文献类型：期刊文献

英文题名：A mixed solvent system for preparation of spherically agglomerated crystals of ascorbic acid

作者：Ren, Fuzheng[1];Zhou, Yaru[1];Liu, Yan[1];Fu, Jinping[1];Jing, Qiufang[1];Ren, Guobin[1]

机构：[1]East China Univ Sci & Technol, Sch Pharm, Lab Pharmaceut Crystal Engn & Technol, Shanghai 200237, Peoples R China

年份：2017

卷号：22

期号：6

起止页码：818

外文期刊名：PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000404371600015)】；

基金：The authors would like to thank the supports from the Shanghai Committee of Science & Technology (14DZ1930802) and National Natural Science Foundation of China (21576080).

语种：英文

外文关键词：Ascorbic acid; binary mixed solvent; micromeritic properties; spherical crystallization

摘要：The objective of this research was to develop a novel solvent system to prepare spherically agglomerated crystals (SAC) of ascorbic acid with improved flowability for direct compression. A spherical agglomeration method was developed by selecting the mixed solvents (n-butyl and ethyl acetate) as a poor solvent and the process was further optimized by using triangular phase diagram and particle vision measurement. Physiochemical properties of SAC were characterized and compared with original drug crystals. It showed that amount of poor solvent, ratio of solvent mixture, and drug concentration are critical for preparation of SAC with desirable properties. The solid state of SAC was same as original crystals according to DSC, XRD, and FT-IR results. There was no significant difference in solubility and dissolution rate of drug between SAC and original crystals. The flowability and packability of SAC as well as the tensile strength and elastic recovery of tablets made from SAC were all significantly improved when compared with original crystals and tablets from crystals. It is concluded that the present method was suitable to prepare SAC of ascorbic acid for direct compression.