RESUMEN
Effects of diabetes mellitus induced by streptozotocin (DMIS) on the pharmacokinetics of Gatifloxacin were investigated after i.v and oral administration (50mg/mg) to control Sprague-Dawley rats and DMIS rats (at 7th and 29th days after administration of streptozotocin (55mg/kg). After i.v administration to DMIS rats, there was no significant difference in clearance, t1/2, Vd and MRT last. But after oral administration of gatifloxacin to DMIS rats Cmax was significantly increased. This could be supported with the marginal increase in AUC and an increase in bioavailability of drug in chronic (78.7% increase) as well as acute conditions (75.3% increases). Streptozotocin induced toxicity did not influence considerably on the pharmacokinetics of gatifloxacin.
RESUMEN
Aim: The aim of this study to develop the controlled delivery of combination drug(s) to periodontal pocket. Materials and Methods: In the present investigation mucoadhesive gel formulations were prepared using carboxy methylcellulose (CMC), methylcellulose (MC), hydroxyethylcellulose (HEC), polyvinylpirrolidone (PVP), polycarbophil (PC), and poloxamer. Each formulation was characterized in terms of polarizing light microscopy, gelation, gel melting, hardness, compressibility, adhesiveness, cohesiveness, syringeability, adhesion to a mucin disk, rheological studies, drug release, and antibacterial activities. Addition of CMC and PVP to the gel favored hexagonal phase formation. The gelation temperature was decreased linearly with an increasing concentration of drug(s), whereas, the melting temperature increased with the concentration of drug(s). Increasing the concentrations of each polymeric component significantly increased formulation hardness, compressibility, adhesiveness, mucoadhesion, and syringeability, yet a decreased cohesiveness. Increased time of contact between the formulation and mucin significantly increased the required force of detachment. Drug release from all formulations was non-diffusion controlled and significantly decreased as the concentration of the polymer was increased, due to the concomitant increased viscosity of the formulations and the swelling kinetics of PC, following contact with the dissolution fluid. Result: Antibacterial studies revealed that a gel with 30% HEC had a growth inhibition zone on agar with all three strains. Conclusion: Formulations containing HEC exhibited superior physical characteristics for improved drug delivery to the periodontal pocket and are now the subject of long-term clinical investigations.