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https://www.readbyqxmd.com/read/29330817/effect-of-levofloxacin-pazufloxacin-enrofloxacin-and-meloxicam-on-the-immunolocalization-of-abcg-2-transporter-protein-in-rabbit-retina
#1
Adil Mehraj Khan, Satyavan Rampal, Naresh Kumar Sood
Adenosine triphosphate-binding cassette (ABC) sub-family G member-2 (ABCG-2) is a transporter protein, implicated for multi-drug efflux from tissues. This study evaluated the effect of fluoroquinolones; levofloxacin, pazufloxacin and enrofloxacin, and non-steroidal anti-inflammatory drug, meloxicam; on the immunolocalization of ABCG-2 transporter protein of rabbit retinas. Thirty-two male rabbits were randomly divided in to eight groups. Control group was gavaged, 2% benzyl alcohol in 5% dextrose since these chemicals are excipients of the drug preparations used in the treatment groups of this study...
January 12, 2018: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/29328661/investigation-of-drug-excipient-interactions-in-biclotymol-amorphous-solid-dispersions
#2
Benjamin Schammé, Nicolas Couvrat, Vincent Tognetti, Laurent Delbreilh, Valérie Dupray, Eric Dargent, Gérard Coquerel
The effect of low molecular weight excipients on drug-excipient interactions, molecular mobility and propensity to recrystallization of an amorphous active pharmaceutical ingredient is investigated. Two structurally related excipients (α-Pentaacetylglucose and β-Pentaacetylglucose), five different drug:excipient ratios (1:5, 1:2, 1:1, 2:1 and 5:1, w/w) and three different solid state characterization tools (Differential Scanning Calorimetry, X-Ray Powder Diffraction and Dielectric Relaxation Spectroscopy) were selected for the present research...
January 12, 2018: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29327746/silk-nanoparticles-from-inert-supports-to-bioactive-natural-carriers-for-drug-delivery
#3
REVIEW
Barbara Crivelli, Sara Perteghella, Elia Bari, Milena Sorrenti, Giuseppe Tripodo, Theodora Chlapanidas, Maria Luisa Torre
Silk proteins have been studied and employed for the production of drug delivery (nano)systems. They show excellent biocompatibility, controllable biodegradability and non-immunogenicity and, if needed, their properties can be modulated by blending with other polymers. Silk fibroin (SF), which forms the inner core of silk, is a (bio)material officially recognized by the Food and Drug Administration for human applications. Conversely, the potential of silk sericin (SS), which forms the external shell of silk, could still be considered under evaluation...
January 12, 2018: Soft Matter
https://www.readbyqxmd.com/read/29323612/pharmacokinetic-analysis-of-intraocular-penetration-of-latanoprost-solutions-with-different-preservatives-in-human-eyes
#4
Yuko Sekine, Marie Shimada, Shoko Satake, Masato Okubo, Akihiro Hisaka, Tadashi Hara, Megumi Honjo, Makoto Aihara
OBJECTIVES: To investigate the effect of excipients on latanoprost penetration into the aqueous humor with clinically available 6 products with different solutions mainly in the types and concentrations of preservatives. METHODS: In 363 patients with cataracts, we instilled 1 latanoprost drop in 1 eye before surgery. The drop was randomly selected by brand name product (A) and 5 generic products (B-F) composed with different excipients. B contains similar excipients to A...
January 11, 2018: Journal of Ocular Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29319295/advances-in-polymer-design-for-enhancing-oral-drug-solubility-and-delivery
#5
Jeffrey M Ting, William W Porter, Jodi M Mecca, Frank S Bates, Theresa M Reineke
Synthetic polymers have enabled amorphous solid dispersions (ASDs) to emerge as an oral delivery strategy for overcoming poor drug solubility in aqueous environments. Modern ASD products noninvasively treat a range of chronic diseases (for example, hepatitis C, cystic fibrosis, and HIV). In such formulations, polymeric carriers generate and maintain drug supersaturation upon dissolution, increasing the apparent drug solubility to enhance gastrointestinal barrier absorption and oral bioavailability. In this Review, we outline several approaches in designing polymeric excipients to drive interactions with active pharmaceutical ingredients (APIs) in spray-dried ASDs, highlighting polymer-drug formulation guidelines from industrial and academic perspectives...
January 10, 2018: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/29317921/baseline-knowledge-of-potential-pet-toxins-a-survey-of-pharmacists
#6
Natalie W Young, Kenneth D Royal, Gigi S Davidson
Background: Consumer expenditures on their family pets are rapidly increasing, part of which can be attributed to prescription and OTC medications. In turn, community pharmacies are seeking and receiving an increased number of prescriptions for animals. Community pharmacists' ability to safely care for animal patients is relatively unexplored. Human medications, their normal dosing and even medication excipients could be lethal in some animal patients. Objective: The overarching objective of this study was to assess pharmacists' baseline knowledge of potential pet poisons...
October 2017: Pharmacy Practice
https://www.readbyqxmd.com/read/29317226/oral-delivery-of-highly-lipophilic-poorly-water-soluble-drugs-self-emulsifying-drug-delivery-systems-sedds-to-improve-oral-absorption-and-enable-high-dose-toxicology-studies-of-a-cetp-inhibitor-in-preclinical-species
#7
Xue-Qing Chen, Theresa Ziemba, Christine Huang, Ming Chang, Carrie Xu, Jennifer X Qiao, Tammy C Wang, Heather J Finlay, Mark E Salvati, Leonard P Adam, Olafur Gudmundsson, Michael J Hageman
BMS-A is a highly lipophilic compound (clogP 10.5) with poor aqueous solubility (< 0.0001 mg/mL at pH 6.5). The compound exhibits low oral exposure when dosed as cosolvent solution formulations. The purpose of this study was to evaluate lipid-based formulations for enabling high-dose toxicology studies and enhancing toxicology margins of BMS-A in pre-GLP studies in non-rodent species. The solubility of BMS-A was screened in lipid and cosolvent/surfactant excipients and prototype formulations were developed...
January 6, 2018: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29315014/contribution-to-the-rheological-testing-of-pharmaceutical-semisolids
#8
B Siska, E Snejdrova, I Machac, P Dolecek, J Martiska
Rheological behaviour of pharmaceutical semisolid preparations significantly affects manufacturing process, administration, stability, homogeneity of incorporated drug, accuracy of dosing, adhesion in the place of application, drug release, and resulting therapeutic effect of the product. We performed test of consistency by penetrometry, rotational, oscillation and creep tests, and squeeze and tack tests of model samples to introduce methods suitable for characterization and comparison of semisolids in practice...
January 9, 2018: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/29313693/poloxamer-407-tpgs-mixed-micelles-as-promising-carriers-for-cyclosporine-ocular-delivery
#9
Maria Aurora Grimaudo, Silvia Pescina, Cristina Padula, Patrizia Santi, Angel Concheiro, Carmen Alvarez-Lorenzo, Sara Nicoli
Cyclosporine is an immunosuppressant agent approved for the treatment of dry eye disease and used off-label for other ocular pathologies. Its formulation and ocular bioavailability is a real challenge due to the large molecular weight (1.2 kDa), high lipophilicity and low water solubility. The aim of the work was to develop an aqueous micellar formulation for an efficient cyclosporine delivery to the ocular tissues, using a water soluble derivative of vitamin E (TPGS: d-alpha tocopheryl polyethylene glycol 1000 succinate) and a poloxamer (poloxamer 407) as excipients...
January 9, 2018: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29310491/influence-of-processing-methods-on-physico-mechanical-properties-of-ibuprofen-hpc-ssl-formulation
#10
Kaushalendra Chaturvedi, Bhavin Y Gajera, Ting Xu, Harsh Shah, Rutesh H Dave
The objective of the present study was to investigate the influence of processing methods on the physical and mechanical properties of formulations containing Ibuprofen and HPC-SSL. The powder blends, containing Ibuprofen and HPC-SSL in ratio of 9:0.5, were processed using melt granulation (MG) by hot melt extrusion (HME) and wet granulation (WG) by high shear mixer. Formulated granules and powder blends were compressed into round flat faced tablets using Riva Piccola tablet press. Differential scanning calorimetry (DSC) and X-ray powder diffraction (XRPD) studies proved that granulation process did not significantly alter the crystallinity of Ibuprofen, however particle density and flow properties were significantly improved...
January 9, 2018: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/29305984/3d-printed-tablets-with-internal-scaffold-structure-using-ethyl-cellulose-to-achieve-sustained-ibuprofen-release
#11
Yan Yang, Huihui Wang, Haichao Li, Zhimin Ou, Gensheng Yang
The object of this study is to prepare and evaluate tablets with predesigned internal scaffold structure using 3D printing to achieve sustained drug release. Model drug (ibuprofen) and sustained release material (ethyl cellulose), together with other excipients, were firstly mixed and extruded into filaments by hot melt extrusion. Then these obtained filaments were printed into tablets by fused deposition modeling. The tablets printability and drug release behavior were influenced by drug content, release modifiers, printing parameters and modeling...
January 3, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29305981/the-effect-of-formulation-additives-on-in-vitro-dissolution-absorption-profile-and-in-vivo-bioavailability-of-telmisartan-from-brand-and-generic-formulations
#12
Enikő Borbás, Zsombor K Nagy, Brigitta Nagy, Attila Balogh, Balázs Farkas, Oksana Tsinman, Konstantin Tsinman, Bálint Sinkó
In this study, brand and four generic formulations of telmisartan, an antihypertensive drug, were used in in vitro simultaneous dissolution-absorption, investigating the effect of different formulation additives on dissolution and on absorption through an artificial membrane. The in vitro test was found to be sensitive enough to show even small differences between brand and generic formulations caused by the use of different excipients. By only changing the type of filler from sorbitol to mannitol in the formulation, the flux through the membrane was reduced by approximately 10%...
January 3, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29305717/influence-of-low-molecular-weight-excipients-on-the-phase-behavior-of-pvpva64-amorphous-solid-dispersions
#13
Kristin Lehmkemper, Samuel O Kyeremateng, Matthias Degenhardt, Gabriele Sadowski
PURPOSE: The oral bioavailability of poorly water-soluble active pharmaceutical ingredients (APIs) can be improved by the preparation of amorphous solid dispersions (ASDs) where the API is dissolved in polymeric excipients. Desired properties of such ASDs like storage stability, dissolution behavior, and processability can be optimized by additional excipients. In this work, the influence of so-called low-molecular-weight excipients (LMWEs) on the phase behavior of ASDs was investigated...
January 5, 2018: Pharmaceutical Research
https://www.readbyqxmd.com/read/29305142/oral-bioavailability-enhancement-of-%C3%AE-lapachone-a-poorly-soluble-fast-crystallizer-by-cocrystal-amorphous-solid-dispersion-and-crystalline-solid-dispersion
#14
Chengyu Liu, Zhengsheng Liu, Yuejie Chen, Zhen Chen, Huijun Chen, Yipshu Pui Feng Qian
The aim of this paper was to compare the in vitro dissolution and in vivo bioavailability of three solubility enhancement technologies for β-lapachone (LPC), a poorly water soluble compound with extremely high crystallization propensity. LPC cocrystal was prepared by co-grinding LPC with resorcinol. LPC crystalline and amorphous solid dispersions (CSD and ASD) were obtained by spray drying with Poloxamer 188 and HPMC-AS, respectively. The cocrystal structure was solved by single crystal x-ray diffraction. All formulations were characterized by WAXRD, DSC, POM and SEM...
January 2, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/29304023/insulin-inclusion-into-a-tragacanth-hydrogel-an-oral-delivery-system-for-insulin
#15
Mokhamad Nur, Todor Vasiljevic
Nanoparticles or microparticles created by physical complexation between two polyelectrolytes may have a prospective use as an excipient for oral insulin administration. Natural polymers such as tragacanth, alginate, dextran, pullulan, hyaluronic acid, gelatin and chitosan can be potential candidates for this purpose. In this research, insulin particles were prepared by the inclusion of insulin into a tragacanth hydrogel. The effect of the pH and concentration relationship involving polyelectrolytes offering individual particle size and zeta potential was assessed by zetasizer and scanning electron microscopy (SEM)...
January 5, 2018: Materials
https://www.readbyqxmd.com/read/29303081/a-new-approach-to-enhance-the-solubility-of-famotidine-tablet-by-using-naturally-isolated-pear-starch
#16
Anjali Kushwaha, Manjul Pratap Singh
PURPOSE- The solubility of drug is affected by various excipients presents in formulation. In case of tablets the role of binders is very important for solubility of dosage form as well as drug. Thus in following study an attempt is made to improve the solubility and dissolution rate of a drug by use of natural excipients. The starch was extracted from the Pear fruits and used as a binder in different concentrations, in famotidine tablets and evaluate them. There are some recent patents on modified starch (WO2011002730A1), directly compressed starch (US6455069B1), pre-compacted starches (US4072535A), which helped in my study...
January 4, 2018: Recent Patents on Drug Delivery & Formulation
https://www.readbyqxmd.com/read/29300842/validated-stability-indicating-methods-for-determination-of-mometasone-furoate-in-presence-of-its-alkaline-degradation-product
#17
Rania A Sayed, Manal M El-Masri, Wafaa S Hassan, Magda Y El-Mammli, Abadalla Shalaby
Two novel stability-indicating TLC densitometric and chemometric methods were developed for the determination of mometasone furoate (MF) in the presence of its alkaline degradation product (MF Deg). The developed TLC densitometric method (Method A) is based on the quantitative densitometric separation of MF from its alkaline degradation product on silica gel 60 F254 and measurement of the bands at 250 nm. The separation was carried out using hexane-chloroform-methanol-acetonitrile (6:6:1:0.3, by volume) as a developing system...
December 29, 2017: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/29300841/determination-of-dicyclohexylamine-in-beeswax-by-aqueous-normal-phase-liquid-chromatography-coupled-with-tandem-mass-spectrometry
#18
Thomas S Thompson, Johan P van den Heever, Stephen F Pernal
Dicyclohexylamine (DCH) is an excipient present in commercial formulations of fumagillin (Fumagilin-B® and Fumidil-B®), an antibiotic which is employed in apiculture for the control of nosema disease. DCH has been demonstrated to be stable in harvested honey; however, its fate in the beehive has not been investigated. In this study, DCH residues were determined in beeswax samples collected from brood chambers and honey supers from various apiaries throughout Alberta. The determination of DCH was performed using a simple extraction procedure followed by low-temperature cleanup and finally analysis with aqueous normal phase liquid chromatography-electrospray ionization tandem mass spectrometry...
December 29, 2017: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/29290821/recent-advances-in-the-application-of-vitamin-e-tpgs-for-drug-delivery
#19
REVIEW
Conglian Yang, Tingting Wu, Yan Qi, Zhiping Zhang
D-ɑ-tocopheryl polyethylene glycol succinate (Vitamin E TPGS or TPGS) has been approved by FDA as a safe adjuvant and widely used in drug delivery systems. The biological and physicochemical properties of TPGS provide multiple advantages for its applications in drug delivery like high biocompatibility, enhancement of drug solubility, improvement of drug permeation and selective antitumor activity. Notably, TPGS can inhibit the activity of ATP dependent P-glycoprotein and act as a potent excipient for overcoming multi-drug resistance (MDR) in tumor...
2018: Theranostics
https://www.readbyqxmd.com/read/29289516/probing-the-particulate-microstructure-of-the-aerodynamic-particle-size-distribution-of-dry-powder-inhaler-combination-products
#20
M W Jetzer, B D Morrical, M Schneider, S Edge, G Imanidis
The in vitro aerosol performance of two combination dry powder inhaler (DPI) products, Foster® NEXThaler® and Seretide® Diskus® were investigated with single particle aerosol mass spectrometry (SPAMS). The in-vitro pharmaceutical performance is markedly different for both inhalers. Foster® NEXThaler® generates a higher fine particle fraction (FPF <5 μm) and a much higher relative extra fine particle fraction (eFPF <2 μm). In terms of the composition of the aerodynamic particle size distribution (APSD), it could be verified with SPAMS that overall Foster® NEXThaler® emits a significantly higher number of fine and extra fine particles with a median aerodynamic diameter (MAD) of 2...
December 28, 2017: International Journal of Pharmaceutics
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