Funct. Mater. 2024; 31 (1): 61-66.
Desloratadine: research on polymorphism and conditions of polymorphic transitions
1SSI "Institute for Single Crystals" NAS of Ukraine, 60 Nauky ave., Kharkiv, 61001, Ukraine
2Farmak JSC, 63 Kyrylivska str., Kyiv 04080, Ukraine
3National Technical University of Ukraine "Igor Sikorsky Kyiv Polytechnic Institute", 37 Pobedy ave., 03056 Kyiv, Ukraine
This paper presents research on the polymorphism of Desloratadine substance, which is an active pharmaceutical ingredient used for the treatment of allergic reactions. Desloratadine has three known polymorphic forms (I-III) simultaneous crystallization of three polymorphs occurs during the substance production. According to the results of our research, Desloratadine polymorphs are prone to polymorphic transitions when external factors change and recrystallization from solvents of various chemical activities. The Desloratadine polymorph II is metastable and is not observed in samples after recrystallization. The solvent affects the polymorphic transitions of the substance. According to our research results, the maximum content of polymorph I was obtained during recrystallization from chloroform (77 mas.%), and for polymorph III – during recrystallization from water (86 mas.%). Pressure and temperature also affect the change in the ratio of polymorphic modifications and the degree of crystallinity in the sample under study.
1. J.Bernstein, Polymorphism in Molecular Crystals 2e, International Union of Crystal (2020) https://doi.org/10.1093/oso/9780199655441.001.0001 |
||||
2. J.Bernstein, Organic Solid State Chemistry, Elsevier, Amsterdam (1987) | ||||
3. J.-P. Brog, C.-L. Chanez, A. Crochet, M.Fromm, RSC Advances, 3, 16905, (2013) https://doi.org/10.1039/c3ra41559g |
||||
4. H.Bokyi, Krystallokhymyia, Nauka, Moscow (1979) [in Russian] | ||||
5. Yu.Yziumov, V.Syiromiatnykov, Fazovye perekhody i symmetryia krystallov, Nauka, Moscow (1984) [in Russian] | ||||
6. S.Sarkar, M.Pavan, S.Cherukuvada, T.Guru Row, Chemical Communications, 52, 5820, (2016) https://doi.org/10.1039/C6CC01612J |
||||
7. C.Rustichelli, G.Gamberini, V.Ferioli, M.Gamberini, R.Ficarra, S.Tommasini, J. of Pharm. and Biomedical Analysis, 23, 41, (2000) https://doi.org/10.1016/S0731-7085(00)00262-4 |
||||
8. H.G. Britain, Polymorphism in pharmaceutical solids, CRC Press (2018) https://doi.org/10.3109/9781420073225 |
||||
9. R.Hilfiker, Polymorphism: in the Pharmaceutical Industry, WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim (2006) | ||||
10. N.Lakshmi Prasanthi, M.Sudhir, N.Jyothi, V.Sri Vajrapriya, American Journal of Advanced Drug Delivery, 4, 058, (2016) | ||||
11. B.Rodriguez-Spong, C.Price, A.Jayasankar, A.Matzger, N.Rodriguez-Hornedo, Advanced Drug Delivery Reviews, 56, 241, (2004) https://doi.org/10.1016/j.addr.2003.10.005 |
||||
12. M.Guerain, J. of Pharmaceutical Sciences, 109, 2640, (2020) https://doi.org/10.1016/j.xphs.2020.05.021 |
||||
13. R.Geha, E.Meltzer, J. of Allergy and Clinical Immunology, 107, 751, (2001) https://doi.org/10.1067/mai.2001.114239 |
||||
14. C.Dong, J. Appl. Cryst. 32, 838 (1999) https://doi.org/10.1107/S0021889899003039 |
||||
15. J.Rodriguez-Carvajal, T.Roisnel, Trans Tech Publications, 1, 123, (2004) https://doi.org/10.4028/www.scientific.net/MSF.443-444.123 |
||||
16. J.Rodriguez-Carvajal, T.Roisnel, Newsletter 20, 35, (1998) | ||||
17. V.Srirambhatla, R.Guo, D.Dawson, S.Price, A.Florence, Cryst. Growth Des., 20, 1800, (2020) https://doi.org/10.1021/acs.cgd.9b01522 |
||||
18. K. McClellan, B. Jarvis, Drugs, 61, 789, (2001). https://doi.org/10.2165/00003495-200161060-00007 |
||||