青蒿素类药物新制剂研究进展

Progress in New Formulation Studies of Artemisinins

青蒿素类药物除抗疟作用外,在治疗肿瘤、免疫和病毒等疾病方面具有潜在的临床应用价值。其传统制剂存在体内代谢迅速、消除半衰期短、生物利用度低、疟原虫复燃率高等缺点。研究显示,将该类药物制备成脂质体、固体分散体、环糊精包合物、自乳化和纳米粒等剂型可以改善其溶解度、提高生物利用度、减慢体内消除速度、增强缓释和靶向作用。因此,研制青蒿素类药物新剂型对提高其临床疗效和新适应证的开发具有重要意义。笔者通过文献检索,对国内外有关青蒿素类药物新剂型的研究进展进行了综述。

Artemisinins were reported to have the potential efficacy of anticancer, immunoregulation, antivirus besides antimalaria. The marketed traditional formulations have the drawbacks of rapid metabolism, short elimination half-life, poor bioavailability, high plasmodium recrudescence rate. New drug delivery systems such as liposomes, solid dispersion, entrapped cyclodextrin complex, self- emulsification and nanoparticles can improve the solubility and bioavailability, slow the elimination and enhance the slow release and targeted action. So it is essential to develop novel dosage forms of artemisinins for improving clinical curative effect and new indications. Literatures about the preparations of artemisinins, which were published in recent years, are summarized and reviewed.