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美法仑的水解及与蛋白质的结合

Hydrolysis and protein binding of melphalan.

作者信息

Chang S Y, Alberts D S, Farquhar D, Melnick L R, Walson P D, Salmon S E

出版信息

J Pharm Sci. 1978 May;67(5):682-4. doi: 10.1002/jps.2600670530.

DOI:10.1002/jps.2600670530
PMID:641810
Abstract

Melphalan (30 microgram/ml) is completely hydrolyzed in water at 37 degrees after 8 hr. At lower temperatures, hydrolysis proceeds at slower rates. The presence of bovine serum albumin retards hydrolysis of melphalan (30 microgram/ml) in water. The melphalan hydrolysis rate is directely releated to the bovine serum albumin concentration. At 37 degrees, 8 g of bovine serum albumin/100 ml of water gives a recovery rate of melphalan similar to that of human plasma. In vitro alkylation of melphalan at 37 degrees with human plasma containing 30 microgram/ml, calculated by equilibrium dialysis, methanol extraction, and high-pressure liquid chromatographic analysis, is 30% after 8 hr.

摘要

美法仑(30微克/毫升)在37摄氏度的水中8小时后会完全水解。在较低温度下,水解速度较慢。牛血清白蛋白的存在会减缓美法仑(30微克/毫升)在水中的水解。美法仑的水解速率与牛血清白蛋白浓度直接相关。在37摄氏度时,8克牛血清白蛋白/100毫升水的美法仑回收率与人血浆相似。通过平衡透析、甲醇萃取和高压液相色谱分析计算,在37摄氏度下,美法仑与含30微克/毫升的人血浆进行体外烷基化反应8小时后为30%。

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