(Marathwada Mitramandal’s College of Pharmacy, Department of Pharmaceutics, Thergaon, Pune, India)
(Government College of Pharmacy, Department of Pharmacology, Aurangabad, Maharashtra, India)
Yıl: 2020Cilt: 17Sayı: 2ISSN: 1304-530X / 2148-6247Sayfa Aralığı: 228 - 234İngilizce

52 0
Extended Hildebrand Solubility Approach: Prediction and Correlation of the Solubility of Itraconazole in Triacetin: Water Mixtures at 298.15°K
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 W as a function of the solubility parameter (δ1 ) of the solvent mixture. Similarly, the solubilities were predicted by direct method based on the use of logarithmic experimental solubilities (logX2 ) against the solubility parameter (δ1 ) 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.
DergiAraştırma MakalesiErişime Açık
  • 1. Pardeike J, Weber S, Haber T, Wagner J, Zarfl HP, Plank H, Zimmer A. Development of an Itraconazole-loaded nanostructured lipid carrier (NLC) formulation for pulmonary application. Int J Pharm. 2011;419:329- 338.
  • 2. Peeters J, Neeskens P, Tollenaere JP, Van Remoortere P, Brewster ME. Characterization of the interaction of 2-hydroxypropyl- β-cyclodextrin with itraconazole at pH 2, 4, and 7. J Pharm Sci. 2002;91:1414-1422.
  • 3. Wu PL, Martin A. Extended Hildebrand solubility approach: p-hydroxybenzoic acid in mixtures of dioxane and water. J Pharm Sci. 1983;72:587-592.
  • 4. Subramanyam CVS, Sreenivasa RM, Venkata Rao J, Gundu Rao P. Irregular solution behaviour of paracetamol in binary solvents. Int J Pharm. 1992;78:17-24.
  • 5. Martin A, Newburger J, Adjei A. Extended Hildebrand solubility approach: solubility of theophylline in polar binary solvents. J Pharm Sci.1980;69:487-491.
  • 6. Bustamante P, Escalera B, Martin A, Selles E. A modification of the extended Hildebrand approach to predict the solubility of structurally related drugs in solvent mixtures. J Pharm Pharmacol. 1993;45:253- 257.
  • 7. Rathi PB, Mourya VK. Extended Hildebrand solubility approach: satranidazole in mixtures of dioxane and water. Indian J Pharm Sci. 2011;73:315-319.
  • 8. Sotomayor RG, Holguín AR, Cristancho DM, Delgado DR, Martínez F. Extended Hildebrand solubility approach applied to piroxicam in ethanol + water mixtures. J Mol Liq. 2013;180:34-38.
  • 9. Delgado DR, Peña MA, Martínez F. Extended Hildebrand solubility approach applied to some sulphapyrimidines in some {methanol (1) + water (2)} mixtures. Phy Chem Liq. 2017;256:176-188.
  • 10. Martin A, Miralles MJ. Extended Hildebrand solubility approach: solubility of tolbutamide, acetohexamide and sulfisomidine in binary solvent mixtures. J Pharm Sci. 2006;71:439-442.
  • 11. Fukui E, Miyamura N, Yoneyama T, Kobayashi M. Drug release from and mechanical properties of press-coated tablets with hydroxypropylmethylcellulose acetate succinate and plasticizers in the outer shell. Int J Pharm. 2001;217;33-43.
  • 12. Chang DP, Garripelli VK, Rea J, Kelley R, Rajagopal K. Investigation of fragment antibody stability and its release mechanism from poly(lactideco-glycolide)-triacetin depots for sustained-release applications. J Pharm Sci. 2015;104:3404-3417.
  • 13. Fiume MZ, Panel CIRRE. Final report on the safety assessment of triacetin. Int J Toxicol. 2003;22:1-10.
  • 14. Yuksel N, Baykara M, Shirinzade H, Suzen, S. Investigation of triacetin effect on indomethacin release from poly (methyl methacrylate) microspheres: evaluation of interactions using FT-IR and NMR spectroscopies. Int J Pharm. 2011;404:102-109.
  • 15. Liu H, Venkatraman SS. Cosolvent effects on the drug release and depot swelling in injectable in situ depot-forming systems. J Pharm Sci. 2012;101:1783-1793.
  • 16. Higuchi T, Connors KA, Phase-solubility techniques. Adv Anal Chem Instr. 1965;4:117-122.
  • 17. Fedors RF. A method for estimating both the solubility parameters and molar volumes of liquids. Polym Eng Sci. 1974;14:147-154.
  • 18. Cárdenas ZJ, Almanza OA, Jouyban A, Martínez F, Acree Jr WE. Solubility and preferential solvation of phenacetin in methanol + water mixtures at 298.15 K. Phy Chem Liq. 2018;56:16-32.
  • 19. Cristancho DM, Delgado DR, Martínez F. Meloxicam solubility in ethanol + water mixtures according to the extended Hildebrand solubility approach. J Solution Chem. 2013;42:1706-1716.
  • 20. Yalkowsky SH, Roseman TJ. Solubilization of drugs by cosolvents. In: Yalkowsky SH (ed). Techniques of Solubilization of Drugs. New York; Marcel Dekker, Inc; 1981:91-134.
  • 21. Rubino JT, Obeng EK. Influence of solute structure on deviations from the log-linear solubility equation in propylene glycol: water mixtures. J Pharm Sci. 1991;80:479-483.
  • 22. Li A, Yalkowsky SH, Solubility of organic solutes in ethanol/water mixtures. J Pharm Sci. 1994;83:1735-1740.
  • 23. Gómez JL, Rodríguez GA, Cristancho DM, Delgado DR, Mora CP, Yurquina A, Martínez F. Extended Hildebrand Solubility Approach applied to Nimodipine in PEG 400 + ethanol mixtures. Rev Colomb Cienc Quím Farm. 2013;42:103-121.
  • 24. Kharwade M, Achyuta G, Subrahmanyam CVS, Sathesh Babu PR. Solubility behavior of lornoxicam in binary solvents of pharmaceutical interest. J Solution Chem. 2012;41:1364-1374.
  • 25. Thimmasetty J, Subrahmanyam CVS, Sathesh Babu PR, Maulik MA. Viswanath BA. Solubility behavior of pimozide in polar and nonpolar solvents: partial solubility parameters approach. J Solution Chem. 2008;37:1365-1378.
  • 26. Rathi PB, Deshpande KV. Extended Hildebrand approach: an empirical model for solubility prediction of etodolac in 1, 4-dioxane and water mixtures. J Solution Chem. 2014;43:1886-1903.
  • 27. Cárdenas ZJ, Jiménez DM, Delgado DR, Peña MA, Martínez F. Extended Hildebrand solubility approach applied to some sulphonamides in propylene glycol + water mixtures. Phy Chem Liq. 2015;53:763-775.

TÜBİTAK ULAKBİM Ulusal Akademik Ağ ve Bilgi Merkezi Cahit Arf Bilgi Merkezi © 2019 Tüm Hakları Saklıdır.