PREPARATION AND EVALUATION OF CO-CRYSTALS OF CARBAMAZEPINE WITH GLUCOMANNAN
Keywords:Carbamazepine, Co-crystals, Glucomannan, Ocimum basilicum
Objective: The objective of the present work was to inhibit transformation of carbamazepine anhydrous to its dihydrate form in aqueous medium by adopting the co-crystal approach.
Methods: Co-crystallization of carbamazepine and glucomannan as co-former was carried out by solution mediated phase transformation. The solution of carbamazepine and glucomannan in ethanol (95%) was agitated for 2 h and the co-crystals obtained were recovered after 24 h.
Results: Co-crystal formation due to hydrogen bonding between carbamazepine and glucomannan as a co-former was confirmed by FTIR study. Inhibition of transformation of co-crystal of carbamazepine to carbamazepine dihydrate in aqueous medium was confirmed by SEM.
Conclusion: Inhibition of transformation of carbamazepine co-crystal to its dihydrate form resulted in its improved dissolution. Dissolution efficiency of carbamazepine in its co-crystal was increased up to 79.26% within 30 min.
Khoo V. Process Induced Phase Transformation of Carbamazepine Dihydrate to its Polymorphic Anhydrates. Powder Technology. 2013;236:114-121.
Hardikar SR, Bhosale AV, Chaundkar D, Saindane A. Dissolution and Bioavailibity Enhancement of Carbamazepine. International Journal of Pharmacy and Pharmaceutical Sciences. 2013; 5 Suppl 1:395-400.
Ali S, Karim Z, Aholghasem J. Solubility and Dissolution Rate of Carbamazepine-Cinnamic Acid Co-Crystal. Journal of Molecular Liquids. 2013; 187:171-176.
Geoff GGZ , Henry RF, Borchardt TB, Lou X. Efficient Co-Crystal Screening using Solution Mediated Phase Transformation. Journal of Pharmaceutical Sciences. 2007; 96 Suppl 5:990-995.
Bethune SJ, Thermodynamic and kinetic parameters that explain crystallization solubility of pharmaceutical co-crystals. 2009;1-58.
Rao CNR. Basic concepts, Instrumentation and Techniques: Chemical applications of infrared spectroscopy. Academic Press, New York and London. 1963.
Porter WW, Elli SC, Metzger AJ. Polymorphism in carbamazepine cocrystals. Crystal Growth and Design. Des 2008; 8(1);14-116.
Nanjwade K, Ali M, Maste M, Nanjwade B. Development and Characterization of Novel Pharmaceutical Crystalline Complex of Lomefloxacin. International Journal of Pharmaceutical Sciences Review and Research. 2012; 4 Suppl 1:227-233.
Fukte SR, Wagh MP, Shilpi R. Coformer Selection: An Important tool in Co-crystal Formation. International Journal of Pharmacy and Pharmaceutical Sciences. 2014; 6 Suppl 7: 9-14.
European Pharmaceutical review. The Proposed Guidelines for the Safety Evaluation of New Excipient. 1997.
Shah K, Borhade S, Londhe V. Utilization of Co-Crystalization for Solubility Enhancement of a Poorly Soluble Antiviral Drugâ€“Ritonavir. International Journal of Pharmacy and Pharmaceutical Sciences. 2014; 6 Suppl 2: 556-558.
Desai H, Rao L, Amin P. Carbamazepine Co-crystals by Solvent Evaporation Technique Formulation and Characterization Studies. American Journal of Pharmatech Research 2014; 4 Suppl 2:478-493.
Chua M., Chan K, Hocking TJ, Williams PA, Perry CJ. Methodologies for the Extraction and Analysis of Konjac Glucomannan from Corms of A. konjac K. Koch. Carbohydrate Polymers. 2012; 87: 2202-2010.
Indian Pharmacopoeia, Government of India, Ministry of Health and Family Welfare, I, Published by the controller of Publications, Delhi, 1996.
Sandler N, Gordan KC. Visualising the Conversion of Carbamazepine in Aqueous Suspension With and Without the Presence of Excipient: A Single Crystal Study using SEM and Raman Spectroscopy, European Journal of Pharmaceutics and Biopharmaceutics. 2006; 64: 326- 335.
Khan KA. The Concept of Dissolution Efficiency. Journal of Pharmacy and Pharmacology 1975; 27: 48-49.