环糊精
挤压
流变学
β-环糊精
化学
BETA(编程语言)
药品
材料科学
药理学
色谱法
复合材料
医学
计算机科学
程序设计语言
作者
Lorena F.B. Malaquias,Lívia L. Sá‐Barreto,Daniel Freire,Izabel Cristina Rodrigues da Silva,Kapish Karan,Thomas Dürig,Eliana Martins Lima,Ricardo Neves Marreto,Guilherme M. Gelfuso,Taís Gratieri,Marcílio Cunha‐Filho
标识
DOI:10.1016/j.carbpol.2018.01.011
摘要
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.
科研通智能强力驱动
Strongly Powered by AbleSci AI