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通过喷雾干燥技术制备并表征载阿仑膦酸盐的壳聚糖微粒。

Preparation and characterisation of alendronate-loaded chitosan microparticles obtained through the spray drying technique.

作者信息

Ochiuz Lacramioara, Peris José-Esteban

机构信息

Department of Pharmacy and Pharmaceutical Technology. Faculty of Pharmacy. University of Valencia. Avda. V. Andres Estellés s/n. 46100-Burjassot, Valencia, Spain.

出版信息

Med Chem. 2009 Mar;5(2):191-6. doi: 10.2174/157340609787582963.

Abstract

Microparticles of chitosan (CHT) containing alendronate sodium (AL) were prepared in four drug:polymer ratios (1:1, 1:2, 1:4, 1:6) using the spray drying technique. The efficiency of the method was evaluated by determining production yield (about 70 %) and microencapsulation efficiency, which was almost 100 % in the case of all four of the formulations studied. Particles had a mean size of between 3.6 and 4.6 microm, and a near-spherical shape. The formulations with the highest content of AL (drug:polymer ratio 1:1 and 1:2) showed an asymmetrical distribution of particles, which were larger in size, and had a higher proportion of irregular particles than the other formulations. FT-IR analysis revealed an ionic interaction between AL and CHT. Differential scanning calorimetry and thermogravimetric analysis confirmed the microencapsulation of AL and the increased thermal stability of encapsulated AL. The dissolution profiles of AL from CHT microspheres, at pH values of 1.2 and 6.8, showed a delayed release of AL from microspheres, and the dissolution rate was dependent on the pH and the drug:polymer ratio. It can be concluded that spray drying is a suitable technique for preparing AL-loaded CHT microspheres, and that the drug:polymer ratio can be used to control the rate of AL release from microspheres.

摘要

采用喷雾干燥技术,以四种药物与聚合物比例(1:1、1:2、1:4、1:6)制备了含阿仑膦酸钠(AL)的壳聚糖(CHT)微粒。通过测定产率(约70%)和微囊化效率来评估该方法的效率,在所研究的所有四种制剂中,微囊化效率几乎为100%。微粒的平均尺寸在3.6至4.6微米之间,形状接近球形。AL含量最高的制剂(药物与聚合物比例为1:1和1:2)显示出颗粒的不对称分布,其尺寸较大,且不规则颗粒的比例高于其他制剂。傅里叶变换红外光谱(FT-IR)分析揭示了AL与CHT之间的离子相互作用。差示扫描量热法和热重分析证实了AL的微囊化以及包封后AL热稳定性的提高。在pH值为1.2和6.8时,AL从CHT微球中的溶出曲线显示出AL从微球中的缓释,溶出速率取决于pH值和药物与聚合物比例。可以得出结论,喷雾干燥是制备载AL的CHT微球的合适技术,并且药物与聚合物比例可用于控制AL从微球中的释放速率。

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