The aim of this work was to compare mesoporous carriers based on silica and magnesium aluminosilicate in the amorphous solid dispersion production. Darunavir has been selected as an active pharmaceutical ingredient that is classified as a Class 2 BCS substance and exists in two commercially available forms: crystalline ethanolate and amorphous. In the course of the study, the conditions for the preparation of amorphous samples with the selected carriers were evaluated within the framework of the most common methods for obtaining solid dispersions - hot-melt extrusion, solvent wetting, and spray drying. It was determined that the obtained dispersion properties almost completely repeat the properties of the corresponding carriers. The resulting dispersions were examined in a dissolution test and the best ones was used to formulate tablets, which were studied in an in vitro dissolution test with the original Prezista. The proposed tablet formulation showed improved dissolution compared to the original one. It was also found that silica supports have a greater positive contribution to darunavir dissolution - both ethanolate or amorphous forms.
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http://dx.doi.org/10.1016/j.ejps.2021.105700 | DOI Listing |
Angew Chem Int Ed Engl
January 2025
Fudan University, 2005 Huhu Rd, Shanghai, CHINA.
All-solid-state lithium metal batteries are regarded as next-generation devices for energy storage due to their safety and high energy density. The issues of lithium dendrites and poor mechanical compatibility with electrodes present the need for developing solid-state electrolytes with high stiffness and damping, but it is a contradictory relationship. Here, inspired by the superstructure of tooth enamel, we develop a composite solid-state electrolyte composed of amorphous ceramic nanotube arrays intertwined with solid polymer electrolytes.
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January 2025
Institute of Drug Metabolism and Pharmaceutical Analysis, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 310058, China.
Freeze drying is one of the common methods to extend the long-term stability of biologicals. Biological products in solid form have the advantages of convenient transportation and stable long-term storage. However, long reconstitution time and extensive visible bubbles are frequently generated during the reconstitution process for many freeze-dried protein formulations, which can potentially affect the management efficiency of staff, patient compliance, and product quality.
View Article and Find Full Text PDFChemistry
January 2025
Universite Claude Bernard Lyon 1, ICBMS, Bâtiment Lederer, 1 Rue Victor Grignard, F-69622, Villeurbanne, FRANCE.
In this article we describe research on the synthesis and characterization of a family of "Janus" amphiphiles composed of disaccharide head groups and alkaloid units joined together via a methylene linker, and bearing a lateral aliphatic chain of varying length. The condensed phases formed by self-organization of the products as a function of temperature were characterized by differential scanning calorimetry, thermal polarized light microscopy, and small angle X-ray scattering, allied with computational modelling and simulations. Structural studies on heating specimens from the solid showed that some homologues exhibited lamellar, columnar and bicontinuous mesophases, whereas the same homologues revealed different phase sequences on cooling from the amorphous liquid.
View Article and Find Full Text PDFSmall
January 2025
Dept. of Plant and Environmental Sciences, Weizmann Institute of Science, Rehovot, 7610001, Israel.
Transient amorphous phases are known as functional precursors in the formation of crystalline materials, both in vivo and in vitro. A common route to regulate amorphous calcium carbonate (ACC) crystallization is via direct interactions with negatively charged macromolecules. However, a less explored phenomenon that can influence such systems is the electrostatically driven formation of Ca-macromolecule dense phases.
View Article and Find Full Text PDFAAPS PharmSciTech
January 2025
Department of Chemistry, Center for Physical and Mathematical Sciences, Federal University of Santa Catarina, Florianópolis, SC, 88040-900, Brazil.
Developing orally administered pediatric formulations presents significant challenges due to the unique characteristics of pediatric patients. Terbinafine hydrochloride (TER), a powerful antifungal agent, is effective against various fungal infections, including Tinea capitis, which is common in children. However, its low aqueous solubility necessitates innovative pharmaceutical strategies to enhance its effectiveness.
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