Albertini Beatrice, Passerini Nadia, Pattarino Franco, Rodriguez Lorenzo
Dipartimento di Scienze Farmaceutiche, Università di Bologna, Bologna, Italy.
Eur J Pharm Biopharm. 2008 May;69(1):348-57. doi: 10.1016/j.ejpb.2007.09.011. Epub 2007 Oct 24.
A new pneumatic atomizer for spray congealing, called wide pneumatic nozzle (WPN), was developed. To evaluate its performance, microparticles containing highly concentrated either solid drug (Propafenone hydrochloride, PRF) or liquid nutraceutical (Vitamin E, VE) have been prepared and characterized. The results showed that the spray congealing nozzle enabled the production of spherical and not aggregated microparticles with high yields (95% w/w) and relatively narrow size distributions; moreover, increasing the viscosity of the suspension from 50 to 500 mPa s, the particle size increased. The loading of the drug was high for microspheres (50% for PRF and 30% for VE) and the encapsulation efficiency was good for all formulations. The drug release was easily modified according to the nature of the used excipients, as both lipophilic (carnauba wax, cetearyl and stearyl alcohols) and hydrophilic (PEG 4000) carriers were employed. Moreover the results evidenced that it was possible to encapsulate actives (VE) that are in a liquid form and to enhance their availability. In conclusion the developed spray congealing nozzle was able to nebulize very viscous systems that are usually not processed by conventional apparatus and to produce microspheres with high and uniform drug content.
开发了一种用于喷雾冷凝的新型气动雾化器，称为宽气动喷嘴（WPN）。为了评估其性能，制备并表征了含有高浓度固体药物（盐酸普罗帕酮，PRF）或液体营养剂（维生素E，VE）的微粒。结果表明，喷雾冷凝喷嘴能够以高收率（95% w/w）生产球形且不聚集的微粒，并且粒径分布相对较窄；此外，将悬浮液的粘度从50 mPa s增加到500 mPa s，粒径会增大。微球的药物载量较高（PRF为50%，VE为30%），并且所有制剂的包封效率都良好。根据所用辅料的性质，药物释放很容易调节，因为同时使用了亲脂性（巴西棕榈蜡、鲸蜡硬脂醇和硬脂醇）和亲水性（聚乙二醇4000）载体。此外，结果证明可以包封液体形式的活性成分（VE）并提高其利用率。总之，所开发的喷雾冷凝喷嘴能够雾化通常无法用传统设备处理的高粘性体系，并生产出药物含量高且均匀的微球。
