The present research work was envisaged to develop bilayer tablets to improve therapeutic efficacy of antilipidemic drugs for the treatment of high cholesterol and triglyceride levels in the blood. The combination of two antilipidemic drugs i.e. lovastatin and oleanolic acid were used for the preparation of bilayer tablets. The formulations comprise of lovastatin as immediate release layer formulated using different superdisintegrants and oleanolic acid as extended release layer containing HPMC K100M. Evaluation of bilayer tablets were performed for the immediate release lovastatin layer and sustain release oleanolic acid layer with optimization of excipients. The immediate release layer of lovastatin showed complete release within 60 min and oleanolic acid release was extended up to 12 h. Among the various formulations BLV9 for immediate release containing sodium starch glycolate (12 mg): Croscarmellose sodium (12 mg) and BOA1 for sustained release containing HPMC K100M (10 mg): Ethyl Cellulose (10 mg)) were optimized based on the better drug release within 30 min and 12 h respectively. Stability studies revealed that the optimized formulation was intact without any deterioration for 6 months. The present study revealed that lovastatin and oleanolic acid bilayer tablets were successfully developed to reduce the level of bad cholesterol and increase the level of good cholesterol in the blood.