| 舒他西林水解反应的研究 |
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| 引用本文： | 胡昌勤,杨敏智,张大超,刘巍,吴铨,梁红,金少鸿. 舒他西林水解反应的研究[J]. 药学学报, 1997, 32(7): 553-557 |
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| 作者姓名： | 胡昌勤 杨敏智 张大超 刘巍 吴铨 梁红 金少鸿 |
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| 作者单位： | 中国药品生物制品检定所 |
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| 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;产生的氨苄西林羟甲酯和舒巴坦羟甲酯经酯酶等进一步水解可释放出甲醛。
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| 关 键 词： | 舒他西林 氨苄西林 舒巴坦 β内酰胺抗生素 |
| 收稿时间： | 1996-11-10 |
STUDIES ON SULTAMICILLIN HYDROLYSIS |
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| CQ Hu,MZ Yang,DC Zhang,W Liu,Q Wu,H Liang and SH Jin. STUDIES ON SULTAMICILLIN HYDROLYSIS[J]. Acta pharmaceutica Sinica, 1997, 32(7): 553-557 |
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| Authors: | CQ Hu MZ Yang DC Zhang W Liu Q Wu H Liang SH Jin |
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| Affiliation: | National Institute for the Control of Pharmaceutical and Biological Products, Beijing 100050. |
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| Abstract: | 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. |
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| Keywords: | Ampicillin Sulbactam β-lactam antibiotics Sultamicillin |
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