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

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标题: Taste masking and rheology improvement of drug complexed with beta-cyclodextrin and hydroxypropyl-β-cyclodextrin by hot-melt extrusion
资源摘要: Publication date: 1 April 2018
Source:Carbohydrate Polymers, Volume 185

Author(s): Lorena F.B. Malaquias, Lívia C.L. Sá-Barreto, Daniel O. Freire, Izabel C.R. Silva, Kapish Karan, Thomas Durig, Eliana M. Lima, Ricardo N. Marreto, Guilherme M. Gelfuso, Tais Gratieri, Marcilio Cunha-Filho

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 <12%. Similarly, floodability exhibited significant enhancement (dispersibility <10%). Whereas extrudates of FLU containing only the polymeric matrix led to a slow drug dissolution efficiency (18.6%) and a partial drug taste masking; extrudates containing cyclodextrin accelerated FLU dissolution (dissolution efficiency approx. 30%) and provided a complete drug taste masking. Moreover, HME process could produce drug complexes with high complexation efficiency and preserve its antifungal activity.





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资源来源机构: Elsevier
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