Dissolution rate of practically insoluble mefenamic acid was improved by roll mixing with sodium lauryl sulfate (SLS) or polyvinylpyrrolidone (PVP). The dissolution rate of the drug roll mixtures with SLS was superior to that of roll mixtures with PVP. The maximal dissolution rate was found in the roll mixtures system with SLS content of 60%. The dissolution rate of mefenamic acid roll mixtures with SLS content of 60% reached to the maximum value after 10 min of roll mixing. The transport of roll mixtures with SLS across rat jejunum was studied by the perfusion method using everted rat jejunum in vitro. The absorption rate of roll mixtures was superior to that of mefanamic acid.