八角茴香油β-环糊精包合物胶囊的制备工艺及稳定性研究

Study on the Preparation and Stability of β-CD Inclusion Compound Capsules with Star Anise Oil

[目的]研究八角茴香油β-CD包合物胶囊的制备工艺,并考察其稳定性。[方法]以八角茴香油与β-CD的比例、包合时间和包合温度为因素,并以包合物收率、包合物含油率和油的收率为指标,采用L9(34)正交试验优选最佳包合条件;然后以休止角和吸湿性为指标,用薄层色谱法(TLC)对包合物进行验证,优选包合物胶囊的处方,并检查胶囊质量。[结果]最佳包合工艺为:八角茴香油:β-CD为1∶6,包合时间为2 h,包合温度50℃;在此条件下,包合物收率为89.84%,包合物含油率为15.93%,油的收率为72.63%。胶囊处方为:包合物200 mg,微晶纤维素100 mg,十二烷基硫酸钠5 mg,硬脂酸镁3 mg;制得的胶囊水分、装量差异和崩解时限均符合药典规定;影响因素试验表明,胶囊剂对高温、高湿度和强光的稳定性明显高于其物理混合物。[结论]八角茴香油包合物胶囊制备工艺简单、易行,质量稳定、可控。

[Objective] To study the preparation technique of β-CD inclusion compound capsules for Star Anise Oil and inspect its stability.[Method] The ratio of Star Anise Oil to β-CD,the inclusion time and temperature were taken for factors,L9（34）orthogonal test was used with the inclusion percentage,volatile oil content,the yield of volatile oil as indicators,to choose the best inclusion conditions;the inclusion compound was identified by the ways of Thin-layer chromatography（TLC）;Choose the best formulation of the inclusion compound capsules with the angle of repose,hygroscopicity for indicators;Check the capsule＇s quality;Stress testing was carried on the capsules.[Results] The optimum preparation conditions were obtained as follows： Star Anise Oil： β-CD was 1∶6;the inclusion time and temperature was 2 h and 50 ℃;the yield of the inclusion compound was 89.84%,the volatile oil content was 15.93%,the yield of volatile oil was 72.63%;The capsules formulation was as follows： inclusion compound-microcrystalline cellulose-lauryl sodium sulfate-Magnesium Stearate（200 mg：100 mg：5 mg：3 mg）;The capsule moisture content,load difference and the disintegration time limit conform to the pharmacopoeia stipulation;Stress testing results showed that the capsules stability was higher than its physical mixture obviously to high temperature,high humidity and high-lights.[Conclusion] The preparation process of β-CD inclusion compound capsules with Star Anise Oil is easy and feasible,the quality is stable and controllable.