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Journal of Pharmaceutical Sciences

Rampurna P Gullapalli, Carolyn L Mazzitelli
Capsules offer an alternate to tablets for oral delivery of therapeutic compounds. One advantage of capsules over tablets is their amenability to deliver not only solids but also non-aqueous liquids and semisolids as a unit dose solid dosage form. Shell component is an essential part of capsule dosage forms. Capsule shells, available as hard or soft shells, are formulated from gelatin or a non-gelatin polymeric material such as hypromellose and starch, water, and with or without a non-volatile plasticizer. The capsule shells may also be formulated to modify the release of their fill contents in a site-specific manner in the gastrointestinal tract...
February 13, 2017: Journal of Pharmaceutical Sciences
R E Cavicchi, Cayla Collett, Srivalli Telikepalli, Zhishang Hu, Michael Carrier, Dean C Ripple
An accurate assessment of particle characteristics and concentrations in pharmaceutical products by flow imaging requires accurate particle sizing and morphological analysis. Analysis of images begins with the definition of particle boundaries. Commonly a single threshold defines the level for a pixel in the image to be included in the detection of particles, but depending on the threshold level, this results in either missing translucent particles or oversizing of less transparent particles due to the halos and gradients in intensity near the particle boundaries...
February 13, 2017: Journal of Pharmaceutical Sciences
M Barrio, J Huguet, I B Rietveld, B Robert, R Céolin, J Ll Tamarit
Understanding the polymorphic behavior of active pharmaceutical ingredients is important for formulation purposes and regulatory reasons. Metacetamol is an isomer of paracetamol and it similarly exhibits polymorphism. In the present paper, it has been found that one of the polymorphs of metacetamol is only stable under increased pressure, which has led to the conclusion that metacetamol like paracetamol is a monotropic system under ordinary (= laboratory) conditions and that it becomes enantiotropic under pressure with the I-II-L triple point coordinates for metacetamol TI-II-L = 535±10 K and PI-II-L = 692±70 MPa...
February 9, 2017: Journal of Pharmaceutical Sciences
Guohua An, Robin K Ohls, Robert D Christensen, John A Widness, Donald M Mock, Peter Veng-Pedersen
Darbepoetin alfa (Darbe) is a hyperglycosylated analogue of recombinant human erythropoietin (Epo). The aim of this study was to develop a population pharmacokinetic model for Darbe following i.v. and s.c. administration to infants. Data from two infant clinical studies (a single i.v. dose study following a 4 μg/kg dose of Darbe, and a single s.c. dose study following 1 μg/kg or 4 μg/kg dose of Darbe) were combined and analyzed simultaneously using non-linear mixed effect modeling approach. Darbe population pharmacokinetics was well described by a 2-compartment model with first order elimination...
February 8, 2017: Journal of Pharmaceutical Sciences
Ali Abdussalam, Osama H Elshenawy, Yousef A Bin Jardan, Ayman O S El-Kadi, Dion R Brocks
Obesity is caused by a number of factors including heredity, lack of exercise and poor diet. Diets rich in fats and/or high carbohydrates are the common culprits leading to obesity. Here we studied the effects of these components on proteins involved in drug disposition. Male rats were given either a normal diet (lean controls), or one rich in fats, carbohydrates (as high fructose corn syrup equivalent) or in combination. After 14 weeks, plasma biochemistry, liver and kidney mRNA and protein for selected CYP and transporters were determined...
February 8, 2017: Journal of Pharmaceutical Sciences
Yoonhee Bae, Hyang-Shuk Rhim, Seulgi Lee, Kyung Soo Ko, Jin Han, Joon Sig Choi
Malignant glioma is the most common and aggressive form of primary brain tumor in adults. In this study, we describe the efficacy of nonviral gene delivery carriers, histidine and arginine or histidine and lysine grafted PAMAM dendrimers (PAMAM-H-R and PAMAM-H-K), in delivering a therapeutic, a tumor-selective killer gene, apoptin, using human glioma cells (U87-MG) and newborn human dermal fibroblast (NB-HDF) cells. We analyzed transfection efficiency using luciferase (Luc) and a pDNA encoding for enhanced fluorescent protein (EGFP), and assessed cell viability in both cells...
February 7, 2017: Journal of Pharmaceutical Sciences
Kumar N Sunil, Tekuri Venkatadri, Darshak R Trivedi
Two novel pharmaceutical co-crystals of anti-inflammatory drug flufenamic acid (FFA) with 2-chloro-4-nitrobenzoic acid (CNB) and ethenzamide (ETZ) have been synthesized by solvent evaporation method as well as by solvent drop assisted grinding method. The synthesized co-crystals were characterized thoroughly by various spectroscopic methods and crystal structures were determined by single-crystal X-ray diffraction technique (SC-XRD). In FFA-CNB co-crystal, robust supramolecular acid-acid homosynthon was observed...
February 6, 2017: Journal of Pharmaceutical Sciences
Yu Jiang, Gary Milavetz, Margaret O James, Guohua An
Dichloroacetic acid (DCA), a halogenated organic acid, is a pyruvate dehydrogenase kinase (PDK) inhibitor that has been used to treat congenital or acquired lactic acidosis and is currently in early phase clinical trials for cancer treatment. DCA was found to inhibit its own metabolism by irreversibly inactivating glutathione transferase zeta 1 (GSTZ1-1), resulting in non-linear kinetics and abnormally high accumulation ratio after repeated dosing. In this analysis, a semi-mechanistic pharmacokinetic-enzyme turn over model was developed for the first time to capture DCA auto-inhibition, gastrointestinal region-dependent absorption, and time dependent change in bioavailability in rats...
February 2, 2017: Journal of Pharmaceutical Sciences
Clémence Chenevas-Paule, Hans-Michael Wolff, Mark Ashton, Martin Schubert, Kalliopi Dodou
Microreservoir-type transdermal drug delivery systems (MTDDS) can prevent drug crystallization; however no current predictive model considers the impact of drug load and hydration on their physical stability. We investigated MTDDS films containing polyvinylpyrrolidone (PVP) as polymeric drug stabilizer in lipophilic pressure sensitive adhesive (silicone). Medicated and unmedicated silicone films with different molar N-vinylpyrrolidone (VP):drug ratios were prepared and characterized by FTIR, differential scanning calorimetry (DSC), scanning electron microscopy (SEM), microscopy, Dynamic Vapour Sorption (DVS) and stability testing for four months at different storage conditions...
February 2, 2017: Journal of Pharmaceutical Sciences
Wenyi Hua, Hui Zhang, Sangwoo Ryu, Xin Yang, Li Di
Human tissue distribution of carbonyl reductase 1 (CBR1) is quite controversial in the literature. To understand the differences, CBR1 protein abundance in human intestine, liver and kidney has been determined using a proteomic approach with LC-MS/MS. The results show that CBR1 distribution in the three tissues is relatively similar, within 2-3 folds of each other. Intestine has the highest CBR1 enzyme level (106 pmol/mg protein) followed by liver (76 pmol/mg protein) and kidney (39 pmol/mg protein). The high abundance of CBR1 in the intestine and kidney suggests the critical role of this enzyme in gut first-pass metabolism and extra-hepatic clearance...
February 1, 2017: Journal of Pharmaceutical Sciences
Mary Warner, Chris Baumle
No abstract text is available yet for this article.
February 1, 2017: Journal of Pharmaceutical Sciences
Yang Song, Anushree Herwadkar, Meera G Patel, Ajay K Banga
The objective of this work was to optimize a gel formulation of cimetidine to maximize its transdermal delivery across microporated skin. Specifically, the effect of extent of ionization in formulation on permeation of cimetidine across microporated skin was studied. Cimetidine was formulated into a gel using propylene glycol, water and carbopol 980NF. Three strengths of gels (0.1% w/w, 0.5% w/w and 0.8% w/w) were made and Tris base was used to adjust the pH of formulations to pH 5, pH 6.8 and pH 7.5. In vitro permeation testing was performed on vertical Franz cells with dermatomed porcine ear skin...
February 1, 2017: Journal of Pharmaceutical Sciences
Kausik K Nanda, William D Blincoe, Leonardo R Allain, W Peter Wuelfing, Paul A Harmon
Metal ions play an important role in oxidative drug degradation. One of the most ubiquitous metal ion impurities in excipients and buffers is Fe(III). In the field of oxidative drug degradation chemistry, the role of Fe(III) has been primarily discussed in terms of its effect in reaction with trace hydroperoxide impurities. However, the role of Fe(III) acting as a direct oxidant of drug molecules, which could operate in the absence of any hydroperoxide impurities is less common. This work focuses on Fe(III)-induced oxidation of some aromatic drug molecules/drug fragments containing benzylic C-H bonds in the absence of initiating peroxides...
January 31, 2017: Journal of Pharmaceutical Sciences
Nathaniel R Maddux, Austin L Daniels, Theodore W Randolph
Sub-visible particles in therapeutic protein formulations are an increasing manufacturing and regulatory concern due to their potential to cause adverse immune responses. Flow imaging microscopy is used extensively to detect sub-visible particles and investigate product deviations, typically by comparing imaging data using histograms of particle descriptors. Such an approach discards much information, and requires effort to interpret differences, which is problematic when comparing many data sets. We propose to compare imaging data by using the Kullback-Leibler divergence, an information theoretic measure of the difference of distributions...
January 31, 2017: Journal of Pharmaceutical Sciences
Caleb Abshire, Hakm Y Murad, Jaspreet S Arora, James Liu, Sree Harsha Mandava, Vijay T John, Damir B Khismatullin, Benjamin R Lee
This study reports, for the first time, development of tyrosine kinase inhibitor-loaded, thermosensitive liposomes (TKI/TSLs) and their efficacy for treatment of renal cell carcinoma when triggered by focused ultrasound (FUS). Uptake of these nanoparticles into renal cancer cells was visualized with confocal and fluorescent imaging of rhodamine B-loaded liposomes. The combination of TKI/TSLs and focused ultrasound was tested in an in vitro tumor model of renal cell carcinoma. According to MTT cytotoxic assay and flow cytometric analysis the combined treatment led to the least viability (23...
January 31, 2017: Journal of Pharmaceutical Sciences
André Luiz Lopes Martins, Aline Carlos de Oliveira, Carolina Machado Ozório Lopes do Nascimento, Luís Antônio Dantas Silva, Marilisa Pedroso Nogueira Gaeti, Eliana Martins Lima, Stephânia Fleury Taveira, Kátia Flávia Fernandes, Ricardo Neves Marreto
The aim of this study was to develop mucoadhesive pellets on a thiolated pectin base using the extrusion-spheronization technique. Thiolation of pectin was performed by esterification with thioglycolic acid. The molecular weight and thiol group content of the pectins were determined. Pellets containing pectin, microcrystalline cellulose and ketoprofen were prepared and their mucoadhesive properties were evaluated through a wash-off test using porcine intestinal mucosa. The in vitro ketoprofen release was also evaluated...
January 31, 2017: Journal of Pharmaceutical Sciences
Cherokee Hoaglund Hyzer, Michele L Williamson, Patrick J Jansen, Michael E Kopach, R Brian Scherer, Steven W Baertschi
Edivoxetine (LY2216684 HCl), although a chemically stable drug substance, has shown the tendency to degrade in the presence of carbohydrates that are commonly used tablet excipients, especially at high excipient:drug ratios. The major degradation product has been identified as N-formyl edivoxetine. Experimental evidence including solution and solid state investigations, is consistent with the N-formylation degradation pathway resulting from a direct reaction of edivoxetine with (1) formic acid (generated from decomposition of microcrystalline cellulose (MCC) or residual glucose), and/or (2) the reducing sugar ends (aldehydic carbons) of either residual glucose or the MCC polymer...
January 31, 2017: Journal of Pharmaceutical Sciences
Wyatt J Roth, Ahmad Almaya, Timothy T Kramer, Jeffrey D Hofer
The purpose of this work was to assess the impact of continuous mixing on tablet critical quality attributes (CQAs) manufactured using a continuous, direct compression process. A nine run design of experiments (DoE) that bracketed the range of commercially relevant mixer speeds, mixer orientations, and mass flow rates was executed using a formulation containing a cohesive drug substance at relatively low drug load. Drug substance dispensed concentration using loss-in-weight feeders was within 1% of target for each experiment with 30 second mass flow relative standard deviation values of 3...
January 30, 2017: Journal of Pharmaceutical Sciences
Malgorzata Szafarz, Kamil Kus, Maria Walczak, Agnieszka Zakrzewska, Michał Niemczak, Juliusz Pernak, Stefan Chlopicki
Treatment with 1-methylnicotinamide (MNA), a major metabolite of nicotinamide, exerts anti-thrombotic, anti-inflammatory, and vasoprotective effects. Yet, pharmacokinetic (PK) profile of MNA has not been fully characterised. In the present work we analyse the PK profile of the MNA given as a nitrate (MNANO3) in comparison to nitrite (MNANO2) or chloride (MNACl) in rats. The bioavailability of MNA administered as MNANO3 equaled 22.4% as compared to MNANO2 or MNACl (9.2% and 9.1%, respectively). Moreover, in single pass intestinal perfusion experiments effective permeability of MNA given as MNANO3 was higher as compared with MNA administered as MNANO2 or MNACl...
January 30, 2017: Journal of Pharmaceutical Sciences
Yan He, Chris Ho, Donglai Yang, Jeane Chen, Edward Orton
Salt formation is one of the primary approaches to improve the developability of ionizable poorly water soluble compounds. Solubility determination of the salt candidates in aqueous media or bio-relevant fluids is a critical step in salt screening. Salt solubility measurements can be complicated due to dynamic changes in both solution and solid phases. Because of the early implementation of salt screening in research, solubility measurements often are performed using minimal amount of material. Some salts have transient high solubility upon dissolution...
January 30, 2017: Journal of Pharmaceutical Sciences
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