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Eduardo Galdón, Marta Casas, Manuel Gayango, Isidoro Caraballo
The deep understanding of products and processes has become a requirement for pharmaceutical industries to follow the Quality by Design principles promoted by the regulatory authorities. With this aim, SeDeM expert system was developed as a useful preformulation tool to predict the likelihood to process drugs and excipients through direct compression. SeDeM system is a step forward in the rational development of a formulation, allowing the normalisation of the rheological parameters and the identification of the weaknesses and strengths of a powder or a powder blend...
October 18, 2016: European Journal of Pharmaceutics and Biopharmaceutics
Yu Sun, Jesper Østergaard
Efficient drug delivery is dependent on the drug substance dissolving in the body fluids, being released from dosage forms and transported to the site of action. A fundamental understanding of the interplay between the physicochemical properties of the active compound and pharmaceutical excipients defining formulation behavior after exposure to the aqueous environments and pharmaceutical performance is critical in pharmaceutical development, manufacturing and quality control of drugs. UV imaging has been explored as a tool for qualitative and quantitative characterization of drug dissolution and release with the characteristic feature of providing real-time visualization of the solution phase drug transport in the vicinity of the formulation...
October 20, 2016: Pharmaceutical Research
Kambham Venkateswarlu, Jami Komala Preethi, Kothapalli Bonnoth Chandrasekhar
Purpose: The aim of present study was to improve the dissolution rate of poorly soluble drug Loperamide (LPM) by liquisolid compact technique. Methods: Liquisolid compacts of LPM were prepared using Propylene glycol (PG) as a solvent, Avicel pH 102 as carrier, Aerosil as coating material and Sodium Starch Glycolate (SSG) as superdisintegrant. Interactions between the drug and excipients were examined by Fourier Transform Infrared (FTIR) spectroscopy. The dissolution studies for LPM liquisolid formulation, marketed product and pure drug were carried out in pH 1...
September 2016: Advanced Pharmaceutical Bulletin
Carlos Cardoso-Palacios, Ingela Lanekoff
Counterfeit pharmaceutical drugs imply an increasing threat to the global public health. It is necessary to have systems to control the products that reach the market and to detect falsified medicines. In this work, molecules in several pharmaceutical tablets were directly analyzed using nanospray desorption electrospray ionization mass spectrometry (nano-DESI MS). Nano-DESI is an ambient surface sampling technique which enables sampling of molecules directly from the surface of the tablets without any sample pretreatment...
2016: Journal of Analytical Methods in Chemistry
Joaquim Suñer-Carbó, Antonio Boix-Montañés, Lyda Halbaut-Bellowa, Nelvis Velázquez-Carralero, Joanna Zamarbide-Ledesma, Nuria Bozal-de-Febrer, Ana Cristina Calpena-Campmany
Local delivery of imidazolic antifungals is limited by its extreme lipophilicity. Multiple emulsions (ME) are a potential vehicle to enhance the delivery of econazole nitrate (ECN), an antifungal targeted to deep-seated epidermal yeast infections. An 1% ECN hydrophilic ME was compared with a commercial formulation in terms of rheology, droplet size and in vitro antifungal activity against Candida species. Comparative in vitro drug release, human skin permeation and drug retention were investigated using vertical diffusion cells...
October 20, 2016: Mycoses
Hetal Patel, Hiral Patel, Mukesh Gohel, Sanjay Tiwari
Context: Microcrystalline cellulose (MCC) is the most widely used excipient for the production of pellets but it retards the release of poorly water soluble drugs. Objective: The present investigation reports incorporation of camphor, cross carmellose sodium (CCS) and spray dried lactose (SDL) into MCC pellets to enhance the dissolution rate of telmisartan. Materials and methods: A full factorial design (3(2)) was used in the study. Concentration of camphor and CCS was selected as independent variables whereas percentage porosity and percentage drug release at 60 min were selected as dependent variables...
September 2016: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
Muhammad Irfan, Sumeira Rabel, Quratulain Bukhtar, Muhammad Imran Qadir, Farhat Jabeen, Ahmed Khan
Over the past few decades, tendency toward innovative drug delivery systems has majorly increased attempts to ensure efficacy, safety and patient acceptability. As discovery and development of new chemical agents is a complex, expensive and time consuming process, so recent trends are shifting toward designing and developing innovative drug delivery systems for existing drugs. Out of those, drug delivery system being very eminent among pediatrics and geriatrics is orally disintegrating films (ODFs). These fast disintegrating films have superiority over fast disintegrating tablets as the latter are associated with the risks of choking and friability...
September 2016: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
Bożena Karolewicz
In the article, groups of multifunctional polymers used in drug dosage form technology were classified and evaluated. These compounds, in addition to their basic function as excipients, may have additional properties, e.g. stimuli sensitivity, enzyme inhibition, intestinal epithelium penetration enhancement, efflux pump inhibition, taste-masking, pharmacological activity and the ability to interact with enzymes responsible for drug metabolism. While classifying specific groups of multifunctional polymers, special emphasis was placed on the advantages of using them when designing new drug...
September 2016: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
Peter Nash, Johan Vanhoof, Stephen Hall, Udayasankar Arulmani, Rita Tarzynski-Potempa, Kristina Unnebrink, Andrew N Payne, Alfred Cividino
INTRODUCTION: Adalimumab, an anti-tumor necrosis factor antibody, is currently available in a 40 mg/0.8 mL formulation. The objective of this analysis was to evaluate injection site-related pain, safety, and tolerability of a 40 mg/0.4 mL formulation of adalimumab that had fewer excipients, a smaller volume, and a delivery presentation with a smaller gauge needle, versus the current 40 mg/0.8 mL formulation in patients with rheumatoid arthritis (RA). METHODS: Two identically designed, phase 2, randomized, single-blind, two-period crossover studies were conducted in Belgium and the Czech Republic (Study 1) and Australia, Canada, and Germany (Study 2)...
August 18, 2016: Rheumatol Ther
Bryce Chiang, Nitin Venugopal, Henry F Edelhauser, Mark R Prausnitz
The purpose of this work was to determine the effect of injection volume, formulation composition, and time on circumferential spread of particles, small molecules and polymeric formulation excipients in the suprachoroidal space (SCS) after microneedle injection into New Zealand White rabbit eyes ex vivo and in vivo. Microneedle injections of 25-150 μL Hank's Balanced Salt Solution (HBSS) containing 0.2 μm red-fluorescent particles and a model small molecule (fluorescein) were performed in rabbit eyes ex vivo, and visualized via flat mount...
October 11, 2016: Experimental Eye Research
Annick Barbaud, Julie Waton
Systemic hypersensitivity (HS) to corticosteroids (CS) is paradoxical but does exist. Some patients with a previous contact allergy to topical CS may develop a systemic contact dermatitis (SCD) while receiving CS orally or intravenously. However, a previous contact sensitization is not mandatory for developing a systemic HS to CS. Acute or delayed urticaria can occur in immediate HS. Immediate HS can be due to excipients, mainly carboxymethylcellulose or to CS themselves. Delayed reactions, mainly maculopapular rash and acute generalized exanthematous pustulosis can occur...
October 12, 2016: Current Pharmaceutical Design
Thomas Schluep, Jason Lickliter, James Hamilton, David L Lewis, Ching-Lung Lai, Johnson Yn Lau, Stephen A Locarnini, Robert G Gish, Bruce D Given
ARC-520 Injection, an RNA interference drug for the treatment of hepatitis B that targets cccDNA-derived viral mRNA transcripts with high specificity, effectively reduces the production of viral proteins and HBV DNA. In this phase I, randomized, double-blind, placebo-controlled study, 54 healthy volunteers (half male, half female) received a single, intravenous dose of 0.01-4.0 mg/kg ARC-520 Injection (N = 36) or placebo (N = 18). Assessments included safety, tolerability, pharmacokinetics, and pharmacodynamics (cytokines and complement)...
October 14, 2016: Clinical Pharmacology in Drug Development
Pei T Mah, Dunja Novakovic, Jukka Saarinen, Stijn Van Landeghem, Leena Peltonen, Timo Laaksonen, Antti Isomäki, Clare J Strachan
PURPOSE: To investigate the effect of compression on the crystallization behavior in amorphous tablets using sum frequency generation (SFG) microscopy imaging and more established analytical methods. METHOD: Tablets containing neat amorphous griseofulvin with/without excipients (silica, hydroxypropyl methylcellulose acetate succinate (HPMCAS), microcrystalline cellulose (MCC) and polyethylene glycol (PEG)) were prepared. They were analyzed upon preparation and storage using attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy, scanning electron microscopy (SEM) and SFG microscopy...
October 13, 2016: Pharmaceutical Research
Vincent Levet, Rémi Rosière, Romain Merlos, Luca Fusaro, Gilles Berger, Karim Amighi, Nathalie Wauthoz
The present study focuses on the development of dry powders for inhalation as adjuvant chemotherapy in lung cancer treatment. Cisplatin was chosen as a potential candidate for a local treatment as it remains the main platinum component used in conventional chemotherapies, despite its high and cumulative systemic toxicities. Bulk cisplatin was reduced to submicron sizes using high-pressure homogenization, mixed with a solubilized lipid and/or PEGylated component and then spray-dried to produce controlled-release dry powder formulations...
October 11, 2016: International Journal of Pharmaceutics
Smita S Kale, Krishnacharya G Akamanchi
Protein aggregation is a major problem of therapeutic proteins because aggregation decreases their therapeutic activity, shelf life and induces immunogenicity. Stabilization against aggregation is commonly attained by addition of different excipients like sugars, surfactants, buffers, salts, amino acids, polymers etc. Generally these excipients are required in combination for stabilization. Sugars are required at a higher concentration and commonly used surfactants like polysorbates have shortcomings due to oxidative degradation...
October 11, 2016: Molecular Pharmaceutics
Scaria P Thomas, Hari K N Sankar
OBJECTIVE: The objective of this study was to develop and validate a simple method for estimation of tramadol hydrochloride (TH) in pure and pharmaceutical dosage forms using a colorimeter. MATERIALS AND METHODS: TH on reaction with Eriochrome Black T in the presence of acetate buffer at pH 3.5 forms a colored complex. This complex was extracted with a fixed volume of chloroform. The optical density of this colored complex was measured against reagent blank using a colorimeter at 520 nm...
September 2016: Indian Journal of Pharmacology
Océane Dubray, Vincent Jannin, Fréderic Demarne, Yann Pellequer, Alf Lamprecht, Arnaud Béduneau
In this present study, the secretory transport of P-gp substrates, rhodamine 123 and digoxin, was evaluated using a Caco-2/HT29-MTX co-culture characterized by an efflux mechanism and a paracellular permeability closer to the human intestinal barrier compared to the Caco-2 monolayer gold standard. The influence of simulated intestinal fluids termed FeSSIF and FaSSIF on the intestinal absorption was also assessed in comparison with a conventional saline buffer. Labrasol(®) ALF and Gelucire(®) 44/14 in saline buffer significantly decreased to 83% and 62%, the P-gp-mediated transport of rhodamine 123 across the co-culture, respectively...
October 6, 2016: International Journal of Pharmaceutics
Justine Thiry, Pierre Lebrun, Chloe Vinassa, Marine Adam, Lauranne Netchacovitch, Eric Ziemons, Philippe Hubert, Fabrice Krier, Brigitte Evrard
The purpose of this work was to increase the solubility and the dissolution rate of itraconazole, which was chosen as the model drug, by obtaining an amorphous solid dispersion by hot melt extrusion. Therefore, an initial preformulation study was conducted using differential scanning calorimetry, thermogravimetric analysis and Hansen's solubility parameters in order to find polymers which would have the ability to form amorphous solid dispersions with itraconazole. Afterwards, the four polymers namely Kollidon(®) VA64, Kollidon(®) 12PF, Affinisol(®) HPMC and Soluplus(®), that met the set criteria were used in hot melt extrusion along with 25wt...
October 5, 2016: International Journal of Pharmaceutics
Kyu-Mok Hwang, Woojin Byun, Cheol-Hee Cho, Eun-Seok Park
The aim of this study was to prepare a highly porous multiparticulate dosage form containing cilostazol for gastroretentive drug delivery. The floating pellets were prepared with glyceryl behenate as a matrix former and camphor as a sublimating agent by extrusion-spheronization and sublimation under vacuum. Granules prepared with sublimation at 60°C displayed a slower dissolution rate and smoother surface morphology than those prepared at lower temperatures. This was unexpected as the reported melting point of glyceryl behenate is higher than 69°C...
October 10, 2016: Pharmaceutical Development and Technology
Laura I Mosquera-Giraldo, Carlos H Borca, Xiangtao Meng, Kevin J Edgar, Lyudmila V Slipchenko, Lynne S Taylor
Polymers play a key role in stabilizing amorphous drug formulations, a recent strategy employed to improve solubility and bioavailability of drugs delivered orally. However, the molecular mechanism of stabilization is unclear, therefore, the rational design of new crystallization-inhibiting excipients remains a substantial challenge. This article presents a combined experimental and computational approach to elucidate the molecular features that improve the effectiveness of cellulose polymers as solution crystallization inhibitors, a crucial first step toward their rational design...
October 7, 2016: Biomacromolecules
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