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Physical–chemical characterization of new anti-inflammatory agent (LPSF/GQ-130) and evaluation of its thermal compatibility with pharmaceutical excipients

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Abstract

LPSF/GQ-130 is a drug candidate, according to reports about its significant anti-inflammatory activity and non-toxicity demonstrated in an acute preclinical study. Despite this, knowledge of its physical–chemical properties is insufficient for the development of medicines. Thus, this work aimed to characterize the raw material at its molecular, particle, and agglomerate level as well as evaluate its thermal compatibility to pharmaceutical excipients. Through spectrometric techniques the molecular structure of the substance was confirmed. For thermal analysis its melting (171.3–176.5 °C) and degradation (238.3–297.4 °C) ranges, besides its purity (99.37 %), were determined. The kinetic non-isothermal degradation supplied the order of thermal reaction (0), the activation energy (96.14 kJ mol−1) and the frequency factor (3.130 × 10−7 min−1). The diffraction of X-rays presented well defined signs in the angles 5.5°, 16.3°, and 44.18° 2θ, suggesting crystalline structure. Scanning electronic microscopy exhibited needle morphology. LPSF/GQ-130 presented Type-III isotherm adsorption/desorption, with a superficial area of 81.3529 m2 g−1 and water content calculated at 1 % using the Karl Fisher method. Laser granulometry calculated its granulometry between 11.65 and 13.10 μm, thus it was characterized as a very fine powder. The prototype was classified as insoluble in water (<0.0187 μg mL−1) and soluble in acetone and acetonitrile, and exhibits instability in basic pH (100 %) and oxidative conditions (30–70 %). In thermal compatibility the excipients PVP K-30, Compritol® 888 ATO, and MYRJ® 59 seem to exercise a protective thermal activity for the prototype.

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Acknowledgements

Centro de Tecnologias Estratégicas do Nordeste (CETENE), Fundação de Ciência e Tecnologia do Estado de Pernambuco, Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES), and the Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq).

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Authors and Affiliations

  1. Laboratório de Tecnologia dos Medicamentos, Universidade Federal de Pernambuco, Recife, PE, Brazil

    Amanda Carla Quintas de Medeiros Vieira, Graziella Silvestre Marques, Cybelly Marques de Melo, Keyla Emanuelle Ramos da Silva, Larissa Araújo Rolim & Pedro José Rolim Neto

  2. Instituto de Ciências Exatas e Tecnologia, Universidade Federal do Amazonas, Itacoatiara, PE, Brazil

    Keyla Emanuelle Ramos da Silva

  3. Laboratório de Planejamento e Síntese de Fármacos, Universidade Federal de Pernambuco, Recife, PE, Brazil

    Maria do Carmo Alves de Lima, Suely Lins Galdino & Ivan da Rocha Pitta

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  1. Amanda Carla Quintas de Medeiros Vieira
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Correspondence to Keyla Emanuelle Ramos da Silva.

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de Medeiros Vieira, A.C.Q., Marques, G.S., de Melo, C.M. et al. Physical–chemical characterization of new anti-inflammatory agent (LPSF/GQ-130) and evaluation of its thermal compatibility with pharmaceutical excipients. J Therm Anal Calorim 115, 2339–2349 (2014). https://doi.org/10.1007/s10973-013-3358-y

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