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https://www.readbyqxmd.com/read/29156348/development-of-photoprotective-antiphototoxic-and-antiphotogenotoxic-formulations-of-ocular-drugs-with-fluoroquinolones
#1
Anna Zgadzaj, Joanna Kornacka, Anita Jastrzębska, Andrzej Parzonko, Sylwester Sommer, Grzegorz Nałęcz-Jawecki
The development of innovative solutions in photosafety of photolabile pharmaceutical products may help to reduce the adverse effects of these products, caused by light exposure. Providing new data in this area of study is particularly important in case of drugs applied topically on sensitive organs such as eyes. The main goal of this research is to investigate whether two potential excipients, namely: p-coumaric acid and benzophenone-4, affect the photodegradation, phototoxicity and photogenotoxicity of water solutions of four fluoroquinolones: ciprofloxacin, lomefloxacin, fleroxacin and clinafloxacin...
November 9, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/29154900/alternative-manufacturing-concepts-for-solid-oral-dosage-forms-from-drug-nanosuspensions-using-fluid-dispensing-and-forced-drying-technology
#2
Bastian Bonhoeffer, Arno Kwade, Michael Juhnke
Flexible manufacturing technologies for solid oral dosage forms with a continuous adjustability of the manufactured dose strength, are of interest for applications in personalized medicine. This study explored the feasibility of using micro-valve technology for the manufacturing of different solid oral dosage form concepts. Hard gelatin capsules filled with excipients, placebo tablets and polymer films, placed in hard gelatin capsules after drying, were considered as substrates. For each concept a basic understanding of relevant formulation parameters and their impact on dissolution behavior has been established...
November 15, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29151132/safety-of-intrathecal-route-focus-to-methylprednisolone-acetate-depo-medrol-use
#3
REVIEW
Joël Schlatter, David Nguyen, Michèle Zamy, Sofiane Kabiche, Jean-Eudes Fontan, Salvatore Cisternino
PURPOSE: Complications of the intrathecal route may cause potential toxicity related to the medical device and properties of the administered drug and/or excipient. A description of clinical and histological effects of polyethylene glycol and miripirium after Depo-Medrol injection, and the adverse reactions of particulate methylprednisolone acetate was conducted. The safety of the intrathecal route with excipients, label and off-label drugs is discussed. METHODS: A bibliographic search in Medline, Google, and Cochrane database from 1940 to June 2016 was performed...
November 18, 2017: European Spine Journal
https://www.readbyqxmd.com/read/29150845/effect-of-sorbitol-on-the-pharmacokinetic-profile-of-lamivudine-oral-solution-in-adults-an-open-label-randomized-study
#4
Kimberly Adkison, Allen Wolstenholme, Yu Lou, Zhiping Zhang, Amy Eld, Teodora Perger, Harald Vangerow, Katy Hayward, Mark Shaefer, Cynthia McCoig
In children aged ≤4 years, the relative bioavailability of lamivudine oral solution was 37% lower than that of a tablet formulation. An open-label, 4-way crossover study was conducted in healthy adults to evaluate the effect of sorbitol, a common liquid excipient, on the pharmacokinetics of lamivudine oral solution (ClinicalTrials.gov identifier, NCT02634073). Sixteen subjects were randomized to 1 of 4 sequences consisting of 4 doses of lamivudine 300 mg (10 mg/mL) alone or with sorbitol 3.2, 10.2, or 13...
November 18, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29149812/architectures-and-mechanical-properties-of-drugs-and-complexes-of-surface-active-compounds-at-air-water-and-oil-water-interfaces
#5
Dipak K Sarker
BACKGROUND: Drugs can represents a multitude of compounds from proteins and peptides, such as growth hormones and insulin and on to simple organic molecules such as flurbiprofen, ibuprofen and lidocaine. Given the chemical nature of these compounds two features are always present. A portion or portions of the molecule that has little affinity for apolar surfaces and media and the opposite a series of part or one large part that has considerable affinity for hydrophilic, polar or charged media and surfaces...
November 17, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/29148846/preparation-and-evaluation-of-curcumin-loaded-self-assembled-micelles
#6
Lu-Lu Wang, Dan-Dan He, Shu-Xia Wang, Yun-Hao Dai, Jian-Ming Ju, Cheng-Lei Zhao
Objective Curcumin being used to treat various chronic diseases while its poor bioavailability issue limited its wide clinical application as a therapeutic agent. The aim of this work was to prepare curcumin-loaded self-assembled micelles using soluplus and solutol®HS15 (SSCMs) to enhance curcumin's solubility and thus oral bioavailability. Methods Optimum formulation was investigated and the optimized ratio of drugs and excipients was obtained and the SSCMs were prepared via ethanol solvent evaporation method...
November 17, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/29147559/factors-affecting-the-physical-stability-aggregation-of-peptide-therapeutics
#7
REVIEW
Karolina L Zapadka, Frederik J Becher, A L Gomes Dos Santos, Sophie E Jackson
The number of biological therapeutic agents in the clinic and development pipeline has increased dramatically over the last decade and the number will undoubtedly continue to increase in the coming years. Despite this fact, there are considerable challenges in the development, production and formulation of such biologics particularly with respect to their physical stabilities. There are many cases where self-association to form either amorphous aggregates or highly structured fibrillar species limits their use...
December 6, 2017: Interface Focus
https://www.readbyqxmd.com/read/29141152/tm-values-and-unfolded-fraction-can-predict-aggregation-rates-for-gcsf-variant-formulations-but-not-under-predominantly-native-conditions
#8
Mathew J Robinson, Paul Matejtschuk, Adrian F Bristow, Paul A Dalby
Protein engineering and formulation optimisation strategies can be taken to minimise protein aggregation in the biopharmaceutical industry. Short-term stability measures such as the mid-point transition temperature (Tm) for global unfolding provide convenient surrogates for longer-term (eg 2-year) degradation kinetics, with which to optimise formulations on practical time-scales. While successful in some cases, their limitations have not been fully evaluated or understood. Tm values are known to correlate with chemical degradation kinetics for wild-type granulocyte colony stimulating factor (GCSF) at pH 4-5...
November 15, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29140306/chitosan-spray-dried-microparticles-for-controlled-delivery-of-venlafaxine-hydrochloride
#9
Inmaculada Aranaz, Ines Paños, Carlos Peniche, Ángeles Heras, Niuris Acosta
Venlafaxine controlled drug delivery systems using different matrixes have been tested to reduce undesirable side effects in the treatment of depression. The legal status of chitosan (Cs) in Pharmacy has dramatically improved after its acceptance as excipient in several Pharmacopeias and, therefore, there is great interest in pharmaceutical formulations based on this polymer. In this paper, chitosan microcapsules cross-linked with sodium tripolyphosphate (TPP) for oral delivery of venlafaxine were formulated using the spray drying technique...
November 15, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29139305/development-of-optimized-self-nanoemulsifying-lyophilized-tablets-snelts-to-improve-finasteride-clinical-pharmacokinetic-behavior
#10
Tarek A Ahmed, Khalid M El-Say, Khaled M Hosny, Bader M Aljaeid
OBJECTIVE: Preparation of an optimized finasteride (FSD) lyophilized tablets loaded with self-nanoemulsifying drug delivery system (SNEDDS). SIGNIFICANCE: Enhance FSD bioavailability in male pattern baldness and benign prostatic hyperplasia. METHODS: Two-step optimization was implemented to achieve the study goals. First; mixture design was used to develop an optimized SNEDDS through which the effect of cosurfactant number of carbon atoms on SNEDDS particle size and thermodynamic stability has been tested...
November 15, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/29138045/cyclodextrins-structure-physicochemical-properties-and-pharmaceutical-applications
#11
Phatsawee Jansook, Noriko Ogawa, Thorsteinn Loftsson
Since their discovery over 100 years ago cyclodextrins (CDs) have been the subject of numerous scientific publications. In 2016 alone CDs were the subject of over 2200 research articles published in peer-reviewed journals and mentioned in over 2300 patents and patent applications, many of which were on pharmaceutical applications. Natural CDs and their derivatives are used as enabling pharmaceutical excipients that enhance aqueous solubility of poorly soluble drugs, increase drug permeability through biological membranes and improve drug bioavailability...
November 11, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29134579/investigation-on-secondary-structure-perturbations-of-proteins-embedded-in-solid-lipid-matrices-as-a-novel-indicator-of-their-biological-activity-upon-in-vitro-release
#12
Farrukh Zeeshan, Misbah Tabbassum, Lene Jorgensen, Natalie J Medlicott
Protein biologics are prone to conformational changes during formulation development. Limited methods are available for conformational analysis of proteins in solid state and in the presences of formulation excipients. The aim of this study was to investigate the secondary structures of proteins encased in solid lipid matrices as a novel indicator of their stability upon in vitro release. Model proteins namely catalase and lysozyme were incorporated into lipid namely Precirol® AT05 (glycerol palmitostearate, melting point 58°C) at 30% w/w loading using melting and mixing and wet granulation methods...
October 6, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29133233/freeze-drying-from-organic-co-solvent-systems-part-1-thermal-analysis-of-co-solvent-based-placebo-formulations-in-the-frozen-state
#13
Claudia Kunz, Sonja Schuldt-Lieb, Henning Gieseler
The use of co-solvent systems has been demonstrated to shorten lengthy freeze drying processes and improve the solubility and stability of certain active pharmaceutical ingredients. The goal of the present study was to evaluate the suitability of two thermal characterization techniques, differential scanning calorimetry and freeze dry microscopy, to identify an optimal co-solvent system. Binary mixtures of a co-solvent (tert-butanol, dimethyl sulfoxide, 1,4-dioxane, acetone or ethanol) and water were investigated...
November 10, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29133172/measuring-the-emulsification-dynamics-and-stability-of-self-emulsifying-drug-delivery-systems
#14
Teófilo Vasconcelos, Sara Marques, Bruno Sarmento
Self-emulsifying drug delivery systems (SEDDS) are one of the most promising technologies in the drug delivery field, particularly for addressing solubility and bioavailability issues of drugs. The development of these drug carriers excessively relies in visual observations and indirect determinations. The present manuscript intended to describe a method able to measure the emulsification of SEDDS, both micro and nano-emulsions, able to measure the droplet size and to evaluate the physical stability of these formulations...
November 10, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/29132674/food-allergy-management
#15
REVIEW
Carla M Davis, John M Kelso
The management of food allergies requires the cooperation of the food allergic person, physician, family, and social contacts. For children, school management of food allergies is a key component of the overall approach. Recognition of the signs and symptoms of allergic reactions and preparation to administer the appropriate treatment of mild and severe symptoms in the event of accidental exposure is necessary. Avoidance of food allergens is facilitated by label reading and dietary guidance is extremely important to minimize nutritional deficiencies...
February 2018: Immunology and Allergy Clinics of North America
https://www.readbyqxmd.com/read/29132112/raman-spectroscopy-as-a-pat-for-pharmaceutical-blending-advantages-and-disadvantages
#16
Daniela Riolo, Alessandro Piazza, Ciro Cottini, Margherita Serafini, Emilio Lutero, Erika Cuoghi, Lorena Gasparini, Debora Botturi, Iari Gabriel Marino, Irene Aliatis, Danilo Bersani, Pier Paolo Lottici
Raman spectroscopy has been positively evaluated as a tool for the in-line and real-time monitoring of powder blending processes and it has been proved to be effective in the determination of the endpoint of the mixing, showing its potential role as process analytical technology (PAT). The aim of this study is to show advantages and disadvantages of Raman spectroscopy with respect to the most traditional HPLC analysis. The spectroscopic results, obtained directly on raw powders, sampled from a two-axis blender in real case conditions, were compared with the chromatographic data obtained on the same samples...
November 8, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29129865/flow-injection-chemiluminescence-method-for-determination-of-hyoscine-butylbromide-using-silver-iii-as-oxidizing-agent
#17
Manzoor Ahmed, Muhammad Asghar, Mohammad Yaqoob, Nusrat Munawar, Farkhanda Shahid, Mida Asad, Abdul Nabi
Diperiodatoargentate(III) (DPA)/silver(III) complex, [Ag(HIO6)2](5-), in sulfuric acid medium has been used to determine hyoscine butylbromide (HBB) by flow injection (FI) coupled with chemiluminescence (CL) detector. A linear standard curve between the CL intensity and concentration range from 0.005 to 20 mg L(-1) was obtained. The determination coefficient (R(2)), limit of detection (3s × blank), relative standard deviation (RSD) for 0.5 mg L(-1) HBB and analytical throughput were 0.9992 (n = 8), 5 × 10(-4) mg L(-1), 1...
2017: Analytical Sciences: the International Journal of the Japan Society for Analytical Chemistry
https://www.readbyqxmd.com/read/29128750/reduction-of-interferences-in-the-analysis-of-children-s-dimetapp-using-ultraviolet-spectroscopy-data-and-target-factor-analysis
#18
Huggins Z Msimanga, Truong Thach Ho Lam, Nathaniel Latinwo, Mihyang Kristy Song, Newsha Tavakoli
A calibration matrix has been developed and successfully applied to quantify actives in Children's Dimetapp®, a cough mixture whose active components suffer from heavy spectral interference. High-performance liquid chromatography/photodiode array instrument was used to identify the actives and any other UV-detectable excipients that might contribute to interferences. The instrument was also used to obtain reference data on the actives, instead of relying on the manufacturer's claims. Principal component analysis was used during the developmental stages of the calibration matrix to highlight any mismatch between the calibration and sample spectra, making certain that "apples" were not compared with "oranges"...
November 3, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/29128422/ampholytic-starch-excipients-for-high-loaded-drug-formulations-mechanistic-insights
#19
Khalil Sakeer, Pompilia Ispas-Szabo, Nassim Benyerbah, Mircea Alexandru Mateescu
Ampholytic starch derivatives are proposed as a new class of excipients carrying simultaneously anionic carboxymethyl (CM) and cationic aminoethyl (AE) groups on starch (St) polymeric chains. Three different types of derivatives were obtained by using the same reagents and varying only the order of their addition in the reaction medium: in one step method (OS) the two reactants were added simultaneously, whereas in two steps method (TS) either CMSt or AESt were prepared separately in the first step, followed by subsequent addition of the second reactant...
November 8, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29127905/dissolution-studies-of-metamizole-sodium-and-pseudoephedrine-sulphate-dosage-forms-comparison-and-correlation-of-electronic-tongue-results-with-reference-studies
#20
Małgorzata Wesoły, Marcin Zabadaj, Krzysztof Cal, Patrycja Ciosek-Skibińska, Wojciech Wróblewski
This work reports a critical evaluation of the results of the release of active substances (APIs) from novel pharmaceutical formulations provided by an electronic tongue system (ET). Detailed dissolution studies of modified-release granules used in pharmacotherapy containing metamizole sodium and pseudoephedrine sulphate were carried out. The impact of the dissolution-modifying excipients (carmellose sodium and hypromellose) on the dissolution process as well as on the outcomes of the sensor array of ion-selective electrodes was investigated...
November 8, 2017: Journal of Pharmaceutical and Biomedical Analysis
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