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https://www.readbyqxmd.com/read/28342786/pharmaceutical-solvates-hydrates-and-amorphous-forms
#1
REVIEW
Anne Marie Healy, Zelalem Ayenew Worku, Dinesh Kumar, Atif M Madi
Active pharmaceutical ingredients (APIs) may exist in various solid forms, which can lead to differences in the intermolecular interactions, affecting the internal energy and enthalpy, and the degree of disorder, affecting the entropy. Differences in solid forms often lead to differences in thermodynamic parameters and physicochemical properties for example solubility, dissolution rate, stability and mechanical properties of APIs and excipients. Hence, solid forms of APIs play a vital role in drug discovery and development in the context of optimization of bioavailability, filing intellectual property rights and developing suitable manufacturing methods...
March 22, 2017: Advanced Drug Delivery Reviews
https://www.readbyqxmd.com/read/28342666/stabilization-study-of-inactivated-foot-and-mouth-disease-virus-vaccine-by-size-exclusion-hplc-and-differential-scanning-calorimetry
#2
Yanli Yang, Qizu Zhao, Zhengjun Li, Lijing Sun, Guanghui Ma, Songping Zhang, Zhiguo Su
The inactivated foot and mouth disease virus (FMDV), which has a sedimentation coefficient of 146S, is crucial to the efficacy of vaccine preparations, but extremely unstable in vitro. It is prone to dissociate into smaller particles referred to as 12S with a concomitant decrease in immunogenicity; therefore, it is of great importance to find the best condition for stabilizing the FMDV. In the present work, the effects of solution pH and temperature on the dissociation of 146S was investigated and potential stabilizers were screened, with aid of high-performance size-exclusion chromatography (HPSEC) for rapid and quantitative determination of 146S, together with differential scanning calorimetry (DSC) technology for thermal stability analysis...
March 22, 2017: Vaccine
https://www.readbyqxmd.com/read/28339395/effect-of-ovariectomy-and-sideritis-euboea-extract-administration-on-large-artery-mechanics-morphology-and-structure-in-middle-aged-rats
#3
Dimitrios P Sokolis, Constantinos A Dimitriou, Pavlos Lelovas, Nikolaos G Kostomitsopoulos, Ismene A Dontas
BACKGROUND: Arterial function is regulated by estrogen, but no consistent pattern of arterial mechanical remodeling in response to depleted estrogen levels is available. OBJECTIVE: To examine long-term effects of ovariectomy (OVX) on the mechanical properties, morphology, and histological structure of carotid artery in middle-aged rats and a potentially protective effect of Sideritis euboea extract (SID), commonly consumed as "mountain tea". METHODS: 10-month-old female Wistar rats were allocated into control (sham-operated), OVX, OVX+SID, and OVX+MALT (maltodextrin; excipient used for dilution of SID) groups...
March 20, 2017: Biorheology
https://www.readbyqxmd.com/read/28339393/postscription-what-lies-beneath-potentially-harmful-excipients-to-avoid-when-compounding-for-small-animals-a-note-of-caution
#4
Erika Rost
No abstract text is available yet for this article.
November 2016: International Journal of Pharmaceutical Compounding
https://www.readbyqxmd.com/read/28336459/correlation-between-calculated-molecular-descriptors-of-excipient-amino-acids-and-experimentally-observed-thermal-stability-of-lysozyme
#5
Helena Meng-Lund, Natascha Friis, Marco van de Weert, Jukka Rantanen, Antti Poso, Holger Grohganz, Lene Jorgensen
A quantitative structure-property relationship (QSPR) between protein stability and the physicochemical properties of excipients was investigated to enable a more rational choice of stabilizing excipients than prior knowledge. The thermal transition temperature and aggregation time were determined for lysozyme in combination with 13 different amino acids using high throughput fluorescence spectroscopy and kinetic static light scattering measurements. On the theoretical side, around 200 2D and 3D molecular descriptors were calculated based on the amino acids' chemical structure...
March 20, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28335640/nebivolol-attenuates-cerebral-vasospasm-both-by-increasing-endothelial-nitric-oxide-and-by-decreasing-oxidative-stress-in-an-experimental-subarachnoid-haemorrhage
#6
Mehmet Arif Aladag, Yusuf Turkoz, Hakan Parlakpinar, Mehmet Gul
OBJECTIVE: Evidence suggests that reduction of nitric oxide (NO) bioavailability due to oxidative stress plays a central role in the pathophysiology of cerebral vasospasm after subarachnoid haemorrhage (SAH). To prevent SAH-induced cerebral vasospasm, therefore we used nebivolol hydrochloride as a NO-mediated vasodilator and an antioxidant drug in an experimental rat model of SAH. MATERIALS AND METHODS: Forty female Wistar rats were divided into control, SAH, SAH plus placebo, and SAH plus nebivolol groups...
March 23, 2017: British Journal of Neurosurgery
https://www.readbyqxmd.com/read/28334923/validated-rp-hplc-dad-method-for-the-quantification-of-insect-repellent-ethyl-2-aminobenzoate-in-membrane-moderated-matrix-type-monolithic-polymeric-device
#7
Johirul Islam, Kamaruz Zaman, Srijita Chakrabarti, Nilutpal Sharma Bora, Santa Mandal, Manash Pratim Pathak, Pakalapati Srinivas Raju, Pronobesh Chattopadhyay
A simple, accurate and sensitive reversed-phase high-performance liquid chromatographic (RP-HPLC) method has been developed for the estimation of ethyl 2-aminobenzoate (EAB) in a matrix type monolithic polymeric device and validated as per the International Conference on Harmonization guidelines. The analysis was performed isocratically on a ZORBAX Eclipse plus C18 analytical column (250 × 4.4 mm, 5 μm) and a diode array detector (DAD) using acetonitrile and water (75:25 v/v) as the mobile phase by keeping the flow-rate constant at 1...
March 14, 2017: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/28333461/suberin-fatty-acids-from-outer-birch-bark-isolation-and-physical-material-characterization
#8
Jyrki Heinämäki, Minni M Pirttimaa, Sami Alakurtti, H Pauliina Pitkänen, Heimo Kanerva, Janne Hulkko, Urve Paaver, Jaan Aruväli, Jouko Yliruusi, Karin Kogermann
The isolation and physical material properties of suberin fatty acids (SFAs) were investigated with special reference to their potential applications as novel pharmaceutical excipients. SFAs were isolated from outer birch bark (OBB) with a new extractive hydrolysis method. The present simplified isolation process resulted in a moderate batch yield and chemical purity of SFAs, but further development is needed for establishing batch-to-batch variation. Cryogenic milling was the method of choice for the particle size reduction of SFAs powder...
March 23, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28324728/hplc-ms-ms-method-for-quantification-of-paclitaxel-from-keratin-containing-samples
#9
Emily A Turner, Alexandra C Stenson, Saami K Yazdani
Local drug delivery of paclitaxel is becoming ever more prevalent. As complex drug/excipient combinations are being developed and tested, new high performance liquid chromatography-mass spectrometry (HPLC-MS) techniques capable of quantifying paclitaxel from such formulations are needed. Here a method for quantifying paclitaxel from aqueous, protein and oil containing samples was developed and validated. Keratin, derived from human hair, is the protein component/paclitaxel excipient in the development and validation of said method...
March 10, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28323098/an-innovative-method-for-the-preparation-of-high-api-loaded-hollow-spherical-granules-for-use-in-controlled-release-formulation
#10
Takumi Asada, Mitsuaki Kobiki, Yasushi Ochiai, Yasunori Iwao, Shigeru Itai
The aim of this study was to prepare controlled-release (CR) granules with suitable particle strength, flowability, particle size distribution (PSD) and density characteristics for blending with other excipients. We also wanted these CR granules to contain large quantities of active pharmaceutical ingredient (API). A high shear mixer was used to mix an API with various polymers at various feed ratios, and the resulting granulated materials were sprayed with solvent. The wet granules were dried using a fluidized bed dryer to give CR granules...
March 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28322163/geriatric-oriented-high-dose-nutraceutical-odts-formulation-and-physicomechanical-characterization
#11
Ahmed M Agiba, Sameh Abdel-Hamid, Maha Nasr, Ahmed S Geneidi
CONTEXT: Oral disintegrating tablets (ODTs) represent a better option than conventional tablets for geriatric population, owing to their fast onset of action and their better patient compliance. OBJECTIVE: Two principal therapeutic high-dose nutraceuticals; chondroitin sulphate and glucosamine were formulated into an oral disintegration tablet (ODT) intended for sublingual administration, and optimized to improve compliance and achieve rapid onset of action in osteoarthritis treatment...
March 20, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28302396/supercritical-antisolvent-co-precipitation-of-rifampicin-and-ethyl-cellulose
#12
Rania Djerafi, Andri Swanepoel, Christelle Crampon, Lonji Kalombo, Philip Labuschagne, Elisabeth Badens, Yasmine Masmoudi
Rifampicin-loaded submicron-sized particles were prepared through supercritical anti-solvent process using ethyl cellulose as polymeric encapsulating excipient. Ethyl acetate and a mixture of ethyl acetate/dimethyl sulfoxide (70/30 and 85/15) were used as solvents for both drug and polymeric excipient. When ethyl acetate was used, rifampicin was crystallized separately without being embedded within the ethyl cellulose matrix while by using the ethyl acetate/dimethyl sulfoxide mixture, reduced crystallinity of the active ingredient was observed and a simultaneous precipitation of ethyl cellulose and drug was achieved...
March 14, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28298984/an-in-vitro-analysis-model-for-investigating-the-staining-effect-of-various-chlorhexidine-based-mouthwashes
#13
Alain-Ayepa Kouadio, Xavier Struillou, Céline Bories, Jean-Michel Bouler, Zahi Badran, Assem Soueidan
BACKGROUND: There are different mouthwashes containing chlorhexidine in different concentrations, as well as various excipients. Chlorhexidine induce stains or discoloration in teeth and mucous membranes. The aim of this work was to design a model to reproduce in vitro staining associated with the use of different mouthwashes containing chlorhexidine. MATERIAL AND METHODS: We used as substrates of natural teeth and elephant ivory slices. Different incubation baths were conducted over 21 days in culture dishes at 37°C...
March 2017: Journal of Clinical and Experimental Dentistry
https://www.readbyqxmd.com/read/28290242/variation-in-impact-of-use-of-different-propellants-and-excipients-in-pharmaceutical-topical-aerosol-then-and-now
#14
Maunab Patra, Meenakshi Patnaik
Skin is the most suitable and recommendable organ of the human body for topical administration of drugs. Drug delivery system is the methodology used to ensure that the drugs entering in to the body through any route into the body, reach its target for pharmacological action. Patients tend to prefer the painless route of drug administration. So, pharmaceutical aerosols were invented meet patient compliance. Many variations in excipients with respect to compatibility to drugs, stability and economy have been used since start to improve the aerosol system of drug delivery...
March 8, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28287743/a-systematic-study-of-molecular-interactions-of-anionic-drugs-with-a-dimethylaminoethyl-methacrylate-copolymer-regarding-solubility-enhancement
#15
Wiebke Saal, Alfred Ross, Nicole Wyttenbach, Jochem Alsenz, Martin Kuentz
The methacrylate-copolymer Eudragit EPO (EPO) has raised interest in solubility enhancement of anionic drugs. Effects on aqueous drug solubility at rather low polymer concentrations are barely known despite their importance upon dissolution and dilution of oral dosage forms. We provide evidence for substantial enhancement (factor 4-230) of aqueous solubility of poorly water-soluble anionic drugs induced by low (0.1-5% (w/w)) concentration of EPO for a panel of seven acidic crystalline drugs. Diffusion data (determined by (1)H nuclear magnetic resonance spectroscopy) indicate that the solubility increasing effect monitored by quantitative ultraperformance liquid chromatography was caused primarily by molecular API polymer interactions in the bulk liquid phase...
March 21, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28286315/formulation-of-hydrophobic-peptides-for-skin-delivery-via-coated-microneedles
#16
Xin Zhao, Sion A Coulman, Stephanie J Hanna, F Susan Wong, Colin M Dayan, James C Birchall
Microneedles (MNs) have been investigated as a minimally-invasive delivery technology for a range of active pharmaceutical ingredients (APIs). Various formulations and methods for coating the surface of MNs with therapeutics have been proposed and exemplified, predominantly for hydrophilic drugs and particulates. The development of effective MN delivery formulations for hydrophobic drugs is more challenging with dosing restrictions and the use of organic solvents impacting on both the bioactivity and the kinetics of drug release...
March 9, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28284921/engineered-particles-demonstrate-improved-flow-properties-at-elevated-drug-loadings-for-direct-compression-manufacturing
#17
Andrea N Trementozzi, Cheuk-Yui Leung, Frederick Osei-Yeboah, Erwin Irdam, Yiqing Lin, J Michael MacPhee, Pierre Boulas, Shyam B Karki, Peter N Zawaneh
Optimizing powder flow and compaction properties is critical for ensuring a robust tablet manufacturing process. The impact of flow and compaction properties of the active pharmaceutical ingredient (API) becomes progressively significant for higher drug load formulations, and for scaling up manufacturing processes. This study demonstrated that flow properties of a powder blend can be improved through API particle engineering, without critically impacting blend tabletability at elevated drug loadings. In studying a jet milled API (D50=24μm) and particle engineered wet milled API (D50=70μm and 90μm), flow functions of all API lots were similarly poor despite the vast difference in average particle size (ffc<4)...
March 8, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28284034/design-development-and-evaluation-of-triphala-tablets
#18
Neelam Mouriya, Anupama Valvi, Rajani Athawale, Narendra Bhatt
Triphala is a combination of three herbs amla, bahera and haritaki, it is widely available in the form churna and is a valued formula since ancient times. The aim of this research was to develop reproducible batches of triphala tablets and evaluation of the optimized batch. Direct compression was the method of choice. The tablets were prepared using different directly compressible excipients MicroceLac, Ludipress, Ludiflash. High Performance Liquid Chromatography (HPLC) method was employed for authentification of the herbs using gallic acid as the marker...
March 10, 2017: Journal of Complementary & Integrative Medicine
https://www.readbyqxmd.com/read/28283431/insight-into-a-novel-strategy-for-the-design-of-tablet-formulations-intended-for-direct-compression
#19
Maxx Capece, Zhonghui Huang, Rajesh Davé
In a recent study, it was demonstrated that improving flow of a model poorly flowing and poorly compactable drug substance, acetaminophen, via dry-coating while using fine excipients may promote direct compression. To validate this novel strategy, particularly for high drug loading formulations, this study investigates the effect of microcrystalline cellulose (MCC) particle size and dry-coating on powder tabletability and flowability. It was determined that blends containing fine-sized MCC (20 μm) resulted in the highest tablet tensile strength and best tabletability since it provides higher inter-particle contact area compared to coarser-sized MCC...
March 7, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28282402/formulation-and-pegylation-optimization-of-the-therapeutic-pegylated-phenylalanine-ammonia-lyase-for-the-treatment-of-phenylketonuria
#20
Sean M Bell, Dan J Wendt, Yanhong Zhang, Timothy W Taylor, Shinong Long, Laurie Tsuruda, Bin Zhao, Phillip Laipis, Paul A Fitzpatrick
Phenylketonuria (PKU) is a genetic metabolic disease in which the decrease or loss of phenylalanine hydroxylase (PAH) activity results in elevated, neurotoxic levels of phenylalanine (Phe). Due to many obstacles, PAH enzyme replacement therapy is not currently an option. Treatment of PKU with an alternative enzyme, phenylalanine ammonia lyase (PAL), was first proposed in the 1970s. However, issues regarding immunogenicity, enzyme production and mode of delivery needed to be overcome. Through the evaluation of PAL enzymes from multiple species, three potential PAL enzymes from yeast and cyanobacteria were chosen for evaluation of their therapeutic potential...
2017: PloS One
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