口腔内粘膜付着性軟膏の製剤特性：水溶性高分子―プラスチベース系

抄録

Ointments which can be adhered on the oral mucosa were prepared by dispersing various water-soluble polymers in oleaginous bases, and the adhesive characteristics, drug release profiles and liquid-bleeding restriction of the ointments were evaluated in search of an optimal formulation. Among the water-soluble polymers investigated, gelatin showed the largest initial adhesive strength, followed by carboxymethylcellulose sodium (CMC-Na) and pullulan. Among the bases, plastibase was found to be an optimal base with adhesiveness. A preparation in which a mixture of gelatin: CMC-Na: pullulan (1:1:1) was dispersed in plastibase at a concentration of 30% or higher, showed the largest initial adhesion strength among the polymer-containing preparations. However, in terms of bleeding restriction and adhesiveness to the oral mucosa, the optimal polymer content in the base was estimated to be 30%. The preparation also showed a satisfactory drug release profile and durable adhesion characteristics. It is suggested that CMC-Na takes part in the initial adhesion strength of the preparation, while gelatin and pullulan take part in the durability of adhesion. The usefulness of the preparation was also supported by the good durability of adhesion in healthy volunteers.