药物纳米结晶的固体化方法以及产品性质的影响因素
he method to solidify the drug nanocrystals and the influence factors of the product's properties.
纳米结晶是提高难溶性药物口服生物利用度的重要手段,具有制备简便、载药量高和易放大等优势而备受科研、生产人员的青睐。但由于在纳米化过程中产生的巨大表面能,纳米结晶为热力学不稳定系统,在储存过程中容易发生聚集、沉降等问题,导致制剂的口服生物利用度下降,因此需要通过固体化的方式提高其稳定性。本文对纳米结晶常用的固体化方法包括喷雾干燥、冷冻干燥、流化床包衣/制粒以及喷雾冷冻干燥的原理以及特点进行了介绍,并针对喷雾干燥以及冷冻干燥简述了影响产品质量的因素。
Nanocrystals play an important role in improving the oral bioavailability of poorly water soluble drugs. Owing to the simple preparation process, high drug loading and good scalability, nanocrystals were popular with many researchers and manufacturers. However, due to the large surface energy generated during the nanonization, nanocrystals are thermodynamically unstable, prone to aggregation and/or sedimentation during the storage, which may results in a poor oral bioavailability. Accordingly, to improve the stability, the solidification is needed. In this paper, we introduced the principle and characteristics of the commonly used solidification methodsfor nanocrystals, including spray drying, freeze drying, fluidized bed coating / granulation and spray freeze drying. What is more, the factors affecting the quality of the spray dried and freeze dried products are described briefly.
何仲贵、侯彦先
药学生物科学研究方法、生物科学研究技术
药剂学难溶性药物口服生物利用度纳米结晶固体化
pharmaceuticspoorly water soluble drugsoral bioavailabilitynanocrystalssolidification
何仲贵,侯彦先.药物纳米结晶的固体化方法以及产品性质的影响因素[EB/OL].(2017-03-22)[2025-08-21].http://www.paper.edu.cn/releasepaper/content/201703-300.点此复制
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