Thermal Analytical Approaches to Characterization and Compatibility Studies of Duloxetine Hydrochloride
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Pharmaceutical Chemistry Journal, Vol. 54, No. 6, September, 2020 (Russian Original Vol. 54, No. 6, June, 2020)
THERMAL ANALYTICAL APPROACHES TO CHARACTERIZATION AND COMPATIBILITY STUDIES OF DULOXETINE HYDROCHLORIDE Andressa Veiga,1 Nayana C. F. Stofella,1 Laiane J. Oliveira,1 Elisa F. Montin,2 Tábata Bauab,2 Lucca C. Malucelli,2 Marco Aurélio S. C. Filho,2 Paulo R. Oliveira,3 and Fábio S. Murakami1,* Original article submitted November 30, 2019. Duloxetine hydrochloride (DLX) is a serotonin and noradrenalin reuptake inhibitor mostly used for the treatment of major depressive and anxiety disorders. Physicochemical characterization of this drug and compatibility studies with excipients are particularly important during pharmaceutical technology development in order to guarantee the quality, safe and effective dosage form. Duloxetine is acid labile, thus the final product must be formulated with enteric coating to prevent degradation in the stomach for proper drug delivery. The major purpose of this work was to characterize this drug in solid-state form through thermal analytical techniques (TG/DTG, DSC), diffuse reflectance infrared Fourier transform (DRIFT) spectrophotometry, morphological analysis by scanning electron microscopy (SEM) and x-ray diffraction (XRD) analysis. The compatibility studies with excipients (1:1 w/w) was carried out using sodium starch glycolate (SSG), lactose (LAC), magnesium stearate (MS), croscarmellose sodium (CS), colloidal silicon dioxide (CSD) and microcrystalline cellulose (MCC). For DLX, the DSC analysis showed a sharp endothermic peak corresponding to the melting process (Tpeak = 168.93°C) and purity determination of 98.74 ± 0.03%. Thermogravimetry (TG) curves revealed a mass loss of approximately 58% during thermal decomposition and the non-isothermal kinetics revealed estimated Ea of 62.73 kJ mol-1 with a reaction order of zero, indicating that DLX thermal decomposition is constant over time, regardless of its concentration. The compatibility results suggest an interaction between DLX and selected excipients (SSG, CS, CSD, MCC) evidenced by the DLX melting point dislocation on the DSC curves. Keywords: duloxetine; depression; compatibility assay; thermal analysis.
ity to concentrate. In addition, advanced stages of depression may lead to suicide. Although depression may affect people at different life stages, it is often prevalent for the elder ones [1]. Antidepressant drugs are widely used for treatment of depressive disorders. Since the 1950s, two types were more recurrent, the tricyclic antidepressants (TADs) and monoamine oxidase inhibitors (MAOIs). Despite high efficacy, the low pharmacological specificity, in addition to overdosage, may lead to adverse reactions when using these drugs. In turn, the search for alternative medications is necessary to overcome these drawbacks [2]. Nowadays the most used antidepressants are the selective serotonin reuptake inhibitors (SSRIs) and serotonin-norepinephrine reuptake inhibitors (SNRIs) [3]. Duloxetine hydrochloride (DLX), chemical
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