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丙酰螺旋霉素(Pro-SPM)为一抗革兰氏阳性球菌为主的新抗生素,体内外药效优于乙酰螺旋霉素(Ac-SPM),急性毒性较小,小鼠LD_(50)口服为3700mg/kg,静脉为354.96mg/kg,大鼠LD_(50)口服为4000mg/kg。Pro-SPM 30mg/kg静脉注射对兔心电图、呼吸无影响,仅引起轻度血压下降。Pro-SPM在兔体内的代谢与Ac-SPM相似,均转变成螺旋霉素,药动学参数提示Pro-SPM的体内代谢慢于Ac-SPM,Pro-SPM的达峰浓度(Cmax)、曲线下面积(AUC)均高于Ac-SPM。兔口服Pro-SPM、Ac-SPM后24小时回收率分别为5.52%、5.25%。Pro-SPM的Ames试验、染色体畸变试验结果均为阴性。
Propionimidyl spiramycin (Pro-SPM) is a new anti-Gram-positive cocci-based new antibiotic. Its pharmacodynamic effect is better than Ac-SPM in vitro and in vivo, and its acute toxicity is lower. LD- ) Orally 3700mg / kg, intravenous 354.96mg / kg, rat LD_ (50) oral 4000mg / kg. Pro-SPM 30mg / kg intravenous injection of rabbit ECG, no effect on breathing, causing only mild drop in blood pressure. The metabolism of Pro-SPM in rabbit is similar to that of Ac-SPM, and all of them are converted to spiramycin. The pharmacokinetic parameters of Pro-SPM suggest that the in vivo metabolism of Pro-SPM is slower than that of Ac-SPM and Pro-SPM Under the area (AUC) were higher than Ac-SPM. Rabbit oral Pro-SPM, Ac-SPM 24 hours after recovery rates were 5.52%, 5.25%. Pro-SPM Ames test, chromosome aberration test results were negative.