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Drug Design, Development and Therapy

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https://www.readbyqxmd.com/read/28053508/critical-role-of-tedizolid-in-the-treatment-of-acute-bacterial-skin-and-skin-structure-infections
#1
REVIEW
Olivia Ferrández, Olatz Urbina, Santiago Grau
Tedizolid phosphate has high activity against the Gram-positive microorganisms mainly involved in acute bacterial skin and skin structure infections, such as strains of Staphylococcus aureus (including methicillin-resistant S. aureus strains and methicillin-sensitive S. aureus strains), Streptococcus pyogenes, Streptococcus agalactiae, the Streptococcus anginosus group, and Enterococcus faecalis, including those with some mechanism of resistance limiting the use of linezolid. The area under the curve for time 0-24 hours/minimum inhibitory concentration (MIC) pharmacodynamic ratio has shown the best correlation with the efficacy of tedizolid, versus the time above MIC ratio and the maximum drug concentration/minimum inhibitory concentration ratio...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28053507/riluzole-5-mg-ml-oral-suspension-for-optimized-drug-delivery-in-amyotrophic-lateral-sclerosis
#2
Ann Margaret Dyer, Alan Smith
The aim of the present work is to extensively evaluate the pharmaceutical attributes of currently available riluzole presentations. The article describes the limitations and risks associated with the administration of crushed tablets, including the potential for inaccurate dosing and reduced rate of absorption when riluzole is administered with high-fat foods, and the advantages that a recently approved innovative oral liquid form of riluzole confers on amyotrophic lateral sclerosis (ALS) patients. The article further evaluates the patented and innovative controlled flocculation technology used in the pseudoplastic suspension formulation to reduce the oral anesthesia seen with crushed tablets, resulting in optimized drug delivery for riluzole...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28053506/development-of-a-chitosan-based-double-layer-coated-tablet-as-a-platform-for-colon-specific-drug-delivery
#3
Min Soo Kim, Dong Woo Yeom, Sung Rae Kim, Ho Yub Yoon, Chang Hyun Kim, Ho Yong Son, Jin Han Kim, Sangkil Lee, Young Wook Choi
A double layer-coated colon-specific drug delivery system (DL-CDDS) was developed, which consisted of chitosan (CTN) based polymeric subcoating of the core tablet containing citric acid for microclimate acidification, followed by an enteric coating. The polymeric composition ratio of Eudragit E100 and ethyl cellulose and amount of subcoating were optimized using a two-level factorial design method. Drug-release characteristics in terms of dissolution efficiency and controlled-release duration were evaluated in various dissolution media, such as simulated colonic fluid in the presence or absence of CTNase...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28053505/spotlight-on-the-9-valent-hpv-vaccine
#4
REVIEW
Pier Luigi Lopalco
Starting in 2006, vaccination against human papillomavirus (HPV) has been progressively implemented in most developed countries. Two vaccines have been successfully used, a bivalent vaccine targeting HPV-related cancers (bHPV) and a quadrivalent vaccine (qHPV) targeting both HPV-related cancers and genital warts. Between December 2014 and June 2015, a new nonavalent HPV vaccine (9vHPV) was granted marketing authorization in the USA and Europe. The 9vHPV was developed from the qHPV and includes five additional HPV types that should increase the level of protection toward HPV-related cancers...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28053504/nitroglycerin-enhances-the-propagation-of-cortical-spreading-depression-comparative-studies-with-sumatriptan-and-novel-kynurenic-acid-analogues
#5
Levente Knapp, Bence Szita, Kitti Kocsis, László Vécsei, József Toldi
BACKGROUND: The complex pathophysiology of migraine is not yet clearly understood; therefore, experimental models are essential for the investigation of the processes related to migraine headache, which include cortical spreading depression (CSD) and NO donor-induced neurovascular changes. Data on the assessment of drug efficacy in these models are often limited, which prompted us to investigate a novel combined migraine model in which an effective pharmacon could be more easily identified...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28031702/development-of-docetaxel-nanocrystals-surface-modified-with-transferrin-for-tumor-targeting
#6
Jin-Seok Choi, Jeong-Sook Park
The purpose of this study was to develop the surface modification of docetaxel nanocrystals (DTX-NCs) with apo-Transferrin human (Tf) for improving the cellular uptake and cytotoxicity of DTX. DTX-NCs were prepared by a nanoprecipitation method, and the surface modified with Tf by an adsorption method (Tf-DTX-NCs). The morphology and particle size of DTX-NCs and Tf-DTX-NCs were characterized using a field emission scanning electron microscope and zetasizer. An in vitro drug release study was performed in phosphate-buffered saline containing 0...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28031701/gastroretentive-behavior-of-orally-administered-radiolabeled-tamarind-seed-formulations-in-rabbits-validated-by-gamma-scintigraphy
#7
Mahboubeh Razavi, Hamed Karimian, Chai Hong Yeong, Mehran Fadaeinasab, Si Lay Khaing, Lip Yong Chung, Didi Erwandi B Mohamad Haron, Mohamed Ibrahim Noordin
This study aimed to formulate floating gastroretentive tablets containing metformin hydrochloric acid (HCl), using various grades of hydrogel such as tamarind powders and xanthan to overcome short gastric residence time of the conventional dosage forms. Different concentrations of the hydrogels were tested to determine the formulation that could provide a sustained release of 12 h. Eleven formulations with different ratios of tamarind seed powder/tamarind kernel powder (TKP):xanthan were prepared. The physical parameters were observed, and in vitro drug-release studies of the prepared formulations were carried out...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28008233/folic-acid-conjugated-amphiphilic-alternating-copolymer-as-a-new-active-tumor-targeting-drug-delivery-platform
#8
Xia Li, Myron R Szewczuk, Cecile Malardier-Jugroot
Targeted drug delivery using polymeric nanostructures is an emerging cancer research area, engineered for safer, more efficient, and effective use of chemotherapeutic drugs. A pH-responsive, active targeting delivery system was designed using folic acid functionalized amphiphilic alternating copolymer poly(styrene-alt-maleic anhydride) (FA-DABA-SMA) via a biodegradable linker 2,4-diaminobutyric acid (DABA). The polymeric template is pH responsive, forming amphiphilic nanostructures at pH 7, allowing the encapsulation of hydrophobic drugs on its interior...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28008232/structure-based-virtual-screening-and-characterization-of-a-novel-il-6-antagonistic-compound-from-synthetic-compound-database
#9
Jing Wang, Chunxia Qiao, He Xiao, Zhou Lin, Yan Li, Jiyan Zhang, Beifen Shen, Tinghuan Fu, Jiannan Feng
According to the three-dimensional (3D) complex structure of (hIL-6⋅hIL-6R⋅gp 130)2 and the binding orientation of hIL-6, three compounds with high affinity to hIL-6R and bioactivity to block hIL-6 in vitro were screened theoretically from the chemical databases, including 3D-Available Chemicals Directory (ACD) and MDL Drug Data Report (MDDR), by means of the computer-guided virtual screening method. Using distance geometry, molecular modeling and molecular dynamics trajectory analysis methods, the binding mode and binding energy of the three compounds were evaluated theoretically...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28008231/protective-effects-of-vitamin-c-and-vitamin-e-against-hysterosalpingography-induced-epithelial-degeneration-and-proliferation-in-rat-endometrium
#10
Şehmus Pala, Remzi Atilgan, Tuncay Kuloğlu, Murat Kara, Melike Başpinar, Behzat Can, Gökhan Artaş
AIM: The aim of this study was to examine the protective effects of vitamin C (VC) and vitamin E (VE) against hysterosalpingography (HSG)-induced epithelial degeneration and proliferation in rat endometrium. MATERIALS AND METHODS: A total of 28 female Wistar albino rats were randomized into four groups: G1 (n=7; abdomen was opened and closed), G2 (n=7; 0.1 mL Lipiodol [ethiodized oil] was administered to each uterine horn in conjunction with X-ray irradiation), G3 (n=7; 50 mg/kg of intraperitoneal (ip) VC was administered, followed by the administration of 0...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28008230/efficacy-and-safety-of-iron-chelation-therapy-with-deferoxamine-deferiprone-and-deferasirox-for-the-treatment-of-iron-loaded-patients-with-nontransfusion-dependent-thalassemia-syndromes
#11
COMMENT
Ali T Taher, John B Porter, Antonis Kattamis, Vip Viprakasit, M Domenica Cappellini
No abstract text is available yet for this article.
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28008229/design-and-in-vitro-in-vivo-evaluation-of-sustained-release-floating-tablets-of-itopride-hydrochloride
#12
Sayed M Ahmed, Adel Ahmed Ali, Ahmed Ma Ali, Omiya A Hassan
PURPOSE: The aim of the present study was to improve the bioavailability of itopride (ITO) and sustain its action by formulating as a floating dosage form. MATERIALS AND METHODS: Sustained-release floating tablets of ITO hydrochloride (HCl) were prepared by direct compression using different hydrocolloid polymers such as hydroxypropyl methylcellulose and ethylcellulose and/or methacrylic acid polymers Eudragit RSPM and Carbopol 934P. The floating property was achieved using an effervescent mixture of sodium bicarbonate and anhydrous citric acid (1:1 mol/mol)...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28008228/spotlight-on-fluticasone-furoate-vilanterol-trifenatate-for-the-once-daily-treatment-of-asthma-design-development-and-place-in-therapy
#13
REVIEW
Timothy E Albertson, Samuel W Bullick, Michael Schivo, Mark E Sutter
The use of inhaled corticosteroids (ICSs) plays a key role in the treatment of asthmatic patients, and international guidelines have designated ICSs as an early maintenance therapy in controlling asthma symptoms. When asthmatic patients remain symptomatic on ICSs, one common option is to add a long-acting beta2 agonist (LABA) to the maintenance treatment. Fixed combination inhalers that contain both an ICS and a LABA have been popular for both chronic obstructive pulmonary disease (COPD) and asthma. Historically, these inhalers have been dosed twice daily...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28008227/transbuccal-delivery-of-betahistine-dihydrochloride-from-mucoadhesive-tablets-with-a-unidirectional-drug-flow-in-vitro-ex-vivo-and-in-vivo-evaluation
#14
Mohamed A El-Nabarawi, Adel A Ali, Heba M Aboud, Amira H Hassan, Amany H Godah
OBJECTIVE: Betahistine dihydrochloride (BH.2HCl), an anti-vertigo histamine analog used in the treatment of Ménière's disease, undergoes extensive first-pass metabolism and suffers from short biological half-life. The aim of the present work was to develop and estimate controlled release mucoadhesive buccal tablets of BH.2HCl with a unidirectional drug flow to overcome this encumbrance. METHODS: A direct compression method was adopted for preparation of the tablets using mucoadhesive polymers like guar gum, hydroxypropyl methyl cellulose K4M, sodium carboxymethyl cellulose and their combinations...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28008226/preparation-and-physicochemical-characterization-of-spray-dried-and-jet-milled-microparticles-containing-bosentan-hydrate-for-dry-powder-inhalation-aerosols
#15
Hyo-Jung Lee, Ji-Hyun Kang, Hong-Goo Lee, Dong-Wook Kim, Yun-Seok Rhee, Ju-Young Kim, Eun-Seok Park, Chun-Woong Park
The objectives of this study were to prepare bosentan hydrate (BST) microparticles as dry powder inhalations (DPIs) via spray drying and jet milling under various parameters, to comprehensively characterize the physicochemical properties of the BST hydrate microparticles, and to evaluate the aerosol dispersion performance and dissolution behavior as DPIs. The BST microparticles were successfully prepared for DPIs by spray drying from feeding solution concentrations of 1%, 3%, and 5% (w/v) and by jet milling at grinding pressures of 2, 3, and 4 MPa...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28003740/dose-dependent-effects-of-cisplatin-on-the-severity-of-testicular-injury-in-sprague-dawley-rats-reactive-oxygen-species-and-endoplasmic-reticulum-stress
#16
Kiran Kumar Soni, Hye Kyung Kim, Bo Ram Choi, Keshab Kumar Karna, Jae Hyung You, Jai Seong Cha, Yu Seob Shin, Sung Won Lee, Chul Young Kim, Jong Kwan Park
Cisplatin (CIS) is used in the treatment of cancer, but its nonspecific systemic actions lead to toxic effects on other parts of the body. This study investigated the severity of CIS toxicity by increasing its dose over a constant time period. Sprague Dawley rats were divided into five treatment groups and control group with CIS (2, 4, 6, 8, and 10 mg/kg) administered intraperitoneally for 5 days. The body and organs were weighed, epididymal sperm was counted, and sperm motility and sperm apoptosis were evaluated...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27994442/determination-of-the-starting-dose-in-the-first-in-human-clinical-trials-with-monoclonal-antibodies-a-systematic-review-of-papers-published-between-1990-and-2013
#17
Hoon Young Suh, Carl C Peck, Kyung-Sang Yu, Howard Lee
A systematic review was performed to evaluate how the maximum recommended starting dose (MRSD) was determined in first-in-human (FIH) studies with monoclonal antibodies (mAbs). Factors associated with the choice of each MRSD determination method were also identified. PubMed was searched for FIH studies with mAbs published in English between January 1, 1990 and December 31, 2013, and the following information was extracted: MRSD determination method, publication year, therapeutic area, antibody type, safety factor, safety assessment results after the first dose, and number of dose escalation steps...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27994441/comparison-of-oral-absorption-models-for-pregabalin-usefulness-of-transit-compartment-model
#18
Taegon Hong, Seunghoon Han, Jongtae Lee, Sangil Jeon, Dong-Seok Yim
Pregabalin is an anticonvulsant used for the treatment of neuropathic pain and partial seizure in adults. The aim of this study was to develop a population pharmacokinetic (PK) model to describe the absorption characteristics of pregabalin given fasted or after meals. Data from five healthy subject PK studies (n=88) of single- or multiple-dose pregabalin (150 mg) were used. Pregabalin was administered twice daily, without meals or 30 min after a meal (regular or high-fat diet) in the morning and 30 min or 4 h after a meal (regular diet) in the evening...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27994440/use-of-bedaquiline-and-delamanid-in-diabetes-patients-clinical-and-pharmacological-considerations
#19
REVIEW
Minhui Hu, Chunlan Zheng, Feng Gao
Antituberculosis (anti-TB) treatment may be affected by both diabetes and hypoglycemic agents in patients with these 2 comorbidities. However, data supporting this conclusion relate only to standard anti-TB therapies. Sirturo(®) (bedaquiline) and Deltyba(®) (delamanid), novel drugs for multidrug-resistant tuberculosis (MDR-TB), are recommended for diabetes patients when another effective treatment regimen cannot be provided. Currently, there are no clinical data related to the use of these agents in diabetes patients...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27994439/impact-of-prostaglandin-glaucoma-drops-on-platelet-activating-factor-action-an-in-vitro-study
#20
Marilita M Moschos, Eirini Nitoda, Irini P Chatziralli, Georgios D Panos, Constantinos A Demopoulos
AIM: The aim of this study was to investigate the effect of different prostaglandin analogs on platelet-activating factor (PAF) levels. METHODS: Three prostaglandin analogs were selected: bimatoprost 0.3 mg/mL, latanoprost 50 μg/mL, and tafluprost 15 μg/mL. Each drug sample was tested for its ability to cause platelet aggregation, which was measured as PAF-induced aggregation, before and after the addition of various concentrations of the examined sample, creating a linear curve of percentage inhibition (ranging from 0% to 100%) versus different concentrations of the sample...
2016: Drug Design, Development and Therapy
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