Yehia Soad A, El-Gazayerly Omaima N, Basalious Emad B
Department of Pharmaceutics, Faculty of Pharmacy, Cairo University Kasr El-Aini Street, Cairo, Egypt.
Curr Drug Deliv. 2009 Jan;6(1):17-27. doi: 10.2174/156720109787048195.
Fluconazole mucoadhesive buccal films were prepared using film forming polymers namely; hydroxypropyl methyl cellulose (HPMC), hydroxyethyl cellulose (HEC), chitosan, Eudragit and sodium alginate (SALG) either alone or in combination with bioadhesive polymers. The bioadhesive polymers studied were sodium carboxymethyl cellulose (SCMC), Carbopol 974P, and polycarbophil (AA-A). The prepared films were characterized by means of film thickness, surface pH, swelling capacity, in vitro adhesion, in vivo residence time, in vitro drug release and in vivo drug release to determine the amount of drug release from selected film formulae using microbiological assay and HPLC. Optimum release behavior, convenient bioadhesion, acceptable elasticity were exhibited by film containing 2% HPMC and 1% SCMC (fresh or stored for 6 months). Determination of the amount of drug released in saliva after application of the selected fluconazole films confirmed the ability of the film to deliver the drug over a period of approximately 300 minutes and to reduce side effects and possibility of drug interaction encountered during systemic therapy of fluconazole, which would be beneficial in the case of oral candidiasis.
使用成膜聚合物制备氟康唑粘膜粘附口腔膜，这些成膜聚合物包括羟丙基甲基纤维素（HPMC）、羟乙基纤维素（HEC）、壳聚糖、丙烯酸树脂和海藻酸钠（SALG），它们单独使用或与生物粘附聚合物组合使用。所研究的生物粘附聚合物有羧甲基纤维素钠（SCMC）、卡波姆974P和聚卡波非（AA - A）。通过膜厚度、表面pH值、溶胀能力、体外粘附性、体内停留时间、体外药物释放和体内药物释放来表征所制备的膜，使用微生物测定法和高效液相色谱法确定所选膜配方的药物释放量。含有2% HPMC和1% SCMC的膜（新鲜的或储存6个月的）表现出最佳的释放行为、良好的生物粘附性和可接受的弹性。在应用所选的氟康唑膜后测定唾液中释放的药物量，证实该膜能够在大约300分钟的时间内递送药物，并减少氟康唑全身治疗期间遇到的副作用和药物相互作用的可能性，这在口腔念珠菌病的情况下将是有益的。
