Development of In Situ Gel for Oral Application

摘要

In situ gel, a new concept of medical product for oral applications was developed using Poloxamer 407 (P) and Carbopol 934 (C) which are thermo- and pH- sensitive sol-gel polymers, respectively. The formulations were evaluated for the physical appearance, pH, viscosity, sol-gel temperature, gel strength and buccal mucoadhesive (adhesion to porcine buccal mucosa). Benzalkonium chloride (BzCl) 0.1% w/v was added in the suitable formulations as a model drug. Formulations containing 20% P (pH = 7.1) and 20% P + 0.6% C (pH = 5.0) showed good physical appearances which turned to gels in buccal conditions. Their mucoadhesive force to porcine buccal mucosa were higher than formulations containing 10 and 15 % P (p<0.05). The present of 0.6 % C in the formulation did not affect gel strength but tended to increase mucoadhesive properties. The release of BzCl from the formulations was performed using Franz diffusion cell at 37°C for 1 hour. There were no different in drug release from both formulations (p<0.05), the amount of drug release was 11.7% ± 4.4 and 10.9% ± 0.8, respectively. In conclusion, formulation containing 20% P and 0.6% C has revealed the most suitable properties as in situ gel for buccal mucosa applications, the release of BzCl was 10.9% ± 0.8 within 1 hour.