Abstract

DEVELOPMENT, OPTIMIZATION AND EVALUATION OF BILAYER TABLET OF NEBIVOLOL AND INDAPAMIDE

Yogesh Baburao Tambade*, Ravindra Bhimrao Laware, Rajashri Dadasaheb Ghogare, Shivprasad Gangadhar Tengale and Shivam Rameshwar Kote

ABSTRACT

The objective of the project was to develop a stable and robust formulation of bilayer tablet of the selected antihypertensive drugs. Hypertension is commonly referred to as high blood pressure. Blood pressure can be defined as the amount of force exerted by our blood on the inside of our arteries & blood vessels. Optimal systolic blood pressure should lie under 120 mm Hg & diastolic pressure should lie under 80 mm Hg. Normal systolic blood pressure is under 130 mm Hg & that of diastolic pressure is under 85 mm Hg. Hypertension is clinically defined as a systolic pressure greater than 140 mm Hg & diastolic pressure greater than 90 mm Hg. The most commonly prescribed drugs for hypertension are beta blockers, diuretics, Angiotensin Converting Enzyme (ACE) inhibitors, Angiotensin antagonists & calcium channel blockers. Combination of the above classes can give better antihypertensive action than can be obtained with single drug from one class. The present study deals with optimization and evaluation of bilayer tablet formulation in which first layer consist of sustained release formulation of diuretic drug while second layer consist of immediate release of selective β-1 blocker. Here sustained release formulation of diuretic drug avoids the side effects associated with the immediate release formulation & also provides effects for longer period of time & when it combines with the immediate release formulation of selective β-1 blocker, combinations of both drugs provides synergistic effects against hypertension. The result of the project would provide a process that would provide stable formulation of bilayer tablets of antihypertensive drugs. In the bilayer tablet, sustained release part was tried to prepare by direct compression & by wet granulation, but finally wet granulation method was selected. Immediate release part was also optimized using wet granulation method. Among different trials with wet granulation, the trial I-11 showed satisfactory in vitro drug release profile as compared to that of innovator for sustained release formulation while the trial N-6 showed satisfactory in vitro drug release profile for immediate release formulation as compared to that of innovator. Hence, the trial I-11 for sustained release part & trial N-6 for immediate release part was selected for the preparation of bilayer tablet.

Keywords: Antihypertensive drugs, wet granulation, immediate release tablets, sustained release tablet, bilayer tablet.