布洛芬-去甲丹皮酚偶合物的制备及其稳定性评价

    Preparation of Ibuprofen-Resacetophenone Conjugate and Its Stability Evaluation

    • 摘要: 目的 制备布洛芬-去甲丹皮酚偶合物(IB-RP),并考察其稳定性。方法 碳酰亚胺法制备IB-RP,利用红外光谱、核磁共振和质谱对其进行结构表征,高效液相色谱法考察不同pH环境和大鼠血浆对其稳定性的影响。结果 结构表征结果显示成功制备IB-RP,偶合物稳定性在高温条件下发生降解,随着pH值的上升其降解速度呈明显上升的趋势。另外,偶合物在血浆中迅速发生降解,其半衰期约为3 min。结论 建立制备IB-RP的方法,其稳定性受pH值的影响,血浆中可迅速降解。

       

      Abstract: OBJECTIVE To prepare ibuprofen-resacetophenone conjugate (IB-RP) and evaluate its stability in vitro. METHODS Carbimide method was employed to prepare IB-RP, and its chemical structure was confirmed through infrared spectrum (IR), 1H-NMR and MS, respectively. The affect of different pH condition and rats plasma on the stability of IB-RP were observed and detected by HPLC. RESULTS The structure characterization results validated the synthesis of IB-RP. The stability of conjugate was affected by high temperature and the degradation rate was increased significantly under higher pH condition, too. In addition, IB-RP was degraded readily in rat plasma with 3 min half-life. CONCLUSION The preparation method of IB-RP is established, and its stability is influenced by pH value and plasma environment.

       

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