吡喹酮脂质体对泡球蚴病的治疗效果探讨  

EVALUATION OF THE EFFICACY OF PRAZIQUANTEL-LIPOSOME AGAINST ALVEOCOCCOSIS

作　　者：李富荣[1] 蒋次鹏[1] 曹和洵[1] 王琪[1] 

机构地区：[1]兰州医学院包虫病研究室,兰州730000

出　　处：《中国寄生虫学与寄生虫病杂志》1993年第4期251-254,共4页Chinese Journal of Parasitology and Parasitic Diseases

摘　　要：用脂质体包裹抗泡球蚴病药物吡喹酮,经逆相蒸发法制备包裹率为 60％。经高效液相色谱测定法(RP-HPLC)测定吡喹酮及其脂质体在小鼠体内的分布动态变化,表明吡喹酮脂质体(PZQ-Lip)腹腔注射后 1/2—16 h 的血浓度和肝、脾组织内药物含量均明显较普通剂型吡喹酮(PZQ)组为高,半衰期显著延长。口服 LD_(50) 为3 372 mg/kg,较PZQ 毒性 2454 mg/kg 下降约1/4。以 500 mg/kg·d×12 d 灌胃连续 4疗程治疗小鼠继发性腹腔泡球蚴病,PZQ-Lip 的囊肿抑制率达68.72％,较 PZQ组 14.25％疗效明显提高(P<O.01)。对化疗后小鼠内泡球蚴组织学观察,发现PZQ-Lip 对泡球蚴生发层损伤较 PZQ明显。超微结构显示,两者均对小鼠泡球蚴组织有广泛的细胞内效应。本实验表明,PZQ-Lip 的抗泡球蚴作用明显优于 PZQ。In this paper, praziquantel, an anti-hydatidosis drug, was encapsulated with lipsome by REV (Reverse -phase -evaporation) method, the encapsulated percentage was 60%. The drug distribution dynamics in mice of both praziquantel (PZQ) and praziquantel liposome (PZQ-Lip) were determined using RP-HPLC method. The results indicated that the drug concentration of blood, liver and spleen in the PZQ-Lip group was higher than those in the PZQ group from 1/2 to 16 hours post ip. the t 1/2 of the former was considerably prolonged. The toxicity of PZQ -Lip tested by LD50 was decreased about one fourth as compared with PZQ (3372 vs. 2 454 mg/kg). There was a significant difference in the cyst inhibition rate between PZQ-Lip group (68. 7%) and PZQ group (14. 3%)(P<0. 01) as shown by the results of secondary alveococcosis mice treated with either drug at 500 mg/kg· d × 12 d for four consecutive courses. Histological observation of the germinal layer after treatment showed that the damage of PZQ-Lip group was more severe than that of PZQ group. The ul-trastructural observation showed that both drugs had marked effects on the organelles of cells. The above experiments indicated that the efficacy of PZQ-Lip was more effective than PZQ for treatment of alveococcosis.

关 键 词：泡球蚴病 脂质体 吡喹酮 超微结构 

分 类 号：R532.32[医药卫生—内科学]