Volume : 09, Issue : 03, March – 2022

Title:

22.AN OVERVIEW: POLYMORPHISM AND ITS APPLICATIONS IN DRUG DEVELOPMENT PROCESS

Authors :

Belsarkar A.S.*, Shinde A.D., Sonawane S.P

Abstract :

The physical properties, characterization, and uses of polymorphism are highlighted in this article. Polymorphism is important in pharmaceutical compounds and it’s important to research and development of drug and drug discovery. Polymorphism in pharmacological substances is well known for its prevalence and relevance. During medication discovery and development, it is critical to plan and pick the appropriate form from the start. This review introduces the basic concepts of Polymorphism in pharmaceutical compounds and also vibrational spectroscopy in polymorphism applications and study of crystal polymorphism, cocrystals, physicochemical characteristics and uses, polymorphism research methods, Chemical stability and polymorphism, polymorphisms effect on drug substance and drug administration product polymorphism’s impact on bioavailability, solubility, and dissolution bioequivalence (BA) and bioequivalence (BE) polymorphism’s impact on drug product manufacturing, etc. Hence this study topic is undertaken for detail insights of phenomena of polymorphism and its relevance in drug development process.
Key words: Polymorphism, Crystallization, Bioavilability ,API, Polymorph.

Cite This Article:

Please cite this article in press Belsarkar A.S et al, An Overview: Polymorphism And Its Applications In Drug Development Process., Indo Am. J. P. Sci, 2022; 09(3),.

Number of Downloads : 10

References:

1. Bauer, J., Ritonavir: An Extraordinary Example of Conformational Polymorphism’, J.Pharm. Res. 18(6) (2001) 859.
2. Drebushchak, T.N., Chukanov, N.V. and Boldyreva, E.V., Acta Cryst. E62 (2006) O4393.
3. Griesser, U.J.,The Importance of Solvates. In Polymorphism in the Pharmaceutical Industry; Hilfiker, R. Ed.; Wiley-VCH: Weinheim, (2006).
4. Nangia. A., Cryst. Growth Des., 6 (2006) 2.
5. Vishweshwar, P.; McMahon, J.A.; Peterson, M.L.; Hickey, M.B.; Shattock, T.R. and Zaworotko, M.J. Chem Commun. (2005) 4601.
6. Bhramankar Dm -Sunil Jaiswal Biopharmaceutics and Pharmacokinetics.2005.
7. The theory and practice of industrial pharmacy By- Leon Lechmann -Joseph L Kanig.
8. Uzoh O. G., Cruz-Cabeza A. J. and. Price, S. L ,Cryst. Growth Des., 2012, 12(8), 4230.
9. Kitamura, C. et al. Conformational polymorphism and optical properties in the solid state of 1,4,7,10- tetra(n-butyl) tetracene. Cryst Eng Comm 9, 644–647 (2007).
10. Kons, A. et al. Polymorphism of R-encenicline hydrochloride: access to the highest number of structurally characterized polymorphs using desolvation of various solvates. Cryst. Growth Des. 19, 4765–4773 (2019).
11. Delaney, S. P., Pan, D., Yin, S. X., Smith, T. M. &Korter, T. M. Evaluating the roles of conformational strain and cohesive binding in crystalline polymorphs of Aripiprazole. Cryst. Growth Des. 13, 2943–2952 (2013).
12. Lian Yu . Thermochemistry and conformational polymorphism of a hexamorphic crystal system. J. Am. Chem. Soc. 122, 585–591 (2000).
13. Mitchell, C. A., Yu, L. & Ward, M. D. Selective nucleation and discovery of organic polymorphs through epitaxy with single crystal substrates. J. Am. Chem. Soc. 123, 10830–10839 (2001).
14. Wood, R. G., Ayliffe, S. H. & Cullinane, N. M. XXXIII. A crystallographic and x-ray investigation of some diphenylamine derivatives. Lond. Edinb. Dublin Philos. Mag. J. Sci. 19, 405–416 (1935).
15. Braun, D. E. et al. Colored polymorphs: thermochemical and structural features of N -picryl- p -toluidine polymorphs and solvates. Cryst. Growth Des. 8, 1977–1989 (2008).
16. Gentili, D., Gazzano, M., Melucci, M., Jones, D. & Cavallini, M. Polymorphism as an additional functionality of materials for technological applications at surfaces and interfaces. Chem. Soc. Rev. 48, 2502–2517 (2019).
17. Smith, J., MacNamara, E., Raftery, D., Borchardt, T. &Byrn, S. Application of two-dimensional 13C solid- state NMR to the study of conformational polymorphism. J. Am. Chem. Soc. 120, 11710–11713 (1998).
18. Richardson, M. F., Yang, Q.-C., Novotny-Bregger, E. &Dunitz, J. D. Conformational polymorphism of dimethyl 3,6‐dichloro‐2,5‐dihydroxyterephthalate. II. Structural, thermodynamic, kinetic and mechanistic aspects of phase transformations among the three crystal forms. ActaCrystallogr. Sect. B 46, 653–660 (1990).
19. US Department of Health and Human Services, Food and Drug Administration. Center for Drug Evaluation and Research. 2007. Guidance to industry: ANDAs: Pharmaceutical Solid Polymorphism. Chemistry, Manufacturing and Controls 35Information.
20. European Medicines Agency. 2015. Reflection paper on the use of cocrystals of 352 active substances in medicinal products.
21. Bettinetti, G, et al. 2006. Polymorphism, pseudopolymorphism, and amorphismof peracetylated α-, β-, and γ-cyclodextrins. Journal of Pharmaceutical and Biomedical Analysis, 41:1205-1211.
22. Gaskell, DR. 2005. Allotropy and Polymorphism. Reference Module in Materials Science and Materials Engineering. Encyclopedia of Condensed Matter Physics, 8– 17.
23. Brittain, HG. 2007. Polymorphism and solvatomorphism 2005. Journal of 325 Pharmaceutical Sciences, 96(4):705–728.
24. Caira, M, Pienaar, EW, Lötter, AP. 2006. Polymorphism and pseudopolymorphism of the antibacterial nitrofurantoin. Molecular Crystals and Liquid Crystals, 179(1).
25. Veesler.S, F. Puel, G, Fevotte, Polymorphism in processes of crystallization in solution, STP PharmaPratiques 13 (2003).
26. Grzesiak.L.D (2003) Lang. K. Comparison of the four anhydrous polymorphs of carbamazepine and the crystal structure of form I, Journal of Pharmaceutical Sciences 92) analysis: study of pseudo-polymorphs stability, Journal of Pharmaceutical Sciences 94(2005) 1336.
27. Burger.A ,R, Ramberger, On the polymorphism of pharmaceuticals and other molecular crystals. II. Applicability of thermodynamic rules, MikrochimicaActa 72 (1979) 273.
28. Vishweshwar P, McMahon JA, Peterson ML, Hickey MB, Shattock TR, Zaworotko MJ. Crystal engineering of pharmaceutical co-crystals from polymorphic active pharmaceutical ingredients. Chemical communications. 2005; (36):4601-03.
29. Kovacic B1, Vrecer F, Planinšek O. Spherical crystallization of drugs. Acta Pharm. 2012; 62(1):1-14.
30. Nichols G, Frampton CS. Physicochemical characterization of the orthorhombic polymorph of paracetamol crystallized from solution. J Pharm Sci. 1998; 87(6):684-93.
31. T. Ito, R. Sadanaga and Y. Takeuchi, X-Ray Studies on Polymorphism, Maruzen Co, 1950.
32. Zakeri-Milani, P. M. Barzegar-Jalali, M. Azimi,H. Valizadeh, Biopharmaceutical classification of drugs using intrinsic dissolution rate IDR and rat intestinal permeability, Eur. J. Pharm. Biopharm. 73 (2009) 102–106.
33. Haleblian JK and McCrone W: Pharmaceutical applications of polymorphism. J.App Pharm Sci 1969; 58(8): 911-929.
34. Bauer JF: Polymorphism- A critical consideration in pharmaceutical development, manufacturing and stability. J. Valid Technology 2008; 15-23.
35. Smith JR Raftery D: Analysis of Conformational polymorphism in pharmaceutical solids using solid-state NMR and electronic structure calculations. J.PhysicalChem 2006; 110(15): 7766-7776.