双氯芬酸钠/海藻酸钠微球的制备与体外释药行为考察

Studies on preparation of diclofenac sodium/alginate microparticles and release behavior in vitro

目的以海藻酸钠为载体材料,双氯芬酸钠为模型药物,制备载药微球并考察其性质及体外释放行为。方法本文采用海藻酸钠为药物载体,采用喷雾干燥法制备双氯芬酸钠/海藻酸钠微球。考察于双氯芬酸钠/海藻酸钠投料比对载药微球理化性质的影响。采用扫描电镜对所得到的微球进行形貌观察。同时考察其体外药物释放行为。结果所得到的载药微球形态呈不规则的扁平状,粒径分布较为均匀。通过控制投料比,可以得到不同粒径(5.64～9.58μm),载药量(5.76～18.43%)和包封率(35.45～43.92%)的载药微球。体外药物释放行为结果显示微球在含有0.5%氯化钙的PBS(pH=7.4)溶液的药物释放时间可以持续96h,具有一定的缓释效果。结论通过喷雾干燥法制备的双氯芬酸钠/海藻酸钠载药微球具有较高载药量和一定的药物缓释效果。

OBJECTIVE To develop a diclofenac sodium/alginate microparticles and study on its release be- havior in vitro. METHODS The spray-drying technology was employed to develop diclofenac sodium/alginate mi-croparticles. The morphology of developed microparicles was observed by a SEM. The effect of drug/polymer ratio on the properties of microparticles as weU as its in vitro release behavior were also investigated. RESULTS With the SEM observation, the developed microparicles showed applanation in shape with uniform particle size distribution. By changing the drug/polymer ratio,the various particle size of microparticles ranging from 5. 641μm to 9.58μm as well as drug loading capacity （5.76 ~ 18.43% ） and loading effiency （35.45 -43.92% ） could be gained. Moreover, in vitro release study revealed that the developed microparticles exhibited sustained release behavior in the period of 96h study. CONCLUSION The developed diclofena sodium/alginate microparticles with great loading capacity as well as sustained release behavior might have potential application in drug delivery.