Bilayer tablets were prepared by using combination of fast dissolving lisinopril along with sustained release gliclazide. The FTIR study conducted using a combination of drugs along with excipients and polymers revealed that combination can be safely prepared. The precompression parameter of powder blends for preparation of individual layers suggested good flowability and compressibility. Lisinopril was formulated as fast dissolving layer using sodium starch glycolate, croscarmellose sodium as superdisintegrants and evaluated for physical parameter and disintegration time. The optimized lisinopril fast dissolving layer (L-6) with highest in vitro release of 99.73% was selected. Gliclazide was formulated as sustained release layer using different polymer matrix like hydroxyethylcellulose, hydroxypropylcellulose, and ethylcellulose and evaluated for physical parameter along with in vitro release studies. The optimized sustained release layers (G-5) which extend the gliclazide release more than 8hrs was selected. Finally bilayer tablets were prepared by double compression of optimized gliclazide sustained release layer and lisinopril fast dissolving layer. Bilayer tablets were evaluated for hardness, thickness, weight variation, friability, in vitro disintegration time and in vivo antidiabetic activity using wistar rats. All the physical parameters were in acceptable limit of pharmacopeial specification. The in vivo antidiabetic activity suggested that lisinopril potentiate hypoglycemic effect of gliclazide and blood glucose level was constantly maintained upto 24 h. Hence bilayer tablets of lisinopril and gliclazide as fast and sustained release combination could be used to improve patient compliance towards the effective management of diabetes along with diabetic hypertension and nephropathy.