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壳聚糖-海藻酸盐作为微晶纤维素在挤出/滚圆法中替代制粒助剂的应用。

Use of chitosan-alginate as alternative pelletization aid to microcrystalline cellulose in extrusion/spheronization.

作者信息

Charoenthai Nattawut, Kleinebudde Peter, Puttipipatkhachorn Satit

机构信息

Department of Manufacturing Pharmacy, Faculty of Pharmacy, Mahidol University, Sri-Ayudhya Road, Bangkok 10400, Thailand.

出版信息

J Pharm Sci. 2007 Sep;96(9):2469-84. doi: 10.1002/jps.20855.

Abstract

Two types of different molecular weight chitosan were investigated as a pelletization aid in extrusion/spheronization using water as granulation liquid. Spherical pellets with a maximum fraction of 60% w/w chitosan could be produced when 1.25-2.5% w/w sodium alginate was included in the formulations with no microcrystalline cellulose (MCC). Chitosan with lower molecular weight of 190 kDa showed a better pellet forming property. The pellets obtained had acceptable physical characteristics and a fast drug release. The results from Fourier transform infrared spectroscopy, differential scanning calorimetry and (13)C CP-MAS nuclear magnetic resonance spectroscopy confirmed the formation of polyelectrolyte complex (PEC) between chitosan and sodium alginate, which might be a reason for successful pelletization by extrusion/spheronization. Moreover, the presence of PEC might influence the physical characteristics and dissolution behavior of chitosan-alginate pellets. The results indicated an achievement in production of pellets by extrusion/spheronization without using MCC. Moreover, chitosan combined with sodium alginate could be used as a promising alternative pelletization aid to MCC in extrusion/spheronization.

摘要

研究了两种不同分子量的壳聚糖,将其作为挤出/滚圆造粒中的制粒助剂,以水作为制粒液体。当配方中不含有微晶纤维素(MCC),且包含1.25-2.5% w/w的海藻酸钠时,可生产出壳聚糖含量最高为60% w/w的球形颗粒。分子量为190 kDa的低分子量壳聚糖表现出更好的成粒性能。所得到的颗粒具有可接受的物理特性和快速的药物释放性能。傅里叶变换红外光谱、差示扫描量热法和(13)C CP-MAS核磁共振光谱的结果证实了壳聚糖和海藻酸钠之间形成了聚电解质复合物(PEC),这可能是通过挤出/滚圆成功制粒的原因。此外,PEC的存在可能会影响壳聚糖-海藻酸钠颗粒的物理特性和溶解行为。结果表明在不使用MCC的情况下通过挤出/滚圆成功生产出了颗粒。此外,壳聚糖与海藻酸钠结合可作为挤出/滚圆中一种有前景的替代MCC的制粒助剂。

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