Pharmaceuticals Solubility is Still Nowadays Widely Studied
Everywhere Fleming Martínez1*, Abolghasem Jouyban2,3, William E. Acree Jr.4 1Grupo de Investigaciones Farmacéutico Fisicoquímicas, Departamento de Farmacia, Facultad de Ciencias, Universidad Nacional de Colombia –Sede Bogotá, Cra. 30 No. 45-03, Bogotá D.C., Colombia. 2Pharmaceutical Analysis Research Center and Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
3 Kimia Idea Pardaz Azarbayjan (KIPA) Science Based Company, Tabriz University of Medical Sciences, Tabriz, Iran. 4Department of Chemistry, University of North Texas, Denton, TX 76203-5070, USA.
Equilibrium solubility is a thermodynamic property physico-chemical properties such as Abraham or
of great importance in pharmaceutical area from Catalan parameters within the common cosolvency both practical and theoretical viewpoints. It is models for providing better predictions and involved in several pharmaceutical procedures like extending the applicability of the models to drug purification processes, drug identification, and include additional solute-solvent combinations.6 homogenous pharmaceutical dosage forms design.1 Moreover, from solubility values and some Although solubility is a macroscopic property it is thermodynamic properties of the solvent mixture employed to analyze the respective molecular free of drug, the preferential solvation of several interactions involved in dissolution processes.2 drugs has been analyzed by means of the inverse Drug solubility defines the possible state of the Kirkwood-Buff integrals (IKBI) method. If the pharmaceutical dosage form under consideration. solubility increases constantly with the proportion This is of fundamental relevance if liquid solutions of cosolvent to reach the maximum in the neat are solicited. Moreover, it is generally observed cosolvent, the solute is preferentially solvated by that the more soluble drugs also exhibit higher water in water-rich mixtures but preferentially dissolution rates in the respective solvents.3 In this solvated by cosolvent in cosolvent-rich mixtures. way, the experimental determination and On the other hand, when the maximum solubility is correlation of the solubility of drugs in neat and obtained in a cosolvent-water mixture instead of mixed solvents has been a constantly increasing the neat cosolvent, the solute is preferentially research subject. Normally, the specific references solvated in water-rich and cosolvent-rich mixtures report the effect of temperature and/or mixtures but preferentially solvated by cosolvent in those composition on solubility. Temperature effect is mixtures of similar proportions of water and commonly evaluated by using several empirical or cosolvent.7 Finally, it is noteworthy the increasing semiempirical models like van’t Hoff, Apelblat, in the number of articles published in several Buchowski-Ksiazczak and Wilson. Mixtures journals around the world dealing with solubility composition effect is evaluated by means of and solution thermodynamics of drugs in neat and Yalkowsky-Roseman log-linear and the Nearly mixed solvents reveal that despite of various Ideal Binary Solvent/Redlich-Kister (NIBS/R-K) available solubility prediction methods reported in models as cosolvency prediction tools. the literature, one needs to rely on the experimental Furthermore, the combined effects of temperature determination of drug’s solubility and further and mixtures composition are analyzed by means improvements in the solubility prediction methods of the Jouyban-Acree model.4 Observed deviations is still required.8 Development of better predictive from predicted solubility values by some of these methods is greatly facilitated by accurate solubility models have been attributed to specific measurements using modern instrumentation and interactions. For instance, negative deviations to technology. Yalkowsky model in water-rich mixtures has been interpreted as the effect of hydrophobic hydration References around the non-polar groups of the solute, which 1. Jouyban A. Handbook of Solubility Data for reduce the solubility, whereas, the positive Pharmaceuticals. Boca Raton. FL: CRC Press; deviations observed in cosolvent-rich mixtures has 2010. p. 40-6. been considered as an effect of the solute solvation 2. Marcus Y. On the preferential solvation of by the cosolvent to obtain a less polar entity.5 A drugs and PAHs in binary solvent mixtures. J number of attempts were made to include some
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