塞来昔布纳米晶体的制备与表征.pdfVIP

中国医药工业杂志 Chinese Journal of Pharmaceuticals 2015 , 46 (4) • 358 • 塞来昔布纳米晶体的制备与表征 黄婷lZ ，林巧平2 ，钱勇气许向F时，周建平1* (1.中国药科大学药剂学教研室，江苏南京 210009; 2. 江苏先声药业有限公司，江苏南京 210042) 摘要:采用反溶剂沉淀法联合高压均质法技术制备塞来苦布的纳米晶体，提高其溶出度。以塞来昔布初混悬液形貌、纳米 晶体混悬液粒子粒径和多分散系数 (PDI) 为指标，考察稳晶剂种类和比例、高压均质参数、固化方式等的影响。结果表 明，将聚维嗣K30 25 mg 与十二炕基硫酸纳2.5mg 联用作稳晶剂， 500 bar 下循环 10 次，得到的纳米晶体粒径为 (283.67土 20.84)nm , PDI 为 0.16:1:0.01 (n=3) 。喷雾干燥得到的产品复溶后能分散成均一混悬液，粒径为 (623.33:1:28.71) nm。采用 X 射线衍射、差示扫描量热法、扫描电镜、透射电镜、饱和溶解度对原药及纳米晶体性质进行表征分析，结果表明纳米 晶体结构和晶型保持不变。所得纳米晶体的溶出率明显高于原药和物理混合物，且在高温高湿条件下放置lOd 仍较稳定。 关键词:纳米晶体:塞来昔布:反溶剂沉淀法:高压均质:溶出度 中图分类号: R944.9 文献标志码:A 文章编号: 1001-8255 (2015) 04-0358-06 Preparation and Characteristics of Celecoxib Nanocrystals 2 2 2 l HUANG Tingl.2 , LIN Qiaoping , QIAN Yong , XU Xiangyang , ZHOU Jianping * (1. Dept. ofPharmacy, China Pharmaceutical University, Nanjing 210009; 2. Jiangsu Simcere Pharmaceutical Co., Ltd. , Nanjing 210042) ABSTRACT: Celecoxib nanocrystals were prepared by a combined method of antisolvent precipitation and high pressure homogenization to increase the dissolution of celecoxib. The effects of types and ratios of stabilizers, pressure and circle numbers of high pressure homogenization were investigated with appearance of initial suspension, particle size and polydisperse index (PDI) of nanocrystal suspension as indexes. The optimal nanosuspension was prepared with the combined stabilizers of 25 mg of Polyvidone K30 and 2.5 mg of sodium dodecyl sulfate, at the pressure of 500 bar for 10 circles. The particle size and PDI of the nanosuspension were (283.67土20.84) nm and 0.16土0.01 (n=3). Then the nanosuspen