鼻用原位凝胶基质配方的对比研究

Comparison of the Matrix Prescription of Nasal in Situ Gel

目的比较常用的三种类型鼻用原位凝胶典型基质及其胶凝行为特征,为快速优化处方提供参考。方法分别配制不同浓度的卡波姆974P(p H敏感型)、泊洛沙姆407(温度敏感型)、去乙酰结冷胶(离子敏感型)溶液,比较上述溶液加入增黏剂后及其与人工鼻液混合前后的胶凝行为变化,优选出鼻用原位凝胶的基质处方并进一步评价其凝胶强度和持水性。结果所考察的卡波姆974P各体系均无法形成凝胶;21%泊洛沙姆407+0.3%聚维酮组、20%泊洛沙姆407+0.3%羟丙甲纤维素组在34℃时可形成凝胶;去乙酰结冷胶组及加入0.2%海藻酸钠组均可形成凝胶,其中0.5%去乙酰结冷胶+0.2%海藻酸钠组加入人工鼻液前后黏度相差最大,所形成的的凝胶强度较大、持水性佳。结论 0.5%去乙酰结冷胶为基质、0.2%海藻酸钠为增黏剂时体系的胶凝行为最优,能与人工鼻液混合形成强度、持水性均良好的凝胶。

Objective To compare different kinds of nasal in situ gel matrix in gelation characteristics and provide reference for rapid formulation optimization. Methods Solutions of Carbomer 974P( p H- sensitivity),Poloxamer 407( themo- sensitivity),deacetylated gellan gum( ion- sensitivity) with different concentration were prepared,and then their gelation behavior were compared before and after addition of the artificial nasal fuild( ANF). The optimized formulation were further evaluated by its gel strength and water- binding capacity. Results After mixed with ANF,Carbomer 974 P solutions could not form gel,whereas the solutions of 21% Poloxamer 407 + 0. 3% PVP,20% Poloxamer 407 + 0. 3% HPMC gelled quickly. Besides,all systems of deacetylated gellan gum with sodium alginate could form strong gel with excellent water- binding capacity. Conclusion The ionic- sensitive system of 0. 5% gellan gum and 0. 2% adhesive alginate exhibits excellent gelling properties,and they are suitable for nasal administration.