Formulation and Pharmacokinetics of Ketorolac Tromethamine Fast Dissolving Tablets

Abstract

Objective:

The current study is intended to develop the fast dissolving tablets of Ketorolac tromethamine using different superdisintegrants to improve the dissolution rate and absorption rate to produce the bioavailability enhancement and rapid onset of action.

Methods:

In this, Ketorolac tromethamine fast dissolving tablets were prepared using different superdisintegrants and evaluated for different physical parameters, in vitro dissolution studies and in vivo pharmacokinetics to demonstrate the bioavailability enhancement.

Results & Discussions:

From the in vitro drug release studies, in case of optimized formulation, the cumulative percent drug release in 15 min (Q15) was found to be 94.34±1.68 where as the conventional tablets showed 28.78±0.82 in 15 min. The initial dissolution rate and dissolution efficiency of optimized formulation was 6.29%/min and 53.43 but it was 1.92%/min and 14.03 in conventional tablets. From the in vivo pharmacokinetic evaluation, the optimized formulation showed peak plasma concentration (C_max) as 1 248.39 ng/ml at 1 h T_max, but they were found to be 988.22 ng/ml at 2 h T_max, in case of conventional tablets. The area under the curve for the optimized and conventional tablets was 3 890.68 and 3 173.07 ng-h/ml.

Conclusion:

Hence the development of fast dissolving tablets using superdisintegrants was a good approach to improve the dissolution rate and absorption rate of Ketorolac tromethamine.

Key words

absorption rate - dissolution efficiency - in vitro drug release studies - initial dissolution rate - pharmacokinetic evaluation

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