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Development of Ethylcellulose Microparticles for Taste Masking of Fexofenadine
Chemical & Pharmaceutical Bulletin ( IF 1.7 ) Pub Date : 2024-01-23 , DOI: 10.1248/cpb.c23-00754
Yuri Ikeuchi-Takahashi 1 , Machi Morii 1 , Kurumi Yamazaki 1 , Aoi Shimana 1 , Ikki Shibazaki 1 , Yasuko Obata 1
Affiliation  

For taste masking of fexofenadine hydrochloride (FXD), ethylcellulose (EC) microparticles with FXD were developed. The amounts of EC, Tween 80, and polyvinyl alcohol (PVA) in the composition had little effect on initial drug release properties. Based on the results of the drug recovery and the drug release properties, FXD(EC200) was the optimal FXD microparticle formulation. From the results of Fourier transform infrared spectroscopy spectra and X-ray diffraction patterns of FXD(EC200), FXD amorphization in the microparticles and interaction between FXD and other components were suggested, and the formation of a solid dispersion of FXD was suggested. Because the possibility of the complex of PVA and FXD on the particle surface was suggested, sodium lauryl sulfate (SLS) was added to the composition. The initial drug release from FXD microparticles with SLS was further suppressed compared with FXD(EC200). From these results, FXD microparticles with SLS can be prepared as a controlled-release formulation and are expected to be useful for masking the bitter tasting particulates.

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中文翻译:

用于非索非那定掩味的乙基纤维素微粒的开发

为了掩味盐酸非索非那定 (FXD),开发了带有 FXD 的乙基纤维素 (EC) 微粒。组合物中EC、吐温80和聚乙烯醇(PVA)的量对初始药物释放特性几乎没有影响。根据药物回收率和药物释放特性的结果,FXD(EC200)是最佳的FXD微粒制剂。从FXD(EC200)的傅里叶变换红外光谱和X射线衍射图的结果表明,FXD在微粒中发生非晶化以及FXD与其他组分之间的相互作用,并表明FXD固体分散体的形成。因为暗示了PVA和FXD在颗粒表面上形成复合物的可能性,所以将十二烷基硫酸钠(SLS)添加到组合物中。与 FXD(EC200) 相比,使用 SLS 的 FXD 微粒的初始药物释放被进一步抑制。根据这些结果,含有 SLS 的 FXD 微粒可以制备成控释制剂,并有望用于掩盖苦味颗粒。

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更新日期:2024-01-22
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