CAJ | 학술논문

目的：优化二氢杨梅素脂质体的处方及工艺，并考察其性质。方法：采用薄膜-超声法制备的二氢杨梅素脂质体，以包封率为指标，采用单因素法考察处方及工艺，在此基础上采用正交试验对二氢杨梅素脂质体的处方工艺进行筛选与优化；采用透射电镜观察其形态，采用动态透析法考察其体外释放的特性，并进行初步稳定性研究。结果：二氢杨梅素脂质体最佳处方和工艺条件为：磷脂与胆固醇的摩尔比为1：1，二氢杨梅素加入量4.0 mg，PBS缓冲液pH为5.0，超声时间3 min。优化后脂质体的包封率为58.1%，电镜下呈球形或近球形小囊泡状，48 h体外累计释放率达到76.29%，4℃下避光放置30天药物含量为加入量的96.57%。结论：二氢杨梅素脂质体处方及制备工艺简单且重复性好，制剂稳定性良好。
목적：우화이경양매소지질체적처방급공예，병고찰기성질。방법：채용박막-초성법제비적이경양매소지질체，이포봉솔위지표，채용단인소법고찰처방급공예，재차기출상채용정교시험대이경양매소지질체적처방공예진행사선여우화；채용투사전경관찰기형태，채용동태투석법고찰기체외석방적특성，병진행초보은정성연구。결과：이경양매소지질체최가처방화공예조건위：린지여담고순적마이비위1：1，이경양매소가입량4.0 mg，PBS완충액pH위5.0，초성시간3 min。우화후지질체적포봉솔위58.1%，전경하정구형혹근구형소낭포상，48 h체외루계석방솔체도76.29%，4℃하피광방치30천약물함량위가입량적96.57%。결론：이경양매소지질체처방급제비공예간단차중복성호，제제은정성량호。
This study was aimed to optimize dihydromyricetin liposome formulations by orthogonal design in order to study its characterization. Dihydromyricetin liposomes were prepared with thin-film ultrasonic dispersion technology. Formulations of dihydromyricetin liposomes were optimized with entrapment efficiency as the optimized index. The formulation and technology were evaluated by the single factor. Based on this, orthogonal design was made on the screening and optimization of dihydromyricetin liposome. Its morphology was observed by transmission electron micro-scope. Its in vitro drug-release behavior was studied by equilibrium dialysis. The preliminary stability was studied. The results showed that the optimized formulation and technology of dihydromyricetin liposome was when the molar ratio of lecithin and cholesterol was 1:1, the dosage of dihydromyricetin was 4.0 mg. The pH of PBS was 5.0, ultra-sonic time was 3 min. The encapsulation efficiency of dihydromyricetin liposome was 58.1%. Its morphology was small spherical or nearly spherical vesicle with observation in transmission electron microscope. It showed that the in vitro release of dihydromyricetin liposome arrived 76.29% in 48 h. The drug content was still 96.57% of dosage for 30 days at 4oC in the dark place. It was concluded that the optimized formulation and preparation technology of di-hydromyricetin liposome were simple, replicable and stable.