Faculty of Pharmacy, Department of Pharmaceutical Sciences, University of Florence, via Ugo Schiff 6, 50149 Sesto Fiorentino, Italy.
J Pharm Sci. 2010 Jul;99(7):3019-29. doi: 10.1002/jps.22068.
A new mucoadhesive film for topical administration in the oral cavity of flufenamic acid, a poorly soluble anti-inflammatory drug, has been developed, using complexation with hydroxypropyl-beta-cyclodextrin (HPbetaCD) to improve drug dissolution and release rate. Buccal films were prepared utilising chitosan as mucoadhesive polymer, KollicoatIR as film-forming polymer and glycerol as plasticiser. Different combinations of these components were used and the obtained films were characterised for weight, thickness, swelling, mucoadhesive and mechanical properties. The film containing chitosan 2%, glycerol 7.5% and KollicoatIR 1% showed the best properties for the development of the film formulation. The selected film was loaded with the plain drug and its colyophilised and coground products with HPbetaCD, and in vitro release studies in simulated saliva were performed. The improved drug dissolution properties, obtained by complexation with HPbetaCD, were critical to achieve complete release from film formulation during 4-5 h. On the contrary, film loaded with the plain drug showed incomplete release, not exceeding 70% release after 5 h. The developed film formulation containing the drug as complex with HPbetaCD can assure a prolonged drug release directly at the inflammation site and can be proposed as a new therapeutic tool in the treatment of oral mucosa inflammations.
已开发出一种用于将在口腔中局部给药的新的、具有黏膜黏附性的氟芬那酸薄膜，该药物是一种难溶性的抗炎药物，使用与羟丙基-β-环糊精（HPβCD）的包合作用来改善药物的溶解和释放速率。利用壳聚糖作为黏膜黏附性聚合物、KollicoatIR 作为成膜聚合物以及甘油作为增塑剂来制备颊用膜。使用了这些成分的不同组合，并对所得到的膜进行了重量、厚度、溶胀、黏膜黏附性和机械性能的特性研究。含有壳聚糖 2%、甘油 7.5%和 KollicoatIR 1%的膜显示出了用于开发膜配方的最佳特性。选择的膜被加载有普通药物及其与 HPβCD 的共冻干和共研磨产物，并在模拟唾液中进行了体外释放研究。通过与 HPβCD 的包合作用获得的改善的药物溶解性质对于在 4-5 小时内从膜制剂中实现完全释放至关重要。相反，含有普通药物的膜显示出不完全释放，在 5 小时后释放不超过 70%。包含药物与 HPβCD 的复合物的开发的膜制剂可确保在炎症部位延长药物释放，并可作为治疗口腔黏膜炎症的新的治疗工具。
