Objectives: The aim of the study is to explore the suitability of an empirical approach for the extended Hildebrand solubility approach (EHSA) to predict and correlate the solubility of the crystalline drug itraconazole (ITRA) in triacetin: water mixtures.
Materials And Methods: The physicochemical properties of ITRA like fusion enthalpy, solubility parameter, and ideal mole fraction solubility were estimated. The solubilities of ITRA in mixed solvent blends comprising triacetin: water were determined at 298.15°K. Theoretical solubilities were back calculated using a polynomial regression equation of the interaction energy parameter as a function of the solubility parameter (δ) of the solvent mixture. Similarly, the solubilities were predicted by direct method based on the use of logarithmic experimental solubilities ( ) against the solubility parameter (δ) of the solvent mixture. The predictive capabilities of both EHSA and the direct method were compared using mean percent deviations.
Results: The solubility of ITRA was increased in all the triacetin: water blends and was highest in the blend in which the solubility parameter of ITRA equaled that of the solvent mixture. The prediction capacities of the direct method (mean % deviation was -1.89%) were better than those of EHSA (mean % deviation was 9.76%) in the fifth order polynomial.
Conclusion: The results indicated that the solubility of any crystalline solute can be adequately predicted and correlated with the mere knowledge of physicochemical properties and EHSA. The information could be of help in process and formulation development.
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http://dx.doi.org/10.4274/tjps.galenos.2019.20438 | DOI Listing |
Int J Pharm
January 2025
Department of Industrial Pharmacy, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand; Academy of Science, The Royal Society of Thailand, Bangkok 10300, Thailand; Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand; Center for Global Health Research, Saveetha Medical College and Hospitals, Saveetha Institute of Medical and Technical Sciences, Saveetha University, Chennai 602105, Tamil Nadu, India. Electronic address:
Hot-melt extrusion (HME) has emerged as a versatile and efficient technique in pharmaceutical formulation development, particularly for enhancing the solubility and bioavailability of poorly water-soluble drugs. This review delves into the fundamental principles of HME, exploring its application in drug delivery systems. A comprehensive analysis of polymers utilized in HME, such as hydroxypropyl methylcellulose, ethyl cellulose, hydroxypropyl cellulose, and polyvinylpyrrolidone, is presented, highlighting their roles in achieving controlled drug release and improved stability.
View Article and Find Full Text PDFCureus
August 2024
Department of Pharmaceutics, College of Pharmacy, Hawler Medical University, Erbil, IRQ.
Introduction: The hen's egg test on chorioallantoic membrane (HET-CAM) assay is a cost-effective and well-validated, non-animal-based method for evaluating the irritant potential and eye toxicity of substances. A colloidal dispersion of a surfactant and a cosurfactant with a nanosize range is called a nanoemulsion (NE), which is formed by mixing immiscible liquids and stabilized by surfactants. Patients with glaucoma are commonly prescribed Brimonidine (BR), an alpha-2 adrenergic agonist, to lower their intraocular pressure.
View Article and Find Full Text PDFSpectrochim Acta A Mol Biomol Spectrosc
January 2025
Vocational School of Food, Agriculture and Livestock, Bingol University, 12000 Bingol, Turkey; Chemistry Programme, Institute of Sciences, Bingol University, 12000 Bingol, Turkey. Electronic address:
Vitamin K is one of the most important fat-soluble vitamins and while there are two main types of vitamin K in nature, known as K1 (phylloquinone) and K2 (menaquinones), there is also a synthetic type of vitamin K known as K3 (menadione). Recent studies have shown that it is crucial to know the non-covalent interactions, ADME and molecular docking of molecules in different solvent media. Therefore, we have performed some quantum chemical calculations, ADME and intra-and intermolecular interaction calculations of a number of K1, K2 and K3 such as K1-water (K1 + W), K1-methanol (K1 + M), K1-triacetin (K1 + T), K2-water (K2 + W), K2-methanol (K2 + M), K2-triacetin (K2 + T), K3-water (K3 + W), K3-methanol (K3 + M), K3-triacetin (K3 + T) performed by Density Functional Theory (DFT) and Multiwfn: A multifunctional wavefunction analyzer.
View Article and Find Full Text PDFAnn Pharm Fr
November 2024
Bioequivalence Study Centre, Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700032, West Bengal, India. Electronic address:
Objective: Regardless of having desired therapeutic properties many of the recently approved drugs are removed from the developmental pipeline for their clinical use due to low solubility and permeability. Conventional dosage forms are found relatively unsuitable for achieving desired pharmacokinetic and pharmacodynamics profiles. Cilnidipine is 1,4 dihydropyridine derivative calcium channel blocker used for the treatment of hypertension.
View Article and Find Full Text PDFACS Omega
July 2024
Division of Chemical Engineering, Center of Innovative and Applied Bioprocessing (CIAB), Knowledge City, Sector-81, Mohali, Punjab 140306, India.
The development of biodegradable mulch for agricultural applications represents a sustainable approach to reducing plastic pollution. Poly(vinyl alcohol) (PVA) is one of the nontoxic and biodegradable polymers that can be used as mulching film. However, a major drawback of PVA is its moisture sensitivity, which limits its applications.
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