In vitro/in vivo evaluation of HPMC/alginate based extended-release matrix tablets of cefpodoxime proxetil

• The developed HPMC/alginate based matrix tablets release the drug for 24 h hence, the formulation can be considered as a once-daily.
• In vivo pharmacokinetic studies in rabbits also confirmed the prolonged release for matrix tablet compared to conventional tablet.
• The developed matrix tablets improve the rate of bacterial killing and hasten the cure from the indications, and therefore increases compliance.

The purpose of this research was to assessment of antimicrobial activity and in vitro/in vivo evaluation of cefpodoxime proxetil extended-release (ER) tablet for once daily administration. The tablets were prepared using combination of biodegradable polysaccharides including hydroxypropyl methylcellulose and sodium alginate as matrix material to achieve pH-independent ER release. The tablets were found within the permissible limits for various physicochemical parameters. The in vitro drug release showed that the drug was released over a period of 24 h in a sustained release manner. The drug release followed Higuchi kinetics as these plots showed the highest linearity (R2 = 0.9833), but a close relationship was also observed with zero-order kinetics (R2 = 0.9088) and the drug release mechanism was found to be of anomalous or non-Fickian type. Further, in vitro drug release was assessed by antimicrobial assay and it revealed that drug release through 24 h periods was above the MIC. In vivo investigation in rabbits showed ER pharmacokinetic profile of cefpodoxime from the matrix tablets. A good correlation of drug absorption in vivo and drug release in vitro (R2 = 0.9785) was observed. These results suggested that the investigated CFP matrix tablets have a potential for extended-release dosage forms.