Bérard V, Lesniewska E, Andrès C, Pertuy D, Laroche C, Pourcelot Y
Pharmacy Division L.P.G., U.F.R. Pharmacy, University of Bourgogne, F-21079, Dijon, France.
Int J Pharm. 2002 Jan 31;232(1-2):213-24. doi: 10.1016/s0378-5173(01)00913-9.
In the dry powder inhalers (DPIs), the adhesion results of the interactions between the active substance and the excipient. The carrier and the micronized drug particle morphologies are believed to affect the delivery of the drug. In this work, the couple studied was the lactose monohydrate and micronized zanamivir, used for the treatment of influenza. In a first approach, observations by scanning electron microscopy (SEM) have shown that the relative humidity (RH) greatly influenced the zanamivir amount fixed on the lactose monohydrate surface. This paper deals with the direct measurement in controlled atmosphere by atomic force microscopy (AFM) of the forces and the interaction ranges between a zanamivir probe and a lactose substrate. Selected zanamivir crystals were attached to the standard AFM probe. Different RH have been used in order to determine influent parameters permitting to identify the nature of adhesion forces between them. This study demonstrated that the increase of RH modified progressively the surface topology of the two components and increased the adhesion force.
在干粉吸入器（DPI）中，活性物质与辅料之间相互作用的结果表现为黏附。载体和微粉化药物颗粒的形态被认为会影响药物的递送。在这项研究中，所研究的组合是用于治疗流感的一水乳糖和微粉化扎那米韦。在第一种方法中，扫描电子显微镜（SEM）观察表明，相对湿度（RH）极大地影响了固定在一水乳糖表面的扎那米韦量。本文论述了通过原子力显微镜（AFM）在可控气氛中直接测量扎那米韦探针与乳糖底物之间的力及相互作用范围。将选定的扎那米韦晶体附着于标准AFM探针上。采用了不同的相对湿度以确定影响参数，从而识别它们之间黏附力的性质。这项研究表明，相对湿度的增加逐渐改变了两种组分的表面拓扑结构并增加了黏附力。
