Characterization of carbamazepine-Gelucire 50/13 microparticles prepared by a spray-congealing process using ultrasounds.
Characterization of carbamazepine-Gelucire 50/13 microparticles prepared by a spray-congealing process using ultrasounds.
复制标题
使用超声波喷雾凝结工艺制备的卡马西平-Gelucire 50/13 微粒的表征。
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发表时间：
2002
期刊：
影响因子：
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通讯作者：
L. Rodriguez
中科院分区：
文献类型：
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作者：
N. Passerini;B. Perissutti;M. Moneghini;D. Voinovich;B. Albertini;C. Cavallari;L. Rodriguez
在本研究中，研究了利用新型超声雾化器的喷雾凝结技术制备不同药聚合物比的卡马西平(CBZ)-Gelucire 50/13增强释放的无溶剂微球。扫描电镜分析表明，可以获得球形和非聚集的微颗粒；微球的普遍粒径在150 ~ 250 μ m之间，包封率达到90%。体外溶出度试验显示，微球的CBZ溶出率明显高于纯药物和药物- gelucire 50/13物理混合物。差示扫描量热法、热阶显微法、x射线粉末衍射法和漫反射傅里叶变换红外光谱法均证实了CBZ原晶型的相稳定性；此外，没有发现药物与Gelucire 50/13之间的相互作用。本研究结果表明，利用超声雾化器的喷雾凝结技术可以作为一种提高CBZ等水溶性较差药物溶出率的新方法。
In this work, the utilization of a spray-congealing technique using a new ultrasonic atomizer to prepare enhanced-release, solvent-free microspheres of carbamazepine (CBZ)-Gelucire 50/13 in different drug-to-polymer ratios was considered. Scanning electron microscopy analysis showed that it was possible to obtain spherically shaped and nonaggregated microparticles; the prevalent particle size was in the range 150-250 microm and the microspheres had a good encapsulation efficiency (> 90% in the prevalent size fraction). The in vitro dissolution tests displayed a significant increase of the CBZ dissolution rate from microspheres compared with pure drug and to drug-Gelucire 50/13 physical mixture. Differential scanning calorimetry, hot stage microscopy, X-ray powder diffractometry, and diffuse reflectance Fourier transform infrared spectroscopy demonstrated phase stability of the original polymorph of CBZ in all the systems; moreover, no interactions between the drug and Gelucire 50/13 were found. The results of this study suggested that the spray-congealing technique using the ultrasonic atomizer could be considered as a new and interesting method to enhance the dissolution rate of a poorly water-soluble drug as CBZ.