Optimization, characterization and in vitro/vivo evaluation of azilsartan nanocrystals

作     者：Jingjing Ma Yinxian Yang Yinghua Sun Jin Sun 

作者机构：Shenyang Pharmaceutical University 

出 版 物：《Asian Journal of Pharmaceutical Sciences》 (亚洲药物制剂科学（英文）)

年 卷 期：2017年第12卷第4期

页      面：344-352页

核心收录：

学科分类：100702[医学-药剂学] 1007[医学-药学(可授医学、理学学位)] 1006[医学-中西医结合] 100602[医学-中西医结合临床] 10[医学] 

基　　金：financially supported by Science research project of Department of Education Liaoning Province(No.L2013390) 

主　　题：Azilsartan Nanocrystals Sodium deoxycholate Freeze drying Dissolution Oral bioavailability 

摘      要：Azilsartan(AZL), a poorly soluble drug, was considered to be fit for nanocrystals to improve its solubility. Our study intended to prepare AZL nanocrystals by means of bead milling method. Eight stabilizers or their binary combination and the milling time were set to be variable factors to optimize AZL nanosuspension formulation, and six types of freezedrying supports were investigated to reduce the aggregation of particles during the solidification. AZL nanocrystals with or without sodium deoxycholate(NaDC) as combined stabilizer with Poloxamer 188(F68) were prepared owning mean particle sizes of about 300 nm and 460 nm. During the screening processes, the formulation containing NaDC showed a smaller particle size and better stability during lyophilization. The irregular shape and crystal form changing in AZL nanocrystals were discovered by various characterizations. And with physical mixture as reference, nanocrystals showed its improvement about in-vitro dissolution and in-vivo bioavailability. In conclusion, the nanocrystals of AZL could be prepared well in our study. Additionally, our results suggested that NaDC was an appreciated excipient on the nanocrystals platform, which can exhibit the abilities of size-reduction and stabilitymaintaining on freeze-drying.