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丁香酚前体药物的合成及其微乳的制备
Synthesis of the Eugenol ester prodrug and study on its Microemulsion Formulation
【Author】 ZHAO Xiu-li, CHEN Da-wei, QIAO Ming-xin, HU Hai-yang School of Pharmacy, Shenyang Pharmceutical University, Shenyang110016, China
【机构】 沈阳药科大学药学院；
【摘要】 目的:合成丁香酚布洛芬前体药物,改善丁香酚的刺激性和稳定性,在此基础上制备其微乳制剂。方法:以布洛芬和丁香酚为原料,经过酯化反应合成了布洛芬前体药物丁乔酚布洛芬酯,利用伪三元相图法制备微乳相图,并从中选择了最优的微乳制剂处方。结果:前体药物制成微乳后,其溶解度为64mg／ml,是在其在水中溶解度的21,000倍。结论;将中药成分丁香酚改造成前体药物并应于微乳制剂具有良好的发展前景。
【Abstract】 OBJECTIVE To synthesis ibuprofen eugenol ester (IEE) and investigate microemulsion formulation of it. METHODS: Ibuprofen-eugenol ester was synthesized by acyl chloride method using eugenol and ibuprofen as the raw materials. Pseudo-ternary phase diagrams was prepared and the optimized formulation was choiced. RESULTS: The solubility of IEE in the optimized microemulsion formulation was 64mg/ml,which was about 21,000 times higher than that in water. CONCLUSION: Eugenol ester microemulsion might be a promising dosage form of Chinese traditiona Medicine.
【Key words】 Eugenol ibuprofen ester； Eugenol； Ibuprofen； systhesis； prodrug； Pseudo-ternary phase diagram； Microemulsion；
- 【会议录名称】 “以岭医药杯”第八届全国青年药学工作者最新科研成果交流会论文集
- 【会议名称】“以岭医药杯”第八届全国青年药学工作者最新科研成果交流会
- 【会议时间】2006-04
- 【会议地点】中国河北石家庄
- 【分类号】TQ461
- 【主办单位】中国药学会