Aquino Rita Patrizia, Stigliani Mariateresa, Del Gaudio Pasquale, Mencherini Teresa, Sansone Francesca, Russo Paola
Department of Pharmacy, University of Salerno, Via Giovanni Paolo II, No. 132, 84084 Fisciano, Italy.
ScientificWorldJournal. 2014;2014:838410. doi: 10.1155/2014/838410. Epub 2014 Dec 16.
The aim of this research was to evaluate the potential of the nanospray drier as a novel apparatus for the manufacturing of a dry powder for inhalation containing ketoprofen lysinate, a nonsteroidal anti-inflammatory drug able to control the inflammation in cystic fibrosis patients. We produced several ketoprofen lysinate and leucine powder batches by means of nanospray dryer, studying the influence of process parameters on yield, particle properties (size distribution and morphology), and, mainly, aerodynamic properties of powders. Micronized particles were prepared from different hydroalcoholic solutions (alcohol content from 0 to 30% v/v) using ketoprofen in its lysine salt form and leucine as dispersibility enhancer in different ratios (from 5 to 15% w/w) with a total solid concentration ranging from 1 to 7% w/v. Results indicated that the spray head equipped with a 7 µm nozzle produced powders too big to be inhaled. The reduction of nozzle size from 7 to 4 µm led to smaller particles suitable for inhalation but, at the same time, caused a dramatic increase in process time. The selection of process variables, together with the nozzle pretreatment with a surfactant solution, allowed us to obtain a free flowing powder with satisfying aerosol performance, confirming the usefulness of the nanospray drier in the production of powder for inhalation.
本研究的目的是评估纳米喷雾干燥器作为一种新型设备用于制造含赖氨酸酮洛芬的吸入用干粉的潜力，赖氨酸酮洛芬是一种能够控制囊性纤维化患者炎症的非甾体抗炎药。我们通过纳米喷雾干燥器制备了几批赖氨酸酮洛芬和亮氨酸粉末，研究了工艺参数对产率、颗粒性质（粒度分布和形态）以及主要是粉末空气动力学性质的影响。使用赖氨酸盐形式的酮洛芬和亮氨酸作为分散性增强剂，以不同比例（5%至15% w/w），从不同的水醇溶液（酒精含量从0至30% v/v）制备微粉化颗粒，总固体浓度范围为1%至7% w/v。结果表明，配备7 µm喷嘴的喷头产生的粉末太大，无法吸入。将喷嘴尺寸从7 µm减小到4 µm导致产生适合吸入的较小颗粒，但同时导致工艺时间大幅增加。工艺变量的选择，以及用表面活性剂溶液对喷嘴进行预处理，使我们能够获得具有令人满意的气溶胶性能的自由流动粉末，证实了纳米喷雾干燥器在吸入用粉末生产中的实用性。
