相转化水凝胶微针的制备和处方优化  

The Preparation and Prescription Optimization of Phase Transition Microneedle

作　　者：张蓉[1] 沈炎冰[1] 苗晴晴 李程[1] 尹芹[1] 吴飞[1] 

机构地区：[1]上海交通大学药学院,上海201100

出　　处：《现代生物医学进展》2016年第22期4213-4216,共4页Progress in Modern Biomedicine

基　　金：国家自然科学基金面上项目(81173001)

摘　　要：目的:考察分子量为4 k Da的透明质酸,羧甲基纤维素钠对相转化水凝胶微针的影响以及对药物体外释放的影响。方法:制备含有不同浓度透明质酸或羧甲基纤维素钠的微针,利用显微镜观察微针的外观形态,用高效液相色谱法检测药物的体外释放,并用统计分析软件检测体外释放率的差异性。结果:含有透明质酸的微针出现相分离现象,体外释放24 h,释放率为55%左右;羧甲基纤维素钠的微针未出现相分离现象,体外释放24 h,释放率能达到60%左右,两种微针在3 h和24 h时体外释放率无显著性差异,在12 h时有显著性差异(P<0.05)。结论:透明质酸与聚乙烯醇混合易出现相分离现象,可应用于微针的浓度范围较窄,羧甲基纤维素钠微针不易出现相分离现象。在12 h体外释放方面,含有羧甲基纤维素钠的微针处方优于含有透明质酸的微针处方,但是哪一种辅料更优还需要进一步的实验验证。Objective： To investigate the influence of 4 kDa hyaluronic acid （HA） and carboxymethylcellulose sodium （CMC-Na） on the phase transition microneedle and the influence on drug release in vitro. Methods： Preparation of microneedles containing different concentration of HA or CMC-Na, the shape of microneedle was observed by microscope, drug release was investigated by high performance liquid chromatography （HPLC） in vitro, the difference of drug release between microneedle with HA and CMC-Na was detected by statistical product and service solutions （SPSS）. Results： Phase separation was observed when preparing microneedle with HA, but not observed on microneedle with CMC-Na. Drug release ofmicroneedle with HA and CMC-Na which was significant different at 12 h （P〈0.05） was about 55% and 60% at 24 h in vitro, respectively. Conclusion： Microneedle with HA was easy to appear phase separation, so applicable scope of hyaluronic acid was very narrow. For 12 h drug release in vitro, prescription of microneedle with CMC-Na was superior to prescription of microneedle with HA, but which excipient is better requires further studies.

关 键 词：透明质酸 羧甲基纤维素钠 微针 体外释放 

分 类 号：R-332[医药卫生] R94