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Journal of Pharmaceutical Sciences

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https://www.readbyqxmd.com/read/28109793/a-study-of-fasoracetam-s-solid-state-forms-a-potential-anti-alzheimer-pharmaceutical
#1
Bram Harmsen, Koen Robeyns, Johan Wouters, Tom Leyssens
Different solid state forms of the research chemical fasoracetam, which counters the effects of Alzheimer's disease, have been subjected to a thermal and structural analysis. Single crystals were obtained from solution evaporation and from the melt. Single crystal x-ray analyses of the crystals show the existence of two hydrated and one non-hydrated crystalline form of fasoracetam. Under ambient conditions, the hydrate form I is found to be the most stable form, showing a melting point of 57°C. This low melting point, combined with possible water losses could cause problems when formulating the hydrated form and impact the storage conditions of the compound...
January 18, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28108379/-dark-singlet-oxygen-and-epr-spin-trapping-as-convenient-tools-to-assess-photolytic-drug-degradation
#2
Peter Persich, Steven Hostyn, Céline Joie, Guy Winderickx, Jeroen Pikkemaat, Edwin P Romijn, Bert U W Maes
Forced degradation studies are an important tool for a systematic assessment of decomposition pathways and identification of reactive sites in active pharmaceutical ingredients (APIs). Two methodologies have been combined in order to provide a deeper understanding of singlet-oxygen related degradation pathways of APIs under light irradiation. Firstly, we report that a "dark" singlet oxygen test enables the investigation of drug reactivity towards singlet oxygen independently of photolytic irradiation processes...
January 17, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28104414/dissolution-failure-of-solid-oral-drug-products-in-field-alert-reports
#3
Dajun Sun, Meng Hu, Mark Browning, Rick L Friedman, Wenlei Jiang, Liang Zhao, Hong Wen
From 2005 to 2014, 370 data entries of dissolution failures of solid oral drug products were assessed with respect to the solubility of drug substances, dosage forms (immediate release (IR) vs. modified release (MR)), and manufacturers (brand-name vs. generic). The study results show that the solubility of drug substances does not play a significant role in dissolution failures; however, MR drug products fail dissolution tests more frequently than IR drug products. When multiple variables were analyzed simultaneously, poorly water-soluble IR drug products failed the most dissolution tests, followed by poorly soluble MR drug products and very soluble MR drug products...
January 16, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28093291/editorial
#4
EDITORIAL
Ronald T Borchardt
No abstract text is available yet for this article.
January 13, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28093290/editorial
#5
EDITORIAL
Ronald T Borchardt
No abstract text is available yet for this article.
January 13, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28093289/r-and-s-warfarin-were-transported-by-breast-cancer-resistance-protein-from-in-vitro-to-pharmacokinetic-pharmacodynamic-studies
#6
Meng-Syuan Yang, Chung-Ping Yu, Pei-Dawn Lee Chao, Shiuan-Pey Lin, Yu-Chi Hou
Warfarin, a racemate of R- and S-warfarin, is an important oral anticoagulant with narrow therapeutic window. Being an acidic drug, warfarin (pKa = 4.94) exists mainly as anion under physiological pH. We hypothesized that the transport of warfarin anion across cell membrane was mediated by breast cancer resistance protein (BCRP), an efflux transporter having a variety of acidic substrates. This study aimed to verify that warfarin was a substrate of BCRP. Cell lines and mice were used for transport assay and pharmacokinetic/pharmacodynamic studies, respectively...
January 13, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28093288/assessing-the-impact-of-lithium-chloride-on-the-expression-of-p-glycoprotein-at-the-blood-brain-barrier
#7
Stephanie A Newman, Yijun Pan, Jennifer L Short, Joseph A Nicolazzo
In addition to extruding drugs from the brain, P-glycoprotein (P-gp) at the blood-brain barrier (BBB) facilitates the brain-to-blood clearance of β-amyloid (Aβ) and is down-regulated in Alzheimer's disease (AD). Studies suggest that the mood-stabilising drug lithium exerts a protective effect against AD. While the mechanisms underlying this effect are not fully understood, evidence suggests that lithium chloride (LiCl) increases P-gp expression in vitro, albeit at concentrations substantially outside the therapeutic window...
January 13, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28089688/functional-identification-of-plasma-membrane-monoamine-transporter-pmat-slc29a4-as-an-atenolol-transporter-sensitive-to-flavonoids-contained-in-apple-juice
#8
Yoshihisa Mimura, Tomoya Yasujima, Kinya Ohta, Katsuhisa Inoue, Hiroaki Yuasa
The intestinal absorption of atenolol has recently been reported to be reduced by simultaneous ingestion of fruit juices, such as apple juice. This finding implies a possibility that an unidentified carrier-mediated transport system, which could be interfered by some components of those juices, might be involved in atenolol absorption. In an attempt to explore that possibility, we successfully identified plasma membrane monoamine transporter (PMAT/SLC29A4) as a transporter that can operate for cellular atenolol uptake in the intestine, using Madin-Darby canine kidney II cells stably expressing PMAT...
January 12, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28089687/stabilizing-effects-for-antibody-formulations-and-safety-profiles-of-cyclodextrin-polypseudorotaxane-hydrogels
#9
Taishi Higashi, Naoko Ohshita, Tatsunori Hirotsu, Yoshihito Yamashita, Keiichi Motoyama, Sawako Koyama, Ruriko Iibuchi, Takayuki Uchida, Shiuhei Mieda, Kenji Handa, Tomoaki Kimoto, Hidetoshi Arima
Antibodies often have poor physicochemical stability during storage and/or transport, which is a serious drawback for the development of antibody-based drugs. In this study, we prepared polypseudorotaxane (PPRX) hydrogels consisting of cyclodextrins (CyDs) and polyethylene glycol (PEG), and evaluated them as stabilizers for commercially available antibody-based drugs. α-CyD and γ-CyD formed PPRX hydrogels with PEG (MW 20,000 Da) in the presence of antibody-based drugs such as omalizumab, palivizumab, panitumumab, and ranibizumab...
January 12, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28089686/simulations-of-cytochrome-p450-3a4-mediated-drug-drug-interactions-by-simple-two-compartment-model-assisted-static-method
#10
Katsumi Iga, Akiko Kiriyama
In order to predict cytochrome P450 3A4 (CYP3A4)-mediated drug-drug interactions (DDIs), a simple two-compartment model assisted, overall inhibition-activity (Ai, overall) method was derived based upon two concepts. One concept was that the increase in blood victim-level and fold increase in the area under the blood victim-level curve (AUCR) produced by DDI are determined entirely by Ai, overall, the hepatic availability of the victim and fraction of urinary excreted unchanged victim, where Ai, overall is determined by the perpetrator-specific CYP isoform inhibition activities (Ai,CYPs, DDI predictor-1) and victim-specific fractional CYP isoform contributions (fm,CYPs, predictor-2)...
January 12, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28089685/evaluation-of-drug-drug-interaction-potential-between-sacubitril-valsartan-lcz696-and-statins-using-a-physiologically-based-pharmacokinetic-model
#11
Wen Lin, Tao Ji, Heidi Einolf, Surya Ayalasomayajula, Tsu-Han Lin, Imad Hanna, Tycho Heimbach, Christopher Breen, Venkateswar Jarugula, Handan He
Sacubitril/valsartan (LCZ696) has been approved for the treatment of heart failure. Sacubitril is an in vitro inhibitor of OATPs. In clinical studies, LCZ696 increased atorvastatin Cmax by 1.7-fold and AUC by 1.3-fold, but had little or no effect on simvastatin or simvastatin acid exposure. A PBPK modelling approach was applied to explore the underlying mechanisms behind the statin-specific LCZ696 drug interaction observations. The model incorporated OATP-mediated clearance (CLint,T) for simvastatin and simvastatin acid to successfully describe the PK profiles of either analyte in the absence or presence of LCZ696...
January 12, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28088457/preformulation-characterization-stabilization-and-formulation-design-for-the-acrylodan-labeled-glucose-binding-protein-sm4-ac
#12
Neha Sahni, Rajoshi Chaudhuri, John M Hickey, Prakash Manikwar, Ajit D'Souza, Andrew Metters, Sangeeta B Joshi, C Russell Middaugh, David B Volkin
This study describes the physicochemical characterization, stabilization and formulation design of SM4-AC, an acrylodan labeled glucose/galactose binding protein for use in a continuous glucose monitoring device. The physical stability profile of SM4-AC as a function of pH and temperature was monitored using a combination of biophysical techniques and the resulting physical stability profile was visualized using an empirical phase diagram. Forced degradation chemical stability studies (Asn deamidation, Met oxidation) of SM4-AC were performed using a combination of capillary isoelectric focusing (cIEF), peptide mapping and reversed phase high performance liquid chromatography (RP-HPLC)...
January 11, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28088456/development-of-a-predictive-model-for-the-long-term-stability-assessment-of-drug-in-adhesive-transdermal-films-using-polar-pressure-sensitive-adhesives-as-carrier-matrix
#13
Clémence Chenevas-Paule, Hans-Michael Wolff, Mark Ashton, Martin Schubert, Kalliopi Dodou
Drug crystallization in transdermal drug delivery systems (TDDS) is a critical quality defect. The impact of drug load and hydration on the physical stability of polar (acrylic) drug-in-adhesive (DIA) films was investigated with the objective to identify predictive formulation parameters with respect to drug solubility and long-term stability. Medicated acrylic films were prepared over a range of drug concentrations below and above saturation solubility; and were characterized by FTIR, differential scanning calorimetry (DSC), polarized microscopy and Dynamic Vapor Sorption (DVS) analysis...
January 11, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28088455/statistical-considerations-concerning-dissimilar-regulatory-requirements-for-dissolution-similarity-assessment-the-example-of-immediate-release-dosage-forms
#14
Magdalena Jasińska-Stroschein, Urszula Kurczewska, Daria Orszulak-Michalak
When performing in vitro dissolution testing, especially in the area of biowaivers, it is necessary to follow regulatory guidelines to minimize the risk of an unsafe or ineffective product being approved. The present study examines model-independent and model-dependent methods of comparing dissolution profiles based on various compared and contrasted international guidelines. Dissolution profiles for immediate release solid oral dosage forms were generated. The test material comprised tablets containing several substances, with at least 85% of the labeled amount dissolved within 15 minutes, 20-30 minutes or 45 minutes...
January 11, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28087316/self-nanoemulsifying-lyophilized-tablets-snelts-for-flash-oral-transmucosal-delivery-of-vitamin-k-development-and-clinical-evaluation
#15
Khalid M El-Say, Tarek A Ahmed, Osama A A Ahmed, Khaled M Hosny, Fathy I Abd-Allah
Owing to limited solubility, vitamin K undergoes low bioavailability with large inter-individual variability after oral administration. This work aimed to prepare self-nanoemulsifying lyophilized tablets (SNELTs) for the flash oral transmucosal delivery of vitamin K. Twenty-one formulae of vitamin K self-nanoemulsifying drug delivery systems (SNEDDS) were prepared using different concentrations of vitamin K, Labrasol, and Transcutol according to mixture design. The SNEDDS was loaded on porous carriers and formulated as lyophilized tablets...
January 10, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28069357/control-strategies-for-drug-product-continuous-direct-compression-state-of-control-product-collection-strategies-and-startup-shutdown-operations-for-the-production-of-clinical-trial-materials-and-commercial-products
#16
Ahmad Almaya, Lawrence De Belder, Robert Meyer, Karthik Nagapudi, Hung-Ren Homer Lin, Ian Leavesley, Jayanthy Jayanth, Gurjit Bajwa, James DiNunzio, Anthony Tantuccio, Dan Blackwood, Admassu Abebe
Continuous Manufacturing (CM) has emerged in the pharmaceutical industry as a paradigm shift with significant advantages related to cost, efficiency, flexibility and higher assurance of quality. The inherent differences from batch processes justify examining the CM control strategy more holistically. This paper describes the current thinking for the control and implementation of CM, using the example of a direct compression process and taking into consideration the ICH Q10 definition of "state of control" and process validation requirements...
January 6, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28065764/development-and-validation-of-an-in-cell-western-for-quantifying-p-glycoprotein-expression-in-human-brain-microvascular-endothelial-hcmec-d3-cells
#17
Mitchell P McInerney, Yijun Pan, Jennifer L Short, Joseph A Nicolazzo
An in-cell western (ICW) protocol detecting the relative expression of P-gp in human cerebro-microvascular endothelial cells (hCMEC/D3) was developed and optimised, with the intention of improving throughput relative to western blotting (WB). For validation of the ICW protocol, hCMEC/D3 cells were incubated with known P-gp upregulators (10 μM rifampicin and 5 μM SR12813) and treated with siRNA targeted against MDR1, before measuring changes in P-gp expression, using both ICW and WB in parallel. To confirm a relationship between the detected P-gp expression and function, the uptake of the P-gp substrate rhodamine-123 was assessed following SR12813 treatment...
January 5, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28063826/evaluation-of-heat-flux-measurement-as-a-new-pat-monitoring-tool-in-freeze-drying
#18
Ilona Vollrath, Victoria Pauli, Wolfgang Friess, Angelika Freitag, Andrea Hawe, Gerhard Winter
This study investigates the suitability of heat flux measurement as a new technique for monitoring product temperature and critical end points during freeze drying. The heat flux sensor is tightly mounted on the shelf and measures non-invasively (no contact with the product) the heat transferred from shelf to vial. Heat flux data were compared to comparative pressure measurement, thermocouple readings and Karl Fischer titration as current state of the art monitoring techniques. The whole freeze drying process including freezing (both by ramp freezing and controlled nucleation), primary and secondary drying was considered...
January 4, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28063825/impact-of-mutations-on-the-higher-order-structure-and-activity-of-a-recombinant-uricase
#19
Flaviu Gruia, Arun Parupudi, Manuel Baca, Chris Ward, Andrew Nyborg, Richard L Remmele, Jared S Bee
This study explores the structural and functional changes associated with a low temperature thermal transition of two engineered bacterial uricase mutants. Uricase has a non-covalent homo-tetrameric structure, with four active sites located at the interface of subunits. Using differential scanning calorimetry, a low temperature transition was identified at 42ºC for mutant A and at 33°C for mutant B. This transition was stabilized by the uricase inhibitor, oxonic acid, suggesting a strong structural relationship to the active site...
January 4, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28063824/development-of-safe-and-potent-o-w-emulsion-of-paclitaxel-to-treat-peritoneal-dissemination
#20
Ken-Ichi Ogawara, Yoshiko Fukuoka, Yuta Yoshizawa, Toshikiro Kimura, Kazutaka Higaki
To develop a safer and more potent paclitaxel (PTX) formulation, we prepared various O/W emulsions by using egg phosphatidylcholine, Tween 80, and a mixture of triglycerides with different fatty acid chain lengths as the co-surfactant, surfactant, and oil phase component, respectively. The mean particle diameters of the PTX-emulsions prepared were around 100 nm. The PTX-emulsions did not provoke histamine release from rat mast cells and did not show any significant hemolytic activity, suggesting that PTX-emulsions are biocompatible...
January 4, 2017: Journal of Pharmaceutical Sciences
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