原辅料及制剂处方工艺对口服固体制剂溶出行为的影响

Effects of APIs,excipients,formulations and technologies on the dissolution profiles of solid oral preparations

2016年5月,国家食品药品监督管理总局发布关于落实《国务院办公厅关于开展仿制药质量和疗效一致性评价的意见》有关事项的公告,明确提出一致性评价的研究内容之一是以参比制剂为对照,进行固体制剂溶出曲线的比较研究。固体制剂的体外溶出行为受到原辅料及制剂处方工艺等多个因素的影响。本文在文献调研的基础上,从原料的晶型和粒度、辅料的种类和用量、原料微粉化技术、片剂制备工艺等因素对口服固体制剂溶出行为的影响进行了综述,以期为开展一致性评价研究提供参考。

In May 2016,CFDA issued the announcement according to the notice of quality and effect consistency evaluation of generic drugs issued by the State Council. In the announcement it was clearly proposed that the comparison study of dissolution profiles between the test preparation and the reference preparation for solid preparations was a part of the consistency evaluation. It was known that many factors such as APIs,excipients,formulations and technologies could affect the dissolution profiles of solid preparations. In this paper,based on a literature retrieval,the effects such as crystal forms and sizes of APIs,types and amounts of excipients,micro powder technologies of APIs and the preparation process of tablets on the dissolution profiles of solid oral preparations were reviewed. It would provide some assistance on the consistency evaluation of generic drugs in our country.