小茴香挥发油贴剂的处方前研究

Pre-formulation study on fennel oil patch

目的对小茴香挥发油进行处方前研究,为设计优良的处方奠定基础。方法利用高效液相色谱法（HPLC）建立测定小茴香挥发油的分析方法,并进行小茴香挥发油的平衡溶解度、油水分配系数、稳定性试验、原辅料相容性试验等处方前研究。结果小茴香挥发油在2.00～120.24μg/mL范围内线性关系良好。小茴香挥发油在蒸馏水、生理盐水、不同p H（2.0、5.0、6.8、7.4、8.0）磷酸盐缓冲液（PBS）中的平衡溶解度分别为21.47、22.89、25.55、16.08、18.29、27.36、28.94μg/mL;在无水乙醇、95%乙醇、乙酸乙酯、丙酮、石油醚中极易溶解。小茴香挥发油的油水分配系数（log P）为3.59。小茴香挥发油稳定性试验及小茴香挥发油贴剂原辅料相容性试验第5天及第10天含量测定结果表明其受条件影响：温度〉光照〉湿度。结论建立的分析方法准确可靠。本研究表明小茴香挥发油几乎不溶或不溶于水及磷酸盐缓冲液,极易溶解于部分有机溶剂。小茴香挥发油在高温和光照下不稳定,易降解;在高湿下较稳定。

Objective To study the pre-formulation of fennel oil so as to design the formulation. Methods A high performance liquid chromatography（ HPLC） method was established to determine the content of fennel oil. Based on the method,equilibrium solubility,oil / water partition coefficient,stability test and material compatibility on fennel oil were investigated. Results A good linear relationship was obtained at the range from 2. 00 to 120. 24μg /mL of fennel oil. The equilibrium solubility of fennel oil in distilled water,saline,and different p H（ 2. 0,5.0,6. 8,7. 4,8. 0） PBS were 21. 47,22. 89,25. 55,16. 08,18. 29,27. 36,28. 94 μg / mL,respectively. The fennel oil was easily soluble in ethanol,95% ethanol,ethyl acetate,acetone,and petroleum ether. The oil / water partition coefficient（ log P） of fennel oil was 3. 59. The results of stability test and material compatibility test in 5and 10 days showed that the content of fennel oil was affected by these conditions： temperature 〉light 〉humidity.Conclusion The HPLC assay was accurate and reliable. The study showed that fennel oil was almost insolubled in water and PBS,and it was easily soluble in some organic solvents. It proved that the fennel oil was unstable and decomposed easily under high temperature and light condition,and it was more stable under high humidity.