湿法研磨结合液相层积技术制备呋喃妥因缓释微丸

发布时间：2018-04-03 21:26

本文选题：呋喃妥因　切入点：缓释微丸　出处：《沈阳药科大学学报》2017年02期

【摘要】：目的制备呋喃妥因缓释微丸,研究药物的晶型稳定性并评价微丸的缓释作用。方法通过湿法研磨技术制备呋喃妥因纳米混悬液;以差示扫描量热法(differential scanning calorimeter,DSC)及粉末X射线衍射法(powder X-ray diffraction,PXRD)研究药物晶型变化;采用液相层积技术制备呋喃妥因缓释微丸;通过体外释放度筛选处方;采用UPLC-MS/MS法测定Beagle犬血浆样品。结果药物经湿法研磨后,粒径由约40μm降至455 nm,晶型稳定。体外释放试验结果表明,在模拟体内胃肠道消化液环境的溶出介质中该制剂在释放前期符合零级释放,后期则符合一级释放。体内试验结果表明,呋喃妥因缓释微丸相对于市售肠溶包衣片的生物利度为143.8%;前者的消除半衰期(t1/2)及平均滞留时间(mean residence time,MRT)均较后者有所延长。结论湿法研磨技术可显著降低药物粒径,提高溶出速率,药物体外释放符合要求,该微丸具有一定缓释效果。
[Abstract]:Aim to prepare furantoin sustained-release pellets, to study the crystal stability of the drug and to evaluate the sustained release effect of the pellets.The formulation was screened by in vitro release and the plasma samples of Beagle dogs were determined by UPLC-MS/MS method.Results after wet grinding, the particle size decreased from about 40 渭 m to 455 nm, and the crystal shape was stable.The results of in vitro release test showed that the release of the preparation was in accordance with the zero order release in the early stage and the first release in the later stage in the dissolution medium simulating the gastrointestinal digestive fluid environment in vivo.The results showed that the bioavailability of furantoin sustained-release pellets was 143.8 compared with that of commercial enteric-coated tablets, the elimination half-life of the former was 1 / 2) and the mean residence time was longer than that of the latter.Conclusion Wet grinding technology can significantly reduce the particle size of the drug and increase the dissolution rate. The drug release in vitro meets the requirements, and the pellet has a certain sustained release effect.
【作者单位】：沈阳药科大学药学院;
【分类号】：R943

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