Optimization of formulation and dissolution study of valsartan oral dosage forms with poor disintegration to ensure bioequivalence
This study aims to develop an optimized formulation for valsartan oral dosage form, a antihypertensive drug, and improve its low dissolution rate. A preformulation study was conducted to evaluate the solubility of valsartan and its compatibility with excipients. Based on the results, tablets were formulated using excipients that demonstrated compatibility. Dissolution profiles were assessed under standard test conditions as well as at pH 1.2, 4.0, and 6.8. The results revealed that the tablets did not disintegrate properly, leading to a low dissolution rate. To address this issue, the proportion of the pH modifier meglumine was reduced, and the proportion of disintegrants was increased. Additionally, various disintegrants were incorporated to optimize the formulation. Dissolution testing of the formulated tablets showed that the composition containing microcrystalline cellulose, croscarmellose sodium, meglumine, copovidone VA64, and magnesium stearate exhibited the most similar dissolution profile to the reference drug. The optimized formulation demonstrated comparable disintegration time and dissolution rates under standard test conditions and at pH 1.2, 4.0, and 6.8. This study successfully optimized the formulation of valsartan oral dosage form, ensuring bioequivalence with the reference product. The findings of this study are expected to serve as fundamental data for future bioequivalence studies and scale-up processes.
2025 Spring Convention