Scholz Patrik, Keck Cornelia M
University of Applied Sciences Kaiserslautern, Applied Pharmacy, Campus Pirmasens, 66953 Pirmasens, Carl-Schurz-Str. 10-16, Germany.
Curr Pharm Des. 2015;21(29):4217-28. doi: 10.2174/1381612821666150901100417.
Many new developed drug actives are poorly soluble, therefore the need to increase the solubility of these actives arises. Nanosuspensions are fast and easy to produce, enhance the bioavailability of poorly soluble drugs and feature many beneficial characteristics. However, nanocrystals in suspension form are physically metastable. Furthermore, the application of nanocrystal suspensions has no retarding effects. To overcome long term stability issues and open up a variety of options for controlled release, nanocrystals can be converted into solid dosage forms by different methods with different outcomes and features. Transformation of nanosuspensions into solid dosage forms opens up manifold options for the development of dosage forms with tailor-made drug release profiles. This review focuses on nanocrystal properties, established and new production techniques, as well as state of the art techniques for transformation of nanosuspensions into solid dosage forms. Nanocrystal technology is already today used in several solid products and holds great potential for future uses.
许多新开发的药物活性成分溶解性很差，因此出现了提高这些活性成分溶解度的需求。纳米混悬液制备快速且简便，能提高难溶性药物的生物利用度，并具有许多有益特性。然而，混悬液形式的纳米晶体在物理上是亚稳的。此外，纳米晶体混悬液的应用没有缓释作用。为了克服长期稳定性问题并开辟多种控释选择，可以通过不同方法将纳米晶体转化为固体剂型，这些方法具有不同的结果和特性。将纳米混悬液转化为固体剂型为开发具有定制药物释放曲线的剂型开辟了多种选择。本综述重点关注纳米晶体的性质、已有的和新的生产技术，以及将纳米混悬液转化为固体剂型的最新技术。纳米晶体技术如今已应用于多种固体产品中，并具有巨大的未来应用潜力。
