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

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。

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.