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https://www.readbyqxmd.com/read/28323098/an-innovative-method-for-the-preparation-of-high-api-loaded-hollow-spherical-granules-for-use-in-controlled-release-formulation
#1
Takumi Asada, Mitsuaki Kobiki, Yasushi Ochiai, Yasunori Iwao, Shigeru Itai
The aim of this study was to prepare controlled-release (CR) granules with suitable particle strength, flowability, particle size distribution (PSD) and density characteristics for blending with other excipients. We also wanted these CR granules to contain large quantities of active pharmaceutical ingredient (API). A high shear mixer was used to mix an API with various polymers at various feed ratios, and the resulting granulated materials were sprayed with solvent. The wet granules were dried using a fluidized bed dryer to give CR granules...
March 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28323062/new-strategies-and-approaches-for-engineering-biosynthetic-gene-clusters-of-microbial-natural-products
#2
REVIEW
Lei Li, Weihong Jiang, Yinhua Lu
With the rapidly growing number of sequenced microbial (meta)genomes, enormous cryptic natural product (NP) biosynthetic gene clusters (BGCs) have been identified, which are regarded as a rich reservoir for novel drug discovery. A series of powerful tools for engineering BGCs has accelerated the discovery and development of pharmaceutically active NPs. Here, we describe recent advances in the strategies for BGCs manipulation, which are driven by emerging technologies, including efficient DNA recombination systems, versatile CRISPR/Cas9 genome editing tools and diverse DNA assembly methods...
March 16, 2017: Biotechnology Advances
https://www.readbyqxmd.com/read/28318088/twenty-five-years-of-dna-encoded-chemical-libraries
#3
EDITORIAL
Dario Neri
Reference library: The availability of DNA-encoded chemical libraries containing billions of compounds facilitates the discovery of binding molecules for pharmaceutical applications and for investigating biological processes. This Special Issue highlights the use of this library technology and some of the latest developments in the field.
March 20, 2017: Chembiochem: a European Journal of Chemical Biology
https://www.readbyqxmd.com/read/28314410/enabling-chemistry-technologies-and-parallel-synthesis-accelerators-of-drug-discovery-programmes
#4
A Vasudevan, A R Bogdan, H F Koolman, Y Wang, S W Djuric
There is a pressing need to improve overall productivity in the pharmaceutical industry. Judicious investments in chemistry technologies can have a significant impact on cycle times, cost of goods and probability of technical success. This perspective describes some of these technologies developed and implemented at AbbVie, and their applications to the synthesis of novel scaffolds and to parallel synthesis.
2017: Progress in Medicinal Chemistry
https://www.readbyqxmd.com/read/28298437/riding-the-metalloproteinase-roller-coaster
#5
Gillian Murphy
To many of us in the field, working on Matrix Metalloproteinases (MMPs) has felt like riding a roller coaster, traveling through times of both excitement and despair. I was fortunate to join the ride when it was a mere carousel of three activities thought to target the proteins that comprise the extracellular matrix (ECM). New technologies brought the thrills of discovery, as we uncovered specific proteinase genes and defined specialised activities in different cellular processes. The MMPs and the sister families of 'A Disintegrin And Metalloproteinase' (ADAMs), ADAMs with ThromboSpondin domains (ADAM-TS) and Astacins are now recognised as key signalling 'scissors' that drive rapid changes in a plethora of cellular pathways...
March 15, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28286315/formulation-of-hydrophobic-peptides-for-skin-delivery-via-coated-microneedles
#6
Xin Zhao, Sion A Coulman, Stephanie J Hanna, F Susan Wong, Colin M Dayan, James C Birchall
Microneedles (MNs) have been investigated as a minimally-invasive delivery technology for a range of active pharmaceutical ingredients (APIs). Various formulations and methods for coating the surface of MNs with therapeutics have been proposed and exemplified, predominantly for hydrophilic drugs and particulates. The development of effective MN delivery formulations for hydrophobic drugs is more challenging with dosing restrictions and the use of organic solvents impacting on both the bioactivity and the kinetics of drug release...
March 9, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28281210/design-of-a-time-controlled-pulsatile-release-system-for-propranolol-using-the-dry-coated-method-in-vitro-and-in-vivo-evaluation
#7
Kai Chen, Yanyan Wang, Xiumei Gai, Haiying Wang, Yuenan Li, Haoyang Wen, Weisan Pan, Xinggang Yang
The objective of this study was to design a time-controlled pulsatile release (TCPR) system containing propranolol (PNH) as an active pharmaceutical ingredient. Here, the developed dosage forms were coated with hydroxypropyl-methylcellulose (HPMC) and other excipients as barrier layer using dry-coated technology. The influence of HPMC, microcrystalline cellulose (MCC), and lactose in the outer coating and the coating weight on drug release were investigated. Then, a three-factor, five-level central composite design (CCD) and response surface method were used to optimize the formula of the coating...
March 9, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28281194/development-considerations-for-nanocrystal-drug-products
#8
Mei-Ling Chen, Mathew John, Sau L Lee, Katherine M Tyner
Nanocrystal technology has emerged as a valuable tool for facilitating the delivery of poorly water-soluble active pharmaceutical ingredients (APIs) and enhancing API bioavailability. To date, the US Food and Drug Administration (FDA) has received over 80 applications for drug products containing nanocrystals. These products can be delivered by different routes of administration and are used in a variety of therapeutic areas. To aid in identifying key developmental considerations for these products, a retrospective analysis was performed on the submissions received by the FDA to date...
March 9, 2017: AAPS Journal
https://www.readbyqxmd.com/read/28274937/mass-spectrometry-approaches-for-identification-and-quantitation-of-therapeutic-monoclonal-antibodies-in-the-clinical-laboratory
#9
Paula M Ladwig, David R Barnidge, Maria A V Willrich
Therapeutic monoclonal antibodies (mAbs) are an important class of drugs used to treat diseases ranging from autoimmune disorders to B cell lymphomas to other rare conditions thought to be untreatable in the past. Many advances have been made in the characterization of immunoglobulins as a result of pharmaceutical companies investing in technologies that allow them to better understand mAbs during the development phase. Mass spectrometry is one of the new advancements utilized extensively by pharma to analyze mAbs, and is now beginning to be applied in the clinical laboratory setting...
March 8, 2017: Clinical and Vaccine Immunology: CVI
https://www.readbyqxmd.com/read/28270070/fine-tuning-antibody-conjugation-methods-using-snap-tag-technology
#10
Karinna Chouman, Mira Woitok, Radoslav Mladenov, Claudia Kessler, Elmar Weinhold, Gisela Hanz, Rainer Fischer, Ivo Meinhold-Heerlein, Andreas Bleilevens, Gerrit Gresch, Anka Maria Haugg, Felix Zeppernick, Dirk Bauerschlag, Nicolai Maass, Elmar Stickeler, Katharina Kolberg, Ahmad Fawzi Hussain
Background Targeted imaging and therapy (theranostics) is a promising approach for the simultaneous improvement of cancer diagnosis, prognosis and management. Therapeutic and imaging reagents are coupled to tumor-targeting molecules such as antibodies, providing a basis for truly personalized medicine. However, the development of antibody-drug conjugates with acceptable pharmaceutical properties is a complex process and several parameters must be optimized, such as the controlled conjugation method and the drug-to-antibody ratio...
February 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28265347/value-added-medicines-what-value-repurposed-medicines-might-bring-to-society
#11
Mondher Toumi, Cécile Rémuzat
Background & objectives: Despite the wide interest surrounding drug repurposing, no common terminology has been yet agreed for these products and their full potential value is not always recognised and rewarded, creating a disincentive for further development. The objectives of the present study were to assess from a wide perspective which value drug repurposing might bring to society, but also to identify key obstacles for adoption of these medicines and to discuss policy recommendations. Methods: A preliminary comprehensive search was conducted to assess how the concept of drug repurposing was described in the literature...
2017: Journal of Market Access & Health Policy
https://www.readbyqxmd.com/read/28251424/visualization-and-non-destructive-quantification-of-inkjet-printed-pharmaceuticals-on-different-substrates-using-raman-spectroscopy-and-raman-chemical-imaging
#12
Magnus Edinger, Daniel Bar-Shalom, Jukka Rantanen, Natalja Genina
PURPOSE: The purpose of this study was to investigate the applicability of Raman spectroscopy for visualization and quantification of inkjet-printed pharmaceuticals. METHODS: Haloperidol was used as a model active pharmaceutical ingredient (API), and a printable ink base containing lactic acid and ethanol was developed. Inkjet printing technology was used to apply haloperidol ink onto three different substrates. Custom-made inorganic compacts and dry foam, as well as marketed paracetamol tablets were used as the substrates...
March 1, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28248238/-omics-informed-drug-and-biomarker-discovery-opportunities-challenges-and-future-perspectives
#13
REVIEW
Holly Matthews, James Hanison, Niroshini Nirmalan
The pharmaceutical industry faces unsustainable program failure despite significant increases in investment. Dwindling discovery pipelines, rapidly expanding R&D budgets and increasing regulatory control, predict significant gaps in the future drug markets. The cumulative duration of discovery from concept to commercialisation is unacceptably lengthy, and adds to the deepening crisis. Existing animal models predicting clinical translations are simplistic, highly reductionist and, therefore, not fit for purpose...
September 12, 2016: Proteomes
https://www.readbyqxmd.com/read/28240312/a-simple-capacitive-method-to-evaluate-ethanol-fuel-samples
#14
Tatiana P Vello, Rafael F de Oliveira, Gustavo O Silva, Davi H S de Camargo, Carlos C B Bufon
Ethanol is a biofuel used worldwide. However, the presence of excessive water either during the distillation process or by fraudulent adulteration is a major concern in the use of ethanol fuel. High water levels may cause engine malfunction, in addition to being considered illegal. Here, we describe the development of a simple, fast and accurate platform based on nanostructured sensors to evaluate ethanol samples. The device fabrication is facile, based on standard microfabrication and thin-film deposition methods...
February 27, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28231302/bioinformatic-prediction-of-g-protein-coupled-receptor-encoding-sequences-from-the-transcriptome-of-the-foreleg-including-the-haller-s-organ-of-the-cattle-tick-rhipicephalus-australis
#15
Sergio Munoz, Felix D Guerrero, Anastasia Kellogg, Andrew M Heekin, Ming-Ying Leung
The cattle tick of Australia, Rhipicephalus australis, is a vector for microbial parasites that cause serious bovine diseases. The Haller's organ, located in the tick's forelegs, is crucial for host detection and mating. To facilitate the development of new technologies for better control of this agricultural pest, we aimed to sequence and annotate the transcriptome of the R. australis forelegs and associated tissues, including the Haller's organ. As G protein-coupled receptors (GPCRs) are an important family of eukaryotic proteins studied as pharmaceutical targets in humans, we prioritized the identification and classification of the GPCRs expressed in the foreleg tissues...
2017: PloS One
https://www.readbyqxmd.com/read/28224904/design-development-and-method-validation-of-a-novel-multi-resonance-microwave-sensor-for-moisture-measurement
#16
Johanna Peters, Wolfgang Taute, Kathrin Bartscher, Claas Döscher, Michael Höft, Reinhard Knöchel, Jörg Breitkreutz
Microwave sensor systems using resonance technology at a single resonance in the range of 2-3 GHz have been shown to be a rapid and reliable tool for moisture determination in solid materials including pharmaceutical granules. So far, their application is limited to lower moisture ranges or limitations above certain moisture contents had to be accepted. Aim of the present study was to develop a novel multi-resonance sensor system in order to expand the measurement range. Therefore, a novel sensor using additional resonances over a wide frequency band was designed and used to investigate inherent limitations of first generation sensor systems and material-related limits...
April 8, 2017: Analytica Chimica Acta
https://www.readbyqxmd.com/read/28213177/tiered-analytics-for-purity-assessment-of-macrocyclic-peptides-in-drug-discovery-analytical-consideration-and-method-development
#17
Jingfang Jenny Qian Cutrone, Xiaohua Stella Huang, Edward S Kozlowski, Ye Bao, Yingzi Wang, Christopher S Poronsky, Dieter M Drexler, Adrienne A Tymiak
Synthetic macrocyclic peptides with natural and unnatural amino acids have gained considerable attention from a number of pharmaceutical/biopharmaceutical companies in recent years as a promising approach to drug discovery, particularly for targets involving protein-protein or protein-peptide interactions. Analytical scientists charged with characterizing these leads face multiple challenges including dealing with a class of complex molecules with the potential for multiple isomers and variable charge states and no established standards for acceptable analytical characterization of materials used in drug discovery...
February 3, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28210505/nanotechnology-based-approach-in-tuberculosis-treatment
#18
REVIEW
Mohammad Nasiruddin, Md Kausar Neyaz, Shilpi Das
Tuberculosis, commonly known as TB, is the second most fatal infectious disease after AIDS, caused by bacterium called Mycobacterium tuberculosis. Prolonged treatment, high pill burden, low compliance, and stiff administration schedules are factors that are responsible for emergence of MDR and XDR cases of tuberculosis. Till date, only BCG vaccine is available which is ineffective against adult pulmonary TB, which is the most common form of disease. Various unique antibodies have been developed to overcome drug resistance, reduce the treatment regimen, and elevate the compliance to treatment...
2017: Tuberculosis Research and Treatment
https://www.readbyqxmd.com/read/28205144/recommended-best-practices-for-process-monitoring-instrumentation-in-pharmaceutical-freeze-drying-2017
#19
Steven Nail, Serguei Tchessalov, Evgenyi Shalaev, Arnab Ganguly, Ernesto Renzi, Frank Dimarco, Lindsay Wegiel, Steven Ferris, William Kessler, Michael Pikal, Greg Sacha, Alina Alexeenko, T N Thompson, Cindy Reiter, James Searles, Paul Coiteux
Recommended best practices in monitoring of product status during pharmaceutical freeze drying are presented, focusing on methods that apply to both laboratory and production scale. With respect to product temperature measurement, sources of uncertainty associated with any type of measurement probe are discussed, as well as important differences between the two most common types of temperature-measuring instruments-thermocouples and resistance temperature detectors (RTD). Two types of pressure transducers are discussed-thermal conductivity-type gauges and capacitance manometers, with the Pirani gauge being the thermal conductivity-type gauge of choice...
February 15, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28195483/development-of-oromucosal-dosage-forms-by-combining-electrospinning-and-inkjet-printing
#20
Mirja Palo, Karin Kogermann, Ivo Laidmäe, Andres Meos, Maren Preis, Jyrki Heinämäki, Niklas Sandler
Printing technology has been shown to enable flexible fabrication of solid dosage forms for personalized drug therapy. Several methods can be applied for tailoring the properties of the printed pharmaceuticals. In this study, the use of electrospun fibrous substrates in the fabrication of inkjet-printed dosage forms was investigated. A single-drug formulation with lidocaine hydrochloride (LH) and a combination drug system containing LH and piroxicam (PRX) for oromucosal administration were prepared. The LH was deposited on the electrospun and cross-linked gelatin substrates by inkjet printing, whereas PRX was incorporated within the substrate fibers during electrospinning...
February 14, 2017: Molecular Pharmaceutics
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