三吡萘啶在动物模型上的长效预防抗疟作用  

STUDIES ON RESIDUAL ANTIMALARIAL ACTIVITY OF TRIPYNADINE IN MICE AND MONKEYS"

作　　者：陈林[1] 戴祖瑞[1] 马志明[1] 郑贤育 陈昌[2] 

机构地区：[1]第二军医大学抗疟药研究室,上海200433 [2]中国预防医学科学院寄生虫病研究所,上海200025

出　　处：《中国寄生虫学与寄生虫病杂志》1993年第3期190-194,共5页Chinese Journal of Parasitology and Parasitic Diseases

基　　金：国家自然科学基金;编号3880719

摘　　要：本文报告了用 4.5倍ED_(50) 剂量的三吡萘啶游离碱喂饲小鼠,给药后 20 d再用伯氏疟原虫 ANKA 株原虫1×10~7个攻击,小鼠全部获得保护。三吡萘啶磷酸盐对鼠疟的滞效作用虽较其游离碱及哌喹磷酸盐稍好,但进行猴疟实验喂药时易引起恒河猴呕吐,难于准确计算给药量。三吡萘啶羟萘酸盐对鼠疟的滞效抗疟作用则不如其磷酸盐,也不如其游离碱。三吡萘啶游离碱总剂量为200 mg/kg,对食蟹猴疟原虫B株确有 20 d的滞效抗疟作用,但总剂量降至 100 mg/kg 时,其滞效作用即明显下降。总之,三吡萘啶游离碱对猴疟的长效抗疟作用似较哌喹稍逊。This paper reports the experiments in which tripynadine free base at a dose 4. 5 times that of ED50 was given to mice by intragastric administration. On the 20th day following the administration the mice were inoculated with 1 × 107 RBC infected with Plasmodium berghei ANKA strain. The infection rate was zero, implying that all mice had acquired protection. Although the residual activity time of tripynadine phosphate was longer than that of tripynadine free base or piperaquine phosphate, but tripynadine phosphate caused vomiting in monkeys during the medication. The residual antimalarial activity of tripynadine hydroxynaph-thoate was less than that of tripynadine phosphate or tripynadine free base. A total dose .of 200 mg/kg of tripynadine free base ensured residual antimalarial activity against P. cynomolgi bastianellii for 20 days. However, the residual activity decreased evidently when the total dose was reduced to 100 mg/kg. In short, it seems that the residual antimalarial activity of tripynadine free base is slightly less than that of piperaquine in monkeys.

关 键 词：三吡萘啶 哌喹 抗疟药 药理学 

分 类 号：R978.61[医药卫生—药品]