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Pharmaceutical Development and Technology

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https://www.readbyqxmd.com/read/28368746/continuous-production-of-aqueous-suspensions-of-ultra-fine-particles-of-curcumin-using-ultrasonically-driven-mixing-device
#1
Komal Pandey, Amruta Chatte, Sameer Dalvi
Developing drug formulations for poorly water-soluble drugs is a major challenge for pharmaceutical industries as the poor water solubility limits bioavailability of these drugs. Production of nanoparticles/microparticles of these drugs is one of the ways to improve dissolution rates by increasing interfacial area for dissolution. Curcumin, a compound obtained from the rhizome of curcuma longa (turmeric roots), is a pharmaceutically viable molecule. However, poor aqueous solubility limits its therapeutic use...
April 24, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28436282/the-effect-of-chamomile-extract-obtained-in-supercritical-carbon-dioxide-conditions-on-physicochemical-and-usable-properties-of-pharmaceutical-ointments
#2
Emilia Klimaszewska, Artur Seweryn, Anna Małysa, Małgorzata Zięba, Joanna Lipińska
The study investigated the effect of chamomile extract obtained in supercritical carbon dioxide conditions on the basic properties of pharmaceutical ointments. A total of five formulations were designed and prepared, differing in the weight ratio of sunflower oil to chamomile extract (5:0; 3.5:1.5; 2.5:2.5; 1.5:3.5 and 0:5). An increase in the concentration of chamomile extract was found to be accompanied by a decrease in hardness, adhesive power and flow limit. Based on viscosity measurements it was shown that ointments containing the hydrophobic plant extract under study were prone to larger drops in viscosity under the effect of the set shear rate...
April 22, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28430010/prolonged-injectable-formulation-of-nafarelin-using-in-situ-gel-combination-delivery-system
#3
Behnoush Alizadeh, Nika Bahari Javan, Hamid Akbari Javar, Mohammad Reza Khoshayand, Farid Abedin Dorkoosh
The principal purpose of the present study was to prepare and characterize a complex drug delivery system consisting of Nafarelin- poly (3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) nanoparticles (NPs) in combination with sodium alginate/poloxamer 407 in situ gel. Nafarelin loaded PHBV NPs were prepared via double emulsion solvent evaporation technique. Box-Behnken Response Surface Methodology was utilized to optimize NPs. Mean particle size, polydispersity index (PDI), entrapment efficiency (EE) and drug loading (DL) of the optimized NPs were measured...
April 21, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28425310/comments-on-prediction-of-the-aqueous-solubility-using-the-general-solubility-equation-gse-versus-genetic-algorithm-and-support-vector-machine-model
#4
Doaa Alantary, Samuel Yalkowsky
The General Solubility Equation (GSE) is the state of the art method for estimating the aqueous solubilities of organic compounds. It is an extremely simple equation that expresses aqueous solubility as a function of only two inputs: the octanol-water partition coefficient calculated by readily available softwares like clogp and acdlogp, and the commonly known melting point of the solute. Recently, Bahadori, et al. (2016) proposed that their genetic algorithm support vector machine is a "better" predictor...
April 20, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28425308/the-effect-of-molecular-weights-of-microencapsulating-polymers-on-viability-of-mouse-cloned-pancreatic-%C3%AE-cells-biomaterials-osmotic-forces-and-potential-applications-in-diabetes-treatment
#5
Armin Mooranian, Ryu Tackechi, Emma Jamieson, Grant Morahan, Hani Al-Salami
INTRODUCTION: Ideal cell-containing microcapsules should be capable of maintaining cell viability and exhibit significant structural stability to support cellular functionality. To date, such microcapsules remain unavailable, thus, this study used our well-established microencapsulating methods to examine a total of 32 different microencapsulating formulations and correlate polymers' molecular weights (Mwt) and UDCA addition, with cell viability and microcapsules' stability, postmicroencapsulation...
April 20, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28406344/fabrication-and-evaluation-of-eudragit%C3%A2-polymeric-films-for-transdermal-delivery-of-piroxicam
#6
Doungdaw Chantasart, Preeda Tocanitchart, Amaraporn Wongrakpanich, Veerawat Teeranachaideekul, Varaporn Buraphacheep Junyaprasert
The aims of this work were to develop and characterize the prolonged release piroxicam transdermal patch as a prototype to substitute oral formulations, to reduce side effects and improve patient compliance. The patches were composed of film formers (Eudragit(®)) as a matrix backbone, with PVC as a backing membrane and PEG200 used as a plasticizer. Results from X-ray diffraction patterns and Fourier transform-infrared spectroscopy indicated that loading piroxicam into films changed the drug crystallinity from needle to an amorphous or dissolved form...
April 13, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28379057/metoclopramide-nasal-spray-in-vitro-evaluation-and-in-vivo-pharmacokinetic-studies-in-dogs
#7
Ying Li, Xianpeng Fan, Wanqing Li, Peng Yang, Hui Zhang, Daoquan Tang, Xiaoxin Yin, Jianxu Sun, Aiping Zheng
Metoclopramide (MCP) can effectively alleviate motion sickness-caused nausea and vomiting. Nasal administration offers the greatest patient compliance. It is suitable for self-administration and offers rapid and complete absorption, no first-pass effects, and high bioavailability. In present study, a MCP nasal spray was prepared and evaluated in vitro and in vivo. Nasal cilia toxicity of Bufo toads was used to screen the preservative types and concentrations. Rabbit nasal mucosa was used to evaluate the mucosa permeability of different MCP nasal sprays with different penetration enhancers and preservative...
April 5, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28378604/pva-peg-physically-cross-linked-hydrogel-film-as-a-wound-dressing-experimental-design-and-optimization
#8
Afnan Sh Ahmed, Uttam Kumar Mandal, Muhammad Taher, Deny Susanti, Juliana Md Jaffri
The development of hydrogel films as wound healing dressings is of a great interest owing to their biological tissue-like nature. Polyvinyl alcohol/polyethylene glycol (PVA/PEG) hydrogels loaded with asiaticoside, a standardized rich fraction of Centella asiatica, were successfully developed using the freeze-thaw method. Response surface methodology with Box-Behnken experimental design was employed to optimize the hydrogels. The hydrogels were characterized and optimized by gel fraction, swelling behavior, water vapor transmission rate and mechanical strength...
April 5, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28378601/can-we-estimate-the-critical-micelle-concentration-of-amphiphilic-drug-bases-from-molecular-connectivity-indices
#9
Wiebke Saal, Nicole Wyttenbach, Jochem Alsenz, Martin Kuentz
Self-aggregation of drugs is since many years an important topic in the pharmaceutical sciences. Drugs can aggregate similar to surfactants and thereby exhibit a critical micelle concentration (CMC). The present work focused on amphiphilic drug bases and it was aimed to predict log(CMC) based on chemical structure alone. A dataset of 35 compounds was gathered mostly form the literature and complemented with own measurements based on ultrasonic resonator technology. The hydrophilic-lipophilic balance (HLB) values of the protonated bases were calculated and provided a range of 22...
April 5, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28375669/significant-solubility-of-carbon-dioxide-in-soluplus%C3%A2-facilitates-impregnation-of-ibuprofen-using-supercritical-fluid-technology
#10
Rana Obaidat, Mohammed Alnaief, Philip Jaeger
Treatment of Soluplus® with supercritical carbon dioxide allows promising applications in preparing dispersions of amorphous solids. Several characterization techniques ware employed to reveal this effect, including CO2 gas sorption under high pressure and physicochemical characterizations techniques. A gravimetric method was used to determine the solubility of carbon dioxide in the polymer at elevated pressure. The following physicochemical characterizations were used: thermal analysis, X-ray diffraction, Fourier transform, infra-red spectroscopy and scanning electron microscopy...
April 4, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28375037/the-influence-of-stevia-on-the-flow-shear-and-compression-behavior-of-sorbitol-a-pharmaceutical-excipient-for-direct-compression
#11
Hana Hurychová, Pavel Ondrejček, Zdenka Šklubalová, Barbora Vraníková, Tomáš Svěrák
Good flow and compaction properties are necessary for manipulation of particulate material in the pharmaceutical industry. The influence of the addition of an alternative sweetener, rebaudioside A, in a concentration 0.2% w/w and 0.5% w/w on the flow, shear and compaction properties of sorbitol for direct compaction, Merisorb® 200, was investigated in this work. Rebaudioside A worsened the flow properties of sorbitol: the Hausner ratio, the compressibility index and the mass flow rate through the aperture of a model hopper...
April 4, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28368674/partially-pegylated-pamam-dendrimers-as-solubility-enhancers-of-silybin
#12
Carola Diaz, José L Guzmán, Verónica A Jiménez, Joel B Alderete
PEGylated PAMAM-G4 dendrimers with substitution percentages of 50% and intermediate size PEG chains (0.55 and 2.0 kDa) were synthesized and evaluated as solubility enhancers and potential supramolecular carriers for the poorly soluble drug Silybin (SIL). Aqueous solubility profiles revealed that the PEGylated system with 2.0 kDa chains induced a five-fold solubility increase for SIL and the largest drug-loading capacity within the systems under study with an average complex stoichiometry of 71:1 according to the Higuchi-Connors formulation for multiple binding sites...
April 3, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28368673/development-and-evaluation-of-orally-disintegrating-tablets-comprising-taste-masked-mirtazapine-granules
#13
Simay Yıldız, Eren Aytekin, Burçin Yavuz, Sibel Bozdağ Pehlivan, İmran Vural, Nurşen Ünlü
INTRODUCTION: Orally disintegrating tablets (ODTs) provide an important treatment option for pediatric, geriatric, and psychiatric patients. In our previous study, we have performed the initial studies for the formulation development and characterization of new ODT formulations containing a bitter taste drug, mirtazapine, coated with 6% (w/w) Eudragit® E-100 (first group of formulations, FGF) without taste evaluation. In present study, coating ratio of the drug was increased to 8% (w/w) (second group of formulations, SGF) to examine the effect of increased coating ratio of drug on in vitro characterization of the formulations including in vitro taste masking study...
April 3, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28368215/effects-of-lipid-formulations-on-clove-extract-spray-dried-powders-comparison-of-physicochemical-properties-storage-stability-and-in-vitro-intestinal-permeation
#14
Diego F Cortes-Rojas, Claudia R F Souza, Mong-Jen Chen, Guenther Hochhaus, Wanderley P Oliveira
Clove is an aromatic plant spice with potent antioxidant and anti-inflammatory activity. Eugenol is the main compound which contributes to such medicinal and nutritional benefits. To date, the formulation of unstable, volatile, and poorly water soluble compounds remains a challenging task. Lipid formulations can be used to improve physicochemical and biopharmaceutical properties of poorly soluble compounds. The aim of the present study is to investigate the effects of lipids such as Gelucire and Compritol on physicochemical properties, stability and in vitro intestinal permeation of spray dried powdered formulations loaded with clove's bioactive compounds...
April 3, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28361586/determination-and-application-of-the-permitted-daily-exposure-pde-for-topical-ocular-drugs-in-multipurpose-manufacturing-facilities
#15
Ester Lovsin Barle, Jean-Claude Bizec, Milica Glogovac, Kamila Gromek, Gian Christian Winkler
Limits for the carryover of product residues should be based on toxicological evaluation such as described in the 'Guideline on setting health based exposure limits for use in risk identification in the manufacture of different medicinal products in shared facilities' (EMA, 2014). The toxicological evaluation should be performed also for locally administered drugs to ensure patient safety. Currently, there is no guidance on setting PDE for ocular drug substances in particular. The purpose of this investigation was to identify and describe a method for calculating a PDE value for topical ocular drugs (PDEocular)...
March 31, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28359224/evaluation-of-porphyrin-loaded-dry-alginate-foams-containing-poloxamer-407-and-%C3%AE-cyclodextrin-derivatives-intended-for-wound-treatment
#16
Victoria J Valerón Bergh, Elin Johannessen, Therese Andersen, Hanne Hjorth Tønnesen
Dry alginate foams intended for antibacterial photodynamic therapy (aPDT) of infected wounds were prepared. aPDT is a treatment modality involving light of appropriate wavelength, oxygen and a photosensitizer (PS) to produce radicals that attack biological targets (e.g. bacteria). The hydrophobic 5, 10, 15, 20-tetrakis(4-hydroxyphenyl)porphyrin (THPP) was chosen as a model PS and loaded into the foams. The foams contained a poloxamer (Pluronic F127) and/or β-cyclodextrin (βCD)-derivatives, i.e. methylβCD (MβCD), heptakis(2,6-di-O-methyl)-βCD (HkβCD) or hydroxypropylβCD (HPβCD)...
March 31, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28347210/poly-glycerol-methacrylate-based-degradable-nanoparticles-for-delivery-of-small-interfering-rna
#17
Noha G Morsi, Shimaa M Ali, Sherouk S Elsonbaty, Ahmed A Afifi, Mostafa A Hamad, Hui Gao, Mahmoud Elsabahy
Nucleic acids therapeutic efficiency is generally limited by their low stability and intracellular bioavailability, and by the toxicity of the carriers used to deliver them to the target sites. Aminated poly(glycerol methacrylate) polymers are biodegradable and pH-sensitive polymers that have been used previously to deliver antisense oligonucleotide and showed high transfection efficiency. The purpose of this study is to compare the efficiency and toxicity of aminated linear poly(glycerol methacrylate) (ALT) biodegradable polymer to the most commonly used cationic degradable (i...
March 27, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28347192/a-review-of-recent-developments-on-micro-nanostructured-pharmaceutical-systems-for-intravesical-therapy-of-the-bladder-cancer
#18
Marcela Brito Oliveira, Mônica Villa Nova, Marcos Luciano Bruschi
Bladder cancer (BC) is the most common tumor type of genitourinary tract, which affects more men than women. The conventional treatment is through chemotherapy or immunotherapy, but the radiotherapy and surgery may be necessary in cases of invasive cancer. The search for less invasive, safe and effective therapies has attracted researchers to the development of new drug delivery systems to carry drugs to be administered by catheter into the bladder. The research on intravesical systems for the BC treatment continues at a rapid pace and a variety of micro or nanostructured systems has been used...
March 27, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28346840/fabrication-and-evaluation-of-phytomenadione-as-a-nanostructure-lipid-carrier-for-enhancement-of-bioavailability
#19
Bader Mubarak Aljaeid, Khaled Mohamed Hosny
Owing to its limited aqueous solubility, Phytomenadione (vitamin K) undergoes a low bioavailability (50%) with a large inter-individual variability after oral administration. Therefore, the aim of this work was to incorporate vitamine K into nanostructure lipid carrier systems to improve its aqueous solubility and bioavailability. Phytomenadione was used as a liquid lipid, Precirol ATO5, and Compritol ATO were used as solid lipids, Labrasol and Cremophore EL as water soluble surfactants, Capryol 90 and Lauroglycol as lipid soluble surfactants...
March 27, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28316269/development-of-a-novel-one-step-production-system-for-injectable-liposomes-under-gmp
#20
Ryo Araki, Takashi Matsuzaki, Ayumi Nakamura, Daisaku Nakatani, Shoji Sanada, Hai Ying Fu, Keiji Okuda, Masaki Yamato, Shota Tsuchida, Yasushi Sakata, Tetsuo Minamino
There are few methods available for injectable liposome production under good manufacturing practices (GMP). Injectable liposome production processes under GMP generally consist of liposome formation, size homogenization, organic solvent removal, liposome concentration control and sterilization. However, these complicated and separate processes make it difficult to maintain scalability, reproducibility and sterility. To overcome these limitations, we developed a novel one-step in-line closed liposome production system that integrated all production processes by combining the in-line thermal mixing device with modified counterflow dialysis...
March 20, 2017: Pharmaceutical Development and Technology
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