三氧化二砷（As₂O₃）已有两千多年的药用历史，其药性猛烈，中医经典方剂中常作以毒攻毒之用，主要将As₂O₃用于各类疑难杂症的治疗。现代医学研究发现，As₂O₃在治疗血液系统恶性疾病和抗肿瘤方面效果显著，但其安全剂量小，不良反应强，限制了As₂O₃的临床使用与疗效。随着新型给药系统研究与发展，以及制剂材料、设备技术日渐丰富成熟，各种As₂O₃新剂型应运而生，为推进实现As₂O₃类药物制剂减毒增效这一核心目标提供了强大助力。归纳了As₂O₃古今各种剂型，总结As₂O₃的药用特性、已有制剂类型及其相关临床适应证，并以此为基础探讨As₂O₃制剂的未来发展方向和应用前景，以期为深入发掘As₂O₃临床价值和其新剂型的研发提供参考。

Arsenic trioxide (As₂O₃) has a long medicinal history of more than two thousand years, and its medicinal properties are strong. It is recorded in the classical prescriptions of traditional Chinese medicine that As₂O₃ is mainly used as an antidote for poison in the treatment of difficult and miscellaneous diseases. Modern medical research found that As₂O₃ has significant effect in the treatment of blood system malignant diseases and tumor. However, the small safe dose and strong toxic and side effects limit the clinical application and curative effect of As₂O₃. With the research and development of new drug delivery system, as well as preparation materials and equipment technology becoming more and more mature, various new dosage forms of As₂O₃ came into being. It has provided a powerful boost to the core goal of reducing toxicity and increasing efficiency of As₂O₃ pharmaceutical preparations. In this paper, the ancient and modern preparations and pharmaceutical characteristics of As₂O₃, the types of existing preparations, and the related clinical indications were summarized, on the basis of which the future development direction and application prospect of As₂O₃ preparations were explored, in order to provide reference for the research and development of new preparations of As₂O₃ and in-depth exploration of its clinical value.

国家自然科学基金青年科学基金项目（82003954）；浙江省自然科学基金探索项目（Y23H280030）；浙江中医药大学校级科研基金项目（2020ZZ08）