Measurement of drug solubility is one of the key elements of compound characterization during the drug discovery and development process. A broad variety of solubility assay methods have been developed, including equilibrium method which requires analysis of the equilibrium composition and kinetic method which monitors the concentration of a compound dynamically at the time when a precipitate first appears or disappears in the solution. Despite the numerous experimental methods, precise drug solubility values are hard to obtain for time-consuming, sample size and manual work. In this article, we reported a new method, namely air humidity solubility assay, which measures the relative humidity of the air in equilibrium with the solution at a given temperature, and then calculates solubility from the relative humidity according to extended-non random two liquid (NRTL) model. NaCl was used as a model drug, and the solubility was measured at the temperature of 20-50 ℃. The results indicate that the solubility of NaCl determined with the new method is generally comparable to that determined by gravimetry that is reported in literature. The new method has a relative error of less than 2%. Although the accuracy is lower than that of gravimetry, air humidity solubility assay is more convenient, practical, operational and universal. This method provides a supplement to the existing methods.
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Pharmaceutics
December 2024
Escuela Superior de Medicina, Instituto Politécnico Nacional, Ciudad de México 11340, Mexico.
Curcumin appears to be well tolerated and effective for managing chronic inflammatory pain, but its poor oral bioavailability has been a hurdle in its use as a therapeutic agent. The current study was performed to characterize a novel co-amorphous compound based on curcumin/L-arginine 1:2 (CAC12). : Stability, solubility and structural characterization of the CAC12 were carried out by spectrometry techniques and in vitro assays, whereas the antinociceptive and anti-inflammatory effects were evaluated by CFA or carrageenan models.
View Article and Find Full Text PDFInt J Pharm
January 2025
Department of Pharmaceutics, University of Minnesota, 308 Harvard St. S.E., Minneapolis, MN 55455, USA. Electronic address:
Salt formation has been extensively used to modulate and improve the properties of active pharmaceutical ingredients (API), such as solubility, stability and mechanical properties. Tablets of the anti-angina drug, trimetazidine (TMZ) are currently manufactured using the wet granulation process, rather than the more cost-effective direct compression method. In an effort to address the two main challenges associated with the commercial dihydrochloride salt (TMZ-2HCl), i.
View Article and Find Full Text PDFFood Res Int
February 2025
Institute of Agrochemistry and Food Technology (IATA-CSIC), Carrer del Catedràtic Agustín Escardino Benlloch, 7, 46980 Paterna, Valencia, Spain; Department of Food and Human Nutritional Sciences, University of Manitoba. Winnipeg, Canada. Electronic address:
High-pressure processing (HPP) enhances food safety and shelf life by inactivating microorganisms and preserving food quality, yet its effectiveness in low-humidity environments has not been evaluated. This study investigated the effects of HPP at 500 MPa for 15 min across varying hydration levels (15, 30, 60, 77 %) on rice bran (RB), aiming to identify microbial effectiveness, besides techno-functional and physicochemical properties. HPP effectively reduced mesophilic bacteria, molds and yeast of RB at > 15 % hydration level, achieving reductions of up to 4 logarithmic cycles in the latter, nearing the detection limit of the method.
View Article and Find Full Text PDFBraz J Biol
January 2025
Universidade Tecnológica Federal do Paraná - UTFPR, Departmeno de Química e Ciências Biológicas, Francisco Beltrão, PR, Brasil.
Studies show that propolis has antimicrobial, antifungal, antiviral, anti-inflammatory, antioxidant, antitumor, and immunomodulatory properties, and may protect against diseases such as diabetes, cardiovascular disease, and cancer. We aimed to extract compounds of brown propolis with hydroalcoholic solvents and evaluate their cytotoxic activity on tumor and non-tumor cells by MTT test. We tested the solute:solvent ratio (ethanol:water) and extraction time in a Shaker incubator (710 rpm) before conducting a central composite rotational design (CCRD) to optimize time and solvent mixture.
View Article and Find Full Text PDFPlant Physiol Biochem
January 2025
Center for Nuclear Energy in Agriculture, University of São Paulo, Piracicaba, 13416-000, Brazil.
Increasing nitrogen use efficiency (NUE) remains a crucial topic in contemporary agriculture. Inoculation with endophytic diazotrophic bacteria offers a potential solution, but the results vary with the N-fertilization regime. Here, we examined the efficacy of inoculation with Herbaspirillum seropedicae strain HRC54 in enhancing NUE and promoting the growth of Marandu palisadegrass with varying levels of N-urea (0, 25, 50, and 100 mg N kg soil⁻).
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