Development, intra-gastric performance and pharmacokinetic study of gastroretentive drug delivery system for cefdinir in human volunteers

Ramesh Bomma, Kishan Veerabrahma

Abstract


The objective of this study was to develop sustained-release floating tablets of cefdinir (CFDN) using effervescent technique to prolong gastric residence time (GRT) and compare their pharmacokinetics with immediate release (IR) and conventional sustained release (SR) tablets. The tablets were designed using CaCO3 as gas-former and three grades of polyethylene oxide as release-retardants and further were evaluated for their physical characters, in vitro drug release and buoyancy studies. The optimized formulation (F3) was found to be physically stable when stored at 40 oC/75% RH for 3 months. In vivo radiographic imaging of F3 revealed a mean GRT of 4.83 ± 0.57 h (n=3). Comparative pharmacokinetic study was performed for F3, IR and SR tablets of CFDN in humans. Based on in vivo performance, the difference between tmax, AUC0-∞, t1/2 and MRT of F3, IR and SR tablets were found to be statistically significant (p < 0.05). The difference between Cmax of F3 and IR tablet was statistically significant, but the Cmax of F3 and SR tablet was not statistically significant. The relative bioavailability of F3 was 1.71 fold to IR and 1.24 fold to SR. This improved bioavailability is due to the combined effect of sustained release and increased GRT.


Keywords


Cefdinir, Gastroretentive floating tablets, Polyethylene oxide, Radiographic imaging, Pharmacokinetic study.

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