复方薄荷脑微乳原位凝胶剂的评价

Evaluation of compound microemulsion based in situ gel containing menthol

目的对载复方薄荷脑微乳的原位凝胶滴鼻液(薄荷脑、樟脑、液状石蜡)进行评价。方法薄荷脑和樟脑的低共熔特性制备微乳再将其载入原位凝胶中制得载药微乳凝胶液,从制剂的外观、p H、流变学性质、体外释放度、离体黏膜透过性及对大鼠鼻黏膜形态进行考察。结果体外释放行为符合Higuchi方程,10 h累积释放33.6%,显著优于原制剂的7.6%;10 h离体黏膜累积透过性率11.8%,约为原制剂的5倍;对大鼠鼻黏膜的刺激性较小且可逆。结论复方薄荷脑微乳的原位凝胶滴鼻液具有良好的缓释性能且适合临床使用。

AIM To evaluate the efficacy of nasal microemulsion based in situ gel（ MBG） made up of menthol,camphor and liquid paraffin. METHODS The preparation made from a mixture of menthol and camphor as eutectic microemulsion for in situ gel,had its appearance,p H,rheological property,dissolution,in vitro mucosa permeability and morphology examined. RESULTS The in vitro release profile conformed to Higuchi model,33. 58% cumulative release at 10 h was superior to the previous 7. 60% value of nasal drops without microemulsion.The in vitro permeation percentage 11. 49% was almost 5 folds of the 2. 48% nasal drops without microemulsion.The irritability induced by MBG was rare and slight and reversible. CONCLUSION MBG of compound menthol excels in in vitro release and permeation,and should be appropriate for clinical use.