水溶性壳聚糖-泼尼松龙结合物的合成与表征

 目的合成一系列不同相对分子质量(M_r)的水溶性壳聚糖-泼尼松龙结合物。方法通过控制壳聚糖的乙酰度得到水溶性壳聚糖(WCh i),并用凝胶渗透色谱测定其M_r大小。模型药物通过丁二酸间隔臂与WChi相连,其结构经红外光谱分析、差示扫描量热法分析、高效液相色谱分析和紫外光谱证明,结合的泼尼松龙量用高效液相色谱测定。结果合成的WChi的M_r分别为31×10³,19×10³,11×10³,7.2×10³,3.8×10³,相应的结合物中泼尼松龙含量分别为(8.36±0.04)%,(7.17±0.08)%,(7.21±0.03)%,(6.29±0.03)%,(6.66±0.05)%。结论成功制备了水溶性壳聚糖-泼尼松龙结合物。

Synthesis and Characterization of Water-Soluble Chitosan-Prednisolone Conjugates

OBJECTIVE To synthesize a series of water-soluble chitosan-prednisolone conjugates with various molecular weights.METHODS Water-soluble chitosan(WChi) was prepared through a chemical modification by controlling N-acetylated degree and molecular weight of WChi was determined by gel permeation chromatography(GPC).Then,a model drug,prednisolone,was conjugated into WChi via a succinic acid spacer.The structure was characterized by IR,DSC,HPLC and UV-VIS spectrum and the amount of bound prednisolone was determined by HPLC method.RESULTS The molecular weights of WChi were 31×10³,19×10³,11×10³,7.2×10³ and 3.8×10³,respectively.The amounts of bound prednisolone were(8.36±0.04)%,(7.17±0.08)%,(7.21±0.03)%,(6.29±0.03)% and(6.66±0.05)%,respectively.CONCLUSION The title conjugates were obtained successfully.