Formulation and Optimization of Captopril Sublingual Tablet Using D-Optimal Design

Abstract

The objective of the current study was to develop and optimize a sublingual tablet formulation of captopril which is an effective drug in the treatment of hypertension. Captopril containing tablets were prepared by direct compression method using different ingredients such as polyvinyl pyrrolidone, starch 1500, sodium starch glycolate and lactose (independent variables) and magnesium stearate, talc and aspartame (fixed components). Tablets were evaluated for the physical properties including hardness, disintegration time and friability which were considered as responses in a D-optimal experimental plan. Results were statistically examined using special cubic model and polynomial mathematical equations and found to be statistically significant (p< 0.05) for disintegration time and friability data. Meanwhile linear model was best fitted with hardness data. The obtained results were used to generate optimized overlay plot. The physical data from the numerical optimization were verified and found to be very close to those predicted from the regression analysis. Additional experiments including drug content, in vitro drug dissolution rate and accelerated stability studies were also performed on the optimum formulation. All results were in accordance with the requirements of a sublingual tablet.