Study On Fluconazole Buccal Adhesive Tablets

The preparation of Fluconazole buccal adhesive tablets was investigated, and the studies on bioadhesive tablets aimed at increaseing the residence time and local drug concentration of Fluconazole at oropharyngeal, and remaining stable oral drug inhibitory concentration for a long period of time, and reducing taken dose and gastrointestinal adverse reaction, more directly treating oral candidiasis and other fungal infection desease.Based on the results, the release profile of buccal adhesive tablets and release mechanism were further analyzed and discussed.The research paper is composed of following parts:1. Studies on the adhesive characteristics and affect factors of bioadhesive materialsCharacters such as adhesive force, swelling rate and adhesive time of Carbopol 934P(CP) and HPMC K4M(HPMC) were studied. The results indicated that the bioadhesive force and swelling rate of the buccal adhesive tablets increased with the increase of the amount of CP 934P included in formulation. The bioadhesive time was independent of the amount of CP 934P. There was a relationship among the bioadhesive force,swelling rate and bioadhesive time,which influenced the bioadhesive properties of the buccal adhesive tablet together. when the ratio of CP and HPMC is between 0.5:1～2:1,the bioadhesive force and the bioadheisve time were desirable.2. Preparation of buccal adhesive tablet and studies on its in vitro release behaviorThe direct compression method was selected as the preparation of fluconazole buccal adhesive tablets, and the orthogonal test was investigated for optimizing the formulation, The results implicated that the release of Fluconazole agreed with zero-order equation, and the drug release corresponded to erosion mechanism.3. Studies on Fluconazole buccal adhesive tablets in vivo release behaviorThe release of Fluconazole from buccal adhesive tablets in oral cavity accorded with zero release kinetic,and good correlation existed between the drug release percent in vivo and in vitro. A spectrophotography method and HPLC method were established for testing the salivary concentration of Fluconazole. The effective salivary concentration of Fluconazole (above the MIC) was gained at 0.25h and maintained over 8h by buccal delivery.