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Pharmaceutical Sciences

March 2017, 23, 1-2


doi: 10.15171/PS.2017.01
http://journals.tbzmed.ac.ir/PHARM

Editorial

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

*Corresponding Author: Fleming Martínez, E-mail: fmartinezr@unal.edu.co


©2017 The Authors. This is an open access article and applies the Creative Commons Attribution (CC BY), which permits unrestricted use,
distribution, and reproduction in any medium, as long as the original authors and source are cited. No permission is required from the authors
or the publishers.
Martínez et al.

Mol Liq. 2008;140(1-3):61-7. J Chem Thermodyn. 2016;97:264-76.


doi:10.1016/j.molliq.2008.01.005 doi:10.1016/j.jct.2016.02.002
3. Martin A, Bustamante P, Chun AHC. Physical 6. Jouyban A, Soltanpour S, Soltani S, Tamizi E,
Chemical Principles in the Pharmaceutical Fakhree MAA, Acree WE Jr. Prediction of drug
Sciences. 4th ed. Philadelphia, PA: Lea & solubility in mixed solvents using computed
Febiger; 1993. p. 212-43. Abraham parameters. J Mol Liq.
4. Wang J, Xu A, Xu R. Solubility of 2-nitro-p- 2009;146(3):82-8.
phenylenediamine in nine pure solvents and doi:10.1016/j.molliq.2009.02.003
mixture of (methanol + N-methyl-2- 7. Delgado DR, Peña MÁ, Martínez F, Jouyban A,
pyrrolidone) from T = (283.15 to 318.15) K: Acree WE Jr. Further numerical analyses on the
Determination and modelling. J Chem solubility of sulfapyridine in ethanol + water
Thermodyn. 2017;108:45-58. mixtures. Pharm Sci. 2016;22(3):143-52.
doi:10.1016/j.jct.2017.01.006 doi:10.15171/PS.2016.24
5. Delgado DR, Almanza OA, Martínez F, Peña 8. Jouyban A. Solubility; still a challenging
MA, Jouyban A, Acree WE Jr. Solution subject in pharmaceutical sciences: An editorial.
thermodynamics and preferential solvation of Vitae. 2010;17(3):241-2.
sulfamethazine in (methanol + water) mixtures.

2 | Pharmaceutical Sciences, March 2017, 23, 1-2

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