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目的为减轻双氯芬酸钠的刺激性，研制合成氯芬酸赖氨酸盐，以扩大其应用。方法采用均匀设计方法研究从优化双氯芬酸赖氨酸盐的合成条件；采用四大学谱和元素分析法鉴定其结构；采用兔眼结膜法进行刺激性实验。结果：均匀设计法预测出最佳合成条件，并依此对其优化验证，得率为７７．６％（纯度９８％以上）；产品分子式为Ｃ２０Ｈ２５Ｑ４Ｎ３Ｃｌ２，经ＵＶ，ＩＲ，ＭＳ，１ＨＮＭＲ，１３ＣＮＭＲ，ＤＥＰＴ及元素分析确定无疑；刺激性实验结果表明：本品对免眼结膜的刺激性明显低于双氯芬酸钠（Ｐ＜０．０１）。结论：双氯芬酸赖氨酸盐的刺激性明显较双氯芬酸钠小，而且合成工艺简单、快速、得率高、无污染，适于推广使用和大批量生产
Aim To reduce the irritation of diclofenac sodium, a new synthetic salt of chlorpheniramine lysine was developed to broaden its application. Methods The uniform design method was used to study the synthesis of diclofenac lysinate. The structure was identified by four-spectrum analysis and elemental analysis. The rabbit conjunctiva was used for stimulation experiment. Results: The optimal synthesis conditions were predicted by the uniform design method, and the yield was 77.6% (purity 98%). The molecular formula of the product was C20H25Q4N3Cl2. The product was identified by UV, IR, MS, 1HNMR, 13CNMR, DEPT and elemental analysis were no doubt; irritation test results show that: This product is no irritation to the conjunctiva than diclofenac sodium (P <0.01). CONCLUSION: Diclofenac lysine is significantly less irritating than diclofenac sodium, and the synthesis process is simple, rapid, high yield and non-polluting, which is suitable for promoting the use and mass production