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Enhancing the Pharmaceutical Behavior of Nateglinide by Cocrystallization: Physicochemical Assessment of Cocrystal Formation and Informed Use of Differential Scanning Calorimetry for Its Quantitative Characterization.
Bruni, Giovanna; Maggi, Lauretta; Mustarelli, Piercarlo; Sakaj, Mirena; Friuli, Valeria; Ferrara, Chiara; Berbenni, Vittorio; Girella, Alessandro; Milanese, Chiara; Marini, Amedeo.
Afiliação
  • Bruni G; Department of Chemistry, C.S.G.I, Physical-Chemistry Section, University of Pavia, Via Taramelli 16, 27100 Pavia, Italy. Electronic address: giovanna.bruni@unipv.it.
  • Maggi L; Department of Drug Sciences, University of Pavia, Via Taramelli 12, 27100 Pavia, Italy.
  • Mustarelli P; Department of Chemistry, C.S.G.I, Physical-Chemistry Section, University of Pavia, Via Taramelli 16, 27100 Pavia, Italy.
  • Sakaj M; Department of Chemistry, C.S.G.I, Physical-Chemistry Section, University of Pavia, Via Taramelli 16, 27100 Pavia, Italy.
  • Friuli V; Department of Drug Sciences, University of Pavia, Via Taramelli 12, 27100 Pavia, Italy.
  • Ferrara C; Department of Chemistry, C.S.G.I, Physical-Chemistry Section, University of Pavia, Via Taramelli 16, 27100 Pavia, Italy.
  • Berbenni V; Department of Chemistry, C.S.G.I, Physical-Chemistry Section, University of Pavia, Via Taramelli 16, 27100 Pavia, Italy.
  • Girella A; Department of Chemistry, C.S.G.I, Physical-Chemistry Section, University of Pavia, Via Taramelli 16, 27100 Pavia, Italy.
  • Milanese C; Department of Chemistry, C.S.G.I, Physical-Chemistry Section, University of Pavia, Via Taramelli 16, 27100 Pavia, Italy.
  • Marini A; Department of Chemistry, C.S.G.I, Physical-Chemistry Section, University of Pavia, Via Taramelli 16, 27100 Pavia, Italy.
J Pharm Sci ; 108(4): 1529-1539, 2019 04.
Article em En | MEDLINE | ID: mdl-30476510
ABSTRACT
The aim of this study was to synthetize cocrystals of nateglinide, an antidiabetic agent of biopharmaceutics classification system Class IIa, as a strategy to improve both the solubility and the dissolution rate of the drug. Benzamide was selected by a screening procedure as a suitable coformer, and binary mixtures with different compositions were prepared and analyzed by differential scanning calorimetry (DSC). An in-depth analysis of DSC data allowed obtaining both the eutectic mixture and cocrystal compositions. The rationale of such an analysis was highlighted and explained. Cocrystals were prepared by kneading and solvent evaporation. Their formation was proved by DSC and confirmed by X-ray powder diffraction, solid-state nuclear magnetic resonance, and Fourier-transform infrared spectroscopy. The functional groups involved in the interaction leading to cocrystals formation were investigated by spectroscopic techniques. The in vitro dissolution profiles show that cocrystals have definite better pharmaceutical performances than the pure drug.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Varredura Diferencial de Calorimetria / Química Farmacêutica / Nateglinida / Hipoglicemiantes Idioma: En Ano de publicação: 2019 Tipo de documento: Article
Texto completo
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XML
PubMed Links
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Varredura Diferencial de Calorimetria / Química Farmacêutica / Nateglinida / Hipoglicemiantes Idioma: En Ano de publicação: 2019 Tipo de documento: Article