Lim L Y, Wan L S
Department of Pharmacy, National University of Singapore, Kent Ridge Crescent, Singapore.
J Microencapsul. 1998 May-Jun;15(3):319-33. doi: 10.3109/02652049809006860.
Chitosan microspheres were prepared using an emulsification-coacervation technique. The w/o emulsion comprised a mixture of light and heavy liquid paraffins containing sodium dioctyl sulphosuccinate as the oil phase and chitosan solution as the aqueous phase. Pentasodium tripolyphosphate was included as a counterion. The chitosan microspheres obtained showed a high degree of aggregation. This was markedly reduced, by the incorporation of magnesium stearate in the disperse phase. The resultant microspheres were then discrete, spherical with smooth surfaces. Additionally, with an increasing magnesium stearate content, larger-sized microspheres were produced. The DSC analysis data suggested that the magnesium stearate was converted to stearic acid during the preparation process. Chitosan microspheres containing propranolol hydrochloride were similarly prepared, but their surface was convoluted and their shape not well defined. Unlike the microspheres without drug, the size of the drug-loaded microspheres decreased with increasing magnesium stearate content. The release of propranolol hydrochloride from the microspheres was fast, irrespective of the content of magnesium stearate. Drug encapsulation efficiency was enhanced when a greater amount of magnesium stearate was used.
采用乳化凝聚法制备壳聚糖微球。水包油乳液由含有二辛基磺基琥珀酸钠的轻质和重质液体石蜡混合物作为油相和壳聚糖溶液作为水相组成。加入三聚磷酸五钠作为抗衡离子。得到的壳聚糖微球表现出高度聚集。通过在分散相中加入硬脂酸镁,这种聚集明显减少。所得微球呈离散状,表面光滑呈球形。此外,随着硬脂酸镁含量的增加,会产生更大尺寸的微球。差示扫描量热分析数据表明,硬脂酸镁在制备过程中转化为硬脂酸。类似地制备了含盐酸普萘洛尔的壳聚糖微球,但其表面呈褶皱状且形状不明确。与不含药物的微球不同,载药微球的尺寸随硬脂酸镁含量的增加而减小。无论硬脂酸镁含量如何,微球中盐酸普萘洛尔的释放都很快。当使用更大量的硬脂酸镁时,药物包封效率提高。