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Journal of Pharmaceutical Sciences

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https://www.readbyqxmd.com/read/28454747/sglt1-mediated-transport-in-caco-2-cells-is-highly-dependent-on-cell-bank-origin
#1
B Steffansen, M D L Pedersen, A M Laghmoch, C U Nielsen
The Caco-2 cell line is a well-established in vitro model for studying transport phenomena for prediction of intestinal nutrient and drug absorption. However, for substances depending on transporters such predictions are complicated due to variable transporter expression and limited knowledge about transporter function during multiple cell passaging and cell thawings. In the case of SGLT1, a key transporter of oral absorption of D-glucose, one reason for compromised prediction could be inadequate expression of SGLT1 in Caco-2 cells and thereby limited sensitivity in the determination of SGLT1-mediated permeability (PSGLT1)...
April 25, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28454746/involvement-of-proton-coupled-organic-cation-antiporter-in-varenicline-transport-at-blood-brain-barrier-of-rats-and-in-human-brain-capillary-endothelial-cells
#2
Toshiki Kurosawa, Kei Higuchi, Takashi Okura, Kazumasa Kobayashi, Hiroyuki Kusuhara, Yoshiharu Deguchi
Varenicline is a selective partial α4β2 nicotinic acetylcholine receptor agonist, which is used to help achieve smoking cessation. Here, we investigated varenicline transport at the blood-brain barrier (BBB) by means of in vivo microdialysis, in situ brain perfusion, and brain efflux index (BEI) measurements in rats and in vitro uptake studies in human brain capillary endothelial (hCMEC/D3) cells. Microdialysis demonstrated that varenicline is actively transported from blood to brain in rats. Blood-to-brain uptake transport of varenicline, as measured by the in situ brain perfusion technique, was strongly inhibited by diphenhydramine, a potent inhibitor of proton-coupled organic cation (H(+)/OC) antiporter...
April 25, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28454745/retina-to-blood-transport-of-1-methyl-4-phenylpyridinium-mpp-involves-carrier-mediated-process-at-the-blood-retinal-barrier
#3
Yoshiyuki Kubo, Masakazu Yamamoto, Kensuke Matsunaga, Takuya Usui, Shin-Ichi Akanuma, Ken-Ichi Hosoya
1-Methyl-4-phenylpyridinium (MPP(+)) transport at the blood-retinal barrier (BRB) was investigated. The retinal uptake index (RUI) estimated for [(3)H]MPP(+) was similar to that of [(3)H]D-mannitol, and was insensitive to unlabeled MPP(+), suggesting no positive evidence to support the involvement of carrier-mediated transport in the blood-to-retina transport of MPP(+) at the BRB. A microdialysis investigation showed that the concentration of [(3)H]MPP(+) in the vitreous humor decreased in a biexponential manner, and the rate constant for [(3)H]MPP(+) elimination during terminal phase was greater than that of [(14)C]D-mannitol...
April 25, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28454744/imaging-probes-and-modalities-for-the-study-of-solute-carrier-o-slco-transport-function-in-vivo
#4
Solène Marie, Salvatore Cisternino, Irène Buvat, Xavier Declèves, Nicolas Tournier
Transporters of the Solute Carrier O (SLCO) family, former organic anion-transporting polypeptides (OATP), are now recognized as key players in pharmacokinetics. Imaging is increasingly regarded as a relevant method to elucidate and decipher the intrinsic role of SLCO in controlling drug disposition in plasma and tissues. Current research in this representative field of translational research is based on different imaging modalities including nuclear imaging, such as Single Photon Emission Computed Tomography (SPECT) or Positron Emission Tomography (PET), as well as Magnetic Resonance Imaging (MRI)...
April 25, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28450239/an-evolutionary-search-algorithm-for-covariate-models-in-population-pharmacokinetic-analysis
#5
Fumiyoshi Yamashita, Atsuto Fujita, Yukako Sasa, Yuriko Higuchi, Masahiro Tsuda, Mitsuru Hashida
PURPOSE: Building a covariate model is a crucial task in population pharmacokinetics. This study develops a novel method for automated covariate modeling based on gene expression programming (GEP), which not only enables covariate selection, but also the construction of non-polynomial relationships between pharmacokinetic parameters and covariates. METHODS: A GEP algorithm was implemented in Java. To apply GEP to the extended nonlinear least-squares (ELS) analysis, the parameter consolidation and initial parameter value estimation algorithms were further developed and implemented...
April 24, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28450238/osmolality-of-orally-administered-solutions-influences-luminal-water-volume-and-drug-absorption-in-intestine
#6
Kazuki Ichijo, Rika Oda, Marika Ishihara, Ren Okada, Yuri Moteki, Yuta Funai, Takuya Horiuchi, Hisanao Kishimoto, Yoshiyuki Shirasaka, Katsuhisa Inoue
Intestinal water absorption is reportedly influenced by luminal osmolality. In this work, we examined whether differences in the osmolality of the vehicle used for oral administration of drugs influence luminal water volume and drug absorption in the gastrointestinal (GI) tract, by means of in situ rat intestinal closed loop studies using solutions of fluorescein isothiocyanate-dextran 4000 (FD-4; a non-absorbable compound), atenolol (a low-permeability drug) and antipyrine (a high-permeability drug) in various solvents...
April 24, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28450237/a-crispr-cas9-generated-mdck-hmdr1-cell-line-without-endogenous-cmdr1-cabcb1-an-improved-tool-for-drug-efflux-studies
#7
Maria Karlgren, Ivailo Simoff, Maria Backlund, Christine Wegler, Markus Keiser, Niklas Handin, Janett Müller, Patrik Lundquist, Anne-Christine Jareborg, Stefan Oswald, Per Artursson
Madin-Darby canine kidney (MDCK) II cells stably transfected with transport proteins are commonly used models for drug transport studies. However, endogenous expression of especially canine MDR1 (cMDR1) confounds the interpretation of such studies. Here we have established an MDCK cell line stably overexpressing the human MDR1 transporter (hMDR1; P-glycoprotein), and used CRISPR-Cas9 gene editing to knock out the endogenous cMDR1. Genomic screening revealed the generation of a clonal cell line homozygous for a four-nucleotide deletion in the canine ABCB1 gene leading to a frameshift and a premature stop codon...
April 24, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28445697/influence-of-maturation-on-in-vivo-tissue-to-plasma-partition-coefficients-for-cis-and-trans-permethrin
#8
Manoj Amaraneni, Jing Pang, James V Bruckner, Srinivasa Muralidhara, Tanzir B Mortuza, Darren Gullick, Shirin Hooshfar, Catherine A White, Brian S Cummings
Permethrin, the most widely used household insecticide in the U.S., is marketed as a mixture of its cis (CIS) and trans (TRANS) isomers. The major objective of this investigation was to develop and utilize a reliable approach to determine in vivo partition coefficients (PCs) for CIS and TRANS in immature and adult Sprague-Dawley rats. Adult, postnatal day (PND) 21 and PND 15 rats were infused with environmentally relevant concentrations of CIS or TRANS via a s.c. osmotic pump for 48 or 72 h. The adult and PND 21 rats also received an oral loading dose...
April 23, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28438535/a-critical-view-on-in-vitro-analysis-of-p-glycoprotein-p-gp-transport-kinetics
#9
Lasse Saaby, Birger Brodin
Transport proteins expressed in the different barriers of the human body can have great implications on absorption, distribution and excretion of drug compounds. Inhibition or saturation of a transporter can potentially alter these ADME properties, and thereby also the pharmacokinetic profile and bioavailability of drug compounds. P-glycoprotein (P-gp, ABCB1), is an efflux transporter which is present in most of the barriers of the body, including the small intestine, the blood-brain barrier, the liver and the kidney...
April 21, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28438534/editorial
#10
EDITORIAL
Ronald Borchardt
No abstract text is available yet for this article.
April 21, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28438533/association-of-mir-145-with-statin-induced-skeletal-muscle-toxicity-in-human-rhabdomyosarcoma-rd-cells
#11
Shun Saito, Takeo Nakanishi, Yuma Shirasaki, Miki Nakajima, Ikumi Tamai
Skeletal muscle toxicity including rhabdomyolysis in severe case is a major side effect of LDL cholesterol-lowering statin drugs. We, therefore, aimed to explore microRNA (miRNA) expression to understand molecular mechanism of statin-induced toxicity. miRNA expression profiling assay for cerivastatin (1 μM for 48 hr)-treated RD cells showed more than two-fold decrease in 26 miRNA expressions with miR-145 being down-regulated prominently. When RD cells were treated with cerivastatin at 10 μM for 36 hr, mitochondrial dysfunction was observed in 49...
April 21, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28435143/estimation-of-inter-individual-variability-of-pharmacokinetics-of-cyp2c9-substrates-in-humans
#12
Koji Chiba, Keiko Shimizu, Motohiro Kato, Taichi Miyazaki, Takaaki Nishibayashi, Kazuki Terada, Yuichi Sugiyama
The activity of metabolic enzymes varies across individuals and populations. Activity varies even among individuals sharing the same genotype. Genetic polymorphisms in CYP2C9 cause significant inter-individual variability in the metabolism of its substrates. However, the variability of CYP2C9 intrinsic hepatic clearance (CLint,h,CYP2C9) among subjects of the same genotype has not been reported. In this study, we estimated the coefficient of variation (CV) for the intrinsic hepatic clearance of tolbutamide by CYP2C9 for each CYP2C9 genotype using previously reported AUCs and oral clearance (CLoral) values in a Monte Carlo simulation with a dispersion model...
April 20, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28435142/clinical-drug-drug-interaction-evaluations-to-inform-drug-use-and-enable-drug-access
#13
Dinko Rekić, Kellie S Reynolds, Ping Zhao, Lei Zhang, Kenta Yoshida, Madhav Sachar, Micheline Piquette Miller, Shiew-Mei Huang, Issam Zineh
Clinical drug-drug interactions (DDIs) can occur when multiple drugs are taken by the same patient. Significant DDIs can result in clinical toxicity or treatment failure. Therefore, DDI assessment is an integral part of drug development and the benefit-risk assessment of new therapies. Regulatory agencies including the Food and Drug Administration (FDA), the European Medicines Agency (EMA), and the Pharmaceuticals and Medical Devices Agency of Japan (PMDA) have made recommendations in their DDI guidance documents on various methodologies (in vitro, in silico and clinical) to assess DDI potential and inform patient management strategies...
April 20, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28435141/thermodynamic-investigation-of-carbamazepine-saccharin-co-crystal-polymorphs
#14
Sudhir K Pagire, Niten Jadav, Venu R Vangala, Benjamin Whiteside, Anant Paradkar
Polymorphism in active pharmaceutical ingredients (APIs) can be regarded as critical for the potential that crystal form can have on the quality, efficacy and safety of the final drug product. The current contribution aims to characterize thermodynamic interrelationship of a dimorphic co-crystal, FI and FII, involving carbamazepine (CBZ) and saccharin (SAC) molecules. Supramolecular synthesis of CBZ-SAC FI and FII have been performed using thermo-kinetic methods and systematically characterized by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), solubility and slurry measurements...
April 20, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28435140/biowaiver-monographs-for-immediate-release-solid-oral-dosage-forms-enalapril
#15
REVIEW
Roger K Verbeeck, Isadore Kanfer, Raimar Löbenberg, Bertil Abrahamsson, Rodrigo Cristofoletti, D W Groot, Peter Langguth, James E Polli, Alan Parr, Vinod P Shah, Mehul Mehta, Jennifer B Dressman
Literature data relevant to the decision to allow a waiver of in vivo bioequivalence testing for the marketing authorization of immediate release, solid oral dosage forms containing enalapril maleate are reviewed. Enalapril, a prodrug, is hydrolyzed by carboxylesterases to the active angiotensin-converting enzyme inhibitor enalaprilat. Enalapril as the maleate salt is shown to be highly soluble, but only 60 to 70% of an orally administered dose of enalapril is absorbed from the gastrointestinal tract into the enterocytes...
April 20, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28431966/spray-drying-as-a-reliable-route-to-produce-metastable-carbamazepine-form-iv
#16
Rebecca A Halliwell, Rajni M Bhardwaj, Cameron Brown, Naomi E B Briggs, Jaclyn Dunn, John Robertson, Alison Nordon, Alastair J Florence
Carbamazepine is an active pharmaceutical ingredient used in the treatment of epilepsy that can form at least five polymorphic forms. Metastable form IV was originally discovered from crystallisation with polymer additives however has not been observed from subsequent solvent only crystallisation efforts. This work reports the reproducible formation of phase pure crystalline form IV by spray drying of methanolic carbamazepine solution. Characterisation of the material was carried out using diffraction, SEM and DSC...
April 18, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28431965/origin-of-nanodroplet-formation-upon-dissolution-of-an-amorphous-solid-dispersion-a-mechanistic-isotope-scrambling-study
#17
Anura S Indulkar, Jan E Waters, Huaping Mo, Yi Gao, Shweta A Raina, Geoff G Z Zhang, Lynne S Taylor
It has been observed that certain amorphous solid dispersions (ASDs), upon dissolution, generate drug-rich amorphous nanodroplets. These nanodroplets, present as a dispersed phase, can potentially enhance oral bioavailability of poorly soluble drugs by serving as a drug reservoir that efficiently feeds the continuous aqueous solution phase following absorption of drug. The purpose of this study was to probe the formation mechanism of the nanodroplets. The model system studied was nifedipine (NFD) formulated as an ASD with hydroxypropyl methylcellulose E5 Premium LV (HPMC-E5) or polyvinylpyrrolidone/vinyl acetate (PVPVA)...
April 18, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28431964/microvillus-specific-protein-tyrosine-phosphatase-sap-1-plays-a-role-in-regulating-the-intestinal-paracellular-transport-of-macromolecules
#18
Shingo Mori, Noriyasu Kamei, Yoji Murata, Kozo Takayama, Takashi Matozaki, Mariko Takeda-Morishita
The stomach cancer associated protein tyrosine phosphatase 1 (SAP-1) is a receptor-type protein tyrosine phosphatase that is specifically expressed on the apical membrane of the intestinal epithelium. SAP-1 is known to maintain the balance of phosphorylation of proteins together with protein kinases, however, its biological function and impact on pharmacokinetics in the intestine remain unclear. The present study, therefore, aimed to clarify the relationship between SAP-1 and the intestinal absorption behaviors of typical transporter substrates and macromolecules...
April 18, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28427886/identification-of-excipients-for-stabilizing-fiberless-adenovirus-as-biopharmaceuticals
#19
Grit Kupgan, Shyamal P Choudhari, Nicholas H Flynn, Adane Nigatu, Sravanthi Vupputuri, William D Picking, Wendy L Picking, Joshua D Ramsey
Reducing the promiscuous tropism of native adenovirus by using fiberless adenovirus is advantageous towards its use as a gene therapy vector or vaccine component. The removal of the fiber protein on native adenovirus abrogates several undesirable interactions; however, this approach decreases the particle's physical stability. In order to create stable fiberless adenovirus for pharmaceutical use, the effects of temperature and pH on the particle's stability profile must be addressed. Our results indicate that the stability of fiberless adenovirus is increased when it is stored in mildly acidic conditions around pH 6...
April 17, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28419826/melting-process-of-the-peritectic-mixture-of-lidocaine-and-ibuprofen-interpreted-by-site-percolation-theory-model
#20
Hikaru Kataoka, Yoshinori Sakaki, Kazushi Komatsu, Yohsuke Shimada, Satoru Goto
Eutectic mixtures are often used in the design and delivery of drugs. In this study, we examined the peritectic mixture of lidocaine (LDC) and ibuprofen (IBP) using differential scanning calorimetry, Raman spectroscopy, and microscopy. The obtained phase diagram shows that as the mixture is heated, first LDC melts at 293 K, then IBP dissolves in the liquefied LDC at 310 K, and finally all remaining crystals melt. In the (1)H NMR spectra, the signals of the carboxyl group in IBP and amide or amine group in LDC shift to the low magnetic field in the IBP/LDC mixtures, because of the intermolecular interaction between these moieties...
April 15, 2017: Journal of Pharmaceutical Sciences
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