CAJ | 학술논문

目的：研究喷雾干燥法制备氨茶碱/壳聚糖/β-环糊精微球的制备工艺。方法采用正交设计优化喷雾干燥法制备氨茶碱/壳聚糖/β-环糊精微球的制备条件，考察氨茶碱在β-环糊精溶液中的溶解度以及氨茶碱/壳聚糖/β-环糊精微球的载药量、包封率、产率、含水率和外观形态等特性。结果氨茶碱的溶解度随温度和β-环糊精溶液浓度的增加而增加；根据载药量氨茶碱/壳聚糖/β-环糊精微球喷雾干燥的最佳工艺条件为A1 B3 C1 D3，即进口温度为150℃，进料速度为8ml/min，空气流量为400L/h，壳聚糖分子量为130万；氨茶碱/壳聚糖/β-环糊精微球的载药量、包封率、产率和含水率分别为19．3％±0．5％，77．4％±0．6％，39．5％±1．0％，9．7％±0．7％；扫描电镜显示微球外观圆整，表面光滑或有少许皱褶；喷嘴直径为0．7mm时制得的微球粒径更小且较均一。结论采用正交设计优选了最佳制备工艺，其制得的氨茶碱/壳聚糖/β-环糊精微球具有较高的载药量、包封率、产率和较低的含水率，微球圆整，带少许皱褶，有望成为肺部吸入的理想药物载体。
목적：연구분무간조법제비안다감/각취당/β-배호정미구적제비공예。방법채용정교설계우화분무간조법제비안다감/각취당/β-배호정미구적제비조건，고찰안다감재β-배호정용액중적용해도이급안다감/각취당/β-배호정미구적재약량、포봉솔、산솔、함수솔화외관형태등특성。결과안다감적용해도수온도화β-배호정용액농도적증가이증가；근거재약량안다감/각취당/β-배호정미구분무간조적최가공예조건위A1 B3 C1 D3，즉진구온도위150℃，진료속도위8ml/min，공기류량위400L/h，각취당분자량위130만；안다감/각취당/β-배호정미구적재약량、포봉솔、산솔화함수솔분별위19．3％±0．5％，77．4％±0．6％，39．5％±1．0％，9．7％±0．7％；소묘전경현시미구외관원정，표면광활혹유소허추습；분취직경위0．7mm시제득적미구립경경소차교균일。결론채용정교설계우선료최가제비공예，기제득적안다감/각취당/β-배호정미구구유교고적재약량、포봉솔、산솔화교저적함수솔，미구원정，대소허추습，유망성위폐부흡입적이상약물재체。
Objective To optimize the spray drying technology of theophylline /chitosan/β-cyclodextrin microspheres .Methods The L9(34) orthogonal test was used to optimize the spray drying technology of theophylline /chitosan/β-cyclodextrin microspheres.The dissolubility of theophylline and drug loading ,encapsulation efficiency ,yield,water content and morphology of theophylline /chitosan/β-cyclo-dextrin microspheres were studied ,as the investigating indices .Results The dissolubility of theophylline was gradually increasing with the raise of temperature and the concentration of β-cyclodextrin .According to the drug loading ,and the optimum spray drying conditions of theo-phylline/chitosan/β-cyclodextrin microspheres were A 1 B3 C1 D3 ,namely the inlet gas temperature was 150℃,the feed flow rate was 8ml/min, the drying air flow was 400L/h and the molecular weight of chitosan was 13 ×105.The drug loading,encapsulation efficiency,yield,and water content of the theophylline/chitosan/β-cyclodextrin microspheres were 19.3%±0.5%,7.4%±0.6%,39.5%±1.0%,and 9.7%±0. 7%,respectively .Scanning electron micrograph showed that the microspheres were predominantly spherical with smooth surface or slightly wrinkled.The particle diameter of microspheres was smaller and uniform prepared by atomizing nozzles of 0.7mm.Conclusions These re-sults indicate that theophylline/chitosan/β-cyclodextrin microspheres can be successfully prepared by spray drying method ,not only obtained higher drug loading ,but also higher encapsulation efficiency and yield .The lower water content in the microspheres is highly desirable .Micro-spheres are predominantly spherical with smooth surface or slightly wrinkled .It can serve as promising carrier in pulmonary drug delivery sys-tem.