中国寄生虫学与寄生虫病杂志 ›› 1993, Vol. 11 ›› Issue (4): 251-254.

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吡喹酮脂质体对泡球蚴病的治疗效果探讨

李富荣,蒋次鹏,曹和洵,王琪   

  1. 兰州医学院包虫病研究室
  • 收稿日期:2017-01-06 修回日期:2017-01-06 出版日期:1993-11-30 发布日期:2017-01-06

EVALUATION OF THE EFFICACY OF PRAZIQUANTEL-LIPOSOME AGAINST ALVEOCOCCOSIS

  • Received:2017-01-06 Revised:2017-01-06 Online:1993-11-30 Published:2017-01-06

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(PO.01)。对化疗后小鼠内泡球

关键词: 泡球蚴病, 脂质体, 吡喹酮, 药物代谢动力学, 化学治疗, 组织学, 超微结构

Abstract: 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%)(P0. 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.