LPZQL和PZQL的研制及其抗小鼠的日本血吸虫病活性的比较  

PREPARATION OF LIPOSOME OF LEVO PRAZIQUANTEL AND PRAZIQANTEL AND THEIR COMPARATIVE EFFICACY IN EXPERIMENTAL THERAPY OF SCHITOSOMIASIS IN MICE

作　　者：余瑜[1] 严燊和[1] 胡湘南[1] 靳红卫[1] 王小根[1] 卓超[1] 

机构地区：[1]重庆医科大学药物化学与生物材料研究室,传染病寄生虫病研究所重庆400016

出　　处：《华西药学杂志》1999年第5期315-318,共4页West China Journal of Pharmaceutical Sciences

摘　　要：以提取的大豆卵磷脂为膜材，采用逆相蒸发法制备了左旋吡喹酮脂质体（ＬＰＺＱＬ）和吡喹酮脂质体（ＰＺＱＬ）。用ＡＣ ９２０ 红细胞分析仪和扫描电镜检测显示：ＬＰＺＱＬ 和ＰＺＱＬ 粒径大部分为２～４μｍ ，主要为大单层脂质体，对ＬＰＺＱ 和ＰＺＱ 包裹率达９８％ 以上。用ＬＰＺＱＬ，ＰＺＱＬ和ＰＺＱ 对感染日本血吸虫病的小鼠进行灌胃治疗，探讨了两种脂质体对小鼠抗日本血吸虫病的活性。动物实验表明：ＬＰＺＱＬ疗效较ＰＺＱ 高４ 倍；ＰＺＱＬ疗效较ＰＺＱ 高２ 倍。脂质体作为靶向制剂，降低了ＬＰＺＱ 和ＰＺＱ 的治疗剂量，提高生物利用度，可望成为抗日本血吸虫病的新剂型。LPZQ or PZQ were encapsulated in liposomes. The diameter of LPZQL and PZQL with large unilameller vesicles were about 2 4 μm detected by AC920 red cell analyzer and scanning electron microscope. Encapsulation efficiency of liposome to LPZQ and PZQ was over 98%. The experimental therapy of Schitosomiasis japonica in mice for the comparative efficacy of LPZQL, PZQL and PZQ showed that the efficacy of LPZQL and PZQL were higher 4 and 2 times than that of PZQ,respectively. These results indicated that LPZQL and/or PZQL may be developed to a new type of anti schitosomiasis japonica preparation.

关 键 词：左旋吡喹酮 吡喹酮 日本血吸虫病 抗血吸虫药 

分 类 号：R978.63[医药卫生—药品] R532.210.5[医药卫生—药学]