Sansone F, Aquino R P, Del Gaudio P, Colombo P, Russo P
Department of Pharmaceutical Sciences, University of Salerno, Fisciano (SA), Italy.
Eur J Pharm Biopharm. 2009 May;72(1):206-13. doi: 10.1016/j.ejpb.2008.10.007. Epub 2008 Nov 1.
The aim of the present work was to develop dry powders containing naringin for a direct administration to the lung to combat oxidative stress. Naringin microparticles were prepared by spray-drying the neat flavonoid (2-5% w/v) from different water/ethanol co-solvents. The spray-dried powders were characterised for morphology, density, particle size distribution, residual humidity, crystallinity, solubility, thermal behaviour and respirable fraction. The fine fraction of the powders was measured by single-stage glass impinger and Andersen cascade impactor, using the Turbospin device for the deposition tests, wherein the dose to be aerosolised was premetered in a gelatine capsule. By increasing the ethanol content, the feed liquid turned from a suspension into a solution: the spray of flavonoid suspensions led to powders with high crystallinity degree, low water solubility and high bulk density, while the spray of drug solutions led to more amorphous particles, with higher solubility, lower density and improved aerodynamic behaviour. The optimisation of the operative parameters produced enhanced aerosol performance of the flavonoid powders containing only the active compound.
本研究的目的是开发含有柚皮苷的干粉，以便直接给药至肺部以对抗氧化应激。通过对不同水/乙醇共溶剂中的纯类黄酮（2-5% w/v）进行喷雾干燥来制备柚皮苷微粒。对喷雾干燥粉末的形态、密度、粒度分布、残留湿度、结晶度、溶解度、热行为和可吸入部分进行了表征。使用Turbospin装置进行沉积试验，通过单级玻璃冲击器和安德森级联冲击器测量粉末的细颗粒部分，其中待雾化的剂量预先装入明胶胶囊中。随着乙醇含量的增加，进料液从悬浮液变为溶液：类黄酮悬浮液的喷雾产生了具有高结晶度、低水溶性和高堆积密度的粉末，而药物溶液的喷雾产生了更多的无定形颗粒，具有更高的溶解度、更低的密度和更好的空气动力学性能。操作参数的优化提高了仅含有活性化合物的类黄酮粉末的气溶胶性能。
