CAJ | 학술논문

目的：制备氨茶碱/壳聚糖/β-环糊精肺吸入缓释微球，考察其特性。方法采用喷雾干燥法制备3种不同药物/载体比例的茶碱/壳聚糖/β-环糊精微球A，B，C，通过扫描电镜、激光粒度测定仪、红外光谱仪表征其理化性质，透析法研究其体外释放行为。结果最佳药物/载体比例（ TH∶CTS∶β-CD）为1∶3∶1；扫描电镜结果显示微球外观圆整，表面光滑或有皱折；微球A，B，C 50％的容积粒径为（4．97±0．03）μm，（4．90±0．45）μm，（6．43±0．08）μm，分布范围窄；载药量为35．70％±0．09％，21．09％±0．62％，13．33％±0．33％；包封率为88．79％±0．23％，91．40％±2．71％，85．16％±2．15％；产率为52．98％±1．05％，46．08％±0．13％，45．81％±0．04％；红外光谱结果显示茶碱与壳聚糖和β-环糊精高分子间发生氢键反应；体外释放结果证实茶碱/壳聚糖/β-环糊精微球具有缓释作用，并且与药物/载体比例及药物性质有关。结论喷雾干燥法能成功制备氨茶碱/壳聚糖/β-环糊精缓释微球，符合肺吸入粉雾剂的各项要求，该微球有望成为肺部给药的良好载体。
목적：제비안다감/각취당/β-배호정폐흡입완석미구，고찰기특성。방법채용분무간조법제비3충불동약물/재체비례적다감/각취당/β-배호정미구A，B，C，통과소묘전경、격광립도측정의、홍외광보의표정기이화성질，투석법연구기체외석방행위。결과최가약물/재체비례（ TH∶CTS∶β-CD）위1∶3∶1；소묘전경결과현시미구외관원정，표면광활혹유추절；미구A，B，C 50％적용적립경위（4．97±0．03）μm，（4．90±0．45）μm，（6．43±0．08）μm，분포범위착；재약량위35．70％±0．09％，21．09％±0．62％，13．33％±0．33％；포봉솔위88．79％±0．23％，91．40％±2．71％，85．16％±2．15％；산솔위52．98％±1．05％，46．08％±0．13％，45．81％±0．04％；홍외광보결과현시다감여각취당화β-배호정고분자간발생경건반응；체외석방결과증실다감/각취당/β-배호정미구구유완석작용，병차여약물/재체비례급약물성질유관。결론분무간조법능성공제비안다감/각취당/β-배호정완석미구，부합폐흡입분무제적각항요구，해미구유망성위폐부급약적량호재체。
Objective The objective of this study is to prepare the inhalation sustained-release microspheres of TH/CTS/β-CD and probe into their properties .Methods The three different ratios of TH/CTS/β-CD were prepared by spray drying method .The characteris-tics of TH/CTS/β-CD microspheres were carried out by Scanning Electron Microscopy (SEM),Laser diffraction,Fourier Transform Infrared Spectroscope(FT-IR).Dialysis method was used to study the release behavior in vitro .Results The optimal ratio of drug/carrier(TH:CTS:β-CD) was 1∶3∶1.It showed that the preparations were spherical microspheres with smooth or slightly wrinkled surfaces by SEM .Fifty per-cent of volume diameter were 4.97μm ±0.03μm,4.90μm ±0.45μm,6.43μm ±0.08μm on microspheres A,B,C.The microspheres had a narrower particle size distribution and could meet the requirements of powder for inhalation on particle size .The drug loading were 35.70%± 0.09%,21.09%±0.62%and 13.33%±0.33%.The encapsulation efficiencies were 88.79%±0.23%,91.40%±2.71%and 85.16%±2.51%.The yield of microspheres A ,B,C were 52.98%±1.05%,46.08%±0.13%,45.81%±0.04%.FT-IR spectroscopy revealed that hydrogen bonds were formed between TH and CTS or β-CD.The release content of TH from microspheres was slower at pH 6.8 in vitro and it was related to the ratio of drug/polymer.Conclusion TH/CTS/β-CD microspheres can successfully be prepared by spray drying method and it will be an ideal drug carrier which is used in pulmonary delivery system .