DESIGN AND DEVELOPMENT OF VALSARTAN AN ANTI-HYPERTENSIVE DRUG FORMULATED AS FLOATING PULSATILE RELEASE FORMULATION

Dr. J. Ramesh Babu*, S. Meraj Sultana, Dr. S. Vidyadhara

The objective of the present study was to develop a pulsatile drug delivery system for valsartan, designed to align drug release with the body's circadian rhythm. Initial investigations indicated that β-cyclodextrin significantly enhanced the solubility of valsartan, demonstrating an AL-type solubility curve. Phase solubility studies confirmed a 1:1 molar ratio for the valsartan-β-cyclodextrin inclusion complex, which exhibited markedly improved dissolution efficiency compared to the pure drug, likely due to complex formation. A pulsatile delivery system was formulated using a "tablet-in-capsule" approach, incorporating both a floating tablet and an enteric-coated tablet. The optimized core tablets were placed inside capsules and coated with 4% Eudragit S-100. In-vitro release studies were conducted in 0.1 N HCl for 4 hours, followed by phosphate buffer (pH 6.8) for an additional 3 hours. The coated capsules exhibited minimal drug release in acidic medium and released the majority of the drug in the buffer medium. Among the formulation components, HPMC K4M played a crucial role in modulating the lag time. The final formulation demonstrated a 4-hour lag phase followed by rapid and complete drug release within the next 2 hours. This approach successfully achieved a pulsatile release profile for valsartan with enhanced dissolution performance.