RACEMIZATION OF KETOROLAC IN AQUEOUS-SOLUTION

被引：10

作者：

BRANDL, M

CONLEY, D

JOHNSON, D

机构：

[1] Pharmaceutical Research Syntex Research, Palo Alto, California

来源：

JOURNAL OF PHARMACEUTICAL SCIENCES | 1995年 / 84卷 / 09期

关键词：

D O I：

10.1002/jps.2600840903

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The racemization of ketorolac was studied in aqueous buffered solution at 25 and 80 degrees C and analyzed in detail with respect to the catalytic species in solution. The reaction has a U shaped pH rate profile at 80 degrees C with the pH of maximum stability occurring in the region of pH 3.0-7.5. A T-90 value of 8 months was observed for a 1.5% (R)ketorolac tromethamine solution at pH 7.4 and 25 degrees C. Additionally, the data shows that alternative salt forms are necessary in order to prepare a stable single isomer formulation. Alternative buffers, in particular phosphate buffer, provide formulations exhibiting a T-90 greater than 2 years.

引用

页码：1045 / 1048

页数：4

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