Development of An Oral Sustained-Release Antibiotic Matrix Tablet UsingIn-Vitro/In-VivoCorrelations

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Abstract
A sustained release (SR) cephalexin tablet formulation containing xanthan gum and sodium alginate as matrix formers was evaluated in human volunteers. The formulation was optimized based on response surface analysis and computer simulation of cephalexin plasma levels versus time curves. The optimized formulation was tested in-vivo in human volunteers along with a fast release (FR) capsule formulation. The SR matrix formulation prolonged the cephalexin blood levels up to 8 hours in humans. The matrix formulation reduced variations in cephalexin plasma levels in individual subjects without any dose dumping as compared to the FR formulation. The plasma levels predicted by the computer program using in-vitro release data and the drug's pharmacokinetic parameters showed excellent correlation with in-vivo data. Using the Wagner-Nelson method, there was good correlation between in-vitro dissolution and in-vivo absorption in individual subjects. The relative bioavailability of cephalexin was reduced by about thirty percent. Very little absorption was seen after six to eight hours. The SR matrix formulation is an alternative delivery method to produce prolonged concentrations.

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