CAJ | 학술논문

目的：制备一种包载普伐他汀钠，以获得长效释放的载药微球。方法以京尼平为交联剂制备载普伐他汀钠的壳聚糖微球，考察壳聚糖相对分子质量、油相水相比、反应温度、搅拌速度等对壳聚糖微球形成的影响，通过扫描电镜观察其微观形貌，测定微球的包封率以及不同pH条件下的溶胀度，并考察了普伐他汀钠的体外累积释药情况。结果载普伐他汀钠药微球体外释放时间长达31 d以上，反应条件不同，药物释放速度不同，普伐他汀的包封率可达54.7%。最佳制备条件为：壳聚糖的粘度为200~400 mPa.s，油水比10∶1，搅拌速度850 r/min，温度40℃。结论京尼平交联载普伐他汀钠的壳聚糖微球具有较好的长效缓释能力，并且可通过调节交联时间控制其对药物的释放速度。
목적：제비일충포재보벌타정납，이획득장효석방적재약미구。방법이경니평위교련제제비재보벌타정납적각취당미구，고찰각취당상대분자질량、유상수상비、반응온도、교반속도등대각취당미구형성적영향，통과소묘전경관찰기미관형모，측정미구적포봉솔이급불동pH조건하적용창도，병고찰료보벌타정납적체외루적석약정황。결과재보벌타정납약미구체외석방시간장체31 d이상，반응조건불동，약물석방속도불동，보벌타정적포봉솔가체54.7%。최가제비조건위：각취당적점도위200~400 mPa.s，유수비10∶1，교반속도850 r/min，온도40℃。결론경니평교련재보벌타정납적각취당미구구유교호적장효완석능력，병차가통과조절교련시간공제기대약물적석방속도。
Objective To prepare pravastatin sodium-loaded chitosan microspheres to allow sustained drug release. Methods The drug-loaded chitosan microspheres were prepared by using genipin as the cross-linker. The influences of molecular weight of chitosan, volume ratio of oil and water, reaction temperature, and stirring speed on the formation of chitosan microspheres were investigated. The morphology of the microspheres was observed using scanning electron microscopy. The encapsulation efficiency, swelling ratio under different pH conditions, and in vitro drug release were measured. Results The in vitro release of pravastatin sodium could last for at least 31 days. The drug release rate varied with the reaction condition. The drug entrapment efficiency of the microsphere was 54.7%. The optimal processing conditions were as follows: chitosan viscosity of 200-400 mPa · s, oil-water proportion of 10∶1, stirring speed of 850 r/min, and reaction temperature at 40 ℃. Conclusion The pravastatin sodium-loaded microspheres show good sustained drug release property, and the drug release rate can be modified by controlling the cross-linking time.