Formulation characterization and in-vitro/in-vivo evaluation of orodispersible tablets of Nebivolol HCl

Objective of the present research work was to prepare orodispersible tablets of Nebivolol hydrochloride (NEB) for dysphagic patients. Nebivolol, an anti-hypertensive drug, was chosen as a model drug in this study. Oral bioavailability of nebivolol is only 12% due to extensive first pass hepatic metabolism by Cytochrome P450 2D6 enzyme. Orodispersible tablets of NEB were prepared using different super-disintegrating agents such as crospovidone, croscarmellose sodium and sodium starch glycolate at different concentrations. The best formulation was selected based on disintegration and dissolution profile that was further taken for sublimation studies using camphor, menthol and thymol. Drug-excipients interaction studies were carried out by FTIR spectrophotometer with each of the excipients and optimized formulation. The orodispersible tablet formulation containing 10% w/w of menthol showed disintegration time of 11 sec with more than 98% drug release within 14 min. Therefore, this formulation was optimized and considered for further in vivo studies. In vivo studies of orodispersible tablets in rabbits showed significantly better pharmacokinetic profile (AUC, Tmax, Cmax) compared to marketed conventional tablets. Therefore, from this study it was concluded that, orodispersible tablets of NEB may prove to be more efficacious in the treatment of hypertension in dysphagic patients.

Author(s): Vijayanand P., J. S. Patil and M. Venkata Reddy

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