目的综述水难溶性药物纳米晶体的制备方法,稳定剂在纳米晶体形成过程中的主要应用原理及产品物理性质的表征,为改善水难溶性药物溶解度或口服生物利用度提供理论依据。方法查阅国内外相关文献27篇,回顾纳米晶体技术的发展历程,提供药物纳米晶体技术的最新研究进展。结果药物纳米晶体不仅制备工艺简单,性质考察方便;还能够提高难溶性药物在胃肠道中的溶解度,改善难溶性药物的口服生物利用度。结论药物纳米晶体技术具有实际生产意义和广阔的应用前景。
Objective To review the formulation of poorly water-soluble drugs through nanocrystals technology,stabilizers selection and the principles underlying stabilization during the process,and characterizations of the formulation.Methods History and progress of nanocrystals technologies were reviewed and the latest researches were reported by referring to relevant literatures home and abroad.Results Compared to other nanoformulations,drug nanocrystals are easily to be formulated and characterized.More importantly,it can significantly enhance the dissolution rate of poorly water-soluble drugs in gastrointestinal lumen contents and improve the oral-bioavailability of these drugs.Conclusions The simple but smart formulating process makes nancrystals technology feasible for scale-up production and possessing promising future.