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https://www.readbyqxmd.com/read/28445766/inhibitory-effect-of-emulsifiers-in-sedds-on-protease-activity-just-an-illusion
#1
Noemi Lupo, Una Fidahic, Gergely Hetényi, Janine Griesser, Andreas Bernkop-Schnürch
AIM: Evaluation of inhibitory effect of emulsifiers on pancreatic trypsin and α-chymotrypsin. METHODS: The inhibitory effect of Cremophor EL, Cremophor RH 40, Brij O10, Tween 20, polyethylene glycol 8000, polyethylene glycol 400, Carbitol, Pemulen TR-1, Pemulen TR-2, Carbopol Ultrez 20 and Carbopol Ultrez 21 on pancreatic trypsin and α-chymotrypsin was tested. BAEE (Nα-Benzoyl-L-arginine ethyl ester), BTEE (N-Benzoyl-L-tyrosine ethyl ester), casein and insulin were used as substrates for trypsin and α-chymotrypsin...
April 23, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28438550/lipophilic-salts-of-poorly-soluble-compounds-to-enable-high-dose-lipidic-sedds-formulations-in-drug-discovery
#2
Michael Morgen, Ajay Saxena, Xue-Qing Chen, Warren Miller, Richard Nkansah, Aaron Goodwin, Jon Cape, Roy Haskell, Ching Su, Olafur Gudmundsson, Michael Hageman, Anoop Kumar, Gajendra Singh Chowan, Abhijith Rao, Vinay K Holenarsipur
Self-emulsifying drug delivery systems (SEDDS) have been used to solubilize poorly water-soluble drugs to improve exposure in high-dose pharmacokinetic (PK) and toxicokinetic (TK) studies. However, the absorbable dose is often limited by drug solubility in the lipidic SEDDS vehicle. This study focuses on increasing solubility and drug loading of ionizable drugs in SEDDS vehicles using lipophilic counterions to prepare lipophilic salts of drugs. SEDDS formulations of two lipophilic salts-atazanavir-2-naphthalene sulfonic acid (ATV-2-NSA) and atazanavir-dioctyl sulfosuccinic acid (ATV-Doc)-were characterized and their performance compared to atazanavir (ATV) free base formulated as an aqueous crystalline suspension, an organic solution, and a SEDDS suspension, using in vitro, in vivo, and in silico methods...
April 21, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28434635/readmissions-unplanned-emergency-room-visits-and-surgical-retreatment-rates-after-anti-reflux-procedures
#3
Hsin-Hsiao S Wang, Rohit Tejwani, Steven Wolf, John S Wiener, Jonathan C Routh
INTRODUCTION/BACKGROUND: The choice between endoscopic injection (EI) and ureteroneocystotomy (UNC) for surgical correction of vesicoureteral reflux (VUR) is controversial. OBJECTIVE: To compare postoperative outcomes of EI vs UNC. STUDY DESIGN: This study reviewed linked inpatient (SID), ambulatory surgery (SASD), and emergency department (SEDD) data from five states in the United States (2007-10) to identify pediatric patients with primary VUR undergoing EI or UNC as an initial surgical intervention...
April 7, 2017: Journal of Pediatric Urology
https://www.readbyqxmd.com/read/28425577/postoperative-hemorrhage-and-hospital-revisit-after-transoral-robotic-surgery
#4
Joseph Zenga, Jasmina Suko, Dorina Kallogjeri, Patrik Pipkorn, Brian Nussenbaum, Ryan S Jackson
OBJECTIVES/HYPOTHESIS: To investigate the incidence and complications related to postoperative hemorrhage (POH) after transoral robotic surgery (TORS). STUDY DESIGN: Retrospective review of the State Inpatient Database (SID), the State Ambulatory Surgery Database (SASD), and the State Emergency Department Database (SEDD) from the Healthcare Cost and Utilization Project. METHODS: Patients were identified from the SID, SASD, and SEDD for the states of Florida, New York, and California from 2005 to 2013 who had an International Classification of Diseases, Ninth Edition code for a surgical procedure on the upper aerodigestive tract associated with a code for robotic-assisted surgery...
April 20, 2017: Laryngoscope
https://www.readbyqxmd.com/read/28398288/spatiotemporal-historical-datasets-at-micro-level-for-geocoded-individuals-in-five-swedish-parishes-1813-1914
#5
Finn Hedefalk, Patrick Svensson, Lars Harrie
This paper presents datasets that enable historical longitudinal studies of micro-level geographic factors in a rural setting. These types of datasets are new, as historical demography studies have generally failed to properly include the micro-level geographic factors. Our datasets describe the geography over five Swedish rural parishes, and by linking them to a longitudinal demographic database, we obtain a geocoded population (at the property unit level) for this area for the period 1813-1914. The population is a subset of the Scanian Economic Demographic Database (SEDD)...
April 11, 2017: Scientific Data
https://www.readbyqxmd.com/read/28365295/in-vitro-and-in-vivo-performance-of-monoacyl-phospholipid-based-self-emulsifying-drug-delivery-systems
#6
Thuy Tran, Scheyla D V S Siqueira, Heinz Amenitsch, Anette Müllertz, Thomas Rades
This study investigates the effect of monoacyl phospholipid incorporation on the in vitro and in vivo performance of self-emulsifying drug delivery systems (SEDDS). Monoacyl phosphatidylcholine (Lipoid S LPC 80 (LPC)) was incorporated into four different fenofibrate (FF)-loaded long-chain SEDDS to investigate the impact of LPC on the emulsion droplet size, extent of digestion, colloidal structure evolution and drug precipitation during in vitro lipolysis simulating human conditions and drug bioavailability in a rat model...
March 30, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28349550/photo-absorption-of-p-coumaric-acid-in-aqueous-solution-rism-scf-sedd-theory-approach
#7
Kenji Hirano, Hiroshi Nakano, Yoshihide Nakao, Hirofumi Sato, Shigeyoshi Sakaki
Photo absorption properties of p-coumaric acid, the chromophore of photoactive yellow protein, in aqueous solution were investigated by means of reference interaction site model self-consistent field with spatial electron density distribution (RISM-SCF-SEDD) method. RISM-SCF-SEDD is a combination methodology of electronic structure theory and statistical mechanics for molecular liquids. Here, time-dependent density functional theory was coupled with RISM equation to study the electronic structure of p-coumaric acid in aqueous system...
March 27, 2017: Journal of Computational Chemistry
https://www.readbyqxmd.com/read/28347848/comparison-of-the-protective-effect-of-self-emulsifying-peptide-drug-delivery-systems-towards-intestinal-proteases-and-glutathione
#8
Gergely Hetényi, Janine Griesser, Michael Moser, Frédéric Demarne, Vincent Jannin, Andreas Bernkop-Schnürch
AIM: The aim of this study was to evaluate the protective effect of self-emulsifying drug delivery systems (SEDDS) for therapeutic peptides towards intestinal proteases and reduced glutathione (GSH). METHODS: Sodium docusate was applied as anionic surfactant for hydrophobic ion pairing with leuprorelin (LEU), insulin (INS) and desmopressin (DES). The complexes were loaded into SEDDS that were characterized regarding droplet size distribution and zeta potential. The release profile of the peptides was examined by dialysis membrane method...
March 24, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28323109/self-emulsifying-drug-delivery-systems-design-of-a-novel-vaginal-delivery-system-for-curcumin
#9
S Köllner, I Nardin, R Markt, J Griesser, F Prüfert, A Bernkop-Schnürch
AIM: The aim of this study was to develop a vaginal self-emulsifying delivery system for curcumin being capable of spreading, of permeating the mucus gel layer and of protecting the drug being incorporated in oily nanodroplets towards mucus interactions and immobilization. METHODS: The emulsifying properties of curcumin loaded SEDDS containing 30% Cremophor RH40, 20% Capmul PG-8, 30% Captex 300, 10% DMSO and 10% tetraglycol (SEDD formulation A) as well as 25% PEG 200, 35% Cremophor RH40, 20% Captex 355, 10% Caprylic acid and 10% Tween 80 (SEDD formulation B) after diluting 1+2 with artificial vaginal fluid were characterized regarding droplet size and zeta potential...
March 17, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28283859/combination-of-sedds-and-preactivated-thiomer-technology-incorporation-of-a-preactivated-thiolated-amphiphilic-polymer-into-self-emulsifying-delivery-systems
#10
Gergely Hetényi, Janine Griesser, Isabelle Nardin, Andreas Bernkop-Schnürch
PURPOSE: The aim of the study was to create novel mucoadhesive drug delivery systems by incorporating amphiphilic hydrophobically modified, thiolated and preactivated polymers (preactivated thiomers) into self-emulsifying drug delivery systems (SEDDS). METHODS: L-Cysteine methyl ester was covalently attached to the polymeric backbone of Pemulen TR-2 and preactivated using 2-mercaptonicotinic acid (2-MNA). These thiomers were incorporated in a concentration of 0...
March 10, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28224392/investigation-of-need-of-natural-bioenhancer-for-a-metabolism-susceptible-drug-raloxifene-in-a-designed-self-emulsifying-drug-delivery-system
#11
Poonam Singh Thakur, Narinder Singh, Abhay T Sangamwar, Arvind Kumar Bansal
Bioenhancers can increase the bioavailability of metabolism susceptible drugs. The present study was designed to understand the impact of bioenhancer on permeability and bioavailability of a biopharmaceutical drug disposition classification system (BDDCS) class II drug raloxifene (RLX). RLX undergoes extensive first pass metabolism by UGT enzymes in gastrointestinal tract (GIT) and has an oral bioavailability of about 2%. Self-emulsifying drug delivery system (SEDDS) of RLX was developed using a designed approach and this formulation was loaded with reported bioenhancers: quercetin and piperine...
February 21, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28216465/increased-intestinal-permeation-and-modulation-of-presystemic-metabolism-of-resveratrol-formulated-into-self-emulsifying-drug-delivery-systems
#12
G Mamadou, C Charrueau, J Dairou, N Limas Nzouzi, B Eto, G Ponchel
Despite various beneficial biological properties, resveratrol lacks therapeutic applications because of poor bioavailability due to variable absorption and extensive metabolism. The present study aims at evaluating the capability of self-emulsifying drug delivery systems (SEDDS) to enhance resveratrol permeation across rat intestine and to modulate its presystemic metabolism. For that purpose, semi-solid (SS) and liquid (L) SEDDS were prepared and dispersed in an aqueous buffer to produce nanoemulsions (NE)...
February 17, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28212981/development-of-solid-sedds-vi-effect-of-precoating-of-neusilin%C3%A2-us2-with-pvp-on-drug-release-from-adsorbed-self-emulsifying-lipid-based-formulations
#13
Suhas G Gumaste, Beatryz O S Freire, Abu T M Serajuddin
Adsorption of lipid-based formulations, which are usually liquid, onto silicas has been extensively investigated in the past decade to convert them into solid dosage forms. There are conflicting reports on the ability of commercially available porous silicas, like Neusilin® US2, to release lipid formulations completely, especially after long-term storage. In this study, the release of a model drug, probucol, from different formulations of medium chain lipids and a surfactant, Kolliphor EL (Cremophor EL) or polysorbate 80, were studied after adsorbing them onto Neusilin® US2...
February 14, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28188875/hydrophobic-ion-pairing-key-to-highly-payloaded-self-emulsifying-peptide-drug-delivery-systems
#14
Janine Griesser, Gergely Hetényi, Michael Moser, Frédéric Demarne, Vincent Jannin, Andreas Bernkop-Schnürch
AIM: The aim of this study was the formation and characterization of various ion pairs of therapeutic peptides with different surfactants in order to reach a high payload in self-emulsifying drug delivering systems (SEDDS). METHODS: Hydrophobic ion pairs (HIP) were formed between the anionic surfactants sodium docusate, dodecylsulfate and oleate and the peptides leuprorelin (LEU), insulin (INS) and desmopressin (DES). The efficiency of HIP formation was evaluated by quantifying the amount of formed complexes, log P value determination in n-octanol/water via HPLC and zeta potential measurements...
February 7, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28137696/storage-stability-of-bivalirudin-hydrophilic-versus-lipophilic-solutions
#15
Ožbej Zupančič, Julia Anita Grießinger, Hung Thanh Lam, Andreas Bernkop-Schnürch
It was the aim of this study to incorporate a model peptide bivalirudin in self-emulsifying drug delivery system (SEDDS) and compare its storage stability with conventional aqueous solutions. Firstly, bivalirudin lipophilicity was increased via hydrophobic ion pairing using anionic or cationic surfactants. The chosen bivalirudin docusate complex (BIV/AOT) was incorporated into SEDDS composed of 40% (w/w) Cremophor EL, 20% (w/w) Capmul PG-8, and 40% (w/w) propylene glycol with a drug payload of 0.20% (w/w)...
January 28, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28024890/assessment-of-cell-viability-and-permeation-enhancement-in-presence-of-lipid-based-self-emulsifying-drug-delivery-systems-using-caco-2-cell-model-polysorbate-80-as-the-surfactant
#16
Pengli Bu, Yue Ji, Silpa Narayanan, Damon Dalrymple, Xingguo Cheng, Abu T M Serajuddin
PURPOSE: Lipid-based self-emulsifying drug delivery systems (SEDDS) are commonly used for solubilizing and enhancing oral bioavailability of poorly water-soluble drugs. However, their effects on viability of intestine epithelial cells and influence on membrane permeation are poorly understood. The present study was undertaken for safety assessment of lipid-based formulations containing medium-chain fatty acid esters as lipids and polysorbate 80 as the surfactant using the Caco-2 in vitro model...
March 1, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27992953/age-related-disparities-in-trauma-center-access-for-severe-head-injuries-following-the-release-of-the-updated-field-triage-guidelines
#17
Thomas J Flottemesch, Susan Raetzman, Kevin C Heslin, Katie Fingar, Rosanna Coffey, Marguerite Barrett, Ernest Moy
OBJECTIVE: In 2006, the American College of Surgeons' Committee on Trauma and the Centers for Disease Control and Prevention released field triage guidelines with special consideration for older adults. Additional considerations for direct transport to a Level I or II trauma center (TC) were added in 2011, reflecting perceived undertriage to TCs for older adults. We examined whether age-based disparities in TC care for severe head injury decreased following introduction of the 2011 revisions...
December 19, 2016: Academic Emergency Medicine: Official Journal of the Society for Academic Emergency Medicine
https://www.readbyqxmd.com/read/27910752/submicron-emulsions-and-their-applications-in-oral-delivery
#18
REVIEW
Veenu Mundada, Mitali Patel, Krutika Sawant
A "submicron emulsion" is an isotropic mixture of drug, lipids, and surfactants, usually with hydrophilic cosolvents and with droplet diameters ranging from 10 to 500 nm. Submicron emulsions are of increasing interest in medicine due to their kinetic stability, high solubilizing capacity, and tiny globule size. Because of these properties, they have been applied in various fields, such as personal care, cosmetics, health care, pharmaceuticals, and agrochemicals. Submicron emulsions are by far the most advanced nanoparticulate systems for the systemic delivery of biologically active agents for controlled drug delivery and targeting...
2016: Critical Reviews in Therapeutic Drug Carrier Systems
https://www.readbyqxmd.com/read/27907978/comparison-of-the-single-dose-pharmacokinetics-pharmacodynamics-and-safety-of-two-novel-oral-formulations-of-dimethandrolone-undecanoate-dmau-a-potential-oral-male-contraceptive
#19
R Ayoub, S T Page, R S Swerdloff, P Y Liu, J K Amory, A Leung, L Hull, D Blithe, A Christy, J H Chao, W J Bremner, C Wang
Dimethandrolone (DMA, 7α,11β-dimethyl-19-nortestosterone) has both androgenic and progestational activities, ideal properties for a male hormonal contraceptive. In vivo, dimethandrolone undecanoate (DMAU) is hydrolyzed to DMA. We showed previously that single oral doses of DMAU powder in capsule taken with food are well tolerated and effective at suppressing both LH and testosterone (T), but absorption was low. We compared the pharmacokinetics and pharmacodynamics of two new formulations of DMAU, in castor oil and in self-emulsifying drug delivery systems (SEDDS), with the previously tested powder formulation...
March 2017: Andrology
https://www.readbyqxmd.com/read/27890596/monoacyl-phosphatidylcholine-inhibits-the-formation-of-lipid-multilamellar-structures-during-in-vitro-lipolysis-of-self-emulsifying-drug-delivery-systems
#20
Thuy Tran, Scheyla D V S Siqueira, Heinz Amenitsch, Thomas Rades, Anette Müllertz
The colloidal structures formed during lipolysis of self-emulsifying drug delivery systems (SEDDS) might affect the solubilisation and possibly the absorption of drugs. The aim of the current study is to elucidate the structures formed during the in vitro lipolysis of four SEDDS containing medium-chain glycerides and caprylocaproyl polyoxyl-8 glycerides (Labrasol), with or without monoacyl phosphatidylcholine (MAPC). In situ synchrotron small-angle X-ray scattering (SAXS) was combined with ex situ cryogenic transmission electron microscopy (cryo-TEM) and dynamic light scattering (DLS) to elucidate the generated structures...
November 24, 2016: European Journal of Pharmaceutical Sciences
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