Development of fast dispersing tablets of nebivolol: experimental and computational approaches to study formulation characteristics

Rajamma Abburu Jayaramu,Sateesha Shivally Boregowda,Chandan Kalegowda,Addanki Rahul Deva Varma

doi:10.1590/s1984-82502014000400031

Abstract

Formulation of FDT (fast dispersing tablets) of nebivolol was optimized and evaluated using simplex lattice design (SLD). The influence of type and concentration of three disintegrants viz.,Ac-Di-Sol, Primojel and Polyplasdone XL on hardness, friability and disintegration time of tablet was studied. Response surface plot and the polynomial equations were used to evaluate influence of polymer on the tablet properties. Results were statistically analyzed using ANOVA, and a p < 0.05 was considered statistically significant. Results reveal that fibrous integrity and optimal degree of substitution in Primojel and Ac-Di-Sol are mainly responsible for the hardness of the tablet. Use of Polyplasdone in higher percentage in tablet formulation may result in high friability. Increase in concentration of Ac-Di-Sol increases the disintegration time but increased concentration of Primojel in the tablet formulation decreases the disintegration time. This is also evident from model terms for disintegration time with a high 'F' value of 14.69 and 'p' value of 0.0031 (<0.05). The reason could be that Primojel has higher swelling properties and an optimum hydration capacity, which favors fast disintegration of a tablet. In conclusion, careful selection of disintegrant for FDT could improve their properties. Use of Simplex Lattice Design for formulation development could simplify the formulation process and reduce the production cost.

Highlights

Nebivolol is a selective beta-1 receptor antagonist used for the management of hypertension and angina pain
The amount of drug which is subjected to first pass metabolism is reduced from fast dispersing tablets (FDT) as compared to conventional tablet(Tansel et al, 2011; Shery, Arun, Anroop, 2009)
Super disintegrant is the principle ingredient of the FDT to accommodate rapid disintegration time of the formulation

Summary

INTRODUCTION

Nebivolol is a selective beta-1 receptor antagonist used for the management of hypertension and angina pain It reaches mean peak plasma concentration approximately in 1.5 to 4 h post oral administrations (Na, Larry, 2002). In such cases it is very essential to enhance onset of action of a drug.in this work the goal has been set to formulate and evaluate fast dispersing tablets (FDT) of nebivolol. Efficiency of the formulation is varied according to the type and proportion of disintigrant in it (Deshika,Viness, Yahya, 2009; Alvaro,Consuelo, Ramón, 2011), since each disintegrant works on several unique properties, such as swelling properties (Zhao, Larry, Augsburger,2005), hydration capacity(Seonget al.,2008), among others. The center point represents a formulation containing one third of each ingredient (Tadashi et al, 2011; Shirsand et al.,2010)

MATERIAL AND METHODS

RESULTS AND DISCUSSION

F3 F5 F11

CONCLUSIONS