Studies on Oral Sustain Delivery of Cefixlme from Floating Matrix Tablets Formulation and In Vitro Evaluation

摘要

The objective of the present study was to deyelop Cefixime gastroretentive floating matrix tablets for prolonged gastric retention time and thereby increased drug bioavailability. Cefixime is a third generation Cephalosporins antibiotic which is slowly and incompletely absorbed from the GIT, which resulting into the poor bioavailability 40-50%.The floating tablets were prepared by direct compression method, using polymers like SCMC, Carbopol 934P, and HPMC K100M in an effervescent system and polypropylene foam powder (Accurel) in low density system.The powder blends was subjected for pre-compression parameters and were within prescribed limits and indicated free flowing property .The prepared tablets were evaluated for post- compression parameters such as weight variation, thickness, friability, hardness, drag content, in vitro buoyancy studies and in vitro release studies in 0.1N HC1 (pH1.2) for 12 h. Among all the formulations (Fl to F12), formulation (F8) which showed the buoyancy lag time 52 Sec, remained buoyant for 12h and release of Cefixime sustained over 12h when compared to other formulations. The in vitro data is fitted into different Kinetics models. The optimized formulation F8 followed Zero order kinetics and best fitted Korsmeyer - Peppas model followed by non-fickian diffusion (n=0. 753). FTIR studies revealed that, there was no incompatibility of the drug with excipients used. The stability studies conducted as per the ICH guidelines at 40 +-2°C and 75 +-5% RH for 1 month and the optimized formulation (F8) showed no significant change in physical appearance, drug content, total buoyancy time and in vitro dissolution study after storage. From this study, it was concluded that, the formulation (F8) can be retained for a longer period of time in the stomach and provided prolong release of the drug, hence it may increase the therapeutic efficacy of the drug by increasing the bioavailability.