Formulation, Development and Pharmacokinetics of Ketorolac Tromethamine Colon Targeted Guar Gum Compression Coated Tablets

Abstract

The present study was expected to develop colon-specific guar gum compression coated tablets of ketorolac tromethamine (KTM). In this study, the core and compression coated tablets were prepared by direct compression method and evaluated. Samples obtained from in vitro dissolution and in vivo pharmacokinetic studies were analyzed using the HPLC method at 319 nm using UV detector. From the in vitro dissolution studies, the formulation F4 showed 4.92±0.36 % drug release in 5 h and it was progressively expanded to 99.92±0.68 % in 24 h. From the pharmacokinetic evaluation, the immediate release tablets producing peak plasma concentration (C_max) was 4524.61 ng/ml at 2 h T_max and colon targeted tablets demonstrated C_max=3396.83 ng/ml at 10 h T_max. The area under the plasma KTM concentration versus time curves for the immediate release and compression coated tablets were 10894.67 and 17647.58 ng-h/ml respectively and the mean resident time was 3.92 and 10.25 h respectively. From the above results, colon specific drug release achieved due to substantial integrity of the compression coated guar gum in the upper gastrointestinal tract, but microbial degradation in the colon. In conclusion, development of microbial degradation based guar gum compression coated tablets was suitable to gain colon-specific release of KTM.

Key words:

• Colon-specific
• Direct Compression
• In vitro dissolution studies
• Pharmacokinetic evaluation
• Upper gastrointestinal tract