QbD-Based Optimization of Fast Dissolving Sublingual Tablets of Valsartan

Background

Valsartan, an angiotensin II receptor blocker, is commonly prescribed for managing hypertension and heart failure. However, its poor aqueous solubility and extensive first-pass metabolism limit its bioavailability, necessitating the development of an alternative delivery system. This study aimed to optimize the formulation of a sublingual fast-dissolving tablet of Valsartan to enhance drug dissolution and absorption for rapid therapeutic action.

Methods

A Box-Behnken Design (BBD) was employed to evaluate the influence of three super disintegrants—Sodium Starch Glycolate (SSG), Crospovidone (CP), and Croscarmellose Sodium (CCS)—on critical formulation parameters: disintegration time (DT) and cumulative drug release (CDR%). The optimized formulation (OVSF-18) was selected based on desirability criteria and further subjected to in vitro dissolution studies, release kinetics, and stability assessment to ensure formulation robustness.

Results

The response surface analysis revealed that SSG had the most significant impact on reducing DT, followed by CP, while CCS contributed moderately. The optimized formulation (OVSF-18) exhibited a disintegration time of 33.33 s and achieved 92.33% cumulative drug release within 15 min, demonstrating superior performance compared to marketed tablets. Stability studies confirmed the formulation’s physicochemical integrity over the test period.

Conclusion

The optimized sublingual Valsartan significantly enhances drug dissolution and absorption by circumventing first-pass metabolism, offering a promising alternative to conventional oral formulations. Its rapid onset of action and improved bioavailability make it particularly suitable for hypertensive emergencies and heart failure management. This study establishes a foundation for further clinical evaluation and potential commercialization of sublingual Valsartan tablets as an effective therapeutic option.