The pharmaceutical cocrystals have sparked a lot of attention because of their ability to improve a drug’s physicochemical flaws, like poor water solubility. The amino carboxylic derivative of benzene was used to synthesized the benzocaine-based compounds which shows numerous biological activities. Here the mechanochemical solvent assisted grinding method were used to obtain the benzocaine-based co-crystals which is not reported yet before. The synthesized benzocain co-crystals were further analyzed using P-XRD and FTIR spectroscopic techniques. The shifting of IR peak from its individual compounds are clearly confirm the formation of co-crystal. From P-XRD analysis it is confirms that the benzocain compound and coformer shows different phase compare to its co-crystal which give the confirmation of co-crystal formation. The formation of co-crystals was further supported by taking their melting point which is completely different than pure component and its co-former. The Cambridge Structural Database (CSD) survey were used for structural analysis of reported benzocaine using mercury software. The crystal explorer software were used to calculate the percentage bond interactions in the reported benzocaine compound.
Cite this article:
Jeevan Dontulwar, Anuja G. Kondalkar. Green approach towards Synthesis and Structural Analysis of benzocaine-based compound and its co-crystals. Asian Journal of Research in Chemistry 2023; 16(2):169-4. doi: 10.52711/0974-4150.2023.00028
Jeevan Dontulwar, Anuja G. Kondalkar. Green approach towards Synthesis and Structural Analysis of benzocaine-based compound and its co-crystals. Asian Journal of Research in Chemistry 2023; 16(2):169-4. doi: 10.52711/0974-4150.2023.00028 Available on: https://ajrconline.org/AbstractView.aspx?PID=2023-16-2-12
1. A.V.S. Ksheera Bhavani, A. Lakshmi Usha, Kayala Ashritha, E. Radha Rani. Review on Pharmaceutical Co-Crystals and Design Strategies. Asian Journal of Pharmacy and Technology. 2021; 11(2):175-0.
2. Warid Khayata, Duaa AL Zakri. Two Simple Spectrophotometric Methods for the Simultaneous Determination of Benzocaine and Phenazone. Research J. Pharm. and Tech 2018; 11(6): 2507-2511.
3. Swapnil R. Lahamage, Avinash B. Darekar, Ravindra B. Saudagar. Pharmaceutical Co-Crystallization. Asian J. Res. Pharm. Sci. 6(1): Jan.-Mar., 2016; Page 51-58.
4. Chameli S. Daingade, Bhavna U. Jain, Manish Kondawar. Pharmaceutical Co-Crystalization: A Review. Res. J. Pharma. Dosage Forms and Tech.2019; 11(2):143-146.
5. Sevukarajan M, Thanuja Bachala, Riyaz Sodanapalli, Rahul Nair. Co-Crystals: An Emerging Trend in Pharmaceutical Industry. Research J. Pharm. and Tech. 4(6): June 2011; Page 891-902.
6. Ramu Samineni, Jithendra Chimakurthy, Sumalatha. K, Dharani G, Rachana J, Manasa K, Anitha P. Co-Crystals: A Review of Recent Trends in Co Crystallization of BCS Class II Drugs. Research J. Pharm. and Tech. 2019; 12(7):3117-3124.
7. Vikram R. Shinde, Yogesh V. Pore, J. Venkateshwara Rao. A Novel Co-crystallization Technique to enhance the Physicochemical property of BCS Class-II drugs using Efavirenz as a model drug. Research Journal of Pharmacy and Technology. 2022; 15(4):1603-9.
8. Stahly, G. P. Diversity in Single- and Multiple-Component Crystals. The Search for and Prevalence of Polymorphs and Cocrystals. Crystal Growth & Design. 2007; 7 (6): 1007–1026.
9. Chetan Hasmukh Mehta, Poojary Pooja Srinivas, Anusha SB, Kirollos Bahaa Fathy Mahany, KB Koteshwara, Usha Yogendra Nayak. Computational and Experimental Insights in Design and Development of Aceclofenac Co-Crystals. Research Journal of Pharmacy and Technology. 2022; 15(8):3709-6.
10. A. V. Yadav, A. S. Shete, A. P. Dabke, P. V. Kulkarni, and S. S. Sakhar, CoCrystals: A Novel Approach to Modify Physicochemical Properties of Active Pharmaceutical Ingredients, Indian J Pharm
11. Jino Elsa Thomas, Usha Y Nayak, Jagadish PC, Koteshwara KB. Design and Characterization of Valsartan Co-Crystals to Improve its Aqueous Solubility and Dissolution Behavior. Research J. Pharm. and Tech. 2017; 10(1): 26-30.
12. Madhuri Gaddam, Nagaraju Ravouru. A Crystal Engineering design to enhance the Solubility, Dissolution, Stability and Micromeritic properties of Omeprazole via Co-crystallization Techniques. Research J. Pharm. and Tech. 2021; 14(1):356-362.
13. Polymorphs, Salts, and Cocrystals: What’s in a Name?, American Chemical Society. Cryst. Growth Des. 2012, 12, 2147−2152.
14. Bairagi, Keshab M., et al. Interplay of Halogen and Hydrogen Bonding through Co–Crystallization in Pharmacologically Active Dihydropyrimidines: Insights from Crystal Structure and Energy Framework. Chem Plus Chem. 2021; 86 (8): 1167-1176.
15. Bairagi, Keshab M., et al. Crystal structure of a 1: 1 cocrystal of nicotinamide with 2-chloro-5-nitrobenzoic acid. Acta Crystallographica Section E: Crystallographic Communications. 2019; 75(11): 1712-1718.
16. S. S. Buddhadev, K. C. Garala, Proceedings - Pharmaceutical Cocrystals—A Review. Published: 8 March 2021.
17. Brittain, H.G. Cocrystal systems of pharmaceutical interest: 2010. Cryst. Growth Des. 2011, 12, 1046–1054.
18. Jones, W.; Motherwell, W.S.; Trask, A.V. Pharmaceutical cocrystals: An emerging approach to physical property enhancement. MRS Bull. 2006, 31, 875–879.
19. Demare, Patricia; Regla, Ignacio. Synthesis of Two Local Anesthetics from Toluene: An Organic Multistep Synthesis in a Project-Oriented Laboratory Course. Journal of Chemical Education. 2012; 89 (1): 147.
20. Monographs: Pharmaceutical substances: Benzocainum – Benzocaine. The International Pharmacopoeia. Retrieved September 29, 2009.
21. D’Ans-Lax, Taschenbuch für Chemiker und Physiker, Auflage, Band , Springer Verlag 1982, ISBN 3-540-12263-X.
22. Paczkowska, Magdalena, et al. The analysis of the physicochemical properties of benzocaine polymorphs. Molecules 23.7 (2018): 1737.