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目的以具有优良成型性的壳聚糖(CS)为载体,选用阿苯达唑(ABZ)为模型药物,先制备成固体分散体,再进一步制备阿苯达唑壳聚糖微球(ABZ-LSD-CS),考察微球载药量、包封率、表面形态及理化特性,并考察微球在不同介质中的体外释放特性。方法以液体石蜡为油相,Span-80为乳化剂,戊二醛为交联剂,采用乳化-交联固化法制备ABZ-LSD-CS。应用扫描电镜(SEM)观察微球的表面形态,光学显微镜测量粒径大小及分布;采用红外光谱(FT-IR),X-射线粉末衍射(XRD)法和差示扫描量热(DSC)法表征微球特性,体外动态透析法测定微球在不同介质条件下的释药性能。结果制备出的微球形态圆整,粒径分布较均匀,平均粒径为(153±7)μm,载药量(20.92±0.15)%,包封率(25.37±0.22)%。微球在0.1mol/L HCl、pH3.5和7.4的PBS及生理盐水4种介质中的释放缓慢,其中在pH3.5的PBS中释放效果最好,符合Weibull释放模型。结论该实验制备的ABZ-CS-MS性能良好,具有较好的药物载药量和包封率,微球形态圆整,并且药物的释放时间延长,达到缓释的目的,制备工艺简单易行。
OBJECTIVE To prepare chitosan microspheres (ABZ-1) with excellent formability as carriers and select albendazole (ABZ) as model drug to prepare solid dispersions. LSD-CS). The drug loading, encapsulation efficiency, surface morphology and physical and chemical properties of microspheres were investigated. The in vitro release characteristics of microspheres in different media were also investigated. Methods ABZ-LSD-CS was prepared by emulsion-crosslinking method using liquid paraffin as oil phase, Span-80 as emulsifier and glutaraldehyde as crosslinking agent. The surface morphology of the microspheres was observed by scanning electron microscopy (SEM). The size and distribution of the microspheres were measured by light microscopy. The structure of the microspheres was characterized by FT-IR, XRD and DSC Characterization of microspheres, in vitro dynamic dialysis assay microspheres in different media conditions of drug release performance. Results The morphology of microspheres was round and the particle size distribution was uniform. The mean particle size was (153 ± 7) μm, drug loading (20.92 ± 0.15)% and entrapment efficiency (25.37 ± 0.22)%. The release of microspheres in 0.1mol / L HCl, pH3.5 and 7.4 PBS and saline medium slow release, which in pH3.5 PBS release the best, in line with the Weibull release model. Conclusion The ABZ-CS-MS prepared by this experiment has good performance, good drug loading and entrapment efficiency, round shape of microspheres and prolonged release of drug to achieve sustained release. The preparation process is simple and easy .