FLURBIPROFENGELATIN MICROSPHERES FOR INTRAARTICULAR ADMINISTRATION

AIM: To prepare flurbiprofen gelatin microspheres for intraarticular administration. METHODS: An optimum procedure was established by uniform test for preparing flurbiprofen gelatin microspheres (FP-GMS) with emulsioncongealing method. RESULTS: The particle size focused on 2.5～12.3 μm, the mean size was 7.53 μm, drug content was 5.02% (w/w). The dissolution profiles of the FP-GMS followed Higuchi kinetics. The stability of FPGMS was excellent. In rabbits the mean retention time (MRT) of FPGMS was prolonged vs that of the injection group (P<0.01), after intraarticular cavity administration with FPGMS. The T_max was prolonged 2.03 times and the C_max was decreased 5.57 times vs that of the injection group. Significant linear correlation exists between the dissolution in vitro and absorption in vivo (P<0.01). CONCLUSION: The size distribution of FP-GMS was focalized, and the FP-GMS showed obvious sustained effect both in vitro and in vivo.