Predicting the aerosol performance of dry powder inhalation formulations by interparticulate interaction analysis using inverse gas chromatography.
Predicting the aerosol performance of dry powder inhalation formulations by interparticulate interaction analysis using inverse gas chromatography.
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DOI：
10.1002/jps.20519
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发表时间：
2006
影响因子：
3.8
通讯作者：
H. Tong;B. Shekunov;P. York;A. Chow
中科院分区：
文献类型：
--
作者：
H. Tong;B. Shekunov;P. York;A. Chow
先前的研究已经证明了反相气相色谱（IGC）在区分传统顺序间歇结晶和微粉化制备的沙美特罗辛酸盐（SX）粉末和超临界流体结晶制备的SX粉末的表面能差异方面的应用。在本研究中，从IGC分析中得出的溶解度参数在无限稀释（零覆盖）下被进一步用于评估固-固相互作用对这些SX样品的体外气溶胶性能的影响，无论是否包含乳糖载体。为此，根据相应的溶解度参数计算了样品的内聚SX-SX相互作用强度和粘聚sx -乳糖相互作用强度，并使用多级液体冲击器测定了它们的细颗粒分数。研究发现，只有黏附的SX-乳糖相互作用强于黏附的SX-SX相互作用时，加入乳糖载体才能显著改善SX的气溶胶性能。这两种相互作用形式的强度差异也与添加乳糖载体后细粒分数的增加有显著的相关性。这些结果表明，基于igc的颗粒间相互作用测量可以作为预测干粉吸入配方气溶胶性能的有用手段。
Previous studies have demonstrated the utility of inverse gas chromatography (IGC) in discriminating the differences in surface energy between salmeterol xinafoate (SX) powders prepared by conventional sequential batch crystallization and micronization and by supercritical fluid crystallization. In the present study, solubility parameters derived from IGC analysis at infinite dilution (zero coverage) were further utilized to evaluate the influence of solid-solid interactions on the in vitro aerosol performance of these SX samples, with or without the inclusion of a lactose carrier. To this end, the strength of cohesive SX-SX interactions and that of adhesive SX-lactose interactions were computed for the samples from the corresponding solubility parameters, and their fine particle fractions determined using a multi-stage liquid impinger. It was found that the aerosol performance of SX could be substantially improved by the addition of lactose carrier only if the adhesive SX-lactose interactions were stronger than the cohesive SX-SX interactions. The difference in strength between these two forms of interactions also displayed a significant correlation with the increase in fine particle fraction after the addition of lactose carrier. These results suggest that IGC-based interparticulate interaction measurements may serve as a useful means for predicting the aerosol performance of dry powder inhalation formulations.