| 引用本文: | 朱丽,韩莎,敖桂珍,曹青日,崔京浩*.布洛芬-去甲丹皮酚偶合物的制备及其稳定性评价[J].中国现代应用药学,2011,28(5):455-457. |
| ZHU Li,HAN Sha,AO Guizhen,CAO Qingri,CUI Jinghao*.Preparation of Ibuprofen-Resacetophenone Conjugate and Its Stability Evaluation[J].Chin J Mod Appl Pharm(中国现代应用药学),2011,28(5):455-457. |
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| 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。 |
| 关键词: 布洛芬 去甲丹皮酚 偶合物 稳定性 |
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| 基金项目:科技部国际科技合作项目(2009DFA31330) |
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| Preparation of Ibuprofen-Resacetophenone Conjugate and Its Stability Evaluation |
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ZHU Li,HAN Sha,AO Guizhen,CAO Qingri,CUI Jinghao*
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| 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. |
| Key words: ibuprofen resacetophenone conjugate stability |
