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制备氢溴酸东莨菪碱纳米粒-微球系统(scopolamine hydrobromide nanoparticles-in-microsphere system,SH-NiMS)并考察其体外释放特性。以三聚磷酸钠(TPP)为交联剂,以壳聚糖为载体材料,采用离子交联法制备SH纳米粒,以包封率和载药量为考察指标,采用正交设计综合评分法优化纳米粒处方。调整喷雾干燥仪器参数,以HPMC为载体材料,将制得的SH纳米粒在喷雾干燥作用下制备成包裹纳米粒的微球系统,即NiMS系统。在电镜下观察SH-NiMS的外观、红外检测其结构变化并测定其体外释放特性。纳米粒制备处方经正交试验优化为:壳聚糖/TPP为3∶1(w/w),HPMC浓度0.3%、SH浓度0.2%。喷雾干燥的制备条件调节为蠕动泵速度15%,进口温度110℃,在此条件下制得的SH-NiMS包封产率、载药量和平均粒径分别为94.2%、20.4%和1256.5nm。SH-NiMS外观圆整,性质稳定。结果表明,SH-NiMS制备方法稳定可控,为开发药物新剂型提供了新的思路。
The scopolamine hydrobromide nanoparticles-in-microsphere system (SH-NiMS) was prepared and its in vitro release characteristics were investigated. Using sodium tripolyphosphate (TPP) as crosslinking agent and chitosan as carrier material, SH nanoparticles were prepared by ion-crosslinking method. The entrapment efficiency and drug loading were taken as the investigation indexes. The orthogonal design method Optimize nanoparticle prescription. Adjust the parameters of the spray drying equipment to HPMC as the carrier material, the prepared SH nanoparticles prepared under the action of spray drying microspheres wrapped nanoparticles system, ie, NiMS system. The appearance of SH-NiMS was observed under electron microscope. The structure of SH-NiMS was observed by infrared spectroscopy and its in vitro release characteristics were measured. The preparation prescription of nanoparticles was optimized by orthogonal experiment as follows: chitosan / TPP was 3:1 (w / w), HPMC concentration was 0.3%, SH concentration was 0.2%. The preparation conditions of spray drying were adjusted to peristaltic pump speed 15%, inlet temperature 110 ℃. The SH-NiMS encapsulation yield, drug loading and average particle diameter were 94.2%, 20.4% and 1256.5nm . SH-NiMS round appearance, the nature of stability. The results show that the SH-NiMS preparation method is stable and controllable, which provides a new idea for the development of new dosage forms of drugs.