1,720,956 research outputs found
A comprehensive overview of the role of intermolecular interactions in amorphous solid dispersions
No full textMany recent studies have indicated that drug-polymer intermolecular interactions are an important aspect of amorphous solid dispersions (ASDs) and determine many of the properties of this type of formulations. In this review, a comprehensive overview is given of the latest insights with respect to intermolecular interactions in ASDs. The thermodynamic properties and theoretical considerations of the interactions are discussed, followed by a detailed and critical overview of the various solid-state analysis techniques used to probe interactions at the disposal of the formulation scientist. As the physical stability and the pharmaceutical performance of the ASD are its most crucial properties, the most recent understanding of the influence of drug-polymer interactions on these aspects is addressed as well. It is clear that intermolecular interactions may provide many advantages for ASDs but need to be weighed against the possible disadvantages. Further investigation into the interplay and trade-off between physical stability and dissolution properties is necessary in order to be able to take full advantage of the possible benefits of the interactions.The authors would like to thank Fonds Wetenschappelijk Onderzoek Vlaanderen (FWO) (grant number 1SD5524N) for their support
Molecular miscibility of ASD blend components: an evaluation of (the added value of) solid state NMR spectroscopy and relaxometry
No full textIn order to evaluate the stability of an amorphous solid dispersion (ASD) it is crucial to be able to accurately determine whether the ASD components are homogeneously mixed or not. Several solid-state analysis techniques are at the disposal of the formulation scientist, such as for example modulated differential scanning calorimetry (mDSC) and solid-state nuclear magnetic resonance spectroscopy (ssNMR). ssNMR is a robust, versatile, and accurate analysis technique with a large number of application possibilities. Especially ssNMR relaxometry, which allows the measurement of the proton relaxation times T1H and T1rH, is very useful for evaluating the miscibility of ASDs. In this paper, the miscibility of a model ASD, composed of indomethacin (IND) and poly(vinylpyrrolidone-co-vinyl acetate) (PVPVA), was assessed using mDSC and various ssNMR techniques, in order to compare the different techniques and to evaluate the advantages and disadvantages of each. It was found that measuring the relaxation times via the chemical shift selective carbon signals using 13C-cross-polarization magic angle spinning (13C-CPMAS) is still the golden standard to evaluate miscibility, even giving information about the miscibility at the nm scale. Although non-chemical shift selective 1Hwideline measurements are significantly faster than 13C-CPMAS measurements to determine the relaxation times, the results are often hard to interpret, especially with regard to the T1rH relaxation times. 2D 1H-13C dipolar heteronuclear correlation (dipolar HETCOR) NMR is an additional technique that can be used, and which provides information about the special proximity of 1H and 13C nuclei with respect to each other and therefore about the miscibility of the components at the nm scale. Additionally, it often allows to acquire information regarding the intermolecular interactions and the functional groups involved. Nevertheless, optimalization of the experiments, data processing and interpretation of the results require some expertise. Compared to mDSC, the ssNMR techniques are more sensitive and robust and can often provide information about the miscibility at nm scale. However, mDSC is a very fast analysis technique that requires less optimalization. Therefore, it remains recommended to use mDSC always for a first screening and as a complementary analysis technique. (c) 2025 American Pharmacists Association. Published by Elsevier Inc. All rights are reserved, including those for text and data mining, AI training, and similar technologies.This project is funded by a strategic basic research grant for L.C. from FWO Vlaanderen (Fonds voor Wetenschappelijk Onderzoek Vlaanderen) (grantnumber 1SD5524N). This work is also supported by Hasselt University and FWO Vlaanderen via the Hercules project AUHL/15/2 - GOH3816N
Investigating the Potential of Ethyl Cellulose and a Porosity- Increasing Agent as a Carrier System for the Formulation of Amorphous Solid Dispersions
No full textIn the present work, an insoluble polymer, i.e., ethyl cellulose (EC), was combined with the water-soluble polyvinylpyrrolidone (PVP) as a carrier system for the formulation of amorphous solid dispersions. The rationale was that by conjoining these two different types of carriers a more gradual drug release could be created with less risk for precipitation. Our initial hypothesis was that upon contact with the dissolution medium, PVP would be released, creating a porous EC matrix through which the model drug indomethacin could diffuse. On the basis of observations of EC as a coating material, the effect of the molecular weight of PVP, and the ratio of EC/PVP on the miscibility of the polymer blend, the solid state of the solid dispersion and the drug release from these solid dispersions were investigated. X-ray powder diffraction, modulated differential scanning calorimetry, and solid-state nuclear magnetic resonance were used to unravel the miscibility and solid-state properties of these blends and solid dispersions. Solid-state nuclear magnetic resonance appeared to be a crucial technique for this aspect as modulated differential scanning calorimetry was not sufficient to grasp the complex phase behavior of these systems. Both EC/PVP K12 and EC/PVP K25 blends were miscible over the entire composition range, and addition of indomethacin did not alter this. Concerning the drug release, it was initially thought that more PVP would lead to faster drug release with a higher probability that all of the drug molecules would be able to diffuse out of the EC network as more pores would be created. However, this view on the release mechanism appeared to be too simplistic as an optimum was observed for both blends. On the basis of this work, it could be concluded that drug release from this complex ternary system was affected not only by the ratio of EC/PVP and the molecular weight of PVP but also by interactions between the three components, the wettability of the formulations, and the viscosity layer that was created around the particles.status: Publishe
Exploring the influence of hydrogen bond donor groups on the microstructure and intermolecular interactions of amorphous solid dispersions containing diflunisal structural analogues
No full textThe authors would like to thank Fonds Wetenschappelijk Onderzoek Vlaanderen (FWO) for their support. Mass spectrometry was made possible by the support of the Hercules Foundation of the Flemish Government (grant 20100225-7) . This work is also supported by Hasselt University and FWO Vlaanderen via the Hercules project AUHL/15/2-GOH3816N. Finally, Gunter Reekmans is thanked for some of the NMR measurements
Going Beyond Counting First Authors in Author Co-citation Analysis
Full text linkThe present study examines one of the fundamental aspects of author co-citation analysis (ACA) - the way co-citation
counts are defined. Co-citation counting provides the data on which all subsequent statistical analyses and mappings
are based, and we compare ACA results based on two different types of co-citation counting - the traditional type that
only counts the first one among a cited work's authors on the one hand and a non-traditional type that takes into
account the first 5 authors of a cited work on the other hand. Results indicate that the picture produced through this non-traditional author co-citation counting contains more coherent author groups and is therefore considerably clearer. However, this picture represents fewer specialties in the research field being studied than that produced through the traditional first-author co-citation counting when the same number of top-ranked authors is selected and analyzed. Reasons for these effects are discussed
Variations on the Author
Full text link“Variations on the Author” discusses two of Eduardo Coutinho’s recent films (Um Dia na Vida, from 2010, and Últimas Conversas, posthumously released in 2015) and their contribution to the general question of documentary authorship. The director’s filmography is characterized by a consistent yet self-effacing form of authorial self-inscription: Coutinho often features as an interviewer that rather than express opinions propels discourses; an interviewer that is good at listening. This mode of self-inscription characterizes him as an author who is not expressive but who is nonetheless markedly present on the screen. In Um Dia na Vida, however, Coutinho is completely absent form the image, while Últimas Conversas, on the contrary, includes a confessional prologue that moves the director from the margins to the center of his films. This article examines the ways in which these works stand out in the filmography of a director who offers new insights into the notion of cinematic authorship
Appropriate Similarity Measures for Author Cocitation Analysis
Full text linkWe provide a number of new insights into the methodological discussion about author cocitation analysis. We first argue that the use of the Pearson correlation for measuring the similarity between authors’ cocitation profiles is not very satisfactory. We then discuss what kind of similarity measures may be used as an alternative to the Pearson correlation. We consider three similarity measures in particular. One is the well-known cosine. The other two similarity measures have not been used before in the bibliometric literature. Finally, we show by means of an example that our findings have a high practical relevance.information science;Pearson correlation;cosine;similarity measure;author cocitation analysis
Dispelling the Myths Behind First-author Citation Counts
Full text linkWe conducted a full-scale evaluative citation analysis study of scholars in the XML research field to explore just how different from each other author rankings resulting from different citation counting methods actually are, and to demonstrate the capability of emerging data and tools on the Web in supporting more realistic citation counting methods. Our results contest some common arguments for the continued
use of first-author citation counts in the evaluation of scholars, such as high correlations between author rankings by first-author citation counts and other citation
counting methods, and high costs of using more realistic citation counting methods that are not well-supported by the ISI databases. It is argued that increasingly available digital full text research papers make it possible for citation analysis studies to go beyond what the ISI databases have directly supported and to employ more
sophisticated methods
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