【摘要】 目的:探讨羧甲基壳聚糖（CMCS）的取代度对灯盏花素（BRE）鼻黏膜微球体外释药速度的影响。方法:合成取代度分别为40%,60%,80%的CMCS,并进行取代度检测及红外分析。分别以取代度为40%,60%,80%,95%的CMCS为载体,制备BRE微球,并对其体外释药、空白CMCS微球溶蚀及两者之间的关系进行研究。结果:合成得到3种CMCS的取代度分别为（41.60±1.44）%,（59.39±2.15）%,（80.72±2.38）%。当CMCS的取代度分别为40%,60%,80%,95%时,BRE微球体外释药均呈现缓释特性,分别符合Higuchi方程:累积释放度（Q,%）=41.49t^1/2-11.66（R²=0.984 3）,Q=39.74t^1/2-12.82（R²=0.991 6）,Q=35.35t^1/2-10.89（R²=0.992 8）,Q=31.12t^1/2-8.80（R²=0.990 2）;空白CMCS微球溶蚀分别符合Higuchi方程:累积溶蚀量（A,%）=39.25t^1/2-10.97（R²=0.984 0）,A=37.59t^1/2-12.04（R²=0.990 4）,A=33.61t^1/2-10.61（R²=0.992 5）,A=29.41t^1/2-8.32（R²=0.989 6）。释药与CMCS溶蚀之间均呈现高度一致的线性相关性,且随着CMCS取代度的增加,BRE微球体外释药速度逐渐减慢。结论:CMCS取代度对BRE鼻黏膜微球的体外释药有明显的影响,取代度越高,释药越慢,缓释效果越明显。更多还原

【Abstract】 Objective: To explore the substitution of carboxymethyl chitosan （CMCS） on the drug release in vitro of CMCS microspheres loaded with breviscapine （BRE） for nasal mucous. Methods: CMCS respectively with substitution of 40%,60% and 80% was synthesized,and the substitution was determined and IR spectra were obtained. CMCS with various substitutions （40%,60%,80%and 95%） was used as the vehicle to prepare BRE microspheres,and the drug release in vitro,erosion of blank CMCS microspheres and the relationship between them were investigated. Results: The substitution of the synthesized CMCS was （41.60±1.44） %, （59.39±2.15） % and （80.72±2.38） %,respectively. BRE microspheres with CMCS at the substitution of 40%,60%,80% and 95% as the vehicle all showed significant sustained release property in vitro,which respectively fitted the following Higuchi equation: Q% = 41.49 t^1/2-11.66 （R²= 0.984 3）,Q% = 39.74 t^1/2-12.82 （R²= 0.991 6）,Q% = 35.35 t^1/2-10.89 （R²= 0.992 8） and Q% = 31.12 t^1/2-8.80 （R²= 0.990 2）. The erosion of the blank CMCS microspheres respectively fitted the following equation: A% = 39.25 t^1/2-10.97 （R²=0.984 0）,A% = 37.59 t^1/2-12.04 （R²= 0.990 4）,A% = 33.61 t^1/2-10.61 （R²= 0.992 5） and A% = 29.41 t^1/2-8.32 （R²= 0.989 6）. The linear relationship between the drug release in vitro and the erosion of CMCS was highly uniform,and the higher the substitution of CMCS was,the slower the drug release in vitro. Conclusion: The substitution of CMCS shows significant effect on the drug release in vitro of BRE microspheres,and the high the substitution,the slower the drug release in vitro and more significant the sustained property.更多还原