應(yīng)用于吸入粉霧劑（DPI）的藥物活性成分通常是小粒徑絕緣體，容易在制備與運(yùn)輸過程中攜帶電荷，增加藥物之間以及藥物-載體之間的黏附性，影響藥物在肺部的沉積。了解DPI中粘性粉末靜電作用的影響因素是至關(guān)重要的，影響因素包括粉末的電阻率、粒度分布、晶習(xí)、晶型、引濕性、環(huán)境因素、制備條件以及儲(chǔ)存條件等。還探討了靜電力對(duì)DPI藥物含量均一性、遞送劑量、原料藥與載體的黏附/解吸附能力以及藥物在呼吸道的沉積行為的影響。對(duì)靜電力的認(rèn)知與理解有助于DPI產(chǎn)品的安全性、質(zhì)量以及臨床有效性的提高。

Active pharmaceutical Ingredients of dry inhalation powers (DPI) are typically insulators consisting of relatively small particles and usually charging in the unit operation of preparation and transportation, thus the increasing adhesive and cohesive mixture powders affecting the efficiency of the pulmonary delivery of drugs. This article reviews the factors affecting the electrostatic charging of pharmaceutical powders with a focus on DPI. The influences of particle resistivity, size distribution, crystal morphology, polymorph, hygroscopicity, environmental conditions, pharmaceutical processing, and storage on the electrostatic charge behaviors of powder mixtures. Moreover, the influence of electrostatic charging on the drug content homogeneity, the passage of drug through in inhaler device, drug-carrier adhesion/detachment, and drug deposition on the respiratory airways were discussed. The understanding of electrostatic charging is crucial to improving the safety, quality and efficiency of the DPIs products.

國家科技部重大專項(xiàng)（2017ZX09201002）