异恶唑类。8. 一种异恶唑基萘醌衍生物的制剂前研究。

Isoxazoles. 8. Preformulation studies of an isoxazolylnaphthoquinone derivative.

作者信息

Longhi M R, de Bertorello M M, Granero G E

机构信息

Departmento de Farmacia, Facultad de Ciencias Quimicas, Universidad Nacional de Córdoba, Argentina.

出版信息

J Pharm Sci. 1994 Mar;83(3):336-8. doi: 10.1002/jps.2600830314.

DOI:10.1002/jps.2600830314

PMID:8207677

Abstract

The degradation kinetics of 2-hydroxy-N-(3,4-dimethyl-5-isoxazolyl)-1,4-naphthoquinone 4-imine (1) in a 25% solution of ethyl alcohol in water has been studied. The rate constants were observed to follow pseudo-first-order kinetics in all cases. The pH-rate profile indicated a negligible decomposition at pH values higher than its pKa2 value [5.4 +/- 0.14 (*n = 6)]. Un-ionized 1 was subject to specific acid catalysis. The ionic strength did not affect the stability of the drug. These data can be used to develop a stable oral liquid dosage form of the drug.

摘要

研究了2-羟基-N-(3,4-二甲基-5-异恶唑基)-1,4-萘醌4-亚胺(1)在25%乙醇水溶液中的降解动力学。在所有情况下，速率常数均符合准一级动力学。pH-速率曲线表明，在高于其pKa2值[5.4±0.14(*n = 6)]的pH值下，分解可忽略不计。未电离的1受到特定酸催化。离子强度不影响药物的稳定性。这些数据可用于开发该药物稳定的口服液剂型。