Multi-dimensional visualization for the morphology of lubricant stearic acid particles and their distribution in tablets  

作　　者：Liu Zhang Shailendra Shakya Li Wu Jiangtao Wang Guanghui Jin Huimin Sun Xianzhen Yin Lixin Sun Jiwen Zhang 

机构地区：[1]School of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016,China [2]Center for Drug Delivery Systems,Shanghai Institute of Materia Medica,Chinese Academy of Sciences,Shanghai 201203,China [3]Weihai Disu Pharmaceutical Manufacturer,Weihai 264200,China [4]National Institutes for Food and Drug Control,Beijing 100050,China

出　　处：《Asian Journal of Pharmaceutical Sciences》2020年第1期60-68,共9页亚洲药物制剂科学（英文）

基　　金：The authors are grateful for the financial support from the National Science and Technology Major Project(2017ZX09101001-006);Thanks to the BL13W1 beamline of the SSRF for the precious beam time and help from the team.

摘　　要：The shapes of particles and their distribution in tablets, controlled by pretreatment and tableting process, determine the pharmaceutical performance of excipient like lubricant. This study aims to provide deeper insights to the relationship of the morphology and spatial distribution of stearic acid(SA) with the lubrication efficiency, as well as the resulting tablet property. Unmodified SA particles as flat sheet-like particles were firstly reprocessed by emulsification in hot water to obtain the reprocessed SA particles with spherical morphology. The three-dimensional(3 D) information of SA particles in tablets was detected by a quantitative and non-invasive 3 D structure elucidation technique, namely, synchrotron radiation X-ray micro-computed tomography(SR-μCT). SA particles in glipizide tablets prepared by using unmodified SA(GUT), reprocessed SA(GRT), as well as reference listed drug(RLD) of glipizide tablets were analyzed by SR-μCT. The results showed that the reprocessed SA with better flowability contributed to similarity of breaking forces between that of GRT and RLD. SA particles in GRT were very similar to those in RLD with uniform morphology and particle size, while SA particles in GUT were not evenly distributed. These findings not only demonstrated the feasibility of SR-μCT as a new method in revealing the morphology and spatial distribution of excipient in drug delivery system, but also deepened insights of solid dosage form design into a new scale by powder engineering.The shapes of particles and their distribution in tablets, controlled by pretreatment and tableting process, determine the pharmaceutical performance of excipient like lubricant. This study aims to provide deeper insights to the relationship of the morphology and spatial distribution of stearic acid(SA) with the lubrication efficiency, as well as the resulting tablet property. Unmodified SA particles as flat sheet-like particles were firstly reprocessed by emulsification in hot water to obtain the reprocessed SA particles with spherical morphology. The three-dimensional(3 D) information of SA particles in tablets was detected by a quantitative and non-invasive 3 D structure elucidation technique, namely, synchrotron radiation X-ray micro-computed tomography(SR-μCT). SA particles in glipizide tablets prepared by using unmodified SA(GUT), reprocessed SA(GRT), as well as reference listed drug(RLD) of glipizide tablets were analyzed by SR-μCT. The results showed that the reprocessed SA with better flowability contributed to similarity of breaking forces between that of GRT and RLD. SA particles in GRT were very similar to those in RLD with uniform morphology and particle size, while SA particles in GUT were not evenly distributed. These findings not only demonstrated the feasibility of SR-μCT as a new method in revealing the morphology and spatial distribution of excipient in drug delivery system, but also deepened insights of solid dosage form design into a new scale by powder engineering.

关 键 词：Stearic ACID MORPHOLOGY Spatial DISTRIBUTION SR-μCT GLIPIZIDE TABLETS 

分 类 号：R943[医药卫生—药剂学]