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Formulation of inhalable beclomethasone dipropionate-mannitol composite particles through low-temperature supercritical assisted atomization
The Journal of Supercritical Fluids ( IF 3.4 ) Pub Date : 2020-10-21 , DOI: 10.1016/j.supflu.2020.105095
Hsien-Tsung Wu , Tsung-Hsuan Li , Hong-Ming Tsai , Liang-Jung Chien , Yao-Hsiang Chuang

Mannitol carrier and drug-carrier composite particles were produced via low-temperature supercritical assisted atomization (LTSAA). The enhanced aerosolization of the mannitol carrier particles with added L-leucine could be attributed to the formation of fine corrugated particles, which reduced the interparticle cohesion and led to better flowability of the mannitol carrier particles. A poorly water-soluble drug, beclomethasone dipropionate (BDP), and mannitol co-precipitated during LTSAA with the optimal addition of 9.1 mass % L-leucine. The in vitro aerosolization and dissolution experiments indicated that the fine particles fraction (FPF) of the drug-carrier composite particles was 3.4 times (FPF = 49.9 %) higher than that of the as-received BDP (FPF = 14.7 %) and the 63.2 % drug release time of the drug-carrier composite particles was 15.6 times faster than that of as-received BDP. This study suggests that the drug-carrier composites produced using LTSAA can be employed in the instant formulation of inhalable dry powder.



中文翻译:

通过低温超临界辅助雾化制备可吸入倍氯米松二丙酸酯-甘露醇复合颗粒

甘露醇载体和药物载体复合颗粒是通过低温超临界辅助雾化(LTSAA)制备的。添加了L-亮氨酸的甘露醇载体颗粒增强的雾化作用可归因于波纹状细颗粒的形成,这降低了颗粒间的内聚力并导致了更好的甘露醇载体颗粒的流动性。水溶性差的药物倍氯米松双丙酸酯(BDP)和甘露醇在LTSAA期间共沉淀,最佳添加9.1质量%L-亮氨酸。在体外气雾化和溶解实验表明,细颗粒级分(FPF)的药物-载体复合颗粒的为3.4倍(FPF  = 49.9%)高于原先的BDP(FPF  = 14.7%),药物载体复合颗粒的63.2%药物释放时间比原先的BDP快15.6倍。这项研究表明,使用LTSAA生产的药物载体复合物可用于可吸入干粉的即时制剂。

更新日期:2020-11-02
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