Sweet Sulfamethazine Acesulfamate Crystals With Improved Compaction Property

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Sweet Sulfamethazine Acesulfamate Crystals With Improved Compaction Property

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2019-07

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Sulfamethazine (SMT) is a sulfonamide antibacterial drug used to treat or prevent infections in both humans and animals. However, SMT has an unfavorable taste and poor compaction behavior. To overcome these problems, a 1:1 complex with an artificial sweetener, acesulfame (Acs), was prepared and characterized. The single crystal structure suggests that the new complex, SMT-Acs, is a salt. This was confirmed by analysis of C-N bond length and comparison to multicomponent SMT crystals with known ionization states of SMT and Fourier transformation infrared spectroscopy. The applicability of the ΔpKa rule in multicomponent crystals of SMT is discussed. SMT-Acs exhibits better tabletability than SMT, which is attributed to its greater plasticity as shown by Heckel and Kuentz – Leuenberger analysis. The greater plasticity of SMT-Acs is consistent with the presence of slip planes identified by combined energy framework and topological analysis of the crystal structure.

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University of Minnesota M.S. thesis. July 2019. Major: Pharmaceutics. Advisor: Changquan Sun. 1 computer file (PDF); vii, 52 pages.

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Liu, Sibo. (2019). Sweet Sulfamethazine Acesulfamate Crystals With Improved Compaction Property. Retrieved from the University Digital Conservancy, https://hdl.handle.net/11299/206698.

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