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https://www.readbyqxmd.com/read/28444869/assessment-of-the-usage-of-biodegradable-polymeric-matrix-in-vaginal-devices-to-sustain-progesterone-release-in-cows
#1
José Rodrigo Valim Pimentel, Milton Maturana Filho, Lucio Cardozo-Filho, José Augusto M Agnelli, Jefter Nascimento, Ed Hoffmann Madureira
The usage of timed artificial insemination (TAI) at a low cost leading to better reproductive rates has been the aim of several research groups in the field. Usually during TAI protocols, sustained progesterone (P4 ) release devices are employed. Most devices are constituted of a nylon skeleton covered with a silicon layer with P4 . A device based on biopolymers was developed in order to reduce costs and decrease its environmental impact. In this study, we compared the kinetics of sustained progesterone release among devices manufactured with a polymeric blend made of polyhydroxybutyrate-valerate (PHBV) and poly-ε-caprolactone (PCL) (DISP) which were compared with DIB® (Internal Bovine Device) used as the control...
April 25, 2017: Animal Science Journal, Nihon Chikusan Gakkaihō
https://www.readbyqxmd.com/read/28439742/exploration-of-the-binding-affinities-between-ecdysone-agonists-and-ecr-usp-by-docking-and-mm-pb-gbsa-approaches
#2
Xueping Hu, Jin Xie, Song Hu, Li Zhang, Yanhong Dong
Ecdysone receptor (EcR) is a significant target in the identification of new environmentally friendly pesticides. There are two types of ecdysone agonists: steroidal ecdysone agonists and dibenzoylhydrazines (DBHs). In this study, various modeling methods (homology modeling, molecular docking, MD simulation, binding free energy calculation, and per-residue binding free energy decomposition) were utilized to study the different binding mechanisms of two types of ecdysone agonists. Our theoretical results indicated that the relative binding potencies of DBHs can be ranked sufficiently accurately using the MOE docking method...
May 2017: Journal of Molecular Modeling
https://www.readbyqxmd.com/read/28431780/tolterodine-tartrate
#3
Gennady Ananchenko, Jasmina Novakovic
Tolterodine tartrate belongs to the family of muscarinic receptor antagonists and is indicated for the treatment of overactive urinary bladder syndrome. This chapter provides an overview of physical, analytical, and ADME profiles; highlights methods of chemical synthesis; and discusses stability of tolterodine as a free base and/or its l-tartrate salt in solution and in the solid state. The information presented in this chapter is based on the peer-reviewed literature, compendial reports (USP, EP), and authors' data...
2017: Profiles of Drug Substances, Excipients, and related Methodology
https://www.readbyqxmd.com/read/28422566/content-uniformity-testing-for-stratified-samples-via-parametric-tolerance-interval-testing
#4
Steven Novick, Buffy Hudson-Curtis
Historically in the biopharmaceutical setting, USP <905>has been used to establish that a batch of drug product has acceptable content uniformity. More recently, alternative approaches, such as the two one-sided parametric tolerance interval test (PTI-TOST), have been proposed to establish content uniformity. Traditionally, the PTI-TOST is implemented as a sequential, two-tiered test, under the generally accepted assumption that the data are independently and identically distributed. Since the material is sequenced through the manufacturing process over a period of time, there are conceptually arguable locations within each batch, for instance: beginning, middle, and end...
April 19, 2017: Journal of Biopharmaceutical Statistics
https://www.readbyqxmd.com/read/28420283/design-and-characteristics-of-gellan-gum-beads-for-modified-release-of-meloxicam
#5
Tomasz Osmałek, Bartłomiej Milanowski, Anna Froelich, Mirosław Szybowicz, Wojciech Białowąs, Marcin Kapela, Piotr Gadziński, Katarzyna Ancukiewicz
The aim of the presented work was to design, formulate and evaluate the properties of low-acyl gellan macro beads with the potential application as carriers for oral delivery of meloxicam (MLX) in the prophylaxis of colorectal cancer. The beads were obtained by means of ionotropic gelation technique. Calcium chloride (1.0%, 9.0 × 10(-2) M) was used as the cross-linking agent. Nine different polymer, drug and surfactant (Tween®80) mixtures were used for production of the beads. The quantitative compositions of the mixtures were generated with the application of the Design of Experiments (DoE) modulus from the STATISTICA Software...
April 19, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28416644/evaluation-of-different-estimation-methods-for-accuracy-and-precision-in-biological-assay-validation
#6
Binbing Yu, Harry Yang
Biological assays (bioassays) are procedures to estimate the potency of a substance by studying its effects on living organisms, tissues, and cells. Bioassays are essential tools for gaining insight into biologic systems and processes including, for example, the development of new drugs and monitoring environmental pollutants. Two of the most important parameters of bioassay performance are relative accuracy (bias) and precision. Although general strategies and formulas are provided in USP 〈1033〉, a comprehensive understanding of the definitions of bias and precision remain elusive...
April 17, 2017: PDA Journal of Pharmaceutical Science and Technology
https://www.readbyqxmd.com/read/28409325/velocity-field-visualization-in-usp-dissolution-apparatus-3-using-particle-image-velocimetry
#7
Satish Perivilli, Richard Prevost, Erika Stippler
PURPOSE: The hydrodynamics in USP dissolution apparatus 3, at five different dip rates, was characterized by analyzing phase-averaged velocity fields obtained using Particle Image Velocimetry (PIV). METHODS: Phase locked 2 Component-PIV (2C-PIV) measurements were recorded on a typical dissolution apparatus 3 configuration with a black painted tablet fixed at the center of the bottom porous screen of the reciprocating cylinder. A trigger mechanism was employed to capture data over 12 phase positions for each reciprocation cycle...
April 13, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28397861/preventing-the-return-of-fear-using-reconsolidation-updating-and-methylene-blue-is-differentially-dependent-on-extinction-learning
#8
Allison M Auchter, Jason Shumake, Francisco Gonzalez-Lima, Marie H Monfils
Many factors account for how well individuals extinguish conditioned fears, such as genetic variability, learning capacity and conditions under which extinction training is administered. We predicted that memory-based interventions would be more effective to reduce the reinstatement of fear in subjects genetically predisposed to display more extinction learning. We tested this hypothesis in rats genetically selected for differences in fear extinction using two strategies: (1) attenuation of fear memory using post-retrieval extinction training, and (2) pharmacological enhancement of the extinction memory after extinction training by low-dose USP methylene blue (MB)...
April 11, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28397452/investigation-and-optimization-of-the-effect-of-polymers-on-drug-release-of-norfloxacin-from-floating-tablets
#9
Dipak D Gadade, Kalpana Sarda, Sadhana R Shahi
BACKGROUND: Norfloxacin is fluoroquinolone anti-infective used in the treatment of urinary tract infections, prostatitis, gonorrhea and genital tract infections. It has plasma half life of 3 to 4 h requiring multiple dosing in the treatment. Releaseretarding polymers can be used to modulate the drug release of norfloxacin. OBJECTIVES: The objective of this study was to investigate the effect of release-retarding polymers on the drug release of norfloxacin from floating tablets...
July 2016: Polimery W Medycynie
https://www.readbyqxmd.com/read/28396244/enhanced-release-of-poorly-water-soluble-drugs-from-synergy-between-mesoporous-magnesium-carbonate-and-polymers
#10
Jiaojiao Yang, Caroline Alvebratt, Peng Zhang, Teresa Zardán Gómez de la Torre, Maria Strømme, Christel A S Bergström, Ken Welch
The need to combat poor water solubility has increased interest in supersaturating drug delivery systems. In this study, amorphous mesoporous magnesium carbonate (MMC) was used as a drug carrier to achieve supersaturation of tolfenamic acid and rimonabant, two drug compounds with low aqueous solubility. The potential synergy between MMC and hydroxypropyl methylcellulose (HPMC), a polymer commonly included as a precipitation inhibitor in drug delivery systems, was explored with the aim of extending the time that high supersaturation levels were maintained...
April 8, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28395244/an-isocratic-hydrophilic-interaction-liquid-chromatographic-method-for-simultaneous-determination-of-iodixanol-and-its-related-impurities-in-drug-substance
#11
Bruno D Rondon, Neila M Cassiano, Quezia B Cass
This work reports a simple isocratic hydrophilic interaction liquid chromatographic (HILIC) method for the simultaneous quantification of iodixanol and of its related impurities C, D and E in drug substance. The chromatographic separation was carried out with a Kinetex™ HILIC column, using acetonitrile and formic acid aqueous solution (1.0mmol/L, pH 3.2) (92:08, v/v) as eluent at a flow rate of 0.8mL/min. The autosampler and column temperature were maintained at 20°C and UV detection was set at 243nm. The method was validated in accordance to the ICH guideline and employed for the analysis of two different lots of iodixanol drug substance...
June 5, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28391233/taxonomy-of-self-reported-sedentary-behaviour-tools-tasst-framework-for-development-comparison-and-evaluation-of-self-report-tools-content-analysis-and-systematic-review
#12
P M Dall, E H Coulter, C F Fitzsimons, D A Skelton, Sfm Chastin
OBJECTIVE: Sedentary behaviour (SB) has distinct deleterious health outcomes, yet there is no consensus on best practice for measurement. This study aimed to identify the optimal self-report tool for population surveillance of SB, using a systematic framework. DESIGN: A framework, TAxonomy of Self-reported Sedentary behaviour Tools (TASST), consisting of four domains (type of assessment, recall period, temporal unit and assessment period), was developed based on a systematic inventory of existing tools...
April 8, 2017: BMJ Open
https://www.readbyqxmd.com/read/28388949/characterization-and-virulence-clustering-analysis-of-extraintestinal-pathogenic-escherichia-coli-isolated-from-swine-in-china
#13
Yinchu Zhu, Wenyang Dong, Jiale Ma, Lvfeng Yuan, Hassan M A Hejair, Zihao Pan, Guangjin Liu, Huochun Yao
BACKGROUND: Swine extraintestinal pathogenic Escherichia coli (ExPEC) is an important pathogen that leads to economic and welfare costs in the swine industry worldwide, and is occurring with increasing frequency in China. By far, various virulence factors have been recognized in ExPEC. Here, we investigated the virulence genotypes and clonal structure of collected strains to improve the knowledge of phylogenetic traits of porcine ExPECs in China. RESULTS: We isolated 64 Chinese porcine ExPEC strains from 2013 to 14 in China...
April 8, 2017: BMC Veterinary Research
https://www.readbyqxmd.com/read/28386462/norfloxacin-and-metronidazole-topical-formulations-for-effective-treatment-of-bacterial-infections-and-burn-wounds
#14
REVIEW
Kamal Dua, Venkata Ramana Malipeddi, Jyotsna Madan, Gaurav Gupta, Srikumar Chakravarthi, Rajendra Awasthi, Irene Satiko Kikuchi, Terezinha De Jesus Andreoli Pinto
INTRODUCTION: Our various previous findings have shown the suitability of norfloxacin in the treatment of bacterial infections and burn wounds in alone as well as in combination with Curcuma longa in various topical (ointments, gels, and creams) and transdermal drug delivery systems. AIMS AND METHODS: Keeping these facts in consideration, we have made an another attempt to prepare semisolid formulations containing 1% w/w of norfloxacin and metronidazole with different bases like Carbopol, polyethylene glycol, and hydroxypropylmethyl cellulose for effective treatment of bacterial infections and burn wounds...
June 1, 2016: Interventional Medicine & Applied Science
https://www.readbyqxmd.com/read/28385676/development-of-in-vitro-in-vivo-correlation-of-parenteral-naltrexone-loaded-polymeric-microspheres
#15
Janki V Andhariya, Jie Shen, Stephanie Choi, Yan Wang, Yuan Zou, Diane J Burgess
Establishment of in vitro-in vivo correlations (IVIVCs) for parenteral polymeric microspheres has been very challenging, due to their complex multiphase release characteristics (which is affected by the nature of the drug) as well as the lack of compendial in vitro release testing methods. Previously, a Level A correlation has been established and validated for polymeric microspheres containing risperidone (a practically water insoluble small molecule drug). The objectives of the present study were: 1) to investigate whether a Level A IVIVC can be established for polymeric microspheres containing another small molecule drug with different solubility profiles compared to risperidone; and 2) to determine whether release characteristic differences (bi-phasic vs tri-phasic) between microspheres can affect the development and predictability of IVIVCs...
April 4, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28347684/prognostic-model-for-patients-with-traumatic-brain-injuries-and-abnormal-computed-tomography-scans
#16
Jefferson Rosi Junior, Leonardo C Welling, Marcelo Schafranski, Lin Tchia Yeng, Rogério Ruscito do Prado, Edwin Koterba, Almir Ferreira de Andrade, Manoel Jacobsen Teixeira, Eberval Gadelha Figueiredo
Traumatic brain injury (TBI) is an important cause of death and disability worldwide. The prognosis evaluation is a challenge when many variables are involved. The authors aimed to develop prognostic model for assessment of survival chances after TBI based on admission characteristics, including extracranial injuries, which would allow application of the model before in-hospital therapeutic interventions. A cohort study evaluated 1275 patients with TBI and abnormal CT scans upon admission to the emergency unit of Hospital das Clinicas of University of Sao Paulo and analyzed the final outcome on mortality...
March 24, 2017: Journal of Clinical Neuroscience: Official Journal of the Neurosurgical Society of Australasia
https://www.readbyqxmd.com/read/28344172/physicochemical-attributes-and-dissolution-testing-of-ophthalmic-ointments
#17
Quanying Bao, Rajan Jog, Jie Shen, Bryan Newman, Yan Wang, Stephanie Choi, Diane J Burgess
The investigation of semisolid ophthalmic ointments is challenging due to their complex physicochemical properties and the unique anatomy of the human eye. Using Lotemax(®) as a model ophthalmic ointment, three different manufacturing processes and two excipient sources (Fisher(®) (OWP) and Fougera(®) (NWP)) were used to prepare loteprednol etabonate ointments that were qualitatively and quantitatively the same across the manufactured formulations. Physicochemical properties including drug content and uniformity, particle size and distribution, as well as rheological parameters (onset point, crossover modulus, storage modulus and Power law consistency index) were investigated...
March 24, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28344105/a-new-reconstructed-human-epidermis-for-in-vitro-skin-irritation-testing
#18
Tatiana do Nascimento Pedrosa, Carolina Motter Catarino, Paula Comune Pennacchi, Sílvia Romano de Assis, Fabrícia Gimenes, Márcia Edilaine Lopes Consolaro, Silvia Berlanga de Moraes Barros, Silvya Stuchi Maria-Engler
Different models of reconstructed human epidermis (RHE) are currently validated to assess skin irritation in vitro and ultimately to the animal replacement of the Draize test. The development of a new RHE model is a challenge for many laboratories, representing a potential gain of autonomy and improvement of technological knowledge. The Organization for Economic Co-operation and Development (OECD) encourages the development of new models and, for this purpose, offers a thorough guideline on quality control parameters (OECD TG 439 performance standards)...
March 23, 2017: Toxicology in Vitro: An International Journal Published in Association with BIBRA
https://www.readbyqxmd.com/read/28343940/lithocholic-acid-hydroxyamide-destabilizes-cyclin-d1-and-induces-g0-g1-arrest-by-inhibiting-deubiquitinase-usp2a
#19
Katarzyna Magiera, Marcin Tomala, Katarzyna Kubica, Virginia De Cesare, Matthias Trost, Bartosz J Zieba, Neli Kachamakova-Trojanowska, Marcin Les, Grzegorz Dubin, Tad A Holak, Lukasz Skalniak
USP2a is a deubiquitinase responsible for stabilization of cyclin D1, a crucial regulator of cell-cycle progression and a proto-oncoprotein overexpressed in numerous cancer types. Here we report that lithocholic acid (LCA) derivatives are inhibitors of USP proteins, including USP2a. The most potent LCA derivative, LCA hydroxyamide (LCAHA), inhibits USP2a, leading to a significant Akt/GSK3β-independent destabilization of cyclin D1, but does not change the expression of p27. This leads to the defects in cell-cycle progression...
April 20, 2017: Cell Chemical Biology
https://www.readbyqxmd.com/read/28339392/stability-of-ribavirin-for-inhalation-packaged-in-syringes-or-glass-vials-when-stored-frozen-refrigerated-and-at-room-temperature
#20
Bayli Larson, Lane R Bushman, Matthew L Casciano, Alan R Oldland, Jennifer J Kiser, Tyree H Kiser
The primary aim of this study was to investigate ribavirin solution for inhalation stability under three different conditions (frozen, refrigerated, room temperature) over a 45-day period. A ribavirin 6000-mg vial was reconstituted with 90 mL of Sterile Water for Injection per the package insert to yield a concentration of approximately 67 mg/mL. The solution was then placed in either syringes or empty glass vials and stored in the freezer (-20°C), in the refrigerator (~0°C to 4°C), or at room temperature (~20°C to 25°C)...
November 2016: International Journal of Pharmaceutical Compounding
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