期刊
CARBOHYDRATE POLYMERS
卷 185, 期 -, 页码 19-26出版社
ELSEVIER SCI LTD
DOI: 10.1016/j.carbpol.2018.01.011
关键词
Cyclodextrin; Hot-melt extrusion; Rheology; Palatability; E-tongue; Antifungal assay
资金
- CNPq
- CAPES
- FAP-DF
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 (beta-cyclodextrin or hydroxypropyl-beta-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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