles-from-poly-%C3%AE%C2%B5-caprolactone-and-poly-acrylic-acid-as-a-potential-drug-delivery-carrier
#17
Lida Ahmadkhani, Ali Baghban, Shahram Mohammadpoor, Rovshan Khalilov, Abolfazl Akbarzadeh, Taras Kavetskyy, Siamak Saghfi, Aygun N Nasibova
Through the present paper, a triblock copolymer containing pH-responsive (polyacrylic acid-b-polycaprolactone -b-polyacrylic acid) (PAA-b-PCL-b-PAA) was synthesized by using the ring-opening polymerization (ROP) of ε-caprolactone (ε-CL) and the reversible addition fragmentation chain transfer (RAFT) polymerization of the acrylic acid methods, as the drug carrier. Blends of the nanocrystalline zinc oxide nanoparticles (n-ZnO) and triblock copolymer treated from the solution have been used to make the hybrid polymer-metal oxide for the preparation of the drug loaded nanocomposite...
April 2017: Drug Research
https://www.readbyqxmd.com/read/28166590/the-effect-of-chrysin-loaded-plga-peg-on-metalloproteinase-gene-expression-in-mouse-4t1-tumor-model
#18
Zoheyr Mohammadi, Mohsen Sharif Zak, Khaled Seidi, Meisam Barati, Abolfazl Akbarzadeh, Nosratollah Zarghami
Despite the advances in medicine, cancer remains as one of the leading causes of the death worldwide. Through our previous study, the Chrysin loaded PGLA/PEG has been synthesized, and its physico-chemical properties were characterized. The aim of the present study was to evaluate the Chrysin loaded PGLA/PEG nanoparticle therapeutic effects on TIMP-1, TIMP-2, MMP-2, MMP-9 and PI3k expression in Mouse 4T1 breast tumor model.30 mice were enrolled in the current study, and the mice were randomly divided into 3 groups: untreated (n=10), Chrysin treatment (n=10) and Chrysin-loaded PLGA/PEG-based treatment (n=10)...
April 2017: Drug Research
https://www.readbyqxmd.com/read/28158894/is-the-inhibition-of-dipeptidyl-peptidase-4-ddp-4-enzyme-route-dependent-and-or-driven-by-high-peak-concentration-seeking-answers-with-zydpla1-a-novel-long-acting-dpp-4-inhibitor-in-a-rodent-model
#19
Harilal Patel, Amit A Joharapurkar, Rajesh Bahekar, Prakash Patel, Samadhan G Kshirsagar, Nirav Modi, Ashok Ghoghari, Vishal J Patel, Mukul R Jain, Nuggehally R Srinivas, Pankaj R Patel, Ranjit C Desai
ZYDPLA1 is a long acting enzyme dipeptidyl peptidase-4 (DPP-4) inhibitor. The comparative effect of DPP-4 inhibition after intravenous (IV) and oral administration of ZYDPLA1 in a rat model was evaluated to answer the question of route dependency and/or the need of high plasma levels of ZYDPLA1. The study was conducted using parallel design in male Wistar rats for IV/oral route (n=9 and 6, for IV and oral respectively). A single 30 mg/kg dose of ZYDPLA1 was administered. Plasma samples were analysed for ZYDPLA1 concentration and DPP-4 inhibition...
April 2017: Drug Research
https://www.readbyqxmd.com/read/28158893/efficacy-and-safety-of-phytosomal-curcumin-in-non-alcoholic-fatty-liver-disease-a-randomized-controlled-trial
#20
Yunes Panahi, Parisa Kianpour, Reza Mohtashami, Ramezan Jafari, Luis E Simental-Mendía, Amirhossein Sahebkar
Non-alcoholic fatty liver disease (NAFLD) is a common liver disease characterized by excess lipid deposition in the hepatic tissue and subsequent oxidative and inflammatory damage. Curcumin is a dietary polyphenol with lipid-modifying, antioxidant and anti-inflammatory properties. This study aimed to evaluate the efficacy and safety of supplementation with phytosomal curcumin in subjects with NAFLD.Patients diagnosed with NAFLD (grades 1-3 according to liver ultrasonography) were randomly assigned to the curcumin (phytosomal form; 1 000 mg/day in 2 divided doses) (n=50) or placebo group (n=52) for a period of 8 weeks...
April 2017: Drug Research
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