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https://www.readbyqxmd.com/read/28737406/preclinical-effect-of-absorption-modifying-excipients-on-rat-intestinal-transport-of-five-model-compounds-and-the-intestinal-barrier-marker-51-cr-edta
#1
David Dahlgren, Carl Roos, Anders Lundqvist, Peter Langguth, Christer Tannergren, Markus Sjöblom, E Sjögren, H Lennernas
There is a renewed interest from the pharmaceutical field to develop oral formulations of compounds such as peptides, oligonucleotides, and polar drugs. However, these often suffer from insufficient absorption across the intestinal mucosal barrier. One approach to circumvent this problem is the use of absorption modifying excipient(s) (AME). This study determined the absorption enhancing effect of four AMEs (sodium dodecyl sulfate, caprate, chitosan, N-acetylcysteine) on five model compounds in a rat jejunal perfusion model...
July 24, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28737123/development-and-validation-of-eco-friendly-liquid-chromatographic-and-spectrophotometric-methods-for-simultaneous-determination-of-coformulated-drugs-phenylephrine-hydrochloride-and-prednisolone-acetate
#2
Nadia M Mostafa, Ghada M Elsayed, Nagiba Y Hassan, Dina A El Mously
Five simple, sensitive, and eco-friendly LC and UV spectrophotometric methods have been developed for the simultaneous determination of phenylephrine hydrochloride (PHE) and prednisolone acetate (PRD) in their combined dosage form. The first method was reversed-phase (RP) LC using methanol–water–heptane-1-sulfonic acid sodium salt (75 + 25 + 0.1, v/v/w) as a mobile phase. Separation was achieved using an XSelect HSS reversed-phase C18 analytical column (250 × 4.6 mm, 5µm). The flow rate was 1...
July 24, 2017: Journal of AOAC International
https://www.readbyqxmd.com/read/28736128/the-effect-of-pro-nanolipospheres-pnl-formulation-containing-natural-absorption-enhancers-on-the-oral-bioavailability-of-delta-9-tetrahydrocannabinol-thc-and-cannabidiol-cbd-in-a-rat-model
#3
Irina Cherniakov, Dvora Izgelov, Abraham J Domb, Amnon Hoffman
The lipophilic phytocannabinoids cannabidiol (CBD) and Δ(9)-tetrahydrocannabinol (THC) show therapeutic efficacy in various medical conditions. Both molecules are poorly water soluble and subjected to extensive first pass metabolism in the gastrointestinal tract, leading to a limited oral bioavailability of approximately 9%. We have developed an advanced lipid based Self-Emulsifying Drug Delivery System termed Advanced Pro-NanoLiposphere (PNL) pre-concentrate. The PNL is composed of lipid and emulsifying excipients of GRAS status and are known to increase solubility and reduce Phase I metabolism of lipophilic active compounds...
July 20, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28732731/atomization-of-denatured-whey-proteins-as-a-novel-and-simple-way-to-improve-oral-drug-delivery-system-properties
#4
Hassana Hsein, Ghislain Garrait, Muhammad Ashraful Mumin, Eric Beyssac, Valérie Hoffart
In the sphere of drug delivery, denatured whey protein (DWP) has in recent times gained press. However, to date, no scalable and affordable dosage form has been developed. The objective of our study was to evaluate the potential use of spray-dried DWP as a ready to use excipient for oral drug delivery. Therefore, solid state, FTIR spectra and wettability were studied. Dissolution, mucoadhesion and the effect on paracellular permeability were also evaluated. The spray-dried DWP particles were spherical with 4μm mean diameter...
July 18, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28732254/going-down-the-tubes-impact-on-seizure-control-of-antiepileptic-medication-given-via-percutaneous-feeding-tubes
#5
REVIEW
Caryn Jory, Rohit Shankar, Katy Oak, Janina Oates, Mike Wilcock
BACKGROUND: Long-term feeding by percutaneous endoscopic gastrostomy tube (PEG) is uncommon but can present significant issues when both nutrition and medication have to be fed down the same tube. This is especially important in people with epilepsy where the dose and bioavailability of antiepileptic drugs are critical to maintain adequate seizure control. This group with long-term PEG tubes is particularly vulnerable and dependent on their carers to provide high standard of care. Indeed, approximately half of the people with long-term feeding tubes suffer from severe intellectual disability which requires careful coordination of all members of the multidisciplinary team...
July 18, 2017: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/28730958/engineering-synergistically-active-and-bioavailable-cost-effective-medicines-for-neglected-tropical-diseases-the-role-of-excipients
#6
Dolores R Serrano, Aikaterini Lalatsa, M Auxiliadora Dea-Ayuela
Leishmaniasis is a neglected tropical disease responsible for the ninth largest disease burden in the world threatening 350 million people mostly in developing countries. The lack of efficacy, severe adverse effects, long duration, high cost and parenteral administration of the current therapies result in poor patient compliance and emergence of resistance. Leishmaniasis' unmet need for safer, affordable and more effective treatments is only partly addressed by today's global health product pipeline that focuses on products amenable to rapid clinical development, mainly by reformulating or repurposing existing drugs for new uses...
July 19, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28730935/effect-of-directly-compressible-excipient-and-treated-agar-on-drug-release-of-clopidogrel-oral-disintegrating-tablets
#7
Kambham Venkateswarlu, Manyam Nirosha, Budideti Kishore Kumar Reddy, Badithala Siva Sai Kiran
AIM: In the present investigation, oral dissolving/dispersible/disintegrating tablets (ODTs) of clopidogrel were designed with a view to enhance the bioavailability and patient compliance by two different methods, namely, direct compression and effervescent methods using directly compressible excipient and treated agar (TAG). MATERIALS & METHODS: In the direct compression method, TAG was used as a disintegrant and another method used a mixture of sodium bicarbonate and tartaric acid along with TAG as disintegrants...
July 2017: Therapeutic Delivery
https://www.readbyqxmd.com/read/28730107/induction-of-vascular-endothelial-growth-factor-receptor-expression-in-human-umbilical-vein-endothelial-cells-after-repeated-bevacizumab-treatment-in-vitro
#8
Ji Eun Lee, Jin Young Kim, Jae Ho Jung, Dong Hoon Shin, Sung Who Park
AIM: To investigate the mechanism underlying the loss of responsiveness to anti-vascular endothelial growth factor (VEGF) treatment after repeated injections for choroidal neovascularization, VEGF and VEGF receptor (VEGFR) expressions were evaluated following repeated bevacizumab treatments in hypoxic human umbilical vein endothelial cells (HUVECs) in vitro. METHODS: HUVECs were incubated under hypoxic conditions in two media of different bevacizumab concentrations (1...
2017: International Journal of Ophthalmology
https://www.readbyqxmd.com/read/28729250/stellarex-drug-coated-balloon-for-treatment-of-femoropopliteal-disease-12-month-outcomes-from-the-randomized-illumenate-pivotal-and-pharmacokinetic-studies
#9
Prakash Krishnan, Peter Faries, Khusrow Niazi, Ash Jain, Ravish Sachar, William B Bachinsky, Joseph A Cardenas, Martin Werner, Marianne Brodmann, J A Mustapha, Carlos I Mena-Hurtado, Michael R Jaff, Andrew H Holden, Sean P Lyden
Background -Drug-coated balloons (DCB) are a predominant revascularization therapy for symptomatic femoropopliteal artery disease. Due to differences in excipients, paclitaxel dose and coating morphologies, varying clinical outcomes have been observed with different DCBs. We report the results of two studies investigating the pharmacokinetic (PK) and clinical outcomes of a new DCB to treat femoropopliteal disease. Methods -In the ILLUMENATE Pivotal Study, 300 symptomatic patients (Rutherford class 2-4), were randomized to DCB (N=200) or standard angioplasty (PTA) (N=100)...
July 20, 2017: Circulation
https://www.readbyqxmd.com/read/28729174/challenges-and-strategies-to-facilitate-formulation-development-of-pediatric-drug-products-safety-qualification-of-excipients
#10
Lorrene A Buckley, Smita Salunke, Karen Thompson, Gerri Baer, Darren Fegley, Mark A Turner
A public workshop entitled "Challenges and strategies to facilitate formulation development of pediatric drug products" focused on current status and gaps as well as recommendations for risk-based strategies to support the development of pediatric age-appropriate drug products. Representatives from industry, academia, and regulatory agencies discussed the issues within plenary, panel, and case-study breakout sessions. By enabling practical and meaningful discussion between scientists representing the diversity of involved disciplines (formulators, nonclinical scientists, clinicians, and regulators) and geographies (eg, US, EU), the Excipients Safety workshop session was successful in providing specific and key recommendations for defining paths forward...
July 17, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28727449/the-use-of-maldi-ms-combined-with-differential-hydrogen-deuterium-exchange-for-semi-automated-protein-global-conformational-screening
#11
Gregory F Pirrone, Heather Wang, Nicole Canfield, Alexander S Chin, Timothy A Rhodes, Alexey A Makarov
Matrix-assisted laser desorption/ionization (MALDI) coupled with a time-of-flight (TOF) mass-spectrometry (MS) detector is acknowledged to be very useful for analysis of biological molecules. At the same time, hydrogen-deuterium exchange (HDX) is a well-known technique for studying protein higher-order structure. However, coupling MALDI with HDX may be challenging due to undesired back-exchange reactions during analysis. In this report, we survey an approach that utilizes MALDI coupled with automated sample preparation to compare global conformational changes of proteins under different solution conditions using differential HDX...
July 20, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/28725150/development-and-evaluation-of-ketoprofen-sustained-release-matrix-tablet-using-hibiscus-rosa-sinensis-leaves-mucilage
#12
M Kaleemullah, K Jiyauddin, E Thiban, S Rasha, S Al-Dhalli, S Budiasih, O E Gamal, A Fadli, Y Eddy
Currently, the use of natural gums and mucilage is of increasing importance in pharmaceutical formulations as valuable drug excipient. Natural plant-based materials are economic, free of side effects, biocompatible and biodegradable. Therefore, Ketoprofen matrix tablets were formulated by employing Hibiscus rosa-sinensis leaves mucilage as natural polymer and HPMC (K100M) as a synthetic polymer to sustain the drug release from matrix system. Direct compression method was used to develop sustained released matrix tablets...
July 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28725139/hybrid-polymeric-matrices-for-oral-modified-release-of-desvenlafaxine-succinate-tablets
#13
Wael Samy, Ayman Elnoby, Hanan M El-Gowelli, Nazik Elgindy
Purpose: Desvenlafaxine succinate (DSV) is a water soluble anti-depressant drug, which is rapidly absorbed after oral administration exaggerating its side effects. The current work aimed to prepare controllable release DSV matrix to reduce DSV side effects related to its initial burst. Methods: Fifteen DSV matrix formulations were prepared using different polymers, polymer/drug ratios and matrix excipients and characterized using Differential Scanning Calorimetry (DSC), infrared (IR) spectroscopy, water uptake and in vitro DSV release...
July 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28724167/in-vitro-controlled-release-of-two-new-tuberculocidal-adamantane-aminoethers-from-solid-pharmaceutical-formulations-ii
#14
Marilena Vlachou, Angeliki Siamidi, Dimitrios Spaneas, Dimitrios Lentzos, Polixeni Ladia, Konstantina Anastasiou, Ioannis Papanastasiou, Angeliki-Sofia Foscolos, Markos-Orestis Georgiadis, Vangelis Karalis, Tahsin Kellici, Thomas Mavromoustakos
The aim of the present investigation was to develop matrix tablet formulations for the in vitro controlled release of two new tuberculocidal adamantane aminoethers (compounds III and IV), congeneric to the adamantane derivative SQ109, which is in final clinical trials, and aminoethers (I) and (II), using carefully selected excipients, such as polyvinylpyrrolidone, sodium alginate and lactose. The tablets were prepared using the direct compression method and dissolution experiments were conducted using the US Pharmacopoeia type II apparatus (paddle method) in gastric and intestinal fluids...
July 19, 2017: Drug Research
https://www.readbyqxmd.com/read/28724166/iron-pharmacokinetics-in-women-with-iron-deficiency-anaemia-following-a-single-oral-dose-of-a-novel-formulation-of-tardyferon-prolonged-release-ferrous-sulphate
#15
Andrew Leary, Laurence Barthe, Thierry Clavel, Claudie Sanchez, Zahida Issiakhem, Bruno Paillard, Jean-Marc Edmond
Numerous iron-containing preparations are available on the market; these vary in dosage, salt, chemical state of iron (ferric or ferrous) and in the iron delivery process (immediate or prolonged-release). Tardyferon® is a prolonged-release tablet containing 80 mg ferrous sulphate. The formulation has recently been modified; changes to the excipients which constitute the inert formulation matrix have allowed a decrease in tablet size for easier swallowing. The aim of this multicenter open-label study was to characterize the serum pharmacokinetics of iron in non-pregnant women aged 23-45 years with iron deficiency anaemia (IDA) following single oral administration of 160 mg Tardyferon® under fasting conditions...
July 19, 2017: Drug Research
https://www.readbyqxmd.com/read/28723408/in-line-raman-spectroscopic-monitoring-and-feedback-control-of-a-continuous-twin-screw-pharmaceutical-powder-blending-and-tableting-process
#16
Brigitta Nagy, Attila Farkas, Martin Gyürkés, Szofia Komaromy-Hiller, Balázs Démuth, Bence Szabó, Dávid Nusser, Enikő Borbás, György Marosi, Zsombor Kristóf Nagy
The integration of Process Analytical Technology (PAT) initiative into the continuous production of pharmaceuticals is indispensable for reliable production. The present paper reports the implementation of in-line Raman spectroscopy in a continuous blending and tableting process of a three-component model pharmaceutical system, containing caffeine as model active pharmaceutical ingredient (API), glucose as model excipient and magnesium stearate as lubricant. The real-time analysis of API content, blend homogeneity, and tablet content uniformity was performed using a Partial Least Squares (PLS) quantitative method...
July 16, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28719373/basics-of-sterile-compounding-excipients-used-in-injections
#17
Michael J Akers
This article focuses on the majority of different excipients (all formulation components.
July 2017: International Journal of Pharmaceutical Compounding
https://www.readbyqxmd.com/read/28716757/saturated-phosphatidylcholine-as-matrix-former-for-oral-extended-release-dosage-forms
#18
Marina Kolbina, Roland Bodmeier, Martin Körber
The aim of this study was to evaluate the suitability of saturated phosphatidylcholine (Phospholipon® 90H) as extended release excipient in matrix tablets for three model drugs with different aqueous solubility (theophylline, caffeine and diprophylline). The tablets could be prepared by direct compression because of the favorable phospholipid powder flow properties (Carr's index: 12.64 and angle of repose: 28.85) and good compactibility. Tablets of low porosity were formed already at low pressure of 40MPa and with drug loadings up to 70% due to high plasticity of the phospholipid...
July 14, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28712035/ginsenoside-improves-physicochemical-properties-and-bioavailability-of-curcumin-loaded-nanostructured-lipid-carrier
#19
Ajay Vijayakumar, Rengarajan Baskaran, Han-Joo Maeng, Bong Kyu Yoo
The aim of this study was to develop a ginsenoside-modified nanostructured lipid carrier (G-NLC) dispersion containing curcumin. The NLC was prepared by melt emulsification with slight modification process. Different G-NLC dispersion systems were prepared using lipid carrier matrix composed of ginsenoside, phosphatidylcholine, lysophosphatidylcholine, and hydrogenated bean oil. TEM image of the nanoparticles in the NLC dispersion showed core/shell structure, and there was corona-like layer surrounding the particles in the G-NLC...
July 15, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28711714/review-an-update-on-the-use-of-oral-phospholipid-excipients
#20
Peter van Hoogevest
The knowledge and experiences obtained with oral phospholipid excipients is increasing continuously. Nevertheless the present number of oral products using these excipients as essential excipient is very limited. This is remarkable to note, since phospholipids play a significant role in the food uptake mechanisms of the GI tract and these mechanisms could be translated into suitable dosage forms and corresponding drug delivery strategies. In addition, phospholipid excipients are multifunctional biodegradable, non-toxic excipients, which can be used in oral dosage forms as wetting agents, emulsifier, solubilizer and matrix forming excipients...
July 12, 2017: European Journal of Pharmaceutical Sciences
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