长效缓释微球制剂生产技术的发展现状

Advanced Studies in the Preparation Techniques of Sustained-release Microsphere

长效缓释微球是将药物溶解或分散在高分子骨架材料中的微米级别的药物释放载体,这种新剂型可以显著降低给药频率,同时大分子材料的包裹可以提高药物的稳定性,降低药物的毒副作用,目前广泛应用在蛋白多肽等药物。已有一些用于治疗糖尿病、精神病、子宫内膜异位等疾病的长效缓释微球制剂被批准上市。然而,因为微球的制备工艺繁杂、质量控制困难,至今只在少数产品上应用,现在越来越多的口服难吸收的生物药物开始产品化,长效缓释微球在提高患者依从性方面备受瞩目。本综述对目前典型的微球制备技术做出分析和评判,以期对完善微球制备工艺有所帮助。

Long-acting microspheres,as a kind of micron level drug carrier,are made from drug dissolving or dispersing in polymer materials.This new dosage form can significantly reduce dosing frequency,improve the stability and reduce the side effects of drugs with macromolecular material package.Nowadays,microspheres become widely used in protein polypeptide drugs.Some sustained-release microsphere dosage forms have been launched to the market for diabetes,mental disease and endometriosis.However,only a few microsphere products due to their complicated manufacture processes and difficulties in quality control.As more and more orally non-absorbable biologic medicines are coming to commercialization,microspheres will become more favorable in terms of improving patient compliance.In article the typical microspheres are reviewed with the purpose of helping scientists and students in pharmaceutical sciences to improve the art of microsphere formulation with the analysis and critiques we offered.