Taste masking and rheology improvement of drug complexed with beta-cyclodextrin and hydroxypropyl-β-cyclodextrin by hot-melt extrusion

•Fluconazole-cyclodextrin inclusion complex were produced using hot melt extrusion.•Inclusion complexes were obtained with high complexation efficiency.•Improvements on drug rheology, palatability and dissolution rate were achieved. This study aimed to mask fluconazole (FLU) taste and improve its rh...

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Veröffentlicht in:Carbohydrate polymers 2018-04, Vol.185, p.19-26
Hauptverfasser: Malaquias, Lorena F.B., Sá-Barreto, Lívia C.L., Freire, Daniel O., Silva, Izabel C.R., Karan, Kapish, Durig, Thomas, Lima, Eliana M., Marreto, Ricardo N., Gelfuso, Guilherme M., Gratieri, Tais, Cunha-Filho, Marcilio
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Sprache:eng
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Zusammenfassung:•Fluconazole-cyclodextrin inclusion complex were produced using hot melt extrusion.•Inclusion complexes were obtained with high complexation efficiency.•Improvements on drug rheology, palatability and dissolution rate were achieved. This study aimed to mask fluconazole (FLU) taste and improve its rheological properties by an efficient process of cyclodextrin complexation. For this, hot-melt extrusion (HME) was used to obtain extrudates composed of FLU, hydroxypropylcellulose, and one of two different cyclodextrins (β-cyclodextrin or hydroxypropyl-β-cyclodextrin) maintaining the drug:cyclodextrin molar ratio at 1:0.3 or 1:0.2, respectively. Samples were characterized by physicochemical tests, palatability using e-tongue and antifungal assays. Drug stability was preserved after HME, according to spectroscopy test (correlation coefficient >0.9) and HPLC-assay (100–107%). Flowability was improved in HME systems with compressibility of
ISSN:0144-8617
1879-1344
DOI:10.1016/j.carbpol.2018.01.011