朱巧贞, 梁猷毅, 陶正琴, 丁光生. 防治血吸虫病药物的研究 ⅩⅪ.Sb-58,Sb-126与 TWSb 的毒性、疗效及锑的分布和排泄J. 药学学报, 1959, 7(8): 320-326.
引用本文: 朱巧贞, 梁猷毅, 陶正琴, 丁光生. 防治血吸虫病药物的研究 ⅩⅪ.Sb-58,Sb-126与 TWSb 的毒性、疗效及锑的分布和排泄J. 药学学报, 1959, 7(8): 320-326.
CHU CHIAO-CHEN LIANG YU-I TAO ZHENG-QIN TING KUANG-SHENG, . STUDIES ON ANTIBILHARZIAL DRUGS ⅩⅪ.TOXICITY AND THERAPEUTIC ACTIVITY OF Sb-58,Sb-126 AND TWSb AND THE DISTRIBUTION AND EXCRETION OF ANTIMONY AFTER ADMINISTRATION OF THESE COMPOUNDSJ. Acta Pharmaceutica Sinica, 1959, 7(8): 320-326.
Citation: CHU CHIAO-CHEN LIANG YU-I TAO ZHENG-QIN TING KUANG-SHENG, . STUDIES ON ANTIBILHARZIAL DRUGS ⅩⅪ.TOXICITY AND THERAPEUTIC ACTIVITY OF Sb-58,Sb-126 AND TWSb AND THE DISTRIBUTION AND EXCRETION OF ANTIMONY AFTER ADMINISTRATION OF THESE COMPOUNDSJ. Acta Pharmaceutica Sinica, 1959, 7(8): 320-326.

防治血吸虫病药物的研究 ⅩⅪ.Sb-58,Sb-126与 TWSb 的毒性、疗效及锑的分布和排泄

STUDIES ON ANTIBILHARZIAL DRUGS ⅩⅪ.TOXICITY AND THERAPEUTIC ACTIVITY OF Sb-58,Sb-126 AND TWSb AND THE DISTRIBUTION AND EXCRETION OF ANTIMONY AFTER ADMINISTRATION OF THESE COMPOUNDS

  • 摘要: 犬肌肉注射Sb-58,Sb-126与TWSb 3药各6针后,局部稍有红肿,对血糖及心电图的影响均不显著.食量都减少,以TWSb 组较严重,而且TWSb 对于心及肝的损害亦较其他2药严重.日本血吸虫病犬肌肉注射Sb-58,Sb-126及TWSb 每针剂量分别为6,3与6mg/kg,每天2针,共3天.第6针后1/2小时之血Sb 浓度分别为5.0,4.1及6.5μg/5ml,24小时后均降为约2μg.停药13天后解剖,平均每犬余存虫数分别为60,16和67条.Sb-126组的余存虫退化最多,而且还有1犬完全治愈,因此可以认为Sb-126的疗效稍高.病兔肌肉注射一针等Sb 量的3药后1/2小时,血Sb 浓度以Sb-126组较低(5μg/5ml),TWSb 组最高(21μg/5ml),24小时后均减至1μg/5ml.在肝、肾、脾及血吸虫的含Sb 量,3药相差不多.24小时内由尿排出的Sb 量以TWSb 组为最多(40%),Sb-126最少(25%).Sb-126之疗效较高,可能即由于其排泄较慢.

     

    Abstract: Dogs received intramuscularly 6 injections each of Sb-58,Sb-126 and TWSb.They caused slight irritation locally,but exerted little influence on blood sugar and electrocardiogram.Food intake decreased in all,more pronounced with TWSb,which produced a damage to heart and liver more seriously than the other 2 drugs. Dogs,previously infected with Schistosoma japonicum,were treated i.m.with Sb-58,Sb-126 and TWSb.The dosages were respectively 6,3 and 6 mg/kg b.i.d.for 3 days.The blood Sb concentrations 1/2 hour after the last injection were 5.0,4.1 and 6.5 μg/5 ml respectively,and all dropped to about 2 μg after 24 hours.The dogs were killed after a holding period of 13 days,and the average numbers of worms remained in each dog were found to be 60,16 and 67 respectively.Sb-126 caused the highest degree of degeneration of the helminths and a com- plete cure of 1 dog.Hence,the therapeutic activity of Sb-126 was deemed to be slightly higher. Infected rabbits were given i.m.1 injection each of the 3 antimonials at an equivalent dosage of 2.92 Sb mg/kg.The blood Sb level 1/2 hour later was lowest for Sb-126 (5μg/5 ml)and highest for TWSb(21 μg/5 ml).After 24 hours,the blood Sb levels all lowered to about 1 μg.No marked difference among the 3 drugs with respect to the Sb concentrations was observed in liver,kidney,spleen and schistosomes.The urinary excretion of Sb in 24 hours was greatest for TWSb(40%)and least for Sb-126(25%).It was believed that the slower excretion of Sb-126 was partly responsible for its higher therapeutic efficacy.

     

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