喷雾干燥工艺对布洛芬口服载体壳聚糖/黄原胶多电解质复合物性能的影响

Q4 Pharmacology, Toxicology and Pharmaceutics
A. Ćirić, Jelena Milinković-Budinčić, Đorđe Medarević, V. Dobričić, Milena Rmandić, T. Barudžija, A. Malenović, Lidija Petrović, Ljiljana Đekić
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引用次数: 3

摘要

聚电解质复合物(PECs)是一种有吸引力的载体,具有增强难溶性高剂量低分子量药物口服递送的潜力。固体口服剂型的配方需要干燥的PECs,这可能会影响其物理化学和生物制药性能。本研究旨在研究喷雾干燥对布洛芬壳聚糖/黄原胶PECs性能的影响,并与常温干燥的PECs进行比较,考察其在硬胶囊内的药物释放动力学。喷雾干燥法的收率、布洛芬含量、包封效率和残留水分含量均低于环境干燥法。扫描电镜显示,喷雾干燥PECs具有较好的流动性,这主要归因于其近乎球形的颗粒形状。DSC和PXRD分析证实了布洛芬在喷雾干燥过程中的非晶化。通过常温干燥和喷雾干燥得到的PECs在0.1 M盐酸(pH 1.2)和磷酸盐缓冲液pH 7.4中均具有较高的再水化能力。在12小时内控制干燥PECs的体外布洛芬释放量,约30%的布洛芬释放量。与环境干燥的PECs相比,喷雾干燥的PECs可以更好地控制布洛芬从载体扩散。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Influence of spray-drying process on properties of chitosan/xanthan gum polyelectrolyte complexes as carriers for oral delivery of ibuprofen
Polyelectrolyte complexes (PECs) are attractive carriers with recognized potential to enhance oral delivery of poorly soluble high-dosed low-molecular-weight drugs. The formulation of solid oral dosage forms requires the drying of PECs, which may affect their physicochemical and biopharmaceutical properties. The aim of this study was to investigate the effect of spraydrying on the properties of ibuprofen-loaded chitosan/xanthan gum PECs and to assess the drug release kinetics from such PECs filled into hard capsules in comparison with corresponding PECs which are dried under ambient conditions. The yield, ibuprofen content, entrapment efficiency, and residual moisture content of spray-dried PECs were lower than those of ambient-dried PECs. Better flowability of spray-dried PECs was attributed to the almost spherical particle shape, shown by scanning electron microscopy. DSC and PXRD analysis confirmed the amorphization of ibuprofen during spray-drying. All the investigated PECs, obtained by drying under ambient conditions as well as by spray-drying, had high rehydration capacity both in 0.1 M hydrochloric acid (pH 1.2) and phosphate buffer pH 7.4. In vitro ibuprofen release from dried PECs was controlled during 12 h with the release of approximately 30% of entrapped ibuprofen. Spray-dried PECs provided better control of ibuprofen diffusion from the carrier compared to the ambientdried ones.
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来源期刊
Arhiv za Farmaciju
Arhiv za Farmaciju Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
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19
审稿时长
12 weeks
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