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Thermal Analytical Approaches to Characterization and Compatibility Studies of Duloxetine Hydrochloride

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Pharmaceutical Chemistry Journal Aims and scope

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.

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Acknowledgments

This study was funded in part by the Coordenação de Aperfeiçoamento de Pessoal de Nível Superior—Brasil (CAPES), Finance Code 001.

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Authors and Affiliations

  1. Universidade Federal do Paraná - UFPR, Departamento de Farmácia, Av. Pref. Lothário Meissner, 632 - Jardim Botânico, Curitiba, PR, 80210-170, Brazil

    Andressa Veiga, Nayana C. F. Stofella, Laiane J. Oliveira & Fábio S. Murakami

  2. Universidade Positivo – UP, R. Prof. Pedro Viriato Parigot de Souza, Curitiba, PR, 5300-81280-330, Brazil

    Elisa F. Montin, Tábata Bauab, Lucca C. Malucelli & Marco Aurélio S. C. Filho

  3. Universidade Estadual do Centro-Oeste – UNICENTRO, Rua Simeão Camargo Varela de Sá, 03 -Vila Carli, Guarapuava, PR, 85040-080, Brazil

    Paulo R. Oliveira

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  1. Andressa Veiga
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  2. Nayana C. F. Stofella
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  3. Laiane J. Oliveira
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  7. Marco Aurélio S. C. Filho
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  8. Paulo R. Oliveira
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  9. Fábio S. Murakami
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Correspondence to Fábio S. Murakami.

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Veiga, A., Stofella, N.C.F., Oliveira, L.J. et al. Thermal Analytical Approaches to Characterization and Compatibility Studies of Duloxetine Hydrochloride. Pharm Chem J 54, 659–666 (2020). https://doi.org/10.1007/s11094-020-02249-0

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  • DOI: https://doi.org/10.1007/s11094-020-02249-0

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