IMPROVEMENT OF BIOAVAILABILITY OF CEFUROXIME AXETIL ORAL SUSPENSION BY INCLUSION COMPLEXATION METHOD

  • Renju Prabhakaran Sance Laboratories Pvt Ltd, Kottayam, Kerala, India 686573
  • Janakiraman K.
  • Jyoti Harindran

Abstract

Objective: Cefuroxime axetil, a prodrug of Cefuroxime, is a poorly water soluble drug, thus it has got only limited solubility and dissolution rate in gastric fluids. Also, the bioavailability of Cefuroxime axetil oral suspension is only 40-45% when compared to the 60% bioavailability of tablets. The objective of this study was to develop an oral suspension of Cefuroxime axetil with improved oral bioavailability by inclusion complexation method using Hydroxypropyl beta cyclodextrin [HP-Beta-cylcodextrin]

Methods: The complexation of Cefuroxime axetil and HP-Beta cyclodextrin was carried out at 1:1, 1:2, 1:2.5 and 1:3 ratios respectively. The prepared suspensions were evaluated for various parameters like pH, viscosity, re-dispersibility, pourability, and assay and in-vitro dissolution profile. A leading marketed product and the optimized formulation were evaluated for the pharmacokinetic parameters like Cmax, AUC0-t, AUC0-∞ and Tmax in healthy adult male rabbits.

Results: Considering the in-vitro dissolution profile, formulation with 1:2.5 ratios of Cefuroxime axetil and HP-Beta cyclodextrin was selected as the optimized formulation. The Cmax of Optimized formulation and Marketed product were 148±1.26ng/ml and 126±1.52 ng/ml respectively, and the AUC0-t ofOptimized formulation and Marketed product were 989±16.42 ng. h/ml and 613±24.26 ng. h/ml respectively, which shows a significant improvement in the bioavailability of optimized formulation

Conclusion: From the results obtained it can be observed that there is a significant improvement in the bioavailability of optimized formulation compared to the marketed product. This demonstrates that the inclusion complexation method with HP-Beta cyclodextrin can significantly improve the oral bioavailability of Cefuroxime axetil.

Keywords: Cefuroxime axetil, Bioavailability, Beta cyclodextrin, Inclusion complexation

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References

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How to Cite
Prabhakaran, R., J. K., and J. Harindran. “IMPROVEMENT OF BIOAVAILABILITY OF CEFUROXIME AXETIL ORAL SUSPENSION BY INCLUSION COMPLEXATION METHOD”. International Journal of Pharmacy and Pharmaceutical Sciences, Vol. 8, no. 3, Mar. 2016, pp. 361-4, https://innovareacademics.in/journals/index.php/ijpps/article/view/10462.
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