Improving Physicochemical Properties of Repaglinide Through Pharmaceutical Adduct Formation
Abstract
Background: Many formulation strategies are presently in development in pharmaceutical industry. However, the formation of pharmaceutical adducts is considered to be the most appropriate technique for improving the drug solubility and dissolution as no chemical bond changes are involved in this technique.
Purpose: This technique is highly used for compounds which are not able to give viable formulation products with standard techniques such as salt formation and polymorph generation. In the present study, this method is applied to repaglinide, which is an hypoglycemic agent, with compromised solubility.
Methods: The adducts were prepared by slow evaporation method and characterized using DSC, FTIR and PXRD studies. The solubility and dissolution studies were carried out to determine the increased solubility of drug in adducts. The drug amount interacted with coformers has also been determined.
Results: The present study demonstrates the improvement in solubility and thus dissolution of repaglinide in adducts.
Conclusion: The adducts formed in the present study can be further exploited to prepare formulation of repaglinide adducts with better physicochemical characteristics.
- Page Number : 31-37
- Keywords
Solubility, Repaglinide, Molecular adducts, Soluplus, HPMC - DOI Number
10.15415/jptrm.2020.81005 -
Authors
- Sharen Gill GHG Khalsa College of Pharmacy, Gurusar Sadhar, Ludhiana, Punjab-141104, India
- Poonam Arora Chitkara College of Pharmacy, Chitkara University, Rajpura, Punjab-140401, India
References
- Babu, N.J., & Nangia, A. (2011). Solubility advantage of amorphous drugs and pharmaceutical cocrystals. Crystal Growth & Design, 11(7), 2662-2679. https://doi.org/10.1021/cg200492w
- Bhogala, B.R., Basavoju, S., & Nangia, A. (2005). Three-component carboxylic acid− bipyridine lattice inclusion host. Supramolecular synthesis of ternary cocrystals. Crystal growth & design, 5(5), 1683-1686. https://doi.org/10.1021/cg058012p
- Desiraju, G.R. (2010). Crystal engineering: a brief overview. Journal of Chemical Sciences, 122(5), 667-675. https://doi.org/10.1007/s12039-010-0055-2
- Friščić, T., & Jones, W. (2010). Benefits of cocrystallisation in pharmaceutical materials science: an update. Journal of Pharmacy and Pharmacology, 62(11), 1547-1559. https://doi.org/10.1111/j.2042-7158.2010.01133.x
- Mirza, S., Miroshnyk, I., Heinämäki, J., & Yliruusi, J. (2008). Co-crystals: an emerging approach for enhancing properties of pharmaceutical solids. Dosis : farmaseuttinen aikakauskirja, 24(2), 90-96.
- Sekhon, B.S. (2009). Pharmaceutical co-crystals - a review. ARS Pharmaceutica, 50(3), 99-117.
- Shan, N., & Zaworotko, M.J. (2008). The role of cocrystals in pharmaceutical science. Drug Discovery Today, 13(9-10), 440-446. https://doi.org/10.1016/j.drudis.2008.03.004
- Upadhyay, N., Shukla, T.P., Mathur, A., & Manmohan, J.S. (2011). Pharmaceutical co-crystal: an emerging approach to improve physical property. International journal of Pharmaceutical Science Review & Research, 8(1), 144-148.
- Yadav, A.V., Shete, A.S., Dabke, A.P., Kulkarni, P.V., & Sakhare, S.S. (2009). Co-crystals: a novel approach to modify physicochemical properties of active pharmaceutical ingredients. Indian Journal of Pharmaceutical Sciences, 71(4), 359. https://doi.org/10.4103/0250-474X.57283