Evaluation of Thickening Agents in Preparation of Sodium Gualenate Gargles.

A sodium gualenate gargle (Az-G) for the treatment of pharyngitis, tonsilitis, stomatitis and oral wound was prepared by using various thickening agents carboxymethylcellulose sodium (CMCNa), sodium polyacrylate (PANa) and sodium alginate (AGNa), and the effect of such thickening agents on the release-profiles of sodium gualenate (Az) from Az-G were evaluated both in vitro and in vivo. The mean dissolution time in vitro (MDTin vitro) of Az from preparations with 1.0% or more CMCNa and 2.0% AGNa were significantly higher than that of the control preparation (without thickening agent). However, the preparation with 0.2% PANa did not increase the MDTin vitro significantly despite the fact that the preparation had a higher viscosity than the control preparation. In the application of Az-G to healthy volunteers, the amount of Az adhering to the oral mucosa increased significantly in proportion to the concentration of CMCNa. On the other hand, MDTin vivo increased significantly at 1.0% of CMCNa, though it did not increase significantly at 2.0%. There was no significant rise in the amount of Az adhered on oral mucosa and MDTin vivo in the preparations with PANa and AGNa. The highest values regarding the amount of Az adhering to the oral mucosa, MDTin vivo and the amount of Az released in saliva obtained at 30-33 min after application were observed in the preparation with 1.0% CMCNa. These results suggest CMCNa to be the most excellent thickening agent for the preparation of Az-G and the optimum content was 1.0%.