Institute for Particle Technology, Technische Universität Braunschweig, Volkmaroder Str. 5, 38104 Braunschweig, Germany; PVZ- Center of Pharmaceutical Engineering, Technische Universität Braunschweig, Germany.
Institute for Particle Technology, Technische Universität Braunschweig, Volkmaroder Str. 5, 38104 Braunschweig, Germany; PVZ- Center of Pharmaceutical Engineering, Technische Universität Braunschweig, Germany.
Eur J Pharm Biopharm. 2018 Oct;131:224-231. doi: 10.1016/j.ejpb.2018.08.011. Epub 2018 Aug 25.
Antisolvent precipitation of poorly water-soluble drugs is a promising formulation technique to synthesize amorphous nanoparticles. The dissolution behavior of these nanoparticles is improved because of the high specific surface area and the amorphous state, leading to an enhanced bioavailability of the drug molecules. Nevertheless, stabilization of precipitated drug nanoparticles against agglomeration and recrystallization, which constitutes a key issue for further processing steps, has turned out to be a major challenge. For that reason, the present study presents a synthesis method to produce long-term stable amorphous ibuprofen nanoparticles via antisolvent precipitation. To reach this goal, a new precipitation method was developed: antisolvent melt precipitation (AMP). Formulation strategies (e.g. varying fraction of stabilizer) as well as process parameters (e.g. temperature) were under study to estimate their influence on particle size, size distribution, crystallinity, morphology and stability of synthesized drug nanoparticles.
抗溶剂沉淀法是一种很有前途的药物制剂技术，可以合成无定形纳米颗粒。由于纳米颗粒具有高比表面积和无定形态，其溶解性能得到改善，从而提高了药物分子的生物利用度。然而，为了避免沉淀药物纳米颗粒的团聚和再结晶，需要对其进行稳定化处理，这是进一步加工步骤中的关键问题。因此，本研究提出了一种通过抗溶剂沉淀法制备长期稳定的无定形布洛芬纳米颗粒的合成方法。为了达到这个目的，开发了一种新的沉淀方法：抗溶剂熔融沉淀（AMP）。研究了配方策略（例如稳定剂的比例变化）和工艺参数（例如温度），以评估它们对合成药物纳米颗粒的粒径、粒径分布、结晶度、形态和稳定性的影响。
