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Thermal analysis study of solid dispersions hydrochlorothiazide

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Abstract

Solid dispersions (SD) are used as a technological strategy to increase the aqueous dissolution rate of poorly soluble active pharmaceutical ingredients, such as hydrochlorothiazide (HCTZ), an antihypertensive used frequently in medical clinics. The aim of this study was to characterize solid dispersions of HCTZ obtained with different processing adjuvants, using the DSC, TG, XRPD, FTIR and SEM techniques, and to evaluate the influence of carriers used in biopharmaceutical performance by analyzing dissolution efficiency. The SDs were obtained using the solvent method, and spray drying was used as the drying technique. The carriers used PEG 1500, sodium lauryl sulfate and PVP K30. The calorimetric analysis and XRPD showed amorphous behavior to SDs that used hydrophilic polymer as a carrier, and thermogravimetric analysis showed maintaining thermal stability of the HCTZ for most dispersions. FTIR detected intermolecular interactions of hydrogen bonds, while SEM showed the formation of microparticles with a tendency to sphericity. Acquired morphology associated with amorphization contributed to the increase in dissolution efficiency of dispersions, being that this SD (HCTZ/PVP K30) showed the best increase in dissolution. We therefore concluded that the analytical techniques used were of fundamental importance to the characterization of pharmaceutical products developed as to their physicochemical properties and the prescience of the oral bioavailability of HCTZ.

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Acknowledgements

We thank Coordination of Improvement of Higher Level Personnel (CAPES) for funding this work and to Laboratory of Evaluation and Development of Northeastern Biomaterials (CERTBIO) of the Federal University of Campina Grande and to Materials Engineering Laboratory of the Federal University of Paraíba by analysis provided.

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Authors and Affiliations

  1. Department of Pharmaceutical Sciences, Postgraduate Program in Pharmaceutical Sciences, Federal University of Pernambuco, University City, Recife, PE, Brazil

    Cinthya Maria Pereira de Souza, Fernando José de Lima Ramos Júnior, Fábio Santos de Souza & Rui Oliveira Macêdo

  2. Department of Pharmaceutical Sciences, Unified Laboratories of Pharmaceutical Development and Assays, Federal University of Paraíba, CEP 58051-970, Castelo Branco, João Pessoa, PB, Brazil

    Cinthya Maria Pereira de Souza, Jonh Anderson Borges dos Santos, Agnaldo Luiz do Nascimento, José Venâncio Chaves Júnior, Fernando José de Lima Ramos Júnior, Severino Antônio de Lima Neto, Fábio Santos de Souza & Rui Oliveira Macêdo

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  1. Cinthya Maria Pereira de Souza
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Correspondence to Cinthya Maria Pereira de Souza.

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de Souza, C.M.P., dos Santos, J.A.B., do Nascimento, A.L. et al. Thermal analysis study of solid dispersions hydrochlorothiazide. J Therm Anal Calorim 131, 681–689 (2018). https://doi.org/10.1007/s10973-017-6091-0

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