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目的近年来,药物纳米晶体混悬液在解决难溶性药物制剂问题上所表现出的优势受到广泛关注与肯定。纳米晶体混悬液载药量高、易工业化生产、制备成本相对较低,还能应用于多种给药途径,在增加难溶性药物的生物利用度方面有突出贡献。方法综述了药物纳米晶体混悬液在各种给药途径中所表现出的独特的药动学特征,包括口服、注射、经眼和经肺等,并对其中的影响因素进行分析、讨论。结果与结论药物纳米晶体混悬液独特的理化性质使其在各个给药途径中都显著改善了难溶性药物的药动学特征,显著提高了难溶性药物的生物利用度。但是随着研究的进展纳米晶体混悬液也面临着一些新问题:如何使药物纳米晶体的溶出更加可控,如何减少药物纳米晶体在到达靶部位之前的释药,如何选择或建立模型对纳米晶体固体制剂进行体内-体外相关性(IVIVC)分析将是药物纳米晶体的下一个研究热点。
Objectives In recent years, drug nanocrystal suspensions have received wide attention and affirmation for their advantages in solving the problem of poorly soluble pharmaceutical preparations. Nanocrystalline suspension with high drug loading, easy industrial production, preparation cost is relatively low, but also can be applied to a variety of routes of administration, in increasing the bioavailability of poorly soluble drugs have made outstanding contributions. Methods This review summarizes the unique pharmacokinetic characteristics of drug nanocrystal suspensions in various routes of administration, including oral administration, injection, ocular and pulmonary passage, and analyzes and discusses the influencing factors. RESULTS AND CONCLUSIONS The unique physical and chemical properties of drug nanocrystal suspensions have significantly improved the pharmacokinetic characteristics of poorly soluble drugs in various administration routes and significantly improved the bioavailability of poorly soluble drugs. However, with the progress of research, nanocrystal suspensions also face some new problems: how to make drug nanocrystal dissolution more controllable, how to reduce the release of drug nanocrystals before reaching the target site, how to choose or establish the model for nanocrystals Crystalline solid preparations for in-vitro correlation (IVIVC) analysis of drug nanocrystals will be the next hot spot.