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Incubation time plays a critical role in the accurate measurement of equilibrium solubility of compounds. Substances which dissolve very slowly generally need long incubation times (days or weeks) to reach equilibrium. However, long times may pose several problems, such as decomposition of solute, molding of buffer, and drifting of pH. Higuchi in 1979 proposed the Facilitated Dissolution Method (FDM) to dramatically reduce incubation time. It employs a small volume of water-immiscible organic solvent to partly solubilize the sample and thereby increase the surface area available for dissolution. The method has been used only rarely. In this study we performed a systematic validation of FDM using progesterone as model compound. The reference solubility value, 7.95±0.21μg/mL (p<0.05, n=5), was determined in Britton-Robinson buffer solution (pH7.4) at 25.0°C by the standardized protocol of Saturation Shake-Flask (SSF) method. Also, the solubility was measured by the FDM approach under varied experimental conditions (e.g., type and volume of organic solvent, time of agitation, and amount of solid excess), and compared to the reference value. It was demonstrated that the small amount of organic solvent used in the FDM does not impact the measured solubility, compared to the reference value. Additionally, four compounds of low dissolution rate (dexamethasone, digoxin, haloperidol and cosalane) were used to demonstrate that FDM can reduce the long equilibration time to the standardized 24h (6h stirring and 18h sedimentation). The time dependence of solubility equilibrium was measured by SSF, and the results were compared with those obtained by FDM. Our study, based on >200 solubility experiments, supports the validity of Higuchi's method. In this study we propose a standardized protocol for the FDM, where 1% v/v of organic solvent is used. Octane (or isooctane) was found to be suitable for highly hydrophobic compounds. Alternatively, octanol or 1,2-dichloroethane can be used for less lipophilic compounds.
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http://dx.doi.org/10.1016/j.ejps.2017.05.064 | DOI Listing |
Biopolymers
January 2025
Faculty of Pharmacy, Universiti Teknologi MARA, Selangor Branch, Puncak Alam Campus, Puncak Alam, Selangor, Malaysia.
This study aims to evaluate the impact of formulation parameters on tannic acid-crosslinked gelatine (GelTA) films, intended as a mucoadhesive matrix for extended buccal drug delivery. GelTA films were prepared using the solvent evaporation technique and screened based on their mucoadhesive and dissolution characteristics. The formulation variables included the source of gelatine (bovine and fish), tannic acid concentration, pH of the film-forming solutions, and the type and concentration of plasticisers.
View Article and Find Full Text PDFSci Total Environ
December 2024
Institute of Soil and Water Conservation CAS&MWR, Yangling 712100, China; College of Soil and Water Conservation Science and Engineering, Northwest A&F University, Yangling 712100, China. Electronic address:
Agricultural soils face severe challenges, including water scarcity and heavy metal contamination. Optimizing soil remediation efficiency while minimizing inputs is essential. This study assessed the water retention and heavy metal adsorption properties of L-PH hydrogel through aqueous experiments.
View Article and Find Full Text PDFEur J Pharm Biopharm
December 2024
Departamento de Ciencias Farmacéuticas, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, Haya de la Torre and Medina Allende, Córdoba X5000HUA, Argentina; Unidad de Investigación y Desarrollo en Tecnología Farmacéutica (UNITEFA) CONICET-UNC, Córdoba X5000HUA, Argentina. Electronic address:
Albendazole, an anthelmintic recognized by the World Health Organization as an essential medicine, is known to have limitations in solubility and bioavailability. To improve these properties, binary and ternary multicomponent systems were designed employing different combinations of albendazole desmotropes with maltodextrin and aspartic acid. The impact of these systems in solution was evaluated through phase solubility analysis.
View Article and Find Full Text PDFPharm Nanotechnol
December 2024
M.M. College of Pharmacy, Maharishi Markandeshwar Deemed to be University, Mullana- 133203, Ambala, India.
Background: Tapentadol hydrochloride is a potent analgesic commonly used to manage moderate to severe pain. Rapidly dissolving tablets of Tapentadol offer a significant advantage in enhancing patient compliance by providing quick pain relief. The development of fast-dissolving tablets (FDTs) requires careful consideration of formulation parameters to achieve optimal disintegration and dissolution profiles.
View Article and Find Full Text PDFChemSusChem
December 2024
Universität Greifswald: Universitat Greifswald, Department of Biotechnology & Enzyme Catalysis, Institute of Biochemistry, GERMANY.
As global plastic consumption and littering escalate, innovative approaches to sustainable waste management are crucial. Enzymatic depolymerization has emerged as a promising recycling method for polyesters via monomer recovery under mild conditions. However, current research mainly focuses on using a single plastic feedstock, which can only be derived from complex and costly plastic waste sorting.
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