The relationship between drug concentration, mixing time, blending order and ternary dry powder inhalation performance
The relationship between drug concentration, mixing time, blending order and ternary dry powder inhalation performance
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DOI：
10.1016/j.ijpharm.2010.02.031
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发表时间：
2010-05-31
影响因子：
5.8
通讯作者：
Buckton, Graham
中科院分区：
文献类型：
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作者：
Jones, Matthew D.;Santo, Joao G. F.;Buckton, Graham
一些研究表明，在三元干粉吸入器(DPI)配方中，药物、细颗粒和粗载体的混合顺序会影响细颗粒的输送；其他研究则没有发现差异。考察了硫酸沙丁胺醇浓度(0.5-4.5%(W)/(W))、混合时间和混合顺序(先是药物和乳糖载体，然后是乳糖微粉；还是先是微粉和载体，再是药物)对制剂细颗粒释放的影响。混合15min时，药物浓度和混合顺序对微粒子分数(FPF)没有影响。混合30min时，药物浓度越低，混合效果越好，颗粒越细，混合顺序越好。较高的药物浓度导致混合顺序之间的性能相同。在混合60min时，药物和载体的第一次混合顺序导致0.5%(W)/(W)沙丁胺醇硫酸盐的a_ff较大。以前相互矛盾的研究使用的混合时间为30分钟；这些结果表明，他们相互矛盾的结果可能是由于使用了不同的药物浓度。整个数据集的复杂性表明，混合顺序研究对于研究罚款影响背后的机理是有限的。(C)2010爱思唯尔B.V.保留所有权利。
Some studies have shown that the mixing order of drug, fines and coarse carrier in a ternary dry powder inhaler (DPI) formulation affects fine particle delivery; others have seen no difference. This was investigated by examining the influence of salbutamol sulphate concentration (0.5-4.5%(w)/(w)), mixing time and blending order (drug and lactose carrier first, then lactose fines; versus fines and carrier first, then drug) on formulation in vitro fine particle delivery. With 15 min of mixing, there was no effect of drug concentration or blending order on fine particle fraction (FPF). With 30 min of mixing, lower drug concentrations produced larger FPFs with the fines and carrier first blending order. Higher drug concentrations resulted in equal performance between the blending orders. With 60 min of mixing, the drug and carrier first blending order resulted in larger a FPF at 0.5%(w)/(w) salbutamol sulphate. The previous conflicting studies used a mixing time of 30 min; these results suggest that their conflicting results may have been due to the use of different drug concentrations. The complexity in the whole dataset suggests that blending order studies are of limited use for the investigation of the mechanism behind the effects of fines. (C) 2010 Elsevier B.V. All rights reserved.