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https://www.readbyqxmd.com/read/28088003/the-effect-of-the-antioxidant-on-the-properties-of-thiolated-poly-aspartic-acid-polymers-in-aqueous-ocular-formulations
#1
Mária Budai-Szűcs, Gabriella Horvát, Benjámin Gyarmati, Barnabás Áron Szilágyi, András Szilágyi, Szilvia Berkó, Rita Ambrus, Piroska Szabó-Révész, Giuseppina Sandri, Maria Cristina Bonferoni, Carla Caramella, Erzsébet Csányi
Thiolated polymers are a promising new group of excipients, but their stability against atmospheric oxidation has not been investigated in detail, and only a few efforts have been made to improve their stability. The oxidation of the thiol groups in solutions of thiolated polymers may result in a decrease of mucoadhesion and unpredictable in situ gelation. The aims of our work were to study the stability of aqueous solutions of thiolated polymers and the effects of stabilizing agents. We investigated thiolated poly(aspartic acid) polymers stabilized with dithiothreitol, glutathione or acetylcysteine...
January 11, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28087352/engineering-hot-melt-extruded-solid-dispersion-for-controlled-release-of-hydrophilic-drugs
#2
Shuli Zhang, Xuan Meng, Zheng Wang, Aiping Fan, Guocheng Wang, Yanjun Zhao, Yu Tang
It is often challenging to precisely manipulate the release behavior of hydrophilic drugs that is believed to be crucial for a satisfactory therapeutic outcome. The aim of this work was to regulate the dissolution of hydrophilic drug from hot-melt extruded solid dispersion via rational screening of the pore-forming agents. Venlafaxine hydrochloride and Compritol® 888 ATO was selected as the model drug and carrier excipient, respectively. Hydrophilic polyethylene glycol (PEG 6000) and polyvinylpyrolidone (PVP K30) were chosen as the transient pore-forming agents...
January 10, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28079370/substituted-polyesters-by-thiol-ene-modification-rapid-diversification-for-therapeutic-protein-stabilization
#3
Emma M Pelegri-O'Day, Samantha J Paluck, Heather D Maynard
Many proteins, especially those used as therapeutics, are unstable to storage and shipping temperatures, leading to increased costs in research and industry. Therefore, the design and synthesis of novel stabilizers is an important area of investigation. Herein we report new degradable polymers that stabilize proteins to environmental stressors such as refrigeration and elevated temperature. Specifically, polycaprolactones with different pendant groups were synthesized and surveyed for their ability to stabilize an important therapeutic protein to storage and shipping conditions...
January 12, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28078080/three-cases-of-anaphylaxis-following-injection-of-a-depot-corticosteroid-with-evidence-of-ige-sensitization-to-macrogols-rather-than-the-active-steroid
#4
Nicolaj Brandt, Lene H Garvey, Ulla Bindslev-Jensen, Henrik Fomsgaard Kjaer, Carsten Bindslev-Jensen, Charlotte G Mortz
We present three cases with anaphylaxis after injection of a depot corticosteroid. First, the steroid was suspected as the elicitor, but after evaluation the excipient macrogol was found to be the elicitor. One of the patients had reactions to several unrelated drugs. Increased awareness of anaphylaxis to excipients such as macrogols is needed, especially when allergy tests for the active drug is negative and in patients with a history of repeated anaphylaxis to seemingly unrelated drugs. To establish the correct diagnosis it is important to test with the exact formulation of the culprit drug, as well as all the ingredients including excipients...
2017: Clinical and Translational Allergy
https://www.readbyqxmd.com/read/28075379/veterinary-compounding-regulation-challenges-and-resources
#5
REVIEW
Gigi Davidson
The spectrum of therapeutic need in veterinary medicine is large, and the availability of approved drug products for all veterinary species and indications is relatively small. For this reason, extemporaneous preparation, or compounding, of drugs is commonly employed to provide veterinary medical therapies. The scope of veterinary compounding is broad and focused primarily on meeting the therapeutic needs of companion animals and not food-producing animals in order to avoid human exposure to drug residues. As beneficial as compounded medical therapies may be to animal patients, these therapies are not without risks, and serious adverse events may occur from poor quality compounds or excipients that are uniquely toxic when administered to a given species...
January 10, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/28075194/aerosol-drug-delivery-during-noninvasive-positive-pressure-ventilation-effects-of-intersubject-variability-and-excipient-enhanced-growth
#6
Ross L Walenga, P Worth Longest, Anubhav Kaviratna, Michael Hindle
BACKGROUND: Nebulized aerosol drug delivery during the administration of noninvasive positive pressure ventilation (NPPV) is commonly implemented. While studies have shown improved patient outcomes for this therapeutic approach, aerosol delivery efficiency is reported to be low with high variability in lung-deposited dose. Excipient enhanced growth (EEG) aerosol delivery is a newly proposed technique that may improve drug delivery efficiency and reduce intersubject aerosol delivery variability when coupled with NPPV...
January 11, 2017: Journal of Aerosol Medicine and Pulmonary Drug Delivery
https://www.readbyqxmd.com/read/28070851/development-of-a-sustained-antiplaque-and-antimicrobial-chewing-gum-of-a-decapeptide
#7
Abeer M Al-Ghananeem, Kai P Leung, Jabar Faraj, Patrick P DeLuca
The objective of this paper was to design a chewing gum formulation delivery system in situations where typical dental hygiene practice is not practical. Thus, an analog of decapeptide KSL (KSL-W), known to possess antimicrobial and antiplaque activity, was incorporated into a chewing gum formulation containing cetylpyridinium chloride (CPC). The effect of the excipients, xylitol, and peppermint oil on active ingredients in vitro release was also assessed. Gum formulations were prepared with different excipient parameters, including heating xylitol and gum base at 65 or 85°C, using ground and unground xylitol, and the addition of 1...
January 9, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28067579/hot-melt-extrusion-microencapsulation-of-quercetin-for-taste-masking
#8
Chia Miang Khor, Wai Kiong Ng, Parijat Kanaujia, Kok Ping Chan, Yuancai Dong
Besides its poor dissolution rate, the bitterness of quercetin also poses a challenge for further development. Using carnauba wax, shellac or zein as the shell-forming excipient, this work aimed to microencapsulate quercetin by hot-melt extrusion for taste-masking. In comparison with non-encapsulated quercetin, the microencapsulated powders exhibited significantly reduced dissolution in the simulated salivary pH 6.8 medium indicative of their potentially good taste-masking efficiency in the order of zein > carnauba wax > shellac...
January 9, 2017: Journal of Microencapsulation
https://www.readbyqxmd.com/read/28061966/new-treatments-for-hair-loss
#9
S Vañó-Galván, F Camacho
The treatment of hair loss is an important part of clinical dermatology given the prevalence of the problem and great impact on patients' quality of life. Many new treatments have been introduced in recent years. This review summarizes the main ones in 4 groups: a) For androgenetic alopecia, we discuss new excipients for oral minoxidil, dutasteride, and finasteride as well as new forms of topical application; prostaglandin agonists and antagonists; low-level laser therapy; and regenerative medicine with Wnt signaling activators and stem cell therapy...
January 3, 2017: Actas Dermo-sifiliográficas
https://www.readbyqxmd.com/read/28060709/the-enhancement-of-nasal-drug-absorption-from-powder-formulations-by-the-addition-of-sodium-carboxymethyl-cellulose
#10
Akiko Tanaka, Tomoyuki Furubayashi, Hitomi Yamasaki, Katsuko Takano, Mayuko Kawakami, Shunsuke Kimura, Daisuke Inoue, Hidemasa Katsumi, Toshiyasu Sakane, Akira Yamamoto
For nasal drug absorption, powder formulations can be expected to provide many advantages. The first aim of this study was to examine drug absorption following nasal administration of powder formulations in rats. Pharmaceutical excipients are typically added to most powder formulations. The second aim was to investigate the change in nasal drug absorption of powder formulations in the presence of sodium carboxymethyl cellulose (CMC-Na). Model drugs used were norfloxacin (NFX), warfarin (WF), and piroxicam (PXC)...
January 4, 2017: IEEE Transactions on Nanobioscience
https://www.readbyqxmd.com/read/28056749/development-and-evaluation-of-naproxen-sodium-gel-using-piper-cubeba-for-enhanced-transdermal-drug-delivery-and-therapeutic-facilitation
#11
Sunetra Kaustubh Patwardhan, Manohar J Patil, Anbazhagan Sockalingam
BACKGROUND: The absorption of drug through skin avoids many side effects of oral route like gastric irritation, nausea, systemic toxicity etc and thus improves patient compliance. Naproxen sodium (NPRS) is one of the potent NSAID agents. OBJECTIVE: The present study was aimed to develop and evaluate the gel formulation containing NPRS for transdermal drug delivery reducing the side effects and improving patient compliance. The patents on topical delivery of NSAIDS (US 9012402 B1, US 9072659 B2, US 20150258196 A1) and patents indicating use of herbal penetration enhancers (US 20100273746A1, WO 2005009510 A2, US 6004969 A) helped in selecting the drug, excipients...
January 5, 2017: Recent Patents on Drug Delivery & Formulation
https://www.readbyqxmd.com/read/28053581/optimization-of-formulation-and-processing-of-moringa-oleifera-and-spirulina-complex-tablets
#12
Yi Zheng, Fan Zhu, Dan Lin, Jun Wu, Yichao Zhou, Bohn Mark
Objective: To prepare a more comprehensive nutrition, more balanced proportion of natural nutritional supplement tablets with Moringa oleifera leaves and spirulina the two nutrients which have complementary natural food ingredients. Method: On the basis of research M. oleifera leaves with spirulina nutrient composition was determined on M. oleifera leaves and spirulina ratio of raw materials, and the choice of microcrystalline cellulose, sodium salt of caboxy methyl cellulose(CMC),magnesium stearate excipient, through single factor and orthogonal experiment, selecting the best formula tablets prepared by powder direct compression technology, for preparation of M...
January 2017: Saudi Journal of Biological Sciences
https://www.readbyqxmd.com/read/28050711/torsemide-fast-dissolving-tablets-development-optimization-using-box-bhenken-design-and-response-surface-methodology-in-vitro-characterization-and-pharmacokinetic-assessment
#13
Ahmed A El-Shenawy, Mahmoud M Ahmed, Heba F Mansour, Saleh Abd El Rasoul
The present study planed to develop new fast dissolving tablets (FDTs) of torsemide. Solid dispersions (SDs) of torsemide and sorbitol (3:1) or polyvinylpyrrolidone (PVP) k25 were prepared. The prepared SDs were evaluated for in-vitro dissolution. Fourier transform infrared spectroscopy and differential scanning calorimetry for SDs revealed no drug/excipient interactions and transformation of torsemide to the amorphous form. Torsemide/sorbitol SD was selected for formulation of torsemide FDTs by direct compression method...
January 3, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28044441/trehalose-glycopolymer-enhances-both-solution-stability-and-pharmacokinetics-of-a-therapeutic-protein
#14
Yang Liu, Juneyoung Lee, Kathryn M Mansfield, Jeong Hoon Ko, Sahar Sallam, Chrys Wesdemiotis, Heather D Maynard
Biocompatible polymers such as poly(ethylene glycol) (PEG) have been successfully conjugated to therapeutic proteins to enhance their pharmacokinetics. However, many of these polymers, including PEG, only improve the in vivo lifetimes and do not protect proteins against inactivation during storage and transportation. Herein, we report a polymer with trehalose side chains (PolyProtek) that is capable of improving both the external stability and the in vivo plasma half-life of a therapeutic protein. Insulin was employed as a model biologic, and high performance liquid chromatography and dynamic light scattering confirmed that addition of trehalose glycopolymer as an excipient or covalent conjugation prevented thermal or agitation-induced aggregation of insulin...
January 3, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28043133/long-term-physical-stability-of-pvp-and-pvpva-amorphous-solid-dispersions
#15
Kristin Lehmkemper, Samuel O Kyeremateng, Oliver Heinzerling, Matthias Degenhardt, Gabriele Sadowski
The preparation of amorphous solid dispersion (ASD) formulations is a promising strategy to improve the bioavailability of an active pharmaceutical ingredient (API). By dissolving the API in a polymer it is stabilized in its amorphous form, which usually shows higher water solubility than its crystalline counterpart. To prevent recrystallization, the long-term physical stability of ASD formulations is of big interest. In this work, the solubility of the APIs acetaminophen and naproxen in the excipient polymers poly(vinylpyrrolidone) (PVP K25) and poly(vinylpyrrolidone-co-vinyl acetate) (PVPVA64) was calculated with three models: the Perturbed-Chain Statistical Associating Fluid Theory (PC-SAFT), the Flory-Huggins model (FH), and an empirical model (Kyeremateng et al...
January 3, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28042099/analgesic-and-anti-inflammatory-controlled-released-injectable-microemulsion-pseudo-ternary-phase-diagrams-in-vitro-ex-vivo-and-in-vivo-evaluation
#16
Isabel Pineros, Karla Slowing, Dolores R Serrano, Esther de Pablo, Maria Paloma Ballesteros
PURPOSE: Development of analgesic and anti-inflammatory controlled-released injectable microemulsions utilising lysine clonixinate (LC) as model drug and generally regarded as safe (GRAS) excipients. METHODS: Different microemulsions were optimised through pseudo-ternary phase diagrams and characterised measuring droplet size, viscosity, ex vivo haemolytic activity and in vitro drug release. The anti-inflammatory and analgesic activity was tested in mice (Hot plate test) and rats (Carrageenan-induced paw edema test) respectively and their activity was compared to an aqueous solution of LC salt...
December 29, 2016: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28041969/needle-free-injection-of-vesicular-phospholipid-gels-a-novel-approach-to-overcome-an-administration-hurdle-for-semisolid-depot-systems
#17
Michaela Breitsamer, Gerhard Winter
Vesicular phospholipid gels (VPGs) are depot formulations for the sustained release of drugs which are characterized by a high amount of phospholipids in the formulation. They consist of physiological excipients only and therefore display high biocompatibility. Their manufacture is simple, cheap, solvent free and ideal for the processing of proteins and peptides because of the low stress on the molecule e.g. by elevated temperatures. One major hurdle of VPGs is their high viscosity which makes them hard to almost impossible to inject with conventional, thin needles used for subcutaneous administration...
December 29, 2016: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28039572/formulation-and-optimization-of-multiparticulate-drug-delivery-system-approach-for-high-drug-loading
#18
Neha Shah, Tejal Mehta, Mukesh Gohel
The aim of the present work was to develop and optimize multiparticulate formulation viz. pellets of naproxen by employing QbD and risk assessment approach. Mixture design with extreme vertices was applied to the formulation with high loading of drug (about 90%) and extrusion-spheronization as a process for manufacturing pellets. Independent variables chosen were level of microcrystalline cellulose (MCC)-X 1, polyvinylpyrrolidone K-90 (PVP K-90)-X 2, croscarmellose sodium (CCS)-X 3, and polacrilin potassium (PP)-X 4...
December 30, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28035628/effects-of-histidine-and-sucrose-on-the-biophysical-properties-of-a-monoclonal-antibody
#19
Youngbin Baek, Nripen Singh, Abhiram Arunkumar, Andrew L Zydney
PURPOSE: Histidine is a commonly used buffer in formulation of monoclonal antibodies (mAb), often with excipients like sucrose. The objective of this study was to examine the effects of both histidine and sucrose on the biophysical characteristics of a mAb. METHODS: The hydrodynamic radius of the mAb was determined by dynamic light scattering and confirmed by size exclusion chromatography. Data were also obtained for the osmotic virial coefficients (from osmotic pressure measurements), the solution viscosity, and the mAb thermal stability (using differential scanning calorimetry) at selected conditions...
December 29, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/28035611/the-in-vitro-vivo-evaluation-of-prepared-gastric-floating-tablets-of-berberine-hydrochloride
#20
Jun Ji, Xin He, Xiao-Lin Yang, Wen-Juan Du, Cheng-Long Cui, Ling Wang, Xue Wang, Chun-Feng Zhang, Chang-Run Guo
Currently available antiulcer drugs suffered from serious side effects which limited their uses and prompted the need for a safe and efficient new antiulcer agent. The objective of this project work was to retain the drug in the stomach for better antiulcer activity and less side effects. Hence, the aim of our present work was to prepare a gastric floating tablet of Berberine hydrochloride (Ber) with suitable in vitro/vivo properties. In this study, different Ber gastric floating tablets were prepared by simple direct compression using various amounts of HPMCK15M and Carbopol 971PNF combined with other tablet excipients...
December 29, 2016: AAPS PharmSciTech
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