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系统研究不同药物纳米晶体技术制备快速溶解美洛昔康片

Systematical Investigation of Different Drug Nanocrystal Technologies to Produce Fast Dissolving Meloxicam Tablets.

机构信息

Department of Pharmaceutical Engineering, Qingdao University of Science and Technology, Qingdao, China.

Department of Internal Medicine, Qingdao Shibei District People Hospital, Qingdao, China.

出版信息

AAPS PharmSciTech. 2018 Feb;19(2):783-791. doi: 10.1208/s12249-017-0889-8. Epub 2017 Oct 10.

Abstract

Three different methods, i.e., high-pressure homogenization, wet bead milling, and a combination approach of freeze-drying and high-pressure homogenization, were used to produce meloxicam nanosuspensions, respectively. Wet bead milling led to the nanosuspensions with smallest particle size (88 nm) after 4 h and optimal dissolution performances. Freeze-dried meloxicam powder could highly improve the size reduction efficiency compared to the unmodified drug and particle size of the freeze-dried sample could be reduced to 342 nm after only one homogenization cycle at 1000 bar. The polymorphism transition and change of the particle morphology after the lyophilization might be important reasons to affect the nanosizing processes. Interestingly, the tablets prepared by using nanosuspensions from homogenizer and combination process showed faster dissolution in the first 20 min than the bead milling nanocrystal tablets.

摘要

分别采用高压匀浆法、湿磨法和冷冻干燥-高压匀浆相结合的方法制备美洛昔康纳米混悬剂。湿磨法在 4 小时后得到了最小粒径(88nm)和最佳溶解性能的纳米混悬剂。与未修饰的药物相比,冻干美洛昔康粉末可以大大提高粒径减小的效率,并且在仅经过 1000 巴的 1 个高压匀浆循环后,冻干样品的粒径可以减小至 342nm。冷冻干燥后多晶型转变和颗粒形态的变化可能是影响纳米化过程的重要原因。有趣的是,使用高压匀浆和组合工艺制备的纳米混悬剂制备的片剂在前 20 分钟内显示出比珠磨法制备的纳米晶片剂更快的溶解速度。

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