摘要
为指导合理用药，对舒他西林特性进行了研究。舒他西林是由氨苄西林和舒巴坦通过双酯键连接而成的口服β内酰胺抗生素前药，在中性及偏碱性条件下极易水解，水解时两个酯键的活泼性不同，通常优先形成氨苄西林和舒巴坦羟甲酯；在自发水解液中氨苄西林和舒巴坦之比约３∶１；
Sultamicillin is an oral mutual pro drug composed of double esters of formaldehyde hydrate in which one of the hydroxyl groups is esterified with ampicillin and the other with sulbactam. It is hydrolyzed fast in neutral or weakly alkaline condition. When hydrolyzed, it forms ampicillin and hydroxylmethyl sulbactam or sulbactam and hydroxylmethyl ampicillin by different routes. Usually, the former has priority as the two ester bonds have different activities. The ratio of ampicillin to sulbactam in the products is about 3∶1. Both the hydroxylmethyl sulbactam and the hydroxylmethyl ampicillin can be further catalyzed by esterase to produce formaldehyde.
出处
《药学学报》
CAS
CSCD
北大核心
1997年第7期553-557,共5页
Acta Pharmaceutica Sinica
关键词
舒他西林
水解反应
合理用药
Sultamicillin
Ampicillin
Sulbactam
β lactam antibiotics
