Development and stability test of compound adapalene ointment
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摘要: 目的 制备复方阿达帕林软膏并对其稳定性进行考察和优化。 方法 以PEG400和PEG3350为基质，制备含阿达帕林和莫匹罗星的复方软膏。采用影响因素试验考察和优化药物的稳定性，再经加速试验和长期试验做进一步评价。 结果 阿达帕林原料药在高温、高湿和强光照射下均有良好的稳定性，莫匹罗星原料药的含量在高温下快速降低，在高湿和强光照射下稳定性良好。在pH≤7时，阿达帕林和莫匹罗星有明显的降解现象，而在pH=7.5时稳定性最佳，10 d时的含量>95%。PEG400和PEG3350的比例为2∶1时，软膏的黏度最佳，易于涂展，且采用0.2%三乙醇胺调节pH，显著改善了阿达帕林和莫匹罗星的稳定性。加速试验和长期试验（6个月）结果显示，软膏中阿达帕林和莫匹罗星的含量保持在95%以上。 结论 本实验成功制备了复方阿达帕林软膏，药物稳定性良好。Abstract: Objective To prepare, investigate and optimize the drug stability of compound adapalene ointment. Methods The ointment containing adapalene and mupirocin were prepared with PEG400 and PEG3350 as matrix.Stress test was used to evaluate and optimize the stability of drugs in the ointment.The drug stability was further tested by the acceleration test and long-term test. Results The raw adapalene was stable under high temperature, high humidity and strong light irradiation.The raw mupirocin was stable under high humidity and strong light irradiation, but was highly unstable under high temperature condition.Degradation of adapalene and mupirocin was found with pH ≤ 7.At pH 7.5, the best stability was achieved, with over 95% of the drugs remaining at day 10.Favorable ointment was prepared with PEG400:PEG3350=2:1.The drug stability was promoted by addition of 0.2% triethanolamine significantly.In the acceleration test and long-term test, the percentages of adapalene and mupirocin were above 95%. Conclusion The compound adapalene ointment was successfully prepared and the drug stability was excellent.
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