摘要
目的 采用新型微孔膜乳化法制备粒径均匀、包埋率高、包埋稳定的抗癌剂碘油复乳药物载体。方法 以丝裂霉素为模型药物,将丝裂霉素的水溶液与碘油混合,用均相乳化器制成W/O型初乳后,用适当压力将W/O型初乳通过微孔膜压入外水相,制备出了W/O/W型药物载体,对该药物载体的粒径分布、包埋率、体外控释等进行了研究。结果 以聚氧乙烯氢化蓖麻油(HCO4O)作为碘油相乳化剂,碘油与丝裂霉素水溶液体积比为2:1,制备W/O型初乳时的条件为3 min,8 600 r·min-1时,所得到的丝裂霉素碘油复乳载体粒径均匀,粒径分布系数值达到13.2％以下,药物包埋率达90％左右,在4℃下储存稳定性可达30d以上,在37℃下能以适当的速度释放出药物。结论 采用微孔膜乳化法制备的碘油药物载体粒径均匀、包埋率高、储存稳定,有望成为临床靶向给药的一种新剂型。
OBJECTIVE: To prepare the stable lipiodol double emulsion with uniform size and high encapsulation efficiency as drug carrier by a novel membrane emulsification technique. METHODS: Mitomycin C was used as a model drug. After the W/O emulsion composed of mitomycin C aqueous phase and Lipiodol was prepared by a homogenizer, the W/O emulsion was pressed through the pores of a porous membrane into the external aqueous phase to form the W/O/W double emulsion. The effects of preparation conditions on the size distribution, encapsulation efficiency and release behavior in vitro were investigated. RESULTS: Polyoxyethylene hydrogenerated caster oil (HCO40) was used as the emulsifier in oil phase, the volume ratio between Lipiodol and Mitomycin C solution was 2: 1, and the W/O primary emulsion was prepared by emulsification for 3min at 8 600 r.min-1. The stable double emulsion with uniform size and high encapsulation efficiency was obtained. The size distribution coefficient was lower than 13.2%. The encapsulation efficiency was 90%. The shelf life at 0°C attained to 30 days, and the drug was released steadily at 37°C. CONCLUSION: The W/O/W Lipiodol double emulsion with uniform size, high encapsulation efficiency and long shelf life can be prepared by the membrane emulsification technique. The double emulsion can be used as a new carrier for controlled release drug system.
出处
《中国药学杂志》
EI
CAS
CSCD
北大核心
2004年第7期521-524,共4页
Chinese Pharmaceutical Journal
基金
国家自然科学基金杰出青年科学基金(20125616)
关键词
微孔膜乳化
碘油
W/O/W型复乳
Biological membranes
Emulsification
Emulsions
Lipids
Size determination
