The purpose of the present research is to establish a novel nanosizing technique starting from wet nano-milling, named "dry nanosuspension" technique for poorly water-soluble drugs. The spray freeze-drying (SFD) method was applied instead of the spray-drying one previously developed. Drug particles were milled in the aqueous solution of dispersing agents using an oscillating beads-milling apparatus. The milled nanosuspension was sprayed to the surface of liquid nitrogen, and the resultant iced droplets were freeze-dried to obtain the powdery product. The loading ratio of a dispersing agent was investigated to enhance its redispersing property. Dry nanosuspension, which could be spontaneously dispersed into original nanosuspension in water, was obtained by SFD process. It was assumed that self dispersion property would be attributed to its structure with porous network, in which the primary milled drug crystals were embedded. Such unique structure contributed greatly to immediate release behaviors of the drug in gastrointestinal buffered media. These pharmaceutical properties were enhanced by increasing the ratio of the dispersing agent to the drug and the solid content in suspension to be sprayed. The present technique via wet milling and spray freeze-drying processes would be a novel dissolution-enhanced technology for poorly water-soluble drugs.

译文

本研究的目的是建立一种从湿法纳米研磨开始的新型纳米上浆技术,称为水溶性差的药物的 “干法纳米悬浮液” 技术。采用喷雾冷冻干燥 (SFD) 方法代替了先前开发的喷雾干燥方法。使用振荡珠磨设备在分散剂水溶液中研磨药物颗粒。将研磨的纳米悬浮液喷洒到液氮表面,并将所得的冰滴冷冻干燥以获得粉末状产品。研究了分散剂的负载比,以提高其再分散性能。通过SFD工艺获得了干燥的纳米悬浮液,该悬浮液可以自发地分散到水中的原始纳米悬浮液中。假定自分散特性归因于其具有多孔网络的结构,其中嵌入了初级研磨的药物晶体。这种独特的结构极大地促进了药物在胃肠道缓冲介质中的立即释放行为。通过增加分散剂与药物的比例以及要喷洒的悬浮液中的固体含量,可以增强这些药物性能。本技术通过湿法研磨和喷雾冷冻干燥工艺将是一种新型的水溶性药物溶出增强技术。

+1
+2
100研值 100研值 ¥99课程
检索文献一次
下载文献一次

去下载>

成功解锁2个技能,为你点赞

《SCI写作十大必备语法》
解决你的SCI语法难题!

技能熟练度+1

视频课《玩转文献检索》
让你成为检索达人!

恭喜完成新手挑战

手机微信扫一扫,添加好友领取

免费领《Endnote文献管理工具+教程》

微信扫码, 免费领取

手机登录

获取验证码
登录