scholarly journals Amorphization of Thiamine Chloride Hydrochloride: Effects of Physical State and Polymer Type on the Chemical Stability of Thiamine in Solid Dispersions

2020 ◽  
Vol 21 (16) ◽  
pp. 5935 ◽  
Author(s):  
Seda Arioglu-Tuncil ◽  
Adrienne L. Voelker ◽  
Lynne S. Taylor ◽  
Lisa J. Mauer
Keyword(s):  
Intermolecular Interactions ◽  
Physical State ◽  
Amorphous Polymer ◽  
Solid Dispersions ◽  
Amorphous State ◽  
Moisture Sorption ◽  
Storage Conditions ◽  
X Ray Diffraction ◽  
Unexplored Area ◽  
Polymer Dispersions

Thiamine is an essential micronutrient, but delivery of the vitamin in supplements or foods is challenging because it is unstable under heat, alkaline pH, and processing/storage conditions. Although distributed as a crystalline ingredient, thiamine chloride hydrochloride (TClHCl) likely exists in the amorphous state, specifically in supplements. Amorphous solids are generally less chemically stable than their crystalline counterparts, which is an unexplored area related to thiamine delivery. The objective of this study was to document thiamine degradation in the amorphous state. TClHCl:polymer dispersions were prepared by lyophilizing solutions containing TClHCl and amorphous polymers (pectin and PVP (poly[vinylpyrrolidone])). Samples were stored in controlled temperature (30–60 °C) and relative humidity (11%) environments for 8 weeks and monitored periodically by X-ray diffraction (to document physical state) and HPLC (to quantify degradation). Moisture sorption, glass transition temperature (Tg), intermolecular interactions, and pH were also determined. Thiamine was more labile in the amorphous state than the crystalline state and when present in lower proportions in amorphous polymer dispersions, despite increasing Tg values. Thiamine was more stable in pectin dispersions than PVP dispersions, attributed to differences in presence and extent of intermolecular interactions between TClHCl and pectin. The results of this study can be used to control thiamine degradation in food products and supplements to improve thiamine delivery and decrease rate of deficiency.

scholarly journals Amorphization of Thiamine Mononitrate: A Study of Crystallization Inhibition and Chemical Stability of Thiamine in Thiamine Mononitrate Amorphous Solid Dispersions

2020 ◽  
Vol 21 (24) ◽  
pp. 9370
Author(s):  
Seda Arioglu-Tuncil ◽  
Adrienne L. Voelker ◽  
Lynne S. Taylor ◽  
Lisa J. Mauer
Keyword(s):  
Chemical Stability ◽  
High Performance ◽  
Solid Dispersions ◽  
Amorphous State ◽  
Moisture Sorption ◽  
Amorphous Solid ◽  
Storage Conditions ◽  
X Ray Diffraction ◽  
Salt Form ◽  
Crystallization Inhibition

This study investigated thiamine degradation in thiamine mononitrate (TMN):polymer solid dispersions, accounting for the physical state of the vitamin and the recrystallization tendency of TMN in these dispersions. Results were compared with those from solid dispersions containing a different salt form of thiamine (thiamine chloride hydrochloride (TClHCl)). TMN:polymer dispersions were prepared by lyophilizing solutions containing TMN and amorphous polymers (pectin and PVP (polyvinylpyrrolidone)). Samples were stored in controlled temperature and relative humidity (RH) environments for eight weeks and monitored periodically by X-ray diffraction and high performance liquid chromatography (HPLC). Moisture sorption, glass transition temperature (Tg), intermolecular interactions, and pH were also determined. Similar to the TClHCl:polymer dispersions, thiamine was more chemically labile in the amorphous state than the crystalline state, when present in lower proportions in amorphous TMN:polymer dispersions despite increasing Tg values, when environmental storage conditions exceeded the Tg of the dispersion, and when co-formulated with PVP compared to pectin. When thiamine remained as an amorphous solid, chemical stability of thiamine did not differ as a function of counterion present (TMN vs. TClHCl). However, storage at 75% RH led to hydration of thiamine:PVP dispersions, and the resulting pH of the solutions as a function of thiamine salt form led to a higher chemical stability in the acidic TClHCl samples than in the neutral TMN samples.

scholarly journals Influence of the Physical State of Spray-Dried Flavonoid-Inulin Microparticles on Oxidative Stability of Lipid Matrices

Antioxidants ◽  
2019 ◽  
Vol 8 (11) ◽  
pp. 520 ◽  
Author(s):  
Guibeth Morelo ◽  
Begoña Giménez ◽  
Gloria Márquez-Ruiz ◽  
Francisca Holgado ◽  
Patricio Romero-Hasler ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Oxidative Stability ◽  
Physical State ◽  
Amorphous State ◽  
Polar Compounds ◽  
X Ray Diffraction ◽  
Oxidation Study ◽  
Feed Temperature ◽  
Spray Dried

The effect of the physical state of flavonoid-inulin microparticles (semi-crystalline/amorphous) on the oxidative stability of lipid matrices was studied. Epicatechin (E) and quercetin (Q) microparticles with inulin were formulated at two infeed temperatures (15 °C and 90 °C) by spray drying. X-ray diffraction analyses showed that flavonoid-inulin microparticles obtained at feed temperature of 15 °C were semi-crystalline (E-In-15, 61.2% and Q-In-15, 60%), whereas those at 90 °C were amorphous (Q-In-90, 1.73 and Q-In-90 2.30%). Semi-crystalline state of flavonoid-inulin microparticles enhanced the EE (68.8 and 67.8% for E and Q, respectively) compared to amorphous state (41.6 and 51.1% for E and Q, respectively). However, amorphous Q-microparticles showed the highest antioxidant activity both in methyl linoleate and sunflower oil, increasing the induction period and decreasing the polar compounds and polymer triglyceride formation during long-term oxidation study. Therefore, the physical state of spray-dried flavonoid-inulin microparticles may determine their antioxidant activity in lipid matrices.

scholarly journals Development of a Solid Dispersion of Nystatin with Maltodextrin as a Carrier Agent: Improvements in Antifungal Efficacy against Candida spp. Biofilm Infections

2021 ◽  
Vol 14 (5) ◽  
pp. 397
Author(s):  
Carlos Benavent ◽  
Carlos Torrado-Salmerón ◽  
Santiago Torrado-Santiago
Keyword(s):  
Antifungal Activity ◽  
Solid Dispersions ◽  
Particle Size Analysis ◽  
Size Analysis ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Candida Spp ◽  
Microbiological Techniques ◽  
Characterization Studies ◽  
Candida Albicans Biofilms

The aim of this study was to improve the treatment of Candida albicans biofilms through the use of nystatin solid dispersions developed using maltodextrins as a hyperosmotic carrier. Characterization studies by differential scanning calorimetry, X-ray diffraction, dissolution studies, and particle size analysis were performed to evaluate changes in nystatin crystallinity. Antifungal activity and anti-biofilm efficacy were assessed by microbiological techniques. The results for nystatin solid dispersions showed that the enhancement of antifungal activity may be related to the high proportions of maltodextrins. Anti-biofilm assays showed a significant reduction (more than 80%) on biofilm formation with SD-N:MD [1:6] compared to the nystatin reference suspension. The elaboration process and physicochemical properties of SD-N:MD [1:6] could be a promising strategy for treatment of Candida biofilms.

Degradation of β-carotene in amorphous polymer matrices. Effect of water sorption properties and physical state

2011 ◽  
Vol 91 (14) ◽  
pp. 2587-2593 ◽  
Author(s):  
Ximena A Ramoneda ◽  
Peggy A Ponce-Cevallos ◽  
María del Pilar Buera ◽  
Beatriz E Elizalde
Keyword(s):  
Water Sorption ◽  
Physical State ◽  
Amorphous Polymer ◽  
Polymer Matrices ◽  
Sorption Properties ◽  
Effect Of Water ◽  
Water Sorption Properties ◽  
Β Carotene

W-Doped TiO2 Preparation and Photocatalytic Degradation of Guaiacol

2014 ◽  
Vol 513-517 ◽  
pp. 33-36 ◽  
Author(s):  
Zi Chang Xie ◽  
Ying Wang ◽  
Peng Wang ◽  
Lei Zhang
Keyword(s):  
Photocatalytic Activity ◽  
Visible Light ◽  
Photocatalytic Degradation ◽  
Degradation Rate ◽  
Amorphous State ◽  
X Ray Diffraction ◽  
Model Compounds ◽  
Plant Fibers ◽  
X Ray ◽  
Crystallite Structure

In this paper, W-doped TiO2 (W-TiO2) powder was prepared in hydrothermal method by mixing TiO2 and ammonium metatungstate. The catalysts were characterized by X-ray diffraction and ultraviolet spectrophotometer. The results displayed that W-TiO2 showed an anatase crystallite structure with 2 % W content. W-element in W-TiO2 was amorphous state. The guaiacol was degraded with the W-TiO2 in the visible light. It was a model compounds of lignin existed in the plant fibers. The degradation rate of guaiacol was increased with the photocatalytic time, as high as 88.21 % after 360 min irradiation. It was concluded that the W-TiO2 had an obvious photocatalytic activity under visible light. It can be used in the photocatalytic degradation of lignin.

scholarly journals Iron(II) Complexes with Boron Cluster Anion [B10Cl10]2-: Intermolecular Interactions according to35Cl NQR Spectroscopy and X-ray Diffraction

2017 ◽  
Vol 643 (23) ◽  
pp. 1939-1947 ◽  
Author(s):  
Eleonora A. Kravchenko ◽  
Andrei. A. Gippius ◽  
Irina N. Polyakova† ◽  
Varvara V. Avdeeva ◽  
Elena A. Malinina ◽  
...  
Keyword(s):  
Intermolecular Interactions ◽  
Cluster Anion ◽  
X Ray Diffraction ◽  
X Ray ◽  
Boron Cluster ◽  
Boron Cluster Anion

scholarly journals EFFECT OF SELECTED POLYMERS ON DISSOLUTION AND STABILIZATION OF AMORPHOUS FORM OF MELOXICAM

2017 ◽  
Vol 9 (9) ◽  
pp. 33
Author(s):  
Rana Obaidat ◽  
Bashar Al-taani ◽  
Hanan Al-quraan
Keyword(s):  
Polyethylene Glycol ◽  
Solid Dispersions ◽  
Dissolution Profile ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Polyethylene Glycol 4000 ◽  
Amorphous Form ◽  
Molecular Weights ◽  
Low Solubility ◽  
Reproducible Manner

Objective: Meloxicam is classified as class II corresponding to its high permeability and low solubility (12μg/ml). This study aims to compare the effect of selected polymers on stabilization of amorphous form, and dissolution of meloxicam by preparation of different solid dispersions using selected polymers (chitosan oligomers, polyvinylpyrrolidone K30, and polyethylene glycols).Methods: These solid dispersions were prepared using two different methods; solvent evaporation method for the two molecular weights chitosan carriers (16 and 11KDa) and polyvinylpyrrolidone-K30 and melting method for the two different molecular weights polyethylene glycol (4000 and 6000). The physicochemical properties of solid dispersions were analyzed using differential scanning calorimetry, Fourier transform infra-red analysis, Powder X-ray diffraction, and scanning electron microscopy. Selected dispersions were then compared to two selected marketed drugs (Mobic® and Moven®).Results: Best dissolution rates were obtained for both polyvinylpyrrolidone-K30 and polyethylene glycol 6000, followed by chitosan 16 kDa, chitosan 11 kDa, and polyethylene glycol 4000. Increasing polymeric ratio increased dissolution rate except for chitosan. Precipitation of the drug as amorphous form occurred in chitosan and polyvinylpyrrolidone-K30 dispersions, while no change in crystallinity obtained for polyethylene glycol dispersions. Failure of polyvinylpyrrolidone-K30 in the maintenance of stability during storage time was observed while re-crystallization occurred in chitosan-based dispersions, which ends with preferences to polyethylene glycol dispersions. After comparing the release of selected dispersions with the two selected polymers; all dispersions got a higher release than that of the two marketed drugs release.Conclusion: The dissolution profile of meloxicam has been increased successfully in a reproducible manner.

scholarly journals Влияние режима получения образцов и термообработки на локальную структуру халькогенидного полупроводника Ge-=SUB=-2-=/SUB=-Sb-=SUB=-2-=/SUB=-Te-=SUB=-5-=/SUB=-

2022 ◽  
Vol 56 (3) ◽  
pp. 291
Author(s):  
С.Н. Гарибова ◽  
А.И. Исаев ◽  
С.И. Мехтиева ◽  
С.У. Атаева ◽  
Р.И. Алекперов
Keyword(s):  
Heat Treatment ◽  
Thermal Processing ◽  
Thermal Evaporation ◽  
Amorphous State ◽  
Hexagonal Structure ◽  
Structural Elements ◽  
X Ray Diffraction ◽  
X Ray ◽  
The Matrix ◽  
Close Range

Specifics of "amorphous state - crystal" phase transitions in dependence on the samples obtaining method and thermal processing, as well as changes in the structure and close range order in the arrangement of the atoms of Ge20Sb20.5Te51 chalcogenide semiconductors have been studied by the x-ray diffraction and Raman spectroscopy. It has been shown that Ge20Sb20.5Te51 films obtained by thermal evaporation on an unheated substrate are amorphous; after heat treatment at 220 and 400 °C, transform into a crystalline phase with a cubic and hexagonal structure. The chemical bonds and the main structural elements that form the matrix of the investigated objects, as well as the changes that occur in them during heat treatment, have been determined.

scholarly journals Novel Gliclazide Electrosprayed Nano-Solid Dispersions: Physicochemical Characterization and Dissolution Evaluation

2019 ◽  
Vol 9 (2) ◽  
pp. 231-240
Author(s):  
Khosro Adibkia ◽  
Solmaz Ghajar ◽  
Karim Osouli-Bostanabad ◽  
Niloufar Balaei ◽  
Shahram Emami ◽  
...  
Keyword(s):  
Drug Release ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Amorphous State ◽  
Water Soluble ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Peg 6000

Purpose: In the current study, electrospraying was directed as a novel alternative approach to improve the physicochemical attributes of gliclazide (GLC), as a poorly water-soluble drug, by creating nanocrystalline/amorphous solid dispersions (ESSs). Methods: ESSs were formulated using Eudragit® RS100 and polyethylene glycol (PEG) 6000 as polymeric carriers at various drug: polymer ratios (i.e. 1:5 and 1:10) with different total solution concentrations of 10, 15, and 20% w/v. Morphological, physicochemical, and in-vitro release characteristics of the developed formulations were assessed. Furthermore, GLC dissolution behaviors from ESSs were fitted to various models in order to realize the drug release mechanism. Results: Field emission scanning electron microscopy analyses revealed that the size and morphology of the ESSs were affected by the drug: polymer ratios and solution concentrations. The polymer ratio augmentation led to increase in the particle size while the solution concentration enhancement yielded in a fiber establishment. Differential scanning calorimetry and powder X-ray diffraction investigations demonstrated that the ESSs were present in an amorphous state. Furthermore, the in vitro drug release studies depicted that the samples prepared employing PEG 6000 as carrier enhanced the dissolution rate and the model that appropriately fitted the release behavior of ESSs was Weibull model, where demonstrating a Fickian diffusion as the leading release mechanism. Fourier-transform infrared spectroscopy results showed a probability of complexation or hydrogen bonding, development between GLC and the polymers in the solid state. Conclusion: Hence the electrospraying system avails the both nanosizing and amorphization advantages, therefore, it can be efficiently applied to formulating of ESSs of BCS Class II drugs.

scholarly journals Contribution to the Improvement of an Oral Formulation of Niclosamide, an Antihelmintic Drug Candidate for Repurposing in SARS-CoV-2 and Other Viruses

2020 ◽  
Author(s):  
Eduardo José Barbosa ◽  
Mariana Ribeiro Gubitoso ◽  
Nádia Araci Bou-Chacra ◽  
Stephen R. Byrn ◽  
Flavio M. S. Carvalho ◽  
...  
Keyword(s):  
Solid Dispersions ◽  
Amorphous Solid ◽  
Aqueous Solubility ◽  
Oral Formulation ◽  
Oral Dosage ◽  
Drug Candidate ◽  
Formulation Development ◽  
Polymer Dispersions ◽  
Kinetic Solubility ◽  
Oral Dosage Forms

<p>Niclosamide (NCL) is an effective anthelmintic agent that has been shown to possess broad-spectrum antiviral activity, including against<b> </b>SARS-CoV-2. Due to its poor solubility in aqueous medium, however, the commercially available NCL formulations can act only locally in gastrointestinal worms and are not suitable to achieve plasmatic levels to treat systemic diseases. Consequently, the repurposing of this drug represents a challenge for formulation development with serious risks to the biological availability and can compromise preclinical and clinical outcomes. Herein, we report possible formulation, through the research and development, of stable amorphous solid dispersions to improve its solubility. The results of exploratory screening of NCL-polymer dispersions (performed through X-ray powder diffraction and kinetic solubility studies) indicate that soluplus-niclosamide dispersions can increase its aqueous solubility and, consequently, have the potential to enhance NCL bioavailability. <a>This outcome can be used for the development of oral dosage forms for clinical trials in SARS-CoV-2 and other viruses. </a></p>

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