JIN Rui1, CHENG Kaisheng2, LI Zhiyun2, LI Chunni2, CHEN Dengjun2, ZANG Hongmei1
(1. School of Pharmacy, Anhui Medical University, Hefei 230032, China;2. Hefei Cosource Pharmaceuticals Inc, Hefei 230031, China)
Abstract: In order to find the reasons for the significant difference in dissolution rate of valsartan amlodipine tablets prepared from two batches of valsartan raw materials, dissolution rate of valsartan amlodipine tablets was determined in the dissolution medium of PBS (pH=4.5). The crystal form of valsartan was determined by powder X-ray diffraction, the particle size of valsartan was determined by laser particle size analysis method, particle morphology of valsartan and premixer were observed by optical microscope, and the differences between batches were compared to explore the causes of differences in dissolution rate. The results showed that the crystal forms of the two batches of valsartan were amorphous, and the particle sizes measured in 1% SDS and liquid paraffin were also the same, but there were significant differences in the particle shape of the two batches of valsartan in the powder form and premix. The first batch and the second batch of valsartan raw materials were dendritic and globular, respectively. Therefore, in the case of the same crystal form and particle size, the form of the raw material may affect the dissolution of the preparation. The globular raw material has a small contact surface between other materials during the preparation of the tablet, and it is difficult to bond into a large agglomerate, and the tablet made by globular raw material dissolved faster than dendritic raw material. Moreover, when the crystal form and the particle diameter of the raw material were the same, the particle size cannot be used to distinguish the difference between the raw material batches, and the control of the grain shape of the raw material should be emphasized.
Keywords:valsartan; particle size; dissolution
中图分类号：R944; R969 1 文献标志码：A
收稿日期： 2019-03-01， 修回日期：2019-05-07，在线出版时间：2019-06-21 10:38。
基金项目：安徽省自然科学基金项目，编号：1708085QH196。
第一作者简介：金瑞(1994—)，女，硕士研究生，研究方向为药物新制剂与新剂型。E-mail：2351785194@qq.com。
通信作者简介：臧洪梅(1980—)，女，博士，硕士生导师，研究方向为药物新制剂与新剂型。E-mail：zangweiwei2005@126.com。
文章编号：1008-5548(2019)05-0045-06
DOI:10.13732/j.issn.1008-5548.2019.05.008
