GREEN CHEMICAL SYNTHESIS AND PROPERTIES OF SOLID DISPERSIONS OF BENZIMIDAZOLE –Β. NAPHTHOL BINARY DRUG SYSTEM

Main Article Content

H. Shekhar
Manoj Kumar

Keywords

SLE, Mixing and excessthermodynamic functions, thermal stability, Interfacial energy, Driving force of nucleation, Critical radius

Abstract

With view to synthesize and characterize the enhanced pharmaceutical properties of the solid-liquid dispersions of binary drug system through green chemical technique the present communication have been undertaken for detailed investigation of thermodynamic and interfacial properties of benzimidazole (BI) and β. naphthol (βN) binary eutectic and non-eutectic drug dispersions. Eutectic solid dispersion was observed at 0.657 mole fraction of β. naphthol (βN) and at melting temperature 90°C.


Thermodynamic quantities; Partial and Integral  excess Gibbs energy (gE), excess enthalpy (hE), excess entropy (sE) of eutectic and non-eutectic dispersions were determined with the help of activity coefficient data. The negative deviation from ideal behaviorhas been seen in the system which refers stronger association between unlike molecules during formation of binary mix. The negative value of Gibbs free energy of mixing (DGM) refers the mixing for all eutectic and non-eutectic dispersions is spontaneous. The solid-liquid interfacial characteristics i.e., entropy of fusion per unit volume (DSV), solid-liquid interfacial energy (s), roughness parameter (α), grain boundary energy and roughness parameter (α) of eutectic and non-eutectic solid dispersions have been reported.


The size of critical nucleus at different undercoolings has been found in nanoscale, which may be a big significance in pharmaceutical world. The value of roughness parameter, α > 2 was observed which manifests the faceted and irregular growth leads in the system.

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References

1. Arora Shefali. Study of Some Benzimidazole Compounds as Antibacterial and Antifungal Agents. J. Pharm. Sci. & Res. 3 (2011) 1310-1314.
2. Michele Tonelli, Matteo Simone, et al. Antiviral activity of benzimidazole derivatives. II. Antiviral activity of 2-phenylbenzimidazole derivatives. Bioorganic & Medicinal Chemistry 18 (2010) 2937-2953.
3. Ingle R. G. and Magar D. D. Heterocyclic Chemistry of Benzimidazoles and potential Activities of Derivatives. Int. J. Drug Res. Tech. 1 (2011) 26-32.
4. Chinnadurai Satheeshkumar1, Mahalingam Ravivarma1, et al., Synthesis, Antimicrobial and Molecular Docking studies of Benzimidazole and Benzotriazole based Dicationic Sulphonophanes. Canadian Chemical Transactions 2 (2014) 248-257.
5. Rajakumar P., Sekar K., Shanmugaiah V., Mathivanan N. Synthesis of some novel imidazole-based diactionic carbazolophanes as potential antibacterials. Bioorg. Med. Chem. Lett. 18 (2008) 4416-4419.
6. Boiani M., Gonzalez M. Imidazole and benzimidazole derivatives as chemotherapeutic agents. Mini-Rev. Med. Chem. 5 (2005) 409-424.
7. Zhang L., Peng X. M., Damu G. L. V., Geng R. X., Zhou C. H. Comprehensive Review in Current Developments of Imidazole-Based Medicinal Chemistry. Med. Res. Rev. (2013) 1-98.
8. Sharma M. C.,Kohli D. V., Sharma Smita and Sharma A. D. Synthesis and antihypertensive activity of some new benzimidazole derivatives of 4’-(6-methoxy-2-substituted-benzimidazole-1-ylmethyl)- biphenyl-2-carboxylic acid in the presences of BF3.OEt2. Pelagia Research Library 1 (2010) 104-115.
9. S. Khokra L. &Choudhary Deepika. Benzimidazole an important Scaffold in drug Discovery. Asian Journal of Biochemical and Pharmaceutical Research 3 (2011).
10. Yu. L. & Reutzel-Edens S. M. Crystallization, Encyclopedia of Food Sciences and Nutrition (Second Ed.), Elsivier Science Ltd. Amsterdam (2003).
11. Shekhar H. and kumar Manoj. Thermodynamic and interfacial studies on solid dispersion of phenothiazine-2-methylimidazole drug system, Journal of Chemistry and Pharmaceutical Research, 7(2015) 37-45.
12. Salim S. S., Ph. D. Thesis, Study of Multiphase Organic Materials, V. K. S. University, Ara, Bihar (2009).
13. Kant Vishnu and Shekhar H., Phase Behaviour, Molecular Interaction and Morphological Studies on Co-crystals of nicotinamide-p-Nitroaniline Drug System, International Journal of Pure and Applied Chemistry, 9 (2014) 127-137.
14. Shekhar H. and Salim S.S., Themodynamics of Organic Alloys: Mixing and Excess Function. J. Indian Chem. Soc. 91 (2014) 2189-2196.
15. Kumar Manoj and Shekhar H.,Thermodynamic and Interfacial Investigation of Phenothiazine-Resorcinol Binary System. Internation Journal of Chemistry 4 (2015) 257-268.
16. Wisniak J. & Tamir A. Mixing and Excess Thermodynamic Properties (a literature source book), Phys. Sci. Data 1, Elsevier, New York (1978).
17. Singh, N. B. & Glicksman, M. E. Determination of the mean solid-liquid interface energy of pivalic acid. Journal Cryst Growth 98 (1989) 573-580.
18. Turnbull, D. Formation of Crystal nuclei in Liquid Metals. J. Chem. Phys. 21 (1950) 1022-1027.
19. Hunt J. D & Lu S. Z. 1994. Hand Book of Crystal Growth Ed. DTJ Hurle, Elsevier, Amsterdam, 112.
20. Shekhar H. & Kant Vishnu. Thermodynamics of Nicotinamide Based Binary Drug System, Lambert Academic publishing Germany (2013).
21. Gupta P., Agrawal T. Das S. S. & Singh N. B. Solvent Free Reactions, Reactions of Nitrophenols in 8-Hydroxyquinoline-Benzoic Acid Eutectic Melt, Journal of Thermal Analysis and Calorimetry 104 (2011) 1167-1176.
22. Chadwick G. A. Metallography of Phase Transformation, Butterworths, London 61 (1972).
23. Nieto R., Gonzalez M. C. and Herrero F. Thermodynamics of mixtures, Function of mixing and excess functions, American Journal of Physics 67 (1999) 1096-1099.
24. Hunt, J. D. & Jackson, K. A. Binary Eutectic Solidification. Trans Metall Soc AIME. 236 (1966) 843-852.
25. Bai Xian-Ming & Li Mo. Calculation of Solid-liquid interfacial free energy: A classical nucleation theory based approach, J. of Chem. Phy. 124(2006) 124707-12.