Formulation and Evaluation of Bilayer Floating Tablets of Trimetazidine hydrochloride and Metoprolol succinate

Abstract:

The objective of the present investigation was to develop bilayer floating tablets of Trimetazidine hydrochloride and Metoprolol succinate for stable angina pectoris insufficiently controlled by monotherapy with beta-blocker. Bilayer floating tablets was formulated using wet granulation technique and it consists of two layers, i.e. immediate release layer containing Metoprolol succinate and floating sustained release layer containing Trimetazidine hydrochloride. The immediate release layer comprised of Sodium Starch Glycolate as a super disintegrant and the sustained release layer comprised of Ethyl cellulose, HPMC K4M, HPMC K100M and Xanthan gum as release retarding polymers. Sodium bicarbonate was used as a gas generating agent in the floating layer. The immediate release layer (M3) containing 4% Sodium Starch Glycolate was found to be optimum and released 99.61% of Metoprolol in 15 m. The floating sustained release tablet of Trimetazidine hydrochloride (BFT8) containing Ethyl cellulose (5%), Xanthan gum (10%) and HPMC K100M (20%) showed sustained release up to 12 h. The final optimized formulation (BFT8) released 99.87 % of Trimetazidine in 12 h while the floating lag time was 4 m and the tablet remained floatable throughout the studies. The drug release was inversely proportional to the polymer concentration. The formulation BFT8 may be a better alternative to the available combination for the treatment of angina pectoris. Keywords: Bilayer floating tablet, Trimetazidine hydrochloride, Metoprolol succinate, angina pectoris.