SHI Jing1��2��QIU Li-yan1�� WU Chao1�� JIN Yi1�� ��SHENTU Jian-zhong3
1. College of Pharmaceutical Sciences��Zhejiang University��Hangzhou 310031��China�� 2. Zhejiang Medical College��Hangzhou 310053��China�� 3. Department of Clinical Pharmacology��First Affiliated Hospital��Zhejiang University��Hangzhou 310003��China
Abstract��
OBJECTIVE To study and evaluate the formulation of bilayer oral mucoadhesive films of fentanyl. METHODS The mucoad-hesive films were produced by spreading drug on bioadhesive and protective films.Their mucoadhesion in vitro and adhesive time in vivo, drug release rate and penetration through excised oral mucosa were investigated in order to determine an optimum formulation.RESULTS Alginale sodium,CMC-Na and PVA in a ratio of 2:1:2 were an optimum formulation,and its bioadhesive force was (203��21) g��cm-2,the adhesive time in vino was 120 min.Its release curve conformed to Higuchi formulation. A high permeation rate of 10.527��g��cm-2��h-1 was showed in vitro.The permeation of the oral mucoadhesive films followed the Fick's first diffusion law.The addition of glycyrrhizin to the films increased the fentanyl release rate and penetration, though a little decrease of bioadhesive force was observed.CONCLUSION The fentanyl bilayer oral mucoadhesive films may be a promising vehicle for the transbuccal delivery of fentanyl.